Chemicals
Showing 10501–10650 of 41137 results
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AZ 7371 is a non-covalent inhibitor of decaprenylphosphoryl-β-D-ribose 2’-epimerase (DprE1; IC50 = 10 nM), an enzyme involved in mycobacterial cell wall biogenesis.{32839} It inhibits wild-type M. smegmatis DprE1 and DprE1 harboring the drug-resistance mutation C394G (IC50 = 0.01 µM for both) but not the Y321H mutation (IC50 = >10 µM).{54377} AZ 7371 is active against wild-type M. tuberculosis DprE1 (MIC = 1.56 µM) and M. tuberculosis harboring C387S or C387G mutations (MICs = 0.39 and 0.78 µM, respectively), which confer resistance to the antibiotic BTZ043 (Item No. 22930), but not the Y314H mutation (MIC = >200 µM). It is selective for these targets over Gram-positive and Gram-negative bacteria but does inhibit phosphodiesterase 6 (PDE6; IC50 = 4 µM).
Brand:CaymanSKU:-Available on backorder
AZ 7371 is a non-covalent inhibitor of decaprenylphosphoryl-β-D-ribose 2’-epimerase (DprE1; IC50 = 10 nM), an enzyme involved in mycobacterial cell wall biogenesis.{32839} It inhibits wild-type M. smegmatis DprE1 and DprE1 harboring the drug-resistance mutation C394G (IC50 = 0.01 µM for both) but not the Y321H mutation (IC50 = >10 µM).{54377} AZ 7371 is active against wild-type M. tuberculosis DprE1 (MIC = 1.56 µM) and M. tuberculosis harboring C387S or C387G mutations (MICs = 0.39 and 0.78 µM, respectively), which confer resistance to the antibiotic BTZ043 (Item No. 22930), but not the Y314H mutation (MIC = >200 µM). It is selective for these targets over Gram-positive and Gram-negative bacteria but does inhibit phosphodiesterase 6 (PDE6; IC50 = 4 µM).
Brand:CaymanSKU:-Available on backorder
AZ 7371 is a non-covalent inhibitor of decaprenylphosphoryl-β-D-ribose 2’-epimerase (DprE1; IC50 = 10 nM), an enzyme involved in mycobacterial cell wall biogenesis.{32839} It inhibits wild-type M. smegmatis DprE1 and DprE1 harboring the drug-resistance mutation C394G (IC50 = 0.01 µM for both) but not the Y321H mutation (IC50 = >10 µM).{54377} AZ 7371 is active against wild-type M. tuberculosis DprE1 (MIC = 1.56 µM) and M. tuberculosis harboring C387S or C387G mutations (MICs = 0.39 and 0.78 µM, respectively), which confer resistance to the antibiotic BTZ043 (Item No. 22930), but not the Y314H mutation (MIC = >200 µM). It is selective for these targets over Gram-positive and Gram-negative bacteria but does inhibit phosphodiesterase 6 (PDE6; IC50 = 4 µM).
Brand:CaymanSKU:-Available on backorder
AZ 7371 is a non-covalent inhibitor of decaprenylphosphoryl-β-D-ribose 2’-epimerase (DprE1; IC50 = 10 nM), an enzyme involved in mycobacterial cell wall biogenesis.{32839} It inhibits wild-type M. smegmatis DprE1 and DprE1 harboring the drug-resistance mutation C394G (IC50 = 0.01 µM for both) but not the Y321H mutation (IC50 = >10 µM).{54377} AZ 7371 is active against wild-type M. tuberculosis DprE1 (MIC = 1.56 µM) and M. tuberculosis harboring C387S or C387G mutations (MICs = 0.39 and 0.78 µM, respectively), which confer resistance to the antibiotic BTZ043 (Item No. 22930), but not the Y314H mutation (MIC = >200 µM). It is selective for these targets over Gram-positive and Gram-negative bacteria but does inhibit phosphodiesterase 6 (PDE6; IC50 = 4 µM).
Brand:CaymanSKU:-Available on backorder
Janus-associated kinases (JAKs) are cytoplasmic tyrosine kinases that are required for activating the signaling of certain cytokines and growth factor receptors. Many myeloproliferative diseases have been linked to a mutation in JAK2 where a switch from valine to phenylalanine occurs at the 617 position (V617F).{27171} Furthermore, constitutive activation of the JAK2 signaling pathway is associated with aggressive adult T cell leukemia/lymphoma.{27172} AZ 960 inhibits JAK2 with a Ki value of 0.45 nM in vitro.{27171} It can decrease STAT3/5 phosphorylation and inhibit cell proliferation in a SET-2 human megakaryoblastic cell line that is heterozygous for the JAK2 V617F mutation with a GI50 value of 33 nM.{27171} AZ 960 can also induce apoptosis in human T cell lymophotropic virus type 1-infected (IC50 = ~1 µM), which corresponds to a downregulation of phosphorylated forms of JAK2 and Bcl-2 family proteins.{27172}
Brand:CaymanSKU:-Out of stock
Janus-associated kinases (JAKs) are cytoplasmic tyrosine kinases that are required for activating the signaling of certain cytokines and growth factor receptors. Many myeloproliferative diseases have been linked to a mutation in JAK2 where a switch from valine to phenylalanine occurs at the 617 position (V617F).{27171} Furthermore, constitutive activation of the JAK2 signaling pathway is associated with aggressive adult T cell leukemia/lymphoma.{27172} AZ 960 inhibits JAK2 with a Ki value of 0.45 nM in vitro.{27171} It can decrease STAT3/5 phosphorylation and inhibit cell proliferation in a SET-2 human megakaryoblastic cell line that is heterozygous for the JAK2 V617F mutation with a GI50 value of 33 nM.{27171} AZ 960 can also induce apoptosis in human T cell lymophotropic virus type 1-infected (IC50 = ~1 µM), which corresponds to a downregulation of phosphorylated forms of JAK2 and Bcl-2 family proteins.{27172}
Brand:CaymanSKU:-Out of stock
Janus-associated kinases (JAKs) are cytoplasmic tyrosine kinases that are required for activating the signaling of certain cytokines and growth factor receptors. Many myeloproliferative diseases have been linked to a mutation in JAK2 where a switch from valine to phenylalanine occurs at the 617 position (V617F).{27171} Furthermore, constitutive activation of the JAK2 signaling pathway is associated with aggressive adult T cell leukemia/lymphoma.{27172} AZ 960 inhibits JAK2 with a Ki value of 0.45 nM in vitro.{27171} It can decrease STAT3/5 phosphorylation and inhibit cell proliferation in a SET-2 human megakaryoblastic cell line that is heterozygous for the JAK2 V617F mutation with a GI50 value of 33 nM.{27171} AZ 960 can also induce apoptosis in human T cell lymophotropic virus type 1-infected (IC50 = ~1 µM), which corresponds to a downregulation of phosphorylated forms of JAK2 and Bcl-2 family proteins.{27172}
Brand:CaymanSKU:-Out of stock
Dual-specificity tyrosine-(Y)-phosphorylation regulated kinase 1B (DYRK1B) belongs to a family of nuclear-localized protein kinases and participates in the regulation of the cell cycle with key roles in proliferation and differentiation.{28991} It is upregulated in solid tumors and gain-of-function mutations in the gene encoding this kinase have been linked to metabolic syndrome.{28992,26374} AZ191 is a cell-permeable azaindole that inhibits the serine/threonine kinase activity of DYRK1B (IC50 = 17 nM) with 5-fold and 110-fold selectivity against the related family members DYRK1A and DYRK2, respectively.{28993} This compound has been used as a probe to elucidate the mechanism of DYRK1B regulation of cell cycle progression.{28993}
Brand:CaymanSKU:-Available on backorder
Dual-specificity tyrosine-(Y)-phosphorylation regulated kinase 1B (DYRK1B) belongs to a family of nuclear-localized protein kinases and participates in the regulation of the cell cycle with key roles in proliferation and differentiation.{28991} It is upregulated in solid tumors and gain-of-function mutations in the gene encoding this kinase have been linked to metabolic syndrome.{28992,26374} AZ191 is a cell-permeable azaindole that inhibits the serine/threonine kinase activity of DYRK1B (IC50 = 17 nM) with 5-fold and 110-fold selectivity against the related family members DYRK1A and DYRK2, respectively.{28993} This compound has been used as a probe to elucidate the mechanism of DYRK1B regulation of cell cycle progression.{28993}
Brand:CaymanSKU:-Available on backorder
Dual-specificity tyrosine-(Y)-phosphorylation regulated kinase 1B (DYRK1B) belongs to a family of nuclear-localized protein kinases and participates in the regulation of the cell cycle with key roles in proliferation and differentiation.{28991} It is upregulated in solid tumors and gain-of-function mutations in the gene encoding this kinase have been linked to metabolic syndrome.{28992,26374} AZ191 is a cell-permeable azaindole that inhibits the serine/threonine kinase activity of DYRK1B (IC50 = 17 nM) with 5-fold and 110-fold selectivity against the related family members DYRK1A and DYRK2, respectively.{28993} This compound has been used as a probe to elucidate the mechanism of DYRK1B regulation of cell cycle progression.{28993}
Brand:CaymanSKU:-Available on backorder
Dual-specificity tyrosine-(Y)-phosphorylation regulated kinase 1B (DYRK1B) belongs to a family of nuclear-localized protein kinases and participates in the regulation of the cell cycle with key roles in proliferation and differentiation.{28991} It is upregulated in solid tumors and gain-of-function mutations in the gene encoding this kinase have been linked to metabolic syndrome.{28992,26374} AZ191 is a cell-permeable azaindole that inhibits the serine/threonine kinase activity of DYRK1B (IC50 = 17 nM) with 5-fold and 110-fold selectivity against the related family members DYRK1A and DYRK2, respectively.{28993} This compound has been used as a probe to elucidate the mechanism of DYRK1B regulation of cell cycle progression.{28993}
Brand:CaymanSKU:-Available on backorder
AZ3451 is an allosteric antagonist of proteinase-activated receptor 2 (PAR2) that inhibits calcium mobilization by wild-type and 10 mutant forms of PAR2 induced by the PAR2 ligand SLIGRL in a FLIPR assay (IC50s = 23 and 12-780 nM, respectively).{46658} It is selective for PAR2 over PAR4 and PAR1 (IC50s = 50,000 nM, respectively, in a β-arrestin-2 recruitment assay). AZ3541 completely inhibits SLIGRL-induced phosphorylation of ERK in 1321N1 astrocytoma cells when used at a concentration of 10 µM.
Brand:CaymanSKU:29671 - 1 mgAvailable on backorder
AZ3451 is an allosteric antagonist of proteinase-activated receptor 2 (PAR2) that inhibits calcium mobilization by wild-type and 10 mutant forms of PAR2 induced by the PAR2 ligand SLIGRL in a FLIPR assay (IC50s = 23 and 12-780 nM, respectively).{46658} It is selective for PAR2 over PAR4 and PAR1 (IC50s = 50,000 nM, respectively, in a β-arrestin-2 recruitment assay). AZ3541 completely inhibits SLIGRL-induced phosphorylation of ERK in 1321N1 astrocytoma cells when used at a concentration of 10 µM.
Brand:CaymanSKU:29671 - 10 mgAvailable on backorder
AZ3451 is an allosteric antagonist of proteinase-activated receptor 2 (PAR2) that inhibits calcium mobilization by wild-type and 10 mutant forms of PAR2 induced by the PAR2 ligand SLIGRL in a FLIPR assay (IC50s = 23 and 12-780 nM, respectively).{46658} It is selective for PAR2 over PAR4 and PAR1 (IC50s = 50,000 nM, respectively, in a β-arrestin-2 recruitment assay). AZ3541 completely inhibits SLIGRL-induced phosphorylation of ERK in 1321N1 astrocytoma cells when used at a concentration of 10 µM.
Brand:CaymanSKU:29671 - 25 mgAvailable on backorder
AZ3451 is an allosteric antagonist of proteinase-activated receptor 2 (PAR2) that inhibits calcium mobilization by wild-type and 10 mutant forms of PAR2 induced by the PAR2 ligand SLIGRL in a FLIPR assay (IC50s = 23 and 12-780 nM, respectively).{46658} It is selective for PAR2 over PAR4 and PAR1 (IC50s = 50,000 nM, respectively, in a β-arrestin-2 recruitment assay). AZ3541 completely inhibits SLIGRL-induced phosphorylation of ERK in 1321N1 astrocytoma cells when used at a concentration of 10 µM.
Brand:CaymanSKU:29671 - 5 mgAvailable on backorder
AZ82 is a small molecule inhibitor of KIFC1/HSET, a kinesin-14 family protein that is important for assembling bipolar spindles in cancer cells containing supernumerary centrosomes.{38506} AZ82 binds to the KIFC1/microtubule complex and inhibits its microtubule-stimulated activity (IC50 = 300 nM) in an ATP-competitive (Ki = 43 nM) and microtubule-noncompetitive manner but does not inhibit basal KIFC1 activity at a concentration of 100 µM.{38507} It is selective for KIFC1 over a panel of nine kinesin motor proteins at a concentration of 5 µM. AZ82 induces multipolar spindle formation in cancer cell lines with high (BT549), but not low (HeLa and MCF-7), numbers of extra chromosomes.
Brand:CaymanSKU:21898 -Out of stock
AZ82 is a small molecule inhibitor of KIFC1/HSET, a kinesin-14 family protein that is important for assembling bipolar spindles in cancer cells containing supernumerary centrosomes.{38506} AZ82 binds to the KIFC1/microtubule complex and inhibits its microtubule-stimulated activity (IC50 = 300 nM) in an ATP-competitive (Ki = 43 nM) and microtubule-noncompetitive manner but does not inhibit basal KIFC1 activity at a concentration of 100 µM.{38507} It is selective for KIFC1 over a panel of nine kinesin motor proteins at a concentration of 5 µM. AZ82 induces multipolar spindle formation in cancer cell lines with high (BT549), but not low (HeLa and MCF-7), numbers of extra chromosomes.
Brand:CaymanSKU:21898 -Out of stock
AZ82 is a small molecule inhibitor of KIFC1/HSET, a kinesin-14 family protein that is important for assembling bipolar spindles in cancer cells containing supernumerary centrosomes.{38506} AZ82 binds to the KIFC1/microtubule complex and inhibits its microtubule-stimulated activity (IC50 = 300 nM) in an ATP-competitive (Ki = 43 nM) and microtubule-noncompetitive manner but does not inhibit basal KIFC1 activity at a concentration of 100 µM.{38507} It is selective for KIFC1 over a panel of nine kinesin motor proteins at a concentration of 5 µM. AZ82 induces multipolar spindle formation in cancer cell lines with high (BT549), but not low (HeLa and MCF-7), numbers of extra chromosomes.
Brand:CaymanSKU:21898 -Out of stock
AZ82 is a small molecule inhibitor of KIFC1/HSET, a kinesin-14 family protein that is important for assembling bipolar spindles in cancer cells containing supernumerary centrosomes.{38506} AZ82 binds to the KIFC1/microtubule complex and inhibits its microtubule-stimulated activity (IC50 = 300 nM) in an ATP-competitive (Ki = 43 nM) and microtubule-noncompetitive manner but does not inhibit basal KIFC1 activity at a concentration of 100 µM.{38507} It is selective for KIFC1 over a panel of nine kinesin motor proteins at a concentration of 5 µM. AZ82 induces multipolar spindle formation in cancer cell lines with high (BT549), but not low (HeLa and MCF-7), numbers of extra chromosomes.
Brand:CaymanSKU:21898 -Out of stock
AZ9482 is a poly(ADP-ribose) polymerase (PARP) inhibitor (IC50s = 1, 1, 46, 640, 9, and 160 nM for PARP1, -2, -3, -6, TNKS1/PARP5a, and TNKS2, respectively).{53504} It induces centrosome declustering (EC50 = 50 = 3 nM).
Brand:CaymanSKU:30292 - 1 mgAvailable on backorder
AZ9482 is a poly(ADP-ribose) polymerase (PARP) inhibitor (IC50s = 1, 1, 46, 640, 9, and 160 nM for PARP1, -2, -3, -6, TNKS1/PARP5a, and TNKS2, respectively).{53504} It induces centrosome declustering (EC50 = 50 = 3 nM).
Brand:CaymanSKU:30292 - 10 mgAvailable on backorder
AZ9482 is a poly(ADP-ribose) polymerase (PARP) inhibitor (IC50s = 1, 1, 46, 640, 9, and 160 nM for PARP1, -2, -3, -6, TNKS1/PARP5a, and TNKS2, respectively).{53504} It induces centrosome declustering (EC50 = 50 = 3 nM).
Brand:CaymanSKU:30292 - 25 mgAvailable on backorder
AZ9482 is a poly(ADP-ribose) polymerase (PARP) inhibitor (IC50s = 1, 1, 46, 640, 9, and 160 nM for PARP1, -2, -3, -6, TNKS1/PARP5a, and TNKS2, respectively).{53504} It induces centrosome declustering (EC50 = 50 = 3 nM).
Brand:CaymanSKU:30292 - 5 mgAvailable on backorder
Azacyclonol is a CNS depressant.{43955} It reduces transmission through the sympathetic ganglia, decreasing electrically stimulated contractile responses in feline nictitating membrane. It reduces coordinated locomotor activity in mice by greater than 50% when administered at doses of 71, 142, and 213 mg/kg.{43952} Azacyclonol (142 mg/kg) decreases hyperactivity induced by pipradol, D-amphetamine, morphine, and cocaine. It also increases the duration of sleeping time induced by hexobarbital. Azacyclonol is also a metabolite of the histamine H1 receptor antagonist terfenadine (Item No. 20305).{43953,43954} It is formed from terfenadine by the cytochrome P450 (CYP) isoform CYP3A4.{43954}
Brand:CaymanSKU:27303 - 10 gAvailable on backorder
Azacyclonol is a CNS depressant.{43955} It reduces transmission through the sympathetic ganglia, decreasing electrically stimulated contractile responses in feline nictitating membrane. It reduces coordinated locomotor activity in mice by greater than 50% when administered at doses of 71, 142, and 213 mg/kg.{43952} Azacyclonol (142 mg/kg) decreases hyperactivity induced by pipradol, D-amphetamine, morphine, and cocaine. It also increases the duration of sleeping time induced by hexobarbital. Azacyclonol is also a metabolite of the histamine H1 receptor antagonist terfenadine (Item No. 20305).{43953,43954} It is formed from terfenadine by the cytochrome P450 (CYP) isoform CYP3A4.{43954}
Brand:CaymanSKU:27303 - 100 gAvailable on backorder
Azacyclonol is a CNS depressant.{43955} It reduces transmission through the sympathetic ganglia, decreasing electrically stimulated contractile responses in feline nictitating membrane. It reduces coordinated locomotor activity in mice by greater than 50% when administered at doses of 71, 142, and 213 mg/kg.{43952} Azacyclonol (142 mg/kg) decreases hyperactivity induced by pipradol, D-amphetamine, morphine, and cocaine. It also increases the duration of sleeping time induced by hexobarbital. Azacyclonol is also a metabolite of the histamine H1 receptor antagonist terfenadine (Item No. 20305).{43953,43954} It is formed from terfenadine by the cytochrome P450 (CYP) isoform CYP3A4.{43954}
Brand:CaymanSKU:27303 - 25 gAvailable on backorder
Azacyclonol is a CNS depressant.{43955} It reduces transmission through the sympathetic ganglia, decreasing electrically stimulated contractile responses in feline nictitating membrane. It reduces coordinated locomotor activity in mice by greater than 50% when administered at doses of 71, 142, and 213 mg/kg.{43952} Azacyclonol (142 mg/kg) decreases hyperactivity induced by pipradol, D-amphetamine, morphine, and cocaine. It also increases the duration of sleeping time induced by hexobarbital. Azacyclonol is also a metabolite of the histamine H1 receptor antagonist terfenadine (Item No. 20305).{43953,43954} It is formed from terfenadine by the cytochrome P450 (CYP) isoform CYP3A4.{43954}
Brand:CaymanSKU:27303 - 50 gAvailable on backorder
Azadirachtin is a naturally-occurring insecticide originally isolated from the seeds of A. indica.{38747} It inhibits feeding behavior, molting, and/or ovarian development in a species-dependent manner in insects.{38748} Azadirachtin inhibits feeding on G. barbadense leaves and cotyledon disks by third instar H. zea larvae with protection concentrations (PC95s) of 6.2 and 6.8 μg/disk, respectively.{38749} It inhibits ecdysis and growth of H. zea, H. virescens, S. frugiperda, and P. gossypiella with ecdysis inhibition values (EI95s) ranging from 1 to 10 ppm and ED50 values ranging from 0.4 to 0.7 ppm. Azadirachtin inhibits the growth of freshly molted fourth instar E. varivestis larva (LC50 = 1.66 ppm).{38748} It is lethal to A. stephensi first, second, third, and fourth instar larva, pupa, and adults at a concentration of 0.1 ppm.{38750}
Brand:CaymanSKU:21893 -Out of stock
Azadirachtin is a naturally-occurring insecticide originally isolated from the seeds of A. indica.{38747} It inhibits feeding behavior, molting, and/or ovarian development in a species-dependent manner in insects.{38748} Azadirachtin inhibits feeding on G. barbadense leaves and cotyledon disks by third instar H. zea larvae with protection concentrations (PC95s) of 6.2 and 6.8 μg/disk, respectively.{38749} It inhibits ecdysis and growth of H. zea, H. virescens, S. frugiperda, and P. gossypiella with ecdysis inhibition values (EI95s) ranging from 1 to 10 ppm and ED50 values ranging from 0.4 to 0.7 ppm. Azadirachtin inhibits the growth of freshly molted fourth instar E. varivestis larva (LC50 = 1.66 ppm).{38748} It is lethal to A. stephensi first, second, third, and fourth instar larva, pupa, and adults at a concentration of 0.1 ppm.{38750}
Brand:CaymanSKU:21893 -Out of stock
Azadirachtin is a naturally-occurring insecticide originally isolated from the seeds of A. indica.{38747} It inhibits feeding behavior, molting, and/or ovarian development in a species-dependent manner in insects.{38748} Azadirachtin inhibits feeding on G. barbadense leaves and cotyledon disks by third instar H. zea larvae with protection concentrations (PC95s) of 6.2 and 6.8 μg/disk, respectively.{38749} It inhibits ecdysis and growth of H. zea, H. virescens, S. frugiperda, and P. gossypiella with ecdysis inhibition values (EI95s) ranging from 1 to 10 ppm and ED50 values ranging from 0.4 to 0.7 ppm. Azadirachtin inhibits the growth of freshly molted fourth instar E. varivestis larva (LC50 = 1.66 ppm).{38748} It is lethal to A. stephensi first, second, third, and fourth instar larva, pupa, and adults at a concentration of 0.1 ppm.{38750}
Brand:CaymanSKU:21893 -Out of stock
Azadirachtin B is an azadirachtin that has been found in the neem tree, A. indica, and has diverse biological activities, including insecticidal, nematocidal, anticancer, and osteogenic properties.{46667,46668,46669,46670,46671} It has antifeedant activity against P. xylostella third instar larvae when used at a concentration of 3 mg/ml and induces mortality with an LC50 of 1.03 mg/ml.{46668} It induces mortality in M. incognita second instar larvae with an LD50 value of 125.8 ppm.{46669} Azadirachtin B (780 nmol in the drinking water) reduces the number of papillomas formed on mouse skin in a model of skin carcinogenesis induced by peroxynitrite and phorbol 12-myristate 13-acetate (TPA; Item No. 10008014) but is not cytotoxic to HL-60, A549, AZ521, SK-BR-3, or CRL1579 cancer cells (IC50s = >20 µM for all).{46670,46671} It induces osteoblast differentiation and increases the rate of osteoblast proliferation in primary calvarial osteoblast cells when used at concentrations of 100 pM and 10 nM but not 1 pM, 1 µM, or 100 µM.{46667}
Brand:CaymanSKU:29569 - 1 mgAvailable on backorder
Azamulin is a selective, irreversible inhibitor of cytochrome P450 (CYP) 3A isoforms (IC50 values range from 26 to 240 nM for CYP3A4 and CYP3A4/5 from different sources).{30387} It is at least 50-fold less potent against CYP2J2 and 100-fold less effective against all other CYP isoforms.{30387} Azamulin potently blocks the hydroxylation of testosterone and midazolam by CYP3A4.{30387,30386}
Brand:CaymanSKU:-Available on backorder
Azamulin is a selective, irreversible inhibitor of cytochrome P450 (CYP) 3A isoforms (IC50 values range from 26 to 240 nM for CYP3A4 and CYP3A4/5 from different sources).{30387} It is at least 50-fold less potent against CYP2J2 and 100-fold less effective against all other CYP isoforms.{30387} Azamulin potently blocks the hydroxylation of testosterone and midazolam by CYP3A4.{30387,30386}
Brand:CaymanSKU:-Available on backorder
Azamulin is a selective, irreversible inhibitor of cytochrome P450 (CYP) 3A isoforms (IC50 values range from 26 to 240 nM for CYP3A4 and CYP3A4/5 from different sources).{30387} It is at least 50-fold less potent against CYP2J2 and 100-fold less effective against all other CYP isoforms.{30387} Azamulin potently blocks the hydroxylation of testosterone and midazolam by CYP3A4.{30387,30386}
Brand:CaymanSKU:-Available on backorder
Azaserine is a tumor-inhibiting antibiotic isolated from a species of Streptomyces that functions as a glutamine analog.{23660,21899} At 25 μM, it inhibits the glutamine-dependent amidotransferases involved in nucleotide biosynthesis, phosphoribosylformylglycinamidine synthetase and glucosamine-6-phosphate isomerase.{21899,18311} Azaserine also inhibits the hexosamine biosynthetic pathway, which shunts excessive intracellular glucose into the biosynthesis of UDP-N-acetylglucosamine and the formation of O-linked glycoproteins.{23661} Azaserine has been shown to protect against hyperglycemic endothelial damage through its antioxidant effects.{23661}
Brand:CaymanSKU:- Azaserine is a tumor-inhibiting antibiotic isolated from a species of Streptomyces that functions as a glutamine analog.{23660,21899} At 25 μM, it inhibits the glutamine-dependent amidotransferases involved in nucleotide biosynthesis, phosphoribosylformylglycinamidine synthetase and glucosamine-6-phosphate isomerase.{21899,18311} Azaserine also inhibits the hexosamine biosynthetic pathway, which shunts excessive intracellular glucose into the biosynthesis of UDP-N-acetylglucosamine and the formation of O-linked glycoproteins.{23661} Azaserine has been shown to protect against hyperglycemic endothelial damage through its antioxidant effects.{23661}
Brand:CaymanSKU:- Azaserine is a tumor-inhibiting antibiotic isolated from a species of Streptomyces that functions as a glutamine analog.{23660,21899} At 25 μM, it inhibits the glutamine-dependent amidotransferases involved in nucleotide biosynthesis, phosphoribosylformylglycinamidine synthetase and glucosamine-6-phosphate isomerase.{21899,18311} Azaserine also inhibits the hexosamine biosynthetic pathway, which shunts excessive intracellular glucose into the biosynthesis of UDP-N-acetylglucosamine and the formation of O-linked glycoproteins.{23661} Azaserine has been shown to protect against hyperglycemic endothelial damage through its antioxidant effects.{23661}
Brand:CaymanSKU:- Azaserine is a tumor-inhibiting antibiotic isolated from a species of Streptomyces that functions as a glutamine analog.{23660,21899} At 25 μM, it inhibits the glutamine-dependent amidotransferases involved in nucleotide biosynthesis, phosphoribosylformylglycinamidine synthetase and glucosamine-6-phosphate isomerase.{21899,18311} Azaserine also inhibits the hexosamine biosynthetic pathway, which shunts excessive intracellular glucose into the biosynthesis of UDP-N-acetylglucosamine and the formation of O-linked glycoproteins.{23661} Azaserine has been shown to protect against hyperglycemic endothelial damage through its antioxidant effects.{23661}
Brand:CaymanSKU:-
Azasetron is an orally bioavailable antagonist of the serotonin (5-HT) receptor subtype 5-HT3 (Ki = 2.9 nM).{47619,47620} It is selective for 5-HT3 over 5-HT1A and 5-HT2 (IC50 = >10 μM for both), as well as dopamine D1 and D2 and α1- and α2-adrenergic receptors (IC50s = >10 μM), but it does bind to histamine H1 receptors (IC50 = 4.4 μM). Azasetron inhibits contractions induced by 5-HT (Item No. 14332) in isolated guinea pig ileum (pA2 = 7.04) and isolated rabbit heart (pA2 = 10.06). It inhibits emesis induced by cisplatin (Item No. 13119) in dogs and induced by doxorubicin (Item No. 15007) combined with cyclophosphamide (Item No. 13849) in ferrets when administered at a dose of 1 mg/kg.{47619}
Brand:CaymanSKU:28383 - 10 mgAvailable on backorder
Azasetron is an orally bioavailable antagonist of the serotonin (5-HT) receptor subtype 5-HT3 (Ki = 2.9 nM).{47619,47620} It is selective for 5-HT3 over 5-HT1A and 5-HT2 (IC50 = >10 μM for both), as well as dopamine D1 and D2 and α1- and α2-adrenergic receptors (IC50s = >10 μM), but it does bind to histamine H1 receptors (IC50 = 4.4 μM). Azasetron inhibits contractions induced by 5-HT (Item No. 14332) in isolated guinea pig ileum (pA2 = 7.04) and isolated rabbit heart (pA2 = 10.06). It inhibits emesis induced by cisplatin (Item No. 13119) in dogs and induced by doxorubicin (Item No. 15007) combined with cyclophosphamide (Item No. 13849) in ferrets when administered at a dose of 1 mg/kg.{47619}
Brand:CaymanSKU:28383 - 100 mgAvailable on backorder
Azasetron is an orally bioavailable antagonist of the serotonin (5-HT) receptor subtype 5-HT3 (Ki = 2.9 nM).{47619,47620} It is selective for 5-HT3 over 5-HT1A and 5-HT2 (IC50 = >10 μM for both), as well as dopamine D1 and D2 and α1- and α2-adrenergic receptors (IC50s = >10 μM), but it does bind to histamine H1 receptors (IC50 = 4.4 μM). Azasetron inhibits contractions induced by 5-HT (Item No. 14332) in isolated guinea pig ileum (pA2 = 7.04) and isolated rabbit heart (pA2 = 10.06). It inhibits emesis induced by cisplatin (Item No. 13119) in dogs and induced by doxorubicin (Item No. 15007) combined with cyclophosphamide (Item No. 13849) in ferrets when administered at a dose of 1 mg/kg.{47619}
Brand:CaymanSKU:28383 - 25 mgAvailable on backorder
Azasetron is an orally bioavailable antagonist of the serotonin (5-HT) receptor subtype 5-HT3 (Ki = 2.9 nM).{47619,47620} It is selective for 5-HT3 over 5-HT1A and 5-HT2 (IC50 = >10 μM for both), as well as dopamine D1 and D2 and α1- and α2-adrenergic receptors (IC50s = >10 μM), but it does bind to histamine H1 receptors (IC50 = 4.4 μM). Azasetron inhibits contractions induced by 5-HT (Item No. 14332) in isolated guinea pig ileum (pA2 = 7.04) and isolated rabbit heart (pA2 = 10.06). It inhibits emesis induced by cisplatin (Item No. 13119) in dogs and induced by doxorubicin (Item No. 15007) combined with cyclophosphamide (Item No. 13849) in ferrets when administered at a dose of 1 mg/kg.{47619}
Brand:CaymanSKU:28383 - 50 mgAvailable on backorder
Azatadine is an antihistamine with anticholinergic and antiserotonergic activities.{25628},{52335} It is a histamine H1 receptor antagonist (Ki = 3.9 nM).{52336},{32989} Azatadine inhibits histamine- and acetylcholine-induced contractions in isolated guinea pig ilium and contractions induced by serotonin (5-HT; Item No. 14332) in isolated rat uterus (EC50s = 6.5, 10, and 14 nM, respectively).{52335} It delays the onset of dyspnea induced by aerosolized histamine, 5-HT, or acetylcholine in guinea pigs. Azatadine prevents histamine-induced lethality in guinea pigs and paw edema in mice (ED50s = 9 and 68 μg/kg, respectively).{25628} It increases survival in guinea pig and mouse models of anaphylactic shock with 50% protective dose (PD50) values of 0.024 and 0.019 mg/kg, respectively.{52335}
Brand:CaymanSKU:29758 - 100 mgAvailable on backorder
Azatadine is an antihistamine with anticholinergic and antiserotonergic activities.{25628},{52335} It is a histamine H1 receptor antagonist (Ki = 3.9 nM).{52336},{32989} Azatadine inhibits histamine- and acetylcholine-induced contractions in isolated guinea pig ilium and contractions induced by serotonin (5-HT; Item No. 14332) in isolated rat uterus (EC50s = 6.5, 10, and 14 nM, respectively).{52335} It delays the onset of dyspnea induced by aerosolized histamine, 5-HT, or acetylcholine in guinea pigs. Azatadine prevents histamine-induced lethality in guinea pigs and paw edema in mice (ED50s = 9 and 68 μg/kg, respectively).{25628} It increases survival in guinea pig and mouse models of anaphylactic shock with 50% protective dose (PD50) values of 0.024 and 0.019 mg/kg, respectively.{52335}
Brand:CaymanSKU:29758 - 250 mgAvailable on backorder
Azatadine is an antihistamine with anticholinergic and antiserotonergic activities.{25628},{52335} It is a histamine H1 receptor antagonist (Ki = 3.9 nM).{52336},{32989} Azatadine inhibits histamine- and acetylcholine-induced contractions in isolated guinea pig ilium and contractions induced by serotonin (5-HT; Item No. 14332) in isolated rat uterus (EC50s = 6.5, 10, and 14 nM, respectively).{52335} It delays the onset of dyspnea induced by aerosolized histamine, 5-HT, or acetylcholine in guinea pigs. Azatadine prevents histamine-induced lethality in guinea pigs and paw edema in mice (ED50s = 9 and 68 μg/kg, respectively).{25628} It increases survival in guinea pig and mouse models of anaphylactic shock with 50% protective dose (PD50) values of 0.024 and 0.019 mg/kg, respectively.{52335}
Brand:CaymanSKU:29758 - 50 mgAvailable on backorder
Azatadine is an antihistamine with anticholinergic and antiserotonergic activities.{25628},{52335} It is a histamine H1 receptor antagonist (Ki = 3.9 nM).{52336},{32989} Azatadine inhibits histamine- and acetylcholine-induced contractions in isolated guinea pig ilium and contractions induced by serotonin (5-HT; Item No. 14332) in isolated rat uterus (EC50s = 6.5, 10, and 14 nM, respectively).{52335} It delays the onset of dyspnea induced by aerosolized histamine, 5-HT, or acetylcholine in guinea pigs. Azatadine prevents histamine-induced lethality in guinea pigs and paw edema in mice (ED50s = 9 and 68 μg/kg, respectively).{25628} It increases survival in guinea pig and mouse models of anaphylactic shock with 50% protective dose (PD50) values of 0.024 and 0.019 mg/kg, respectively.{52335}
Brand:CaymanSKU:29758 - 500 mgAvailable on backorder
Azathioprine is a purine analog with immunosuppressive effects.{21835} It serves as a prodrug for 6-mercaptopurine, which alters purine processing and DNA synthesis, interfering with the proliferation of lymphocytes and other myeloid cells.{21835,21834} Its immunomodulating actions are used to benefit inflammatory bowel disease, as well as a wide range of additional diseases with immunological or autoimmunological components, including rheumatoid arthritis and lupus nephritis.{21835,21834,21833}
Brand:CaymanSKU:- Azathioprine is a purine analog with immunosuppressive effects.{21835} It serves as a prodrug for 6-mercaptopurine, which alters purine processing and DNA synthesis, interfering with the proliferation of lymphocytes and other myeloid cells.{21835,21834} Its immunomodulating actions are used to benefit inflammatory bowel disease, as well as a wide range of additional diseases with immunological or autoimmunological components, including rheumatoid arthritis and lupus nephritis.{21835,21834,21833}
Brand:CaymanSKU:-
AZD 0156 is an inhibitor of the ataxia-telangiectasia mutated (ATM) kinase (IC50s = 0.04 and 0.57 nM in enzyme and cell-based assays, respectively).{48018} It is selective for ATM over other PI3K-related kinase (PIKK) family kinases including DNA-PK, mTOR, PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ (IC50s = 0.14, 0.20, 0.32, 1.8, 1.1, and 0.27 μM, respectively, in enzyme assays). AZD 0156 (20 mg/kg) enhances the antitumor activity of irinotecan (Item No. 14180) in an SW620 colon cancer mouse xenograft model and olaparib (Item No. 10621) in an HBCx-10 breast cancer patient-derived xenograft (PDX) mouse model when administered at a dose of 5 mg/kg, leading to tumor regression in both models.
Brand:CaymanSKU:25648 - 10 mgAvailable on backorder
AZD 0156 is an inhibitor of the ataxia-telangiectasia mutated (ATM) kinase (IC50s = 0.04 and 0.57 nM in enzyme and cell-based assays, respectively).{48018} It is selective for ATM over other PI3K-related kinase (PIKK) family kinases including DNA-PK, mTOR, PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ (IC50s = 0.14, 0.20, 0.32, 1.8, 1.1, and 0.27 μM, respectively, in enzyme assays). AZD 0156 (20 mg/kg) enhances the antitumor activity of irinotecan (Item No. 14180) in an SW620 colon cancer mouse xenograft model and olaparib (Item No. 10621) in an HBCx-10 breast cancer patient-derived xenograft (PDX) mouse model when administered at a dose of 5 mg/kg, leading to tumor regression in both models.
Brand:CaymanSKU:25648 - 25 mgAvailable on backorder
AZD 0156 is an inhibitor of the ataxia-telangiectasia mutated (ATM) kinase (IC50s = 0.04 and 0.57 nM in enzyme and cell-based assays, respectively).{48018} It is selective for ATM over other PI3K-related kinase (PIKK) family kinases including DNA-PK, mTOR, PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ (IC50s = 0.14, 0.20, 0.32, 1.8, 1.1, and 0.27 μM, respectively, in enzyme assays). AZD 0156 (20 mg/kg) enhances the antitumor activity of irinotecan (Item No. 14180) in an SW620 colon cancer mouse xenograft model and olaparib (Item No. 10621) in an HBCx-10 breast cancer patient-derived xenograft (PDX) mouse model when administered at a dose of 5 mg/kg, leading to tumor regression in both models.
Brand:CaymanSKU:25648 - 5 mgAvailable on backorder
AZD 0156 is an inhibitor of the ataxia-telangiectasia mutated (ATM) kinase (IC50s = 0.04 and 0.57 nM in enzyme and cell-based assays, respectively).{48018} It is selective for ATM over other PI3K-related kinase (PIKK) family kinases including DNA-PK, mTOR, PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ (IC50s = 0.14, 0.20, 0.32, 1.8, 1.1, and 0.27 μM, respectively, in enzyme assays). AZD 0156 (20 mg/kg) enhances the antitumor activity of irinotecan (Item No. 14180) in an SW620 colon cancer mouse xenograft model and olaparib (Item No. 10621) in an HBCx-10 breast cancer patient-derived xenograft (PDX) mouse model when administered at a dose of 5 mg/kg, leading to tumor regression in both models.
Brand:CaymanSKU:25648 - 50 mgAvailable on backorder
AZD 0364 is an inhibitor of ERK2 (IC50 = 50s = 30, 400, 300, and 300 nM, respectively). AZD 0364 inhibits cell growth in A549 non-small cell lung cancer cells (NSCLCs) when used in combination with AZD 6244 (Item No. 11599).{52345} It reduces tumor growth and induces regression in a Calu-6 mouse xenograft model when administered at doses of 15 and 50 mg/kg per day, respectively.{50811}
Brand:CaymanSKU:29827 - 1 mgAvailable on backorder
AZD 0364 is an inhibitor of ERK2 (IC50 = 50s = 30, 400, 300, and 300 nM, respectively). AZD 0364 inhibits cell growth in A549 non-small cell lung cancer cells (NSCLCs) when used in combination with AZD 6244 (Item No. 11599).{52345} It reduces tumor growth and induces regression in a Calu-6 mouse xenograft model when administered at doses of 15 and 50 mg/kg per day, respectively.{50811}
Brand:CaymanSKU:29827 - 10 mgAvailable on backorder
AZD 0364 is an inhibitor of ERK2 (IC50 = 50s = 30, 400, 300, and 300 nM, respectively). AZD 0364 inhibits cell growth in A549 non-small cell lung cancer cells (NSCLCs) when used in combination with AZD 6244 (Item No. 11599).{52345} It reduces tumor growth and induces regression in a Calu-6 mouse xenograft model when administered at doses of 15 and 50 mg/kg per day, respectively.{50811}
Brand:CaymanSKU:29827 - 5 mgAvailable on backorder
The two isoforms of glycogen synthase kinase 3, GSK3α and GSK3β, constitutively phosphorylate and inactivate glycogen synthase, preventing glycogen synthesis.{19045} They also phosphorylate proteins that are relevant to Alzheimer’s disease and osteogenesis.{25567,25565,25566} AZD 1080 is a potent, brain permeable inhibitor of GSK3α and GSK3β (Kis = 6.9 and 31 nM, respectively).{27257,27258} It shows >14-fold selectivity against several kinases, receptors, enzymes, and ion channels.{27257} AZD 1080 inhibits tau phosphorylation in cells.{27257} It shows good bioavailability after oral administration in vivo, inhibiting hippocampal tau phosphorylation and reversing cognitive deficits induced by the NMDA receptor antagonist (+)-MK-801 (Item No. 10009019).{27257} In humans, oral AZD 1080 inhibits GSK3 activity in peripheral blood lymphocytes following an initial delay in response.{27257}
Brand:CaymanSKU:-Out of stock
The two isoforms of glycogen synthase kinase 3, GSK3α and GSK3β, constitutively phosphorylate and inactivate glycogen synthase, preventing glycogen synthesis.{19045} They also phosphorylate proteins that are relevant to Alzheimer’s disease and osteogenesis.{25567,25565,25566} AZD 1080 is a potent, brain permeable inhibitor of GSK3α and GSK3β (Kis = 6.9 and 31 nM, respectively).{27257,27258} It shows >14-fold selectivity against several kinases, receptors, enzymes, and ion channels.{27257} AZD 1080 inhibits tau phosphorylation in cells.{27257} It shows good bioavailability after oral administration in vivo, inhibiting hippocampal tau phosphorylation and reversing cognitive deficits induced by the NMDA receptor antagonist (+)-MK-801 (Item No. 10009019).{27257} In humans, oral AZD 1080 inhibits GSK3 activity in peripheral blood lymphocytes following an initial delay in response.{27257}
Brand:CaymanSKU:-Out of stock
The two isoforms of glycogen synthase kinase 3, GSK3α and GSK3β, constitutively phosphorylate and inactivate glycogen synthase, preventing glycogen synthesis.{19045} They also phosphorylate proteins that are relevant to Alzheimer’s disease and osteogenesis.{25567,25565,25566} AZD 1080 is a potent, brain permeable inhibitor of GSK3α and GSK3β (Kis = 6.9 and 31 nM, respectively).{27257,27258} It shows >14-fold selectivity against several kinases, receptors, enzymes, and ion channels.{27257} AZD 1080 inhibits tau phosphorylation in cells.{27257} It shows good bioavailability after oral administration in vivo, inhibiting hippocampal tau phosphorylation and reversing cognitive deficits induced by the NMDA receptor antagonist (+)-MK-801 (Item No. 10009019).{27257} In humans, oral AZD 1080 inhibits GSK3 activity in peripheral blood lymphocytes following an initial delay in response.{27257}
Brand:CaymanSKU:-Out of stock
The two isoforms of glycogen synthase kinase 3, GSK3α and GSK3β, constitutively phosphorylate and inactivate glycogen synthase, preventing glycogen synthesis.{19045} They also phosphorylate proteins that are relevant to Alzheimer’s disease and osteogenesis.{25567,25565,25566} AZD 1080 is a potent, brain permeable inhibitor of GSK3α and GSK3β (Kis = 6.9 and 31 nM, respectively).{27257,27258} It shows >14-fold selectivity against several kinases, receptors, enzymes, and ion channels.{27257} AZD 1080 inhibits tau phosphorylation in cells.{27257} It shows good bioavailability after oral administration in vivo, inhibiting hippocampal tau phosphorylation and reversing cognitive deficits induced by the NMDA receptor antagonist (+)-MK-801 (Item No. 10009019).{27257} In humans, oral AZD 1080 inhibits GSK3 activity in peripheral blood lymphocytes following an initial delay in response.{27257}
Brand:CaymanSKU:-Out of stock
AZD 1152 is an orally bioavailable prodrug of AZD 1152-HQPA, a selective inhibitor of Aurora kinase B (IC50 = 0.36 nM).{31459} AZD 1152 is converted to AZD 1152-HQPA in plasma. Inhibition of Aurora B results in disruption of spindle checkpoint functions and chromosome alignment, resulting in inhibition of cytokinesis followed by apoptosis.{24932,19817} AZD 1152 inhibits tumor xenograft growth in vivo.{31460,31461}
Brand:CaymanSKU:- AZD 1152 is an orally bioavailable prodrug of AZD 1152-HQPA, a selective inhibitor of Aurora kinase B (IC50 = 0.36 nM).{31459} AZD 1152 is converted to AZD 1152-HQPA in plasma. Inhibition of Aurora B results in disruption of spindle checkpoint functions and chromosome alignment, resulting in inhibition of cytokinesis followed by apoptosis.{24932,19817} AZD 1152 inhibits tumor xenograft growth in vivo.{31460,31461}
Brand:CaymanSKU:- AZD 1152 is an orally bioavailable prodrug of AZD 1152-HQPA, a selective inhibitor of Aurora kinase B (IC50 = 0.36 nM).{31459} AZD 1152 is converted to AZD 1152-HQPA in plasma. Inhibition of Aurora B results in disruption of spindle checkpoint functions and chromosome alignment, resulting in inhibition of cytokinesis followed by apoptosis.{24932,19817} AZD 1152 inhibits tumor xenograft growth in vivo.{31460,31461}
Brand:CaymanSKU:- AZD 1152 is an orally bioavailable prodrug of AZD 1152-HQPA, a selective inhibitor of Aurora kinase B (IC50 = 0.36 nM).{31459} AZD 1152 is converted to AZD 1152-HQPA in plasma. Inhibition of Aurora B results in disruption of spindle checkpoint functions and chromosome alignment, resulting in inhibition of cytokinesis followed by apoptosis.{24932,19817} AZD 1152 inhibits tumor xenograft growth in vivo.{31460,31461}
Brand:CaymanSKU:-
AZD 1152-HQPA is an inhibitor of Aurora kinase B (IC50 = 0.37 nM) that demonstrates ~3,700-fold greater selectivity for Aurora kinase B over Aurora kinase A (IC50 = 1.368 µM).{31459,31461} It does not have activity against a panel of 50 other serine-threonine or tyrosine kinases, including FLT3, JAK2, and Abl.{31459,31461} AZD 1152-HQPA has been shown to inhibit the proliferation of hematopoietic malignant cells (IC50s = 3-40 nM), disrupting spindle checkpoint functions and chromosome alignment, resulting in inhibition of cytokinesis followed by apoptosis, and to inhibit tumor xenograft growth in vivo.{31461,31460}
Brand:CaymanSKU:11602 - 1 mgAvailable on backorder
AZD 1152-HQPA is an inhibitor of Aurora kinase B (IC50 = 0.37 nM) that demonstrates ~3,700-fold greater selectivity for Aurora kinase B over Aurora kinase A (IC50 = 1.368 µM).{31459,31461} It does not have activity against a panel of 50 other serine-threonine or tyrosine kinases, including FLT3, JAK2, and Abl.{31459,31461} AZD 1152-HQPA has been shown to inhibit the proliferation of hematopoietic malignant cells (IC50s = 3-40 nM), disrupting spindle checkpoint functions and chromosome alignment, resulting in inhibition of cytokinesis followed by apoptosis, and to inhibit tumor xenograft growth in vivo.{31461,31460}
Brand:CaymanSKU:11602 - 10 mgAvailable on backorder
AZD 1152-HQPA is an inhibitor of Aurora kinase B (IC50 = 0.37 nM) that demonstrates ~3,700-fold greater selectivity for Aurora kinase B over Aurora kinase A (IC50 = 1.368 µM).{31459,31461} It does not have activity against a panel of 50 other serine-threonine or tyrosine kinases, including FLT3, JAK2, and Abl.{31459,31461} AZD 1152-HQPA has been shown to inhibit the proliferation of hematopoietic malignant cells (IC50s = 3-40 nM), disrupting spindle checkpoint functions and chromosome alignment, resulting in inhibition of cytokinesis followed by apoptosis, and to inhibit tumor xenograft growth in vivo.{31461,31460}
Brand:CaymanSKU:11602 - 25 mgAvailable on backorder
AZD 1152-HQPA is an inhibitor of Aurora kinase B (IC50 = 0.37 nM) that demonstrates ~3,700-fold greater selectivity for Aurora kinase B over Aurora kinase A (IC50 = 1.368 µM).{31459,31461} It does not have activity against a panel of 50 other serine-threonine or tyrosine kinases, including FLT3, JAK2, and Abl.{31459,31461} AZD 1152-HQPA has been shown to inhibit the proliferation of hematopoietic malignant cells (IC50s = 3-40 nM), disrupting spindle checkpoint functions and chromosome alignment, resulting in inhibition of cytokinesis followed by apoptosis, and to inhibit tumor xenograft growth in vivo.{31461,31460}
Brand:CaymanSKU:11602 - 5 mgAvailable on backorder
AZD 1208 is a potent, selective, and orally available inhibitor of all three forms of the proto-oncogene Pim kinase (IC50s = 0.4, 5.0, and 1.9 nM for Pim-1, Pim-2, and Pim-3, respectively).{32021} It causes cell cycle arrest and apoptosis in MOLM-16 megakaryoblastic leukemia cells and inhibits the growth of MOLM-16 xenograft tumors in mice.{32021} It has efficacy against acute myeloid leukemia and glioblastoma cells when combined with mTOR and p110α inhibitors, respectively.{32019,32020}
Brand:CaymanSKU:20235 -Available on backorder
AZD 1208 is a potent, selective, and orally available inhibitor of all three forms of the proto-oncogene Pim kinase (IC50s = 0.4, 5.0, and 1.9 nM for Pim-1, Pim-2, and Pim-3, respectively).{32021} It causes cell cycle arrest and apoptosis in MOLM-16 megakaryoblastic leukemia cells and inhibits the growth of MOLM-16 xenograft tumors in mice.{32021} It has efficacy against acute myeloid leukemia and glioblastoma cells when combined with mTOR and p110α inhibitors, respectively.{32019,32020}
Brand:CaymanSKU:20235 -Available on backorder
AZD 1208 is a potent, selective, and orally available inhibitor of all three forms of the proto-oncogene Pim kinase (IC50s = 0.4, 5.0, and 1.9 nM for Pim-1, Pim-2, and Pim-3, respectively).{32021} It causes cell cycle arrest and apoptosis in MOLM-16 megakaryoblastic leukemia cells and inhibits the growth of MOLM-16 xenograft tumors in mice.{32021} It has efficacy against acute myeloid leukemia and glioblastoma cells when combined with mTOR and p110α inhibitors, respectively.{32019,32020}
Brand:CaymanSKU:20235 -Available on backorder
AZD 1208 is a potent, selective, and orally available inhibitor of all three forms of the proto-oncogene Pim kinase (IC50s = 0.4, 5.0, and 1.9 nM for Pim-1, Pim-2, and Pim-3, respectively).{32021} It causes cell cycle arrest and apoptosis in MOLM-16 megakaryoblastic leukemia cells and inhibits the growth of MOLM-16 xenograft tumors in mice.{32021} It has efficacy against acute myeloid leukemia and glioblastoma cells when combined with mTOR and p110α inhibitors, respectively.{32019,32020}
Brand:CaymanSKU:20235 -Available on backorder
AZD 1283 is an antagonist of the purinergic P2Y12 receptor (IC50 = 25 nM in a GTPγS assay in CHO cells).{52053} It selectively binds to the P2Y12 receptor (Kd = 11 nM) over more than 100 enzymes, receptors, and ion channels, including the P2Y1, platelet activating factor (PAF), and thromboxane A2 receptors, at 10 µM.{52053},{52054} AZD 1283 increases blood flow and inhibits platelet aggregation induced by ADP in a modified Folts dog model of thrombosis with ED50 values of 3 and 10 µg/kg per minute, respectively.
Brand:CaymanSKU:27649 - 1 mgAvailable on backorder
AZD 1283 is an antagonist of the purinergic P2Y12 receptor (IC50 = 25 nM in a GTPγS assay in CHO cells).{52053} It selectively binds to the P2Y12 receptor (Kd = 11 nM) over more than 100 enzymes, receptors, and ion channels, including the P2Y1, platelet activating factor (PAF), and thromboxane A2 receptors, at 10 µM.{52053},{52054} AZD 1283 increases blood flow and inhibits platelet aggregation induced by ADP in a modified Folts dog model of thrombosis with ED50 values of 3 and 10 µg/kg per minute, respectively.
Brand:CaymanSKU:27649 - 10 mgAvailable on backorder
AZD 1283 is an antagonist of the purinergic P2Y12 receptor (IC50 = 25 nM in a GTPγS assay in CHO cells).{52053} It selectively binds to the P2Y12 receptor (Kd = 11 nM) over more than 100 enzymes, receptors, and ion channels, including the P2Y1, platelet activating factor (PAF), and thromboxane A2 receptors, at 10 µM.{52053},{52054} AZD 1283 increases blood flow and inhibits platelet aggregation induced by ADP in a modified Folts dog model of thrombosis with ED50 values of 3 and 10 µg/kg per minute, respectively.
Brand:CaymanSKU:27649 - 25 mgAvailable on backorder
AZD 1283 is an antagonist of the purinergic P2Y12 receptor (IC50 = 25 nM in a GTPγS assay in CHO cells).{52053} It selectively binds to the P2Y12 receptor (Kd = 11 nM) over more than 100 enzymes, receptors, and ion channels, including the P2Y1, platelet activating factor (PAF), and thromboxane A2 receptors, at 10 µM.{52053},{52054} AZD 1283 increases blood flow and inhibits platelet aggregation induced by ADP in a modified Folts dog model of thrombosis with ED50 values of 3 and 10 µg/kg per minute, respectively.
Brand:CaymanSKU:27649 - 5 mgAvailable on backorder
AZD 1981 is a prostaglandin D2 (PGD2; Item No. 12010) receptor antagonist with a pIC50 value of 8.4 for CRTH2/DP2 and >1,000-fold selectivity over DP1.{32940} It has been shown to block functional responses in eosinophils, Th2 cells, and basophils and is currently under clinical evaluation as a potential therapeutic agent in respiratory diseases including asthma.{32940,32112}
Brand:CaymanSKU:20763 -Available on backorder
AZD 1981 is a prostaglandin D2 (PGD2; Item No. 12010) receptor antagonist with a pIC50 value of 8.4 for CRTH2/DP2 and >1,000-fold selectivity over DP1.{32940} It has been shown to block functional responses in eosinophils, Th2 cells, and basophils and is currently under clinical evaluation as a potential therapeutic agent in respiratory diseases including asthma.{32940,32112}
Brand:CaymanSKU:20763 -Available on backorder
AZD 1981 is a prostaglandin D2 (PGD2; Item No. 12010) receptor antagonist with a pIC50 value of 8.4 for CRTH2/DP2 and >1,000-fold selectivity over DP1.{32940} It has been shown to block functional responses in eosinophils, Th2 cells, and basophils and is currently under clinical evaluation as a potential therapeutic agent in respiratory diseases including asthma.{32940,32112}
Brand:CaymanSKU:20763 -Available on backorder
AZD 1981 is a prostaglandin D2 (PGD2; Item No. 12010) receptor antagonist with a pIC50 value of 8.4 for CRTH2/DP2 and >1,000-fold selectivity over DP1.{32940} It has been shown to block functional responses in eosinophils, Th2 cells, and basophils and is currently under clinical evaluation as a potential therapeutic agent in respiratory diseases including asthma.{32940,32112}
Brand:CaymanSKU:20763 -Available on backorder
AZD 2014 is a potent, selective, ATP-competitive mTORC1/2 dual inhibitor that inhibits phosphorylation of both mTORC1 and 2 substrate proteins in whole cells.{33186} It exhibits an IC50 value of 2.81 nM against the isolated recombinant enzyme and >1,000-fold selectivity against all PI3K isoforms.{33186} AZD 2014 has broad antiproliferative effects across multiple cell lines and reduces tumor growth in in vivo models of ER+ breast cancer.{33186}. It has efficacy against acute myeloid leukemia when combined with the pan Pim kinase inhibitor AZD 1208 (Item No. 20235) and enhances the radiosensitivity of different cancer cell types.{32019,33187,33188}
Brand:CaymanSKU:-Available on backorder
AZD 2014 is a potent, selective, ATP-competitive mTORC1/2 dual inhibitor that inhibits phosphorylation of both mTORC1 and 2 substrate proteins in whole cells.{33186} It exhibits an IC50 value of 2.81 nM against the isolated recombinant enzyme and >1,000-fold selectivity against all PI3K isoforms.{33186} AZD 2014 has broad antiproliferative effects across multiple cell lines and reduces tumor growth in in vivo models of ER+ breast cancer.{33186}. It has efficacy against acute myeloid leukemia when combined with the pan Pim kinase inhibitor AZD 1208 (Item No. 20235) and enhances the radiosensitivity of different cancer cell types.{32019,33187,33188}
Brand:CaymanSKU:-Available on backorder