Cayman
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TTC is a redox indicator used to detect cellular respiration.{22804} It is primarily reduced by Complex I in mitochondria and, under anaerobic conditions, is completely reduced to an insoluble red 1,3,5-triphenylformazan.{14422} TTC assays are typically used as a mitochondrial redox potential indicator for cell death.{22804}
Brand:CaymanSKU:-Available on backorder
TTC is a redox indicator used to detect cellular respiration.{22804} It is primarily reduced by Complex I in mitochondria and, under anaerobic conditions, is completely reduced to an insoluble red 1,3,5-triphenylformazan.{14422} TTC assays are typically used as a mitochondrial redox potential indicator for cell death.{22804}
Brand:CaymanSKU:-Available on backorder
![An NMDA receptor agonist (IC50 = 98 and 36 nM for [3H]CGS19755 and [3H]glutamate](https://interpriseusa.com/wp-content/uploads/2021/06/28408.png)
Tetrazolyl glycine is an NMDA receptor agonist.{52237} It binds to rat brain membranes with IC50 values of 98 and 36 nM for [3H]CGS19755 and [3H]glutamate, respectively, in radioligand binding assays. It induces depolarization in rat cortical slices, an effect that is blocked by the NMDA receptor antagonist LY233053. It induces degeneration of GABAergic and cholinergic neurons in the striatum of adult rats and the formation of excitotoxic lesions and seizures in neonatal rats (ED50 = 0.071 mg/kg).{52238,52237} Intrastriatal injection of tetrazolyl glycine (5 µM) increases COX-2 expression in striatal neurons and the vasculature near the striatal injection site in a mouse model of excitotoxicity-induced neuronal injury.{52239}
Brand:CaymanSKU:28408 - 10 mgAvailable on backorder
Tetrazolyl glycine is an NMDA receptor agonist.{52237} It binds to rat brain membranes with IC50 values of 98 and 36 nM for [3H]CGS19755 and [3H]glutamate, respectively, in radioligand binding assays. It induces depolarization in rat cortical slices, an effect that is blocked by the NMDA receptor antagonist LY233053. It induces degeneration of GABAergic and cholinergic neurons in the striatum of adult rats and the formation of excitotoxic lesions and seizures in neonatal rats (ED50 = 0.071 mg/kg).{52238,52237} Intrastriatal injection of tetrazolyl glycine (5 µM) increases COX-2 expression in striatal neurons and the vasculature near the striatal injection site in a mouse model of excitotoxicity-induced neuronal injury.{52239}
Brand:CaymanSKU:28408 - 100 mgAvailable on backorder
Tetrazolyl glycine is an NMDA receptor agonist.{52237} It binds to rat brain membranes with IC50 values of 98 and 36 nM for [3H]CGS19755 and [3H]glutamate, respectively, in radioligand binding assays. It induces depolarization in rat cortical slices, an effect that is blocked by the NMDA receptor antagonist LY233053. It induces degeneration of GABAergic and cholinergic neurons in the striatum of adult rats and the formation of excitotoxic lesions and seizures in neonatal rats (ED50 = 0.071 mg/kg).{52238,52237} Intrastriatal injection of tetrazolyl glycine (5 µM) increases COX-2 expression in striatal neurons and the vasculature near the striatal injection site in a mouse model of excitotoxicity-induced neuronal injury.{52239}
Brand:CaymanSKU:28408 - 25 mgAvailable on backorder
Tetrazolyl glycine is an NMDA receptor agonist.{52237} It binds to rat brain membranes with IC50 values of 98 and 36 nM for [3H]CGS19755 and [3H]glutamate, respectively, in radioligand binding assays. It induces depolarization in rat cortical slices, an effect that is blocked by the NMDA receptor antagonist LY233053. It induces degeneration of GABAergic and cholinergic neurons in the striatum of adult rats and the formation of excitotoxic lesions and seizures in neonatal rats (ED50 = 0.071 mg/kg).{52238,52237} Intrastriatal injection of tetrazolyl glycine (5 µM) increases COX-2 expression in striatal neurons and the vasculature near the striatal injection site in a mouse model of excitotoxicity-induced neuronal injury.{52239}
Brand:CaymanSKU:28408 - 50 mgAvailable on backorder
TTX is a potent marine-derived neurotoxin that reversibly inhibits the inward sodium current through voltage-activated sodium (NaV) channels, blocking nerve and muscle action potentials. It inhibits the NaV current in frog muscle and squid axon with IC50 values of 4.1 and 5.2 nM, respectively, and binds to rat brain membranes with a Kd value of 1.8 nM.{23790} TTX was used in Hodgkin and Huxley’s classic experiments to elucidate the physical biology of nerve action potentials and remains an indispensible neuroscience tool to pharmacologically dissect the contribution of the NaV current in excitable neurons and to rationally design compounds for the treatment of neuropathic pain.{23790}
Brand:CaymanSKU:-
TTX is a potent marine-derived neurotoxin that reversibly inhibits the inward sodium current through voltage-activated sodium (Nav) channels, blocking nerve and muscle action potentials. It inhibits the Nav current in frog muscle and squid axon with IC50 values of 4.1 and 5.2 nM, respectively, and binds to rat brain membranes with a Kd value of 1.8 nM.{23790} TTX was used in Hodgkin and Huxley’s classic experiments to elucidate the physical biology of nerve action potentials and remains an indispensible neuroscience tool to pharmacologically dissect the contribution of the Nav current in excitable neurons and to rationally design compounds for the treatment of neuropathic pain.{23790} This citrate-stabilized form of TTX is designed for improved solubility over pure TTX (Item No. 14963), which is insoluble in water and most organic solvents. This preparation of TTX citrate consists of TTX that has been dissolved in a citrate solution and then lyophilized.
Brand:CaymanSKU:-
Tetromycin A is a tetronic acid-based antibiotic. It reportedly has pronounced activity against Gram-positive bacteria, including methicillin-resistant S. aureus. Related tetromycin derivatives have been found to have anti-trypanosomal activity and inhibit the cysteine protease cathepsin L with Ki values in the low micromolar range.{32273}
Brand:CaymanSKU:20690 -Available on backorder
Tetromycin A is a tetronic acid-based antibiotic. It reportedly has pronounced activity against Gram-positive bacteria, including methicillin-resistant S. aureus. Related tetromycin derivatives have been found to have anti-trypanosomal activity and inhibit the cysteine protease cathepsin L with Ki values in the low micromolar range.{32273}
Brand:CaymanSKU:20690 -Available on backorder
Tetromycin B is a cysteine protease inhibitor with Ki values of 0.62, 1.42, 32.5, and 1.59 μM for rhodesain, falcipain-2, cathepsin L, and cathepsin B, respectively.{32273} It inhibits the growth of T. brucei in vitro (IC50 = 30.87 μM). Tetromycin B is also cytotoxic to HEK293T kidney cells and J774.1 macrophages (IC50s = 71.77 and 20.2 μM, respectively).
Brand:CaymanSKU:23766 - 2.5 mgAvailable on backorder
Tetromycin B is a cysteine protease inhibitor with Ki values of 0.62, 1.42, 32.5, and 1.59 μM for rhodesain, falcipain-2, cathepsin L, and cathepsin B, respectively.{32273} It inhibits the growth of T. brucei in vitro (IC50 = 30.87 μM). Tetromycin B is also cytotoxic to HEK293T kidney cells and J774.1 macrophages (IC50s = 71.77 and 20.2 μM, respectively).
Brand:CaymanSKU:23766 - 500 µgAvailable on backorder
Brand:CaymanSKU:10009848 - 1 eaAvailable on backorder
Brand:CaymanSKU:10009848- 1 eaAvailable on backorder
Brand:CaymanSKU:10009848- 1 ea
Immunogen: Native recombinant human TFAM protein with a C-terminal 6-His tag • Host: Rabbit • Species Reactivity: (+) Human • Applications: WB • MW = ~24 kDa
Brand:CaymanSKU:29297- 100 µl Mitochondrial transcription factor A (TFAM) is a mitochondrial DNA (mtDNA) binding protein that maintains the mitochondrial genome by regulating replication, transcription, and packaging of mtDNA.{59160} It contains two high mobility group (HMG) box domains that bind mtDNA and induce a conformational change that permits binding of mitochondrial RNA polymerase (mtRNAP) to the promoter start site. TFAM binds to mtRNAP, recruiting mitochondrial transcription factor 2 (TFB2M) and initiating transcription. TFAM also maintains mitochondrial genome stability by non-specifically binding to mtDNA, packaging it into nucleoid-like structures. Homozygous knockout of Tfam in mice is embryonic lethal whereas heterozygous Tfam knockdown mice are viable but have reduced mtDNA copy numbers and decreased activity of the mitochondrial respiratory chain complexes I, III, IV, and V in the heart.{59161} Genetic overexpression of Tfam reduces age-induced accumulation of lipid peroxidation products in the brain and memory impairments in mice.{59162} Increased tumor TFAM protein levels are associated with increased tumor size in patients with breast cancer.{59163} SNPs in TFAM have been identified in patients with a variety of neurodegenerative disorders, including Parkinson’s disease, Alzheimer’s disease, and Huntington’s disease.{59160} Cayman’s TFAM Polyclonal Antibody can be used for Western blot (WB) applications. The antibody recognizes TFAM at approximately 24 kDa from human samples.
Brand:CaymanSKU:29297 - 100 µlAvailable on backorder
Immunogen: Native recombinant human TFAM protein with a C-terminal 6-His tag • Host: Rabbit • Species Reactivity: (+) Human • Applications: WB • MW = ~24 kDa
Brand:CaymanSKU:29297- 100 µlAvailable on backorder
TFAP is an inhibitor of COX-1 (IC50 = 0.8 μM).{52060} It is selective for COX-1 over COX-2 (IC50 = 210 μM). TFAP (10 and 30 mg/kg) reduces acetic acid-induced writhing in mice and has analgesic activity in the formalin test in rats when administered at a dose of 30 mg/kg. It does not induce gastric damage in rats when administered at doses up to 300 mg/kg.
Brand:CaymanSKU:26745 - 1 mgAvailable on backorder
TFAP is an inhibitor of COX-1 (IC50 = 0.8 μM).{52060} It is selective for COX-1 over COX-2 (IC50 = 210 μM). TFAP (10 and 30 mg/kg) reduces acetic acid-induced writhing in mice and has analgesic activity in the formalin test in rats when administered at a dose of 30 mg/kg. It does not induce gastric damage in rats when administered at doses up to 300 mg/kg.
Brand:CaymanSKU:26745 - 10 mgAvailable on backorder
TFAP is an inhibitor of COX-1 (IC50 = 0.8 μM).{52060} It is selective for COX-1 over COX-2 (IC50 = 210 μM). TFAP (10 and 30 mg/kg) reduces acetic acid-induced writhing in mice and has analgesic activity in the formalin test in rats when administered at a dose of 30 mg/kg. It does not induce gastric damage in rats when administered at doses up to 300 mg/kg.
Brand:CaymanSKU:26745 - 25 mgAvailable on backorder
TFAP is an inhibitor of COX-1 (IC50 = 0.8 μM).{52060} It is selective for COX-1 over COX-2 (IC50 = 210 μM). TFAP (10 and 30 mg/kg) reduces acetic acid-induced writhing in mice and has analgesic activity in the formalin test in rats when administered at a dose of 30 mg/kg. It does not induce gastric damage in rats when administered at doses up to 300 mg/kg.
Brand:CaymanSKU:26745 - 5 mgAvailable on backorder
TFMB-R-2-HG is a cell-permeable form of (R)-2-hydroxyglutarate ((R)-2-HG).{42076} (R)-2-HG is structurally similar to α-ketoglutarate and competitively inhibits α-ketoglutarate-dependent dioxygenases, including lysine demethylases and DNA hydroxylases.{26775,26774,26769} TFMB-R-2-HG has been used to assess the role of (R)-2-HG in leukemogenesis.{42076}
Brand:CaymanSKU:20461 -Available on backorder
TFMB-R-2-HG is a cell-permeable form of (R)-2-hydroxyglutarate ((R)-2-HG).{42076} (R)-2-HG is structurally similar to α-ketoglutarate and competitively inhibits α-ketoglutarate-dependent dioxygenases, including lysine demethylases and DNA hydroxylases.{26775,26774,26769} TFMB-R-2-HG has been used to assess the role of (R)-2-HG in leukemogenesis.{42076}
Brand:CaymanSKU:20461 -Available on backorder
TFMB-R-2-HG is a cell-permeable form of (R)-2-hydroxyglutarate ((R)-2-HG).{42076} (R)-2-HG is structurally similar to α-ketoglutarate and competitively inhibits α-ketoglutarate-dependent dioxygenases, including lysine demethylases and DNA hydroxylases.{26775,26774,26769} TFMB-R-2-HG has been used to assess the role of (R)-2-HG in leukemogenesis.{42076}
Brand:CaymanSKU:20461 -Available on backorder
Cdc2-like kinase (Clk), among a number of other kinases, phosphorylates serine/arginine-rich proteins which play a role in alternative splicing of pre-mRNA. The Clk family consists of four members, which include Clk1/Sty and Clk2-4. TG003 is a novel benzothiazole compound that demonstrates potent inhibition of Clk1/Sty and Clk4 with IC50 values of 20 and 15 nM, respectively.{19742} TG003 exhibits considerably weaker inhibition of Clk2 and Clk3 (IC50 = 200 nM and >10 μM, respectively).{19742} Through suppression of Clk-mediated phosphorylation, TG003 inhibits SF2/ASF-dependent splicing of β-globin pre-mRNA at 1 μM in vitro.{19742} At 10 μM, TG003 rescues the embryonic defects induced by excessive Clk activity in Xenopus.{19742}
Brand:CaymanSKU:10398 - 1 mgAvailable on backorder
Cdc2-like kinase (Clk), among a number of other kinases, phosphorylates serine/arginine-rich proteins which play a role in alternative splicing of pre-mRNA. The Clk family consists of four members, which include Clk1/Sty and Clk2-4. TG003 is a novel benzothiazole compound that demonstrates potent inhibition of Clk1/Sty and Clk4 with IC50 values of 20 and 15 nM, respectively.{19742} TG003 exhibits considerably weaker inhibition of Clk2 and Clk3 (IC50 = 200 nM and >10 μM, respectively).{19742} Through suppression of Clk-mediated phosphorylation, TG003 inhibits SF2/ASF-dependent splicing of β-globin pre-mRNA at 1 μM in vitro.{19742} At 10 μM, TG003 rescues the embryonic defects induced by excessive Clk activity in Xenopus.{19742}
Brand:CaymanSKU:10398 - 10 mgAvailable on backorder
Cdc2-like kinase (Clk), among a number of other kinases, phosphorylates serine/arginine-rich proteins which play a role in alternative splicing of pre-mRNA. The Clk family consists of four members, which include Clk1/Sty and Clk2-4. TG003 is a novel benzothiazole compound that demonstrates potent inhibition of Clk1/Sty and Clk4 with IC50 values of 20 and 15 nM, respectively.{19742} TG003 exhibits considerably weaker inhibition of Clk2 and Clk3 (IC50 = 200 nM and >10 μM, respectively).{19742} Through suppression of Clk-mediated phosphorylation, TG003 inhibits SF2/ASF-dependent splicing of β-globin pre-mRNA at 1 μM in vitro.{19742} At 10 μM, TG003 rescues the embryonic defects induced by excessive Clk activity in Xenopus.{19742}
Brand:CaymanSKU:10398 - 25 mgAvailable on backorder
Cdc2-like kinase (Clk), among a number of other kinases, phosphorylates serine/arginine-rich proteins which play a role in alternative splicing of pre-mRNA. The Clk family consists of four members, which include Clk1/Sty and Clk2-4. TG003 is a novel benzothiazole compound that demonstrates potent inhibition of Clk1/Sty and Clk4 with IC50 values of 20 and 15 nM, respectively.{19742} TG003 exhibits considerably weaker inhibition of Clk2 and Clk3 (IC50 = 200 nM and >10 μM, respectively).{19742} Through suppression of Clk-mediated phosphorylation, TG003 inhibits SF2/ASF-dependent splicing of β-globin pre-mRNA at 1 μM in vitro.{19742} At 10 μM, TG003 rescues the embryonic defects induced by excessive Clk activity in Xenopus.{19742}
Brand:CaymanSKU:10398 - 5 mgAvailable on backorder
TG100713 is an inhibitor of PI3K (IC50s = 50, 24, 165, and 215 nM for PI3Kγ, PI3Kδ, PI3Kα, and PI3Kβ, respectively).{54092} It inhibits proliferation of human umbilical vein endothelial cells (HUVECs) when used at a concentration of 10 µM. TG100713 (2 µM) inhibits reactivation of latent HIV-1 induced by panobinostat (Item No. 13280), but not prostratin (Item No. 10272) or JQ-1, in 24ST1NLESG cells.{54093}
Brand:CaymanSKU:30195 - 1 mgAvailable on backorder
TG100713 is an inhibitor of PI3K (IC50s = 50, 24, 165, and 215 nM for PI3Kγ, PI3Kδ, PI3Kα, and PI3Kβ, respectively).{54092} It inhibits proliferation of human umbilical vein endothelial cells (HUVECs) when used at a concentration of 10 µM. TG100713 (2 µM) inhibits reactivation of latent HIV-1 induced by panobinostat (Item No. 13280), but not prostratin (Item No. 10272) or JQ-1, in 24ST1NLESG cells.{54093}
Brand:CaymanSKU:30195 - 10 mgAvailable on backorder
TG100713 is an inhibitor of PI3K (IC50s = 50, 24, 165, and 215 nM for PI3Kγ, PI3Kδ, PI3Kα, and PI3Kβ, respectively).{54092} It inhibits proliferation of human umbilical vein endothelial cells (HUVECs) when used at a concentration of 10 µM. TG100713 (2 µM) inhibits reactivation of latent HIV-1 induced by panobinostat (Item No. 13280), but not prostratin (Item No. 10272) or JQ-1, in 24ST1NLESG cells.{54093}
Brand:CaymanSKU:30195 - 25 mgAvailable on backorder
TG100713 is an inhibitor of PI3K (IC50s = 50, 24, 165, and 215 nM for PI3Kγ, PI3Kδ, PI3Kα, and PI3Kβ, respectively).{54092} It inhibits proliferation of human umbilical vein endothelial cells (HUVECs) when used at a concentration of 10 µM. TG100713 (2 µM) inhibits reactivation of latent HIV-1 induced by panobinostat (Item No. 13280), but not prostratin (Item No. 10272) or JQ-1, in 24ST1NLESG cells.{54093}
Brand:CaymanSKU:30195 - 5 mgAvailable on backorder
TG101209 is a potent inhibitor of the tyrosine kinases janus kinase (JAK) 2, FMS-like tyrosine kinase 3, proto-oncogene RET, and JAK3 (IC50 = 6, 25, 17, and 169 nM, respectively).{23418} Through these effects, it induces cell cycle arrest and apoptosis in leukemic cell lines and CD45+ myeloma cells.{23418,23417}
Brand:CaymanSKU:- TG101209 is a potent inhibitor of the tyrosine kinases janus kinase (JAK) 2, FMS-like tyrosine kinase 3, proto-oncogene RET, and JAK3 (IC50 = 6, 25, 17, and 169 nM, respectively).{23418} Through these effects, it induces cell cycle arrest and apoptosis in leukemic cell lines and CD45+ myeloma cells.{23418,23417}
Brand:CaymanSKU:- TG101209 is a potent inhibitor of the tyrosine kinases janus kinase (JAK) 2, FMS-like tyrosine kinase 3, proto-oncogene RET, and JAK3 (IC50 = 6, 25, 17, and 169 nM, respectively).{23418} Through these effects, it induces cell cycle arrest and apoptosis in leukemic cell lines and CD45+ myeloma cells.{23418,23417}
Brand:CaymanSKU:- TG101209 is a potent inhibitor of the tyrosine kinases janus kinase (JAK) 2, FMS-like tyrosine kinase 3, proto-oncogene RET, and JAK3 (IC50 = 6, 25, 17, and 169 nM, respectively).{23418} Through these effects, it induces cell cycle arrest and apoptosis in leukemic cell lines and CD45+ myeloma cells.{23418,23417}
Brand:CaymanSKU:-
Janus kinases (JAKs) are non-receptor kinases that mediate signaling through cytokine receptors, often to members of the signal transducer and activator of transcription (STAT) family.{20362} JAK2V617F and MPLW515L/K are two known mutations that cause dysregulated JAK/STAT signaling in myeloproliferative disorders. TG101348 is a small molecule inhibitor of JAK2 (IC50 = 6 nM) and the related kinases FLT3 (IC50 = 25 nM) and RET (IC50 = 17 nM) with significantly less potent activity against JAK3 (IC50 = 169 nM).{23418} It can inhibit the growth of Ba/F3 cells expressing JAK2V617F or MPLW515L mutations with an IC50 value of 200 nM.{23418} Phase I clinical trial results that focused on safety and efficacy of TG101348 in patients with high- or intermediate-risk primary or post-polycythemia vera/essential thrombocythemia myelofibrosis have been published.{27682}
Brand:CaymanSKU:- Janus kinases (JAKs) are non-receptor kinases that mediate signaling through cytokine receptors, often to members of the signal transducer and activator of transcription (STAT) family.{20362} JAK2V617F and MPLW515L/K are two known mutations that cause dysregulated JAK/STAT signaling in myeloproliferative disorders. TG101348 is a small molecule inhibitor of JAK2 (IC50 = 6 nM) and the related kinases FLT3 (IC50 = 25 nM) and RET (IC50 = 17 nM) with significantly less potent activity against JAK3 (IC50 = 169 nM).{23418} It can inhibit the growth of Ba/F3 cells expressing JAK2V617F or MPLW515L mutations with an IC50 value of 200 nM.{23418} Phase I clinical trial results that focused on safety and efficacy of TG101348 in patients with high- or intermediate-risk primary or post-polycythemia vera/essential thrombocythemia myelofibrosis have been published.{27682}
Brand:CaymanSKU:- Janus kinases (JAKs) are non-receptor kinases that mediate signaling through cytokine receptors, often to members of the signal transducer and activator of transcription (STAT) family.{20362} JAK2V617F and MPLW515L/K are two known mutations that cause dysregulated JAK/STAT signaling in myeloproliferative disorders. TG101348 is a small molecule inhibitor of JAK2 (IC50 = 6 nM) and the related kinases FLT3 (IC50 = 25 nM) and RET (IC50 = 17 nM) with significantly less potent activity against JAK3 (IC50 = 169 nM).{23418} It can inhibit the growth of Ba/F3 cells expressing JAK2V617F or MPLW515L mutations with an IC50 value of 200 nM.{23418} Phase I clinical trial results that focused on safety and efficacy of TG101348 in patients with high- or intermediate-risk primary or post-polycythemia vera/essential thrombocythemia myelofibrosis have been published.{27682}
Brand:CaymanSKU:- Janus kinases (JAKs) are non-receptor kinases that mediate signaling through cytokine receptors, often to members of the signal transducer and activator of transcription (STAT) family.{20362} JAK2V617F and MPLW515L/K are two known mutations that cause dysregulated JAK/STAT signaling in myeloproliferative disorders. TG101348 is a small molecule inhibitor of JAK2 (IC50 = 6 nM) and the related kinases FLT3 (IC50 = 25 nM) and RET (IC50 = 17 nM) with significantly less potent activity against JAK3 (IC50 = 169 nM).{23418} It can inhibit the growth of Ba/F3 cells expressing JAK2V617F or MPLW515L mutations with an IC50 value of 200 nM.{23418} Phase I clinical trial results that focused on safety and efficacy of TG101348 in patients with high- or intermediate-risk primary or post-polycythemia vera/essential thrombocythemia myelofibrosis have been published.{27682}
Brand:CaymanSKU:-
Prostaglandin E2 (PGE2) evokes distinct responses through four different ‘E prostanoid’ (EP) receptors. EP2 is a G protein-coupled receptor that has diverse roles, including those in cancer, inflammation, and neuroprotection.{11615,23324,26528} TG4-155 is a brain penetrant EP2 antagonist (KB = 2.4 nM) that is over 1000-fold less effective at EP4 (KB = 11.4 µM) and a panel of other receptors and channels.{28703,28704} It blocks the induced expression of inflammatory markers in microglial cells treated with the selective EP2 agonist butaprost (Item No. 13740) alone or with LPS and IFNγ.{28703,23348} TG4-155 significantly reduces neurodegeneration in a mouse model of status epilepticus, induced by pilocarpine (Item No. 14487).{28703} It inhibits proliferation, invasion, and inflammatory cytokine expression in cancer cells treated with butaprost.{28704}
Brand:CaymanSKU:-Available on backorder
Prostaglandin E2 (PGE2) evokes distinct responses through four different ‘E prostanoid’ (EP) receptors. EP2 is a G protein-coupled receptor that has diverse roles, including those in cancer, inflammation, and neuroprotection.{11615,23324,26528} TG4-155 is a brain penetrant EP2 antagonist (KB = 2.4 nM) that is over 1000-fold less effective at EP4 (KB = 11.4 µM) and a panel of other receptors and channels.{28703,28704} It blocks the induced expression of inflammatory markers in microglial cells treated with the selective EP2 agonist butaprost (Item No. 13740) alone or with LPS and IFNγ.{28703,23348} TG4-155 significantly reduces neurodegeneration in a mouse model of status epilepticus, induced by pilocarpine (Item No. 14487).{28703} It inhibits proliferation, invasion, and inflammatory cytokine expression in cancer cells treated with butaprost.{28704}
Brand:CaymanSKU:-Available on backorder
Prostaglandin E2 (PGE2) evokes distinct responses through four different ‘E prostanoid’ (EP) receptors. EP2 is a G protein-coupled receptor that has diverse roles, including those in cancer, inflammation, and neuroprotection.{11615,23324,26528} TG4-155 is a brain penetrant EP2 antagonist (KB = 2.4 nM) that is over 1000-fold less effective at EP4 (KB = 11.4 µM) and a panel of other receptors and channels.{28703,28704} It blocks the induced expression of inflammatory markers in microglial cells treated with the selective EP2 agonist butaprost (Item No. 13740) alone or with LPS and IFNγ.{28703,23348} TG4-155 significantly reduces neurodegeneration in a mouse model of status epilepticus, induced by pilocarpine (Item No. 14487).{28703} It inhibits proliferation, invasion, and inflammatory cytokine expression in cancer cells treated with butaprost.{28704}
Brand:CaymanSKU:-Available on backorder
Prostaglandin E2 (PGE2) evokes distinct responses through four different ‘E prostanoid’ (EP) receptors. EP2 is a G protein-coupled receptor that has diverse roles, including those in cancer, inflammation, and neuroprotection.{11615,23324,26528} TG4-155 is a brain penetrant EP2 antagonist (KB = 2.4 nM) that is over 1000-fold less effective at EP4 (KB = 11.4 µM) and a panel of other receptors and channels.{28703,28704} It blocks the induced expression of inflammatory markers in microglial cells treated with the selective EP2 agonist butaprost (Item No. 13740) alone or with LPS and IFNγ.{28703,23348} TG4-155 significantly reduces neurodegeneration in a mouse model of status epilepticus, induced by pilocarpine (Item No. 14487).{28703} It inhibits proliferation, invasion, and inflammatory cytokine expression in cancer cells treated with butaprost.{28704}
Brand:CaymanSKU:-Available on backorder
TG6-10-1 is a potent antagonist of E prostanoid receptor 2 (EP2; Kb = 17.8 nM in C6 glioma cells overexpressing human EP2).{40354} It is 300-, 25-, and 10-fold selective for EP2 over other prostanoid receptors, including human EP3-4, FP and TP, and DP1 receptors, respectively. TG6-10-1 is also selective for EP2 over a panel of 40 enzymes, ion channels, receptors, and neurotransmitter transporters (IC50s >10 μM). In vivo, TG6-10-1 increases survival, decreases weight loss, prevents induction of IL-1β, IL-6, TNF-α, and MCP-1/CCL2 mRNA, and inhibits neuronal cell death in the hippocampus in mouse and rat models of status epilepticus induced by pilocarpine (Item No. 14487) and diisopropyl fluorophosphate, respectively.{40354,40355}
Brand:CaymanSKU:23444 - 1 mgAvailable on backorder
TG6-10-1 is a potent antagonist of E prostanoid receptor 2 (EP2; Kb = 17.8 nM in C6 glioma cells overexpressing human EP2).{40354} It is 300-, 25-, and 10-fold selective for EP2 over other prostanoid receptors, including human EP3-4, FP and TP, and DP1 receptors, respectively. TG6-10-1 is also selective for EP2 over a panel of 40 enzymes, ion channels, receptors, and neurotransmitter transporters (IC50s >10 μM). In vivo, TG6-10-1 increases survival, decreases weight loss, prevents induction of IL-1β, IL-6, TNF-α, and MCP-1/CCL2 mRNA, and inhibits neuronal cell death in the hippocampus in mouse and rat models of status epilepticus induced by pilocarpine (Item No. 14487) and diisopropyl fluorophosphate, respectively.{40354,40355}
Brand:CaymanSKU:23444 - 10 mgAvailable on backorder
TG6-10-1 is a potent antagonist of E prostanoid receptor 2 (EP2; Kb = 17.8 nM in C6 glioma cells overexpressing human EP2).{40354} It is 300-, 25-, and 10-fold selective for EP2 over other prostanoid receptors, including human EP3-4, FP and TP, and DP1 receptors, respectively. TG6-10-1 is also selective for EP2 over a panel of 40 enzymes, ion channels, receptors, and neurotransmitter transporters (IC50s >10 μM). In vivo, TG6-10-1 increases survival, decreases weight loss, prevents induction of IL-1β, IL-6, TNF-α, and MCP-1/CCL2 mRNA, and inhibits neuronal cell death in the hippocampus in mouse and rat models of status epilepticus induced by pilocarpine (Item No. 14487) and diisopropyl fluorophosphate, respectively.{40354,40355}
Brand:CaymanSKU:23444 - 25 mgAvailable on backorder
TG6-10-1 is a potent antagonist of E prostanoid receptor 2 (EP2; Kb = 17.8 nM in C6 glioma cells overexpressing human EP2).{40354} It is 300-, 25-, and 10-fold selective for EP2 over other prostanoid receptors, including human EP3-4, FP and TP, and DP1 receptors, respectively. TG6-10-1 is also selective for EP2 over a panel of 40 enzymes, ion channels, receptors, and neurotransmitter transporters (IC50s >10 μM). In vivo, TG6-10-1 increases survival, decreases weight loss, prevents induction of IL-1β, IL-6, TNF-α, and MCP-1/CCL2 mRNA, and inhibits neuronal cell death in the hippocampus in mouse and rat models of status epilepticus induced by pilocarpine (Item No. 14487) and diisopropyl fluorophosphate, respectively.{40354,40355}
Brand:CaymanSKU:23444 - 5 mgAvailable on backorder
Prostaglandin E2 (PGE2; Item No. 14010) evokes distinct responses through four different ‘E prostanoid’ (EP) receptors. EP2 is a G protein-coupled receptor that has diverse roles, including those in cancer, inflammation, and neuroprotection.{11615,23324,26528} TG6-129 is an antagonist of the EP2 receptor, suppressing PGE2-induced elevation of cAMP in cells expressing EP2 with an IC50 value of 1.6 µM.{30786} It is without effect on EP4, DP1, IP, and β2-adrenergic receptors. TG6-129 reduces the expression of COX-2, IL-1β, IL-12, IL-23, IL-6, and TNF-α induced by the EP2-selective agonist butaprost (Item No. 13740) in P388D1 macrophages.{30786} It has low cell cytotoxicity (CC50 = 326 µM), prolonged plasma half-life, and does not cross the blood-brain barrier.{30786}
Brand:CaymanSKU:-Available on backorder
Prostaglandin E2 (PGE2; Item No. 14010) evokes distinct responses through four different ‘E prostanoid’ (EP) receptors. EP2 is a G protein-coupled receptor that has diverse roles, including those in cancer, inflammation, and neuroprotection.{11615,23324,26528} TG6-129 is an antagonist of the EP2 receptor, suppressing PGE2-induced elevation of cAMP in cells expressing EP2 with an IC50 value of 1.6 µM.{30786} It is without effect on EP4, DP1, IP, and β2-adrenergic receptors. TG6-129 reduces the expression of COX-2, IL-1β, IL-12, IL-23, IL-6, and TNF-α induced by the EP2-selective agonist butaprost (Item No. 13740) in P388D1 macrophages.{30786} It has low cell cytotoxicity (CC50 = 326 µM), prolonged plasma half-life, and does not cross the blood-brain barrier.{30786}
Brand:CaymanSKU:-Available on backorder
Prostaglandin E2 (PGE2; Item No. 14010) evokes distinct responses through four different ‘E prostanoid’ (EP) receptors. EP2 is a G protein-coupled receptor that has diverse roles, including those in cancer, inflammation, and neuroprotection.{11615,23324,26528} TG6-129 is an antagonist of the EP2 receptor, suppressing PGE2-induced elevation of cAMP in cells expressing EP2 with an IC50 value of 1.6 µM.{30786} It is without effect on EP4, DP1, IP, and β2-adrenergic receptors. TG6-129 reduces the expression of COX-2, IL-1β, IL-12, IL-23, IL-6, and TNF-α induced by the EP2-selective agonist butaprost (Item No. 13740) in P388D1 macrophages.{30786} It has low cell cytotoxicity (CC50 = 326 µM), prolonged plasma half-life, and does not cross the blood-brain barrier.{30786}
Brand:CaymanSKU:-Available on backorder
TGN 020 is an aquaporin-4 (AQP4) inhibitor (IC50 = 3.1 μM in X. laevis oocytes transfected with AQP4).{60036} It reduces brain edema and cortical infarction size in a mouse model of transient focal cerebral ischemia induced by middle cerebral artery occlusion (MCAO) when administered at a dose of 200 mg/kg.{60037} TGN 020 (200 mg/kg every 6 hours) reduces bronchoalveolar lavage fluid (BALF) IL-1α, IL-1β, IL-6, TNF-α, IL-23, and IL-17A levels and neutrophil infiltration, as well as increases survival, in a mouse model of LPS-induced acute lung injury.{60038}
Brand:CaymanSKU:30955 - 10 mgAvailable on backorder
TGN 020 is an aquaporin-4 (AQP4) inhibitor (IC50 = 3.1 μM in X. laevis oocytes transfected with AQP4).{60036} It reduces brain edema and cortical infarction size in a mouse model of transient focal cerebral ischemia induced by middle cerebral artery occlusion (MCAO) when administered at a dose of 200 mg/kg.{60037} TGN 020 (200 mg/kg every 6 hours) reduces bronchoalveolar lavage fluid (BALF) IL-1α, IL-1β, IL-6, TNF-α, IL-23, and IL-17A levels and neutrophil infiltration, as well as increases survival, in a mouse model of LPS-induced acute lung injury.{60038}
Brand:CaymanSKU:30955 - 100 mgAvailable on backorder
TGN 020 is an aquaporin-4 (AQP4) inhibitor (IC50 = 3.1 μM in X. laevis oocytes transfected with AQP4).{60036} It reduces brain edema and cortical infarction size in a mouse model of transient focal cerebral ischemia induced by middle cerebral artery occlusion (MCAO) when administered at a dose of 200 mg/kg.{60037} TGN 020 (200 mg/kg every 6 hours) reduces bronchoalveolar lavage fluid (BALF) IL-1α, IL-1β, IL-6, TNF-α, IL-23, and IL-17A levels and neutrophil infiltration, as well as increases survival, in a mouse model of LPS-induced acute lung injury.{60038}
Brand:CaymanSKU:30955 - 25 mgAvailable on backorder
TGN 020 is an aquaporin-4 (AQP4) inhibitor (IC50 = 3.1 μM in X. laevis oocytes transfected with AQP4).{60036} It reduces brain edema and cortical infarction size in a mouse model of transient focal cerebral ischemia induced by middle cerebral artery occlusion (MCAO) when administered at a dose of 200 mg/kg.{60037} TGN 020 (200 mg/kg every 6 hours) reduces bronchoalveolar lavage fluid (BALF) IL-1α, IL-1β, IL-6, TNF-α, IL-23, and IL-17A levels and neutrophil infiltration, as well as increases survival, in a mouse model of LPS-induced acute lung injury.{60038}
Brand:CaymanSKU:30955 - 50 mgAvailable on backorder
TGR5, also known as GPBAR1, is a G protein-coupled receptor (GPCR) belonging to the bile acid receptor subclass.{47562} It is a plasma membrane-bound transmembrane protein and is primarily expressed in spleen and placenta. TGR5 is activated by the endogenous bile acids cholic acid (Item No. 20250), lithocholic acid (Item No. 20253), taurolithocholic acid (Item No. 17275), deoxycholic acid (Item Nos. 20756 | 18231), and chenodeoxycholic acid (Item No. 10011286), among others. Activation of TGR5 by the synthetic agonist INT-777 (Item No. 17678) decreases plasma triglyceride levels and urinary levels of albumin, thiobarbituric acid reactive substances (TBARS), and hydrogen peroxide, as well as prevents diabetic nephropathy, in a db/db mouse model of diabetes.{47563} Activation of TGR5 by INT-777 also prevents hepatic steatosis and increases in fat, liver, and brown adipose tissue mass in a mouse model of diet-induced obesity.{24940} Transgenic overexpression of TGR5 increases glucose tolerance, as well as plasma levels of insulin and glucagon-like peptide 1 (GLP-1), during an oral glucose tolerance test in mice fed a high-fat diet. Increased expression of TGR5 has been found in tissue samples from patients with intestinal-type adenocarcinoma or intestinal metaplasia, but not healthy mucosa.{47564} TGR5 protein levels are also increased in patient-derived Barrett’s esophagous and esophageal adenocarcinoma tissues.{47565} Cayman’s TGR5 (C-Term) Polyclonal Antibody can be used for Western blot and immunohistochemistry (IHC) applications. The antibody recognizes the C-terminal region of TGR5 from human samples.
Brand:CaymanSKU:27343 - 500 µlAvailable on backorder
Immunogen: Synthetic peptide from the C-terminal region of human TGR5 • Host: Rabbit • Species Reactivity: (+) Human • Applications: IHC and WB
Brand:CaymanSKU:27343- 500 µlAvailable on backorder
Immunogen: Synthetic peptide from the C-terminal region of human TGR5 • Host: Rabbit • Species Reactivity: (+) Human • Applications: IHC and WB
Brand:CaymanSKU:27343- 500 µl
Bile acids are a diverse class of amphipathic molecules originally formed in liver and modified by microorganisms in the intestine. In addition to their conventional role in dietary lipid absorption, bile acids have been recognized as signaling molecules that regulate the synthesis and metabolism of bile acids, glucose homeostasis, and energy expenditure. The G protein-coupled membrane receptor for bile acid (TGR5 or GP-BAR1) is the most extensively studied receptor for bile acids. Activation of TGR5 by agonists leads to increase in intracellular cAMP, which signals the reduction of inflammatory cytokine expression in macrophage, increase of glucagon-like peptide (GLP-1) secretion in intestine, and energy expenditure in brown adipose tissue and muscle. Therefore, it has been an interesting drug target in metabolism and inflammation. Cayman’s TGR5 (GP-BAR1) Reporter Assay Kit consists of a 96-well plate coated with a transfection complex containing DNA constructs for expressing TGR5 and a cAMP response element regulated secreted alkaline phosphatase (SEAP) reporter (TGR5 Reverse Transfection Strip Plate). Cells grown on the transfection complex will express TGR5 at the cell surface within 24 hours. Binding of agonists to TGR5 initiates a signal transduction cascade through the GαS and adenylate cyclase pathway resulting in the expression of SEAP which is secreted into the cell culture medium. Aliquots of culture medium are collected at 6-8 hours after stimulation, and SEAP activity is measured following the addition of a luminescence-based alkaline phosphatase substrate provided in the kit. The kit is easy to use and can be readily applied to high-throughput screening for therapeutic compounds regulating activation of TGR5. A selective synthetic agonist, the TGR5 Receptor Agonist (3-[2-chlorophenyl]-N-[4-chlorophenyl]-N,5-dimethyl-4-isoxazolecarboxamide), is included in the kit for use as a positive control.{27533} The kit provides sufficient reagent to measure SEAP activity at three time points using the three included white assay plates.
Brand:CaymanSKU:601440 - 96 wellsAvailable on backorder
TGR5 receptor agonist is an agonist of the bile acid G protein-coupled receptor TGR5 (EC50s = 31.6-158.5 nM in cell-based assays).{27533} It stimulates cAMP formation in HEK293 cells expressing TGR5 (EC50 = 2.3 pM).{27534} TGR5 receptor agonist (1 mg/kg) increases glucagon-like peptide 1 (GLP-1) secretion and decreases glucose levels in the hepatic portal vein in dogs when administered in combination with glucose.{27533} It also inhibits the cytochrome P450 (CYP) isozymes CYP2C19 and CYP3A4 (IC50s = 316.2 and 1,259 nM, respectively).
Brand:CaymanSKU:- TGR5 receptor agonist is an agonist of the bile acid G protein-coupled receptor TGR5 (EC50s = 31.6-158.5 nM in cell-based assays).{27533} It stimulates cAMP formation in HEK293 cells expressing TGR5 (EC50 = 2.3 pM).{27534} TGR5 receptor agonist (1 mg/kg) increases glucagon-like peptide 1 (GLP-1) secretion and decreases glucose levels in the hepatic portal vein in dogs when administered in combination with glucose.{27533} It also inhibits the cytochrome P450 (CYP) isozymes CYP2C19 and CYP3A4 (IC50s = 316.2 and 1,259 nM, respectively).
Brand:CaymanSKU:- TGR5 receptor agonist is an agonist of the bile acid G protein-coupled receptor TGR5 (EC50s = 31.6-158.5 nM in cell-based assays).{27533} It stimulates cAMP formation in HEK293 cells expressing TGR5 (EC50 = 2.3 pM).{27534} TGR5 receptor agonist (1 mg/kg) increases glucagon-like peptide 1 (GLP-1) secretion and decreases glucose levels in the hepatic portal vein in dogs when administered in combination with glucose.{27533} It also inhibits the cytochrome P450 (CYP) isozymes CYP2C19 and CYP3A4 (IC50s = 316.2 and 1,259 nM, respectively).
Brand:CaymanSKU:- TGR5 receptor agonist is an agonist of the bile acid G protein-coupled receptor TGR5 (EC50s = 31.6-158.5 nM in cell-based assays).{27533} It stimulates cAMP formation in HEK293 cells expressing TGR5 (EC50 = 2.3 pM).{27534} TGR5 receptor agonist (1 mg/kg) increases glucagon-like peptide 1 (GLP-1) secretion and decreases glucose levels in the hepatic portal vein in dogs when administered in combination with glucose.{27533} It also inhibits the cytochrome P450 (CYP) isozymes CYP2C19 and CYP3A4 (IC50s = 316.2 and 1,259 nM, respectively).
Brand:CaymanSKU:-
Phosphatidylinositol 3-kinase (PI3K) catalyzes the phosphorylation of phosphatidylinositol at the 3 position to produce the second messengers phosphatidylinositol-3,4-bisphosphate (PtdIns-(3,4)-P2) and PtdIns-(3,4,5)-P3.{8039,12235,13740} Class 1 PI3Ks are composed of a p110 catalytic subunit, of which there are 4 isoforms (p110α, p110β, p110δ, and p100γ), and a p85 regulatory subunit.{13740} TGX-221 is a potent, selective, and cell permeable inhibitor of PI3K p110β.{13192} Inhibition appears to occur at the ATP binding site based on the observed increase in IC50 value from 5 to ~50 nM at ATP concentrations of 50 µM and 1 mM, respectively. TGX-221 inhibits PtdIns-(3,4)-P2 production in platelets with an IC50 value of 50 nM.{13192} Selective inhibition of PI3K p110β results in defective platelet thrombus formation and defines PI3K as a target for antithrombotic therapy.{13192}
Brand:CaymanSKU:10007349 - 1 mgAvailable on backorder
Phosphatidylinositol 3-kinase (PI3K) catalyzes the phosphorylation of phosphatidylinositol at the 3 position to produce the second messengers phosphatidylinositol-3,4-bisphosphate (PtdIns-(3,4)-P2) and PtdIns-(3,4,5)-P3.{8039,12235,13740} Class 1 PI3Ks are composed of a p110 catalytic subunit, of which there are 4 isoforms (p110α, p110β, p110δ, and p100γ), and a p85 regulatory subunit.{13740} TGX-221 is a potent, selective, and cell permeable inhibitor of PI3K p110β.{13192} Inhibition appears to occur at the ATP binding site based on the observed increase in IC50 value from 5 to ~50 nM at ATP concentrations of 50 µM and 1 mM, respectively. TGX-221 inhibits PtdIns-(3,4)-P2 production in platelets with an IC50 value of 50 nM.{13192} Selective inhibition of PI3K p110β results in defective platelet thrombus formation and defines PI3K as a target for antithrombotic therapy.{13192}
Brand:CaymanSKU:10007349 - 10 mgAvailable on backorder
Phosphatidylinositol 3-kinase (PI3K) catalyzes the phosphorylation of phosphatidylinositol at the 3 position to produce the second messengers phosphatidylinositol-3,4-bisphosphate (PtdIns-(3,4)-P2) and PtdIns-(3,4,5)-P3.{8039,12235,13740} Class 1 PI3Ks are composed of a p110 catalytic subunit, of which there are 4 isoforms (p110α, p110β, p110δ, and p100γ), and a p85 regulatory subunit.{13740} TGX-221 is a potent, selective, and cell permeable inhibitor of PI3K p110β.{13192} Inhibition appears to occur at the ATP binding site based on the observed increase in IC50 value from 5 to ~50 nM at ATP concentrations of 50 µM and 1 mM, respectively. TGX-221 inhibits PtdIns-(3,4)-P2 production in platelets with an IC50 value of 50 nM.{13192} Selective inhibition of PI3K p110β results in defective platelet thrombus formation and defines PI3K as a target for antithrombotic therapy.{13192}
Brand:CaymanSKU:10007349 - 5 mgAvailable on backorder
Phosphatidylinositol 3-kinase (PI3K) catalyzes the phosphorylation of phosphatidylinositol at the 3 position to produce the second messengers phosphatidylinositol-3,4-bisphosphate (PtdIns-(3,4)-P2) and PtdIns-(3,4,5)-P3.{8039,12235,13740} Class 1 PI3Ks are composed of a p110 catalytic subunit, of which there are 4 isoforms (p110α, p110β, p110δ, and p100γ), and a p85 regulatory subunit.{13740} TGX-221 is a potent, selective, and cell permeable inhibitor of PI3K p110β.{13192} Inhibition appears to occur at the ATP binding site based on the observed increase in IC50 value from 5 to ~50 nM at ATP concentrations of 50 µM and 1 mM, respectively. TGX-221 inhibits PtdIns-(3,4)-P2 production in platelets with an IC50 value of 50 nM.{13192} Selective inhibition of PI3K p110β results in defective platelet thrombus formation and defines PI3K as a target for antithrombotic therapy.{13192}
Brand:CaymanSKU:10007349 - 500 µgAvailable on backorder
TH-302 is a hypoxia-activated prodrug and DNA alkylating agent with anticancer activity.{43360} It is selectively cytotoxic to H460 human non-small cell lung cancer (NSCLC) cells grown under hypoxic over normoxic conditions (IC50s = 0.019 and 5.1 μM, respectively).{43360} Under hypoxic conditions, TH-302 undergoes a one-electron reduction to form an active radical intermediate that is then further reduced to form a DNA-intercalating hydroxylamine. Under normoxic conditions, the radical intermediate is quenched and induces reformation of the inactive nitroazole prodrug. TH-302 reduces survival of H460 and HT-29 cells in a clonogenic assay (IC50s = 0.2 and 0.2 μM, respectively). In vivo, TH-302 (33 mg/kg per day) inhibits primary tumor growth by 41% in an MIA PaCa-2-RFP mouse orthotopic xenograft model. It inhibits tumor growth by greater than 40% in Calu-6 NSCLC, H82 small cell lung, A375 melanoma, PC-3 prostate, and BxPC-3 pancreatic cancer mouse xenograft models when administered at 50 mg/kg.{43361}
Brand:CaymanSKU:22195 -Out of stock
TH-302 is a hypoxia-activated prodrug and DNA alkylating agent with anticancer activity.{43360} It is selectively cytotoxic to H460 human non-small cell lung cancer (NSCLC) cells grown under hypoxic over normoxic conditions (IC50s = 0.019 and 5.1 μM, respectively).{43360} Under hypoxic conditions, TH-302 undergoes a one-electron reduction to form an active radical intermediate that is then further reduced to form a DNA-intercalating hydroxylamine. Under normoxic conditions, the radical intermediate is quenched and induces reformation of the inactive nitroazole prodrug. TH-302 reduces survival of H460 and HT-29 cells in a clonogenic assay (IC50s = 0.2 and 0.2 μM, respectively). In vivo, TH-302 (33 mg/kg per day) inhibits primary tumor growth by 41% in an MIA PaCa-2-RFP mouse orthotopic xenograft model. It inhibits tumor growth by greater than 40% in Calu-6 NSCLC, H82 small cell lung, A375 melanoma, PC-3 prostate, and BxPC-3 pancreatic cancer mouse xenograft models when administered at 50 mg/kg.{43361}
Brand:CaymanSKU:22195 -Out of stock
TH-302 is a hypoxia-activated prodrug and DNA alkylating agent with anticancer activity.{43360} It is selectively cytotoxic to H460 human non-small cell lung cancer (NSCLC) cells grown under hypoxic over normoxic conditions (IC50s = 0.019 and 5.1 μM, respectively).{43360} Under hypoxic conditions, TH-302 undergoes a one-electron reduction to form an active radical intermediate that is then further reduced to form a DNA-intercalating hydroxylamine. Under normoxic conditions, the radical intermediate is quenched and induces reformation of the inactive nitroazole prodrug. TH-302 reduces survival of H460 and HT-29 cells in a clonogenic assay (IC50s = 0.2 and 0.2 μM, respectively). In vivo, TH-302 (33 mg/kg per day) inhibits primary tumor growth by 41% in an MIA PaCa-2-RFP mouse orthotopic xenograft model. It inhibits tumor growth by greater than 40% in Calu-6 NSCLC, H82 small cell lung, A375 melanoma, PC-3 prostate, and BxPC-3 pancreatic cancer mouse xenograft models when administered at 50 mg/kg.{43361}
Brand:CaymanSKU:22195 -Out of stock
TH-302 is a hypoxia-activated prodrug and DNA alkylating agent with anticancer activity.{43360} It is selectively cytotoxic to H460 human non-small cell lung cancer (NSCLC) cells grown under hypoxic over normoxic conditions (IC50s = 0.019 and 5.1 μM, respectively).{43360} Under hypoxic conditions, TH-302 undergoes a one-electron reduction to form an active radical intermediate that is then further reduced to form a DNA-intercalating hydroxylamine. Under normoxic conditions, the radical intermediate is quenched and induces reformation of the inactive nitroazole prodrug. TH-302 reduces survival of H460 and HT-29 cells in a clonogenic assay (IC50s = 0.2 and 0.2 μM, respectively). In vivo, TH-302 (33 mg/kg per day) inhibits primary tumor growth by 41% in an MIA PaCa-2-RFP mouse orthotopic xenograft model. It inhibits tumor growth by greater than 40% in Calu-6 NSCLC, H82 small cell lung, A375 melanoma, PC-3 prostate, and BxPC-3 pancreatic cancer mouse xenograft models when administered at 50 mg/kg.{43361}
Brand:CaymanSKU:22195 -Out of stock
Human mutT homolog (MTH1) is a nucleotide pool sanitizing enzyme that cleaves oxidized nucleotides (dNTPs) to prevent incorporation of damaged bases during DNA replication. Cancer cells rely on MTH1 activity in order to avoid cell death. TH287 is an MTH1 inhibitor (IC50 = 0.8 nM) that selectively kills cancer cell lines (IC50s = 0.8-3.06 µM) without significant cytotoxicity towards primary or immortalized cells (IC50s = ≥20 µM).{29777} At up to 100 µM it does not show significant effect towards the related nudix hydrolase protein family members MTH2, NUDT5, NUDT12, NUDT14, and NUDT16, as well as other proteins with known nucleoside triphosphate pyrophosphatase activity (dCTPase, dUTPase, and ITPA).{29777}
Brand:CaymanSKU:-Available on backorder
Human mutT homolog (MTH1) is a nucleotide pool sanitizing enzyme that cleaves oxidized nucleotides (dNTPs) to prevent incorporation of damaged bases during DNA replication. Cancer cells rely on MTH1 activity in order to avoid cell death. TH287 is an MTH1 inhibitor (IC50 = 0.8 nM) that selectively kills cancer cell lines (IC50s = 0.8-3.06 µM) without significant cytotoxicity towards primary or immortalized cells (IC50s = ≥20 µM).{29777} At up to 100 µM it does not show significant effect towards the related nudix hydrolase protein family members MTH2, NUDT5, NUDT12, NUDT14, and NUDT16, as well as other proteins with known nucleoside triphosphate pyrophosphatase activity (dCTPase, dUTPase, and ITPA).{29777}
Brand:CaymanSKU:-Available on backorder
Human mutT homolog (MTH1) is a nucleotide pool sanitizing enzyme that cleaves oxidized nucleotides (dNTPs) to prevent incorporation of damaged bases during DNA replication. Cancer cells rely on MTH1 activity in order to avoid cell death. TH287 is an MTH1 inhibitor (IC50 = 0.8 nM) that selectively kills cancer cell lines (IC50s = 0.8-3.06 µM) without significant cytotoxicity towards primary or immortalized cells (IC50s = ≥20 µM).{29777} At up to 100 µM it does not show significant effect towards the related nudix hydrolase protein family members MTH2, NUDT5, NUDT12, NUDT14, and NUDT16, as well as other proteins with known nucleoside triphosphate pyrophosphatase activity (dCTPase, dUTPase, and ITPA).{29777}
Brand:CaymanSKU:-Available on backorder
Human mutT homolog (MTH1) is a nucleotide pool sanitizing enzyme that cleaves oxidized nucleotides (dNTPs) to prevent incorporation of damaged bases during DNA replication. Cancer cells rely on MTH1 activity in order to avoid cell death. TH588 is an MTH1 inhibitor (IC50 = 5 nM) with improved metabolic stability over TH287 (Item No. 18132).{29777} It selectively kills cancer cell lines (IC50s = 2.48-6.37 µM) without significant cytotoxicity towards primary or immortalized cells (IC50s = ≥20 µM) and demonstrates >1,000-fold selectivity for MTH1 over the related nudix hydrolase protein family members MTH2, NUDT5, NUDT12, NUDT14, and NUDT16, as well as other proteins with known nucleoside triphosphate pyrophosphatase activity (dCTPase, dUTPase, and ITPA).{29777} At 30 mg/kg, TH588 induces incorporation of oxidized dNTPs in cancer cells, leading to DNA damage and cell death in B-RafV600E melanoma, SW480 colorectal, or MCF-7 breast tumor mouse xenografts.{29777}
Brand:CaymanSKU:-Available on backorder
Human mutT homolog (MTH1) is a nucleotide pool sanitizing enzyme that cleaves oxidized nucleotides (dNTPs) to prevent incorporation of damaged bases during DNA replication. Cancer cells rely on MTH1 activity in order to avoid cell death. TH588 is an MTH1 inhibitor (IC50 = 5 nM) with improved metabolic stability over TH287 (Item No. 18132).{29777} It selectively kills cancer cell lines (IC50s = 2.48-6.37 µM) without significant cytotoxicity towards primary or immortalized cells (IC50s = ≥20 µM) and demonstrates >1,000-fold selectivity for MTH1 over the related nudix hydrolase protein family members MTH2, NUDT5, NUDT12, NUDT14, and NUDT16, as well as other proteins with known nucleoside triphosphate pyrophosphatase activity (dCTPase, dUTPase, and ITPA).{29777} At 30 mg/kg, TH588 induces incorporation of oxidized dNTPs in cancer cells, leading to DNA damage and cell death in B-RafV600E melanoma, SW480 colorectal, or MCF-7 breast tumor mouse xenografts.{29777}
Brand:CaymanSKU:-Available on backorder
Human mutT homolog (MTH1) is a nucleotide pool sanitizing enzyme that cleaves oxidized nucleotides (dNTPs) to prevent incorporation of damaged bases during DNA replication. Cancer cells rely on MTH1 activity in order to avoid cell death. TH588 is an MTH1 inhibitor (IC50 = 5 nM) with improved metabolic stability over TH287 (Item No. 18132).{29777} It selectively kills cancer cell lines (IC50s = 2.48-6.37 µM) without significant cytotoxicity towards primary or immortalized cells (IC50s = ≥20 µM) and demonstrates >1,000-fold selectivity for MTH1 over the related nudix hydrolase protein family members MTH2, NUDT5, NUDT12, NUDT14, and NUDT16, as well as other proteins with known nucleoside triphosphate pyrophosphatase activity (dCTPase, dUTPase, and ITPA).{29777} At 30 mg/kg, TH588 induces incorporation of oxidized dNTPs in cancer cells, leading to DNA damage and cell death in B-RafV600E melanoma, SW480 colorectal, or MCF-7 breast tumor mouse xenografts.{29777}
Brand:CaymanSKU:-Available on backorder
Human mutT homolog (MTH1) is a nucleotide pool sanitizing enzyme that cleaves oxidized nucleotides (dNTPs) to prevent incorporation of damaged bases during DNA replication. Cancer cells rely on MTH1 activity in order to avoid cell death. TH588 is an MTH1 inhibitor (IC50 = 5 nM) with improved metabolic stability over TH287 (Item No. 18132).{29777} It selectively kills cancer cell lines (IC50s = 2.48-6.37 µM) without significant cytotoxicity towards primary or immortalized cells (IC50s = ≥20 µM) and demonstrates >1,000-fold selectivity for MTH1 over the related nudix hydrolase protein family members MTH2, NUDT5, NUDT12, NUDT14, and NUDT16, as well as other proteins with known nucleoside triphosphate pyrophosphatase activity (dCTPase, dUTPase, and ITPA).{29777} At 30 mg/kg, TH588 induces incorporation of oxidized dNTPs in cancer cells, leading to DNA damage and cell death in B-RafV600E melanoma, SW480 colorectal, or MCF-7 breast tumor mouse xenografts.{29777}
Brand:CaymanSKU:-Available on backorder
In cells, sarco/endoplasmic calcium ATPases (SERCAs) transport free calcium into the sarcoplasmic and endoplasmic reticula, lowering intracellular calcium levels to stop signaling through this cation. Thapsigargin is a non-competitive, cell permeable inhibitor of calcium transport by SERCAs (IC50 values are cell type-dependent and range from ~2-80 nM).{19971,19972} Inhibition of SERCAs leads to an increase in intracellular calcium, which has been linked to cell activation, release of histamine from mast cells, and increased proliferation of certain types of cancer cells.{19971,19965,19970} In vivo, thapsigargin and related sesquiterpene lactones have anti-inflammatory and anti-cancer effects.{19977,19975}
Brand:CaymanSKU:10522 - 1 mgAvailable on backorder
In cells, sarco/endoplasmic calcium ATPases (SERCAs) transport free calcium into the sarcoplasmic and endoplasmic reticula, lowering intracellular calcium levels to stop signaling through this cation. Thapsigargin is a non-competitive, cell permeable inhibitor of calcium transport by SERCAs (IC50 values are cell type-dependent and range from ~2-80 nM).{19971,19972} Inhibition of SERCAs leads to an increase in intracellular calcium, which has been linked to cell activation, release of histamine from mast cells, and increased proliferation of certain types of cancer cells.{19971,19965,19970} In vivo, thapsigargin and related sesquiterpene lactones have anti-inflammatory and anti-cancer effects.{19977,19975}
Brand:CaymanSKU:10522 - 10 mgAvailable on backorder