Cayman
Showing 25351–25500 of 45550 results
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IT-901 is an inhibitor of the NF-κB subunit c-Rel.{42097} It inhibits NF-κB DNA binding in HBL1 cells (IC50 = 0.1 µM) and reduces TNF-α-induced NF-κB activity in a reporter assay (IC50 = 4 µM). IT-901 decreases proliferation of activated B-like (ABC) and germinal center B-like (GCB) human diffuse large B cell lymphoma (DLBCL) cells when used at a concentration of 3 µM. It increases the expression of heme oxygenase-1 (HO-1; Item No. 22731) in DLBCL cells and increases the production of reactive oxygen species (ROS) in the mitochondria of DLBCL cells but not normal leukocytes. IT-901 increases survival in a mouse model of graft versus host disease (GVHD) when administered at a dose of 24 mg/kg every other day beginning eight days after hematopoietic stem cell transplantation (HSCT). It also reduces tumor growth in mouse xenograft models of B cell lymphoma induced by Epstein-Barr virus (EBV), chronic lymphocytic leukemia (CLL), and Richter syndrome.{42097,42098}
Brand:CaymanSKU:22298 -Out of stock
IT1t is a chemokine (C-X-C motif) receptor 4 (CXCR4) antagonist (IC50s = 8 and 11 nM for the human and rat receptors, respectively).{48774} It is selective for CXCR4 over human ether-a-go-go-related gene potassium channels (hERG/Kv11.1; IC50 = 13,240 nM). IT1t inhibits calcium mobilization induced by chemokine (C-X-C-motif) ligand 12 (CXCL12) in CEM cells (IC50 = 1.1 nM) and decreases CXCL12-induced migration of Jurkat cells (IC50 = 79.1 nM).{48774,50131} It inhibits replication of the HIV-1 strain NL4-3 in MT-4 cells and isolated human peripheral blood mononuclear cells (PBMCs) stimulated with phytohemagglutinin (PHA; IC50s = 14.2 and 19 nM, respectively).{50131} IT1t (20 µM) reduces tumor growth in an MDA-MB-231-B zebrafish xenograft model.{50133}
Brand:CaymanSKU:28434 - 10 mgAvailable on backorder
IT1t is a chemokine (C-X-C motif) receptor 4 (CXCR4) antagonist (IC50s = 8 and 11 nM for the human and rat receptors, respectively).{48774} It is selective for CXCR4 over human ether-a-go-go-related gene potassium channels (hERG/Kv11.1; IC50 = 13,240 nM). IT1t inhibits calcium mobilization induced by chemokine (C-X-C-motif) ligand 12 (CXCL12) in CEM cells (IC50 = 1.1 nM) and decreases CXCL12-induced migration of Jurkat cells (IC50 = 79.1 nM).{48774,50131} It inhibits replication of the HIV-1 strain NL4-3 in MT-4 cells and isolated human peripheral blood mononuclear cells (PBMCs) stimulated with phytohemagglutinin (PHA; IC50s = 14.2 and 19 nM, respectively).{50131} IT1t (20 µM) reduces tumor growth in an MDA-MB-231-B zebrafish xenograft model.{50133}
Brand:CaymanSKU:28434 - 25 mgAvailable on backorder
IT1t is a chemokine (C-X-C motif) receptor 4 (CXCR4) antagonist (IC50s = 8 and 11 nM for the human and rat receptors, respectively).{48774} It is selective for CXCR4 over human ether-a-go-go-related gene potassium channels (hERG/Kv11.1; IC50 = 13,240 nM). IT1t inhibits calcium mobilization induced by chemokine (C-X-C-motif) ligand 12 (CXCL12) in CEM cells (IC50 = 1.1 nM) and decreases CXCL12-induced migration of Jurkat cells (IC50 = 79.1 nM).{48774,50131} It inhibits replication of the HIV-1 strain NL4-3 in MT-4 cells and isolated human peripheral blood mononuclear cells (PBMCs) stimulated with phytohemagglutinin (PHA; IC50s = 14.2 and 19 nM, respectively).{50131} IT1t (20 µM) reduces tumor growth in an MDA-MB-231-B zebrafish xenograft model.{50133}
Brand:CaymanSKU:28434 - 5 mgAvailable on backorder
Itacitinib is an inhibitor of JAK1.{36733} It is greater than 20- and 200-fold selective for JAK1 over JAK2 and JAK3, respectively.
Brand:CaymanSKU:27597 - 1 mgAvailable on backorder
Itacitinib is an inhibitor of JAK1.{36733} It is greater than 20- and 200-fold selective for JAK1 over JAK2 and JAK3, respectively.
Brand:CaymanSKU:27597 - 10 mgAvailable on backorder
Itacitinib is an inhibitor of JAK1.{36733} It is greater than 20- and 200-fold selective for JAK1 over JAK2 and JAK3, respectively.
Brand:CaymanSKU:27597 - 25 mgAvailable on backorder
Itacitinib is an inhibitor of JAK1.{36733} It is greater than 20- and 200-fold selective for JAK1 over JAK2 and JAK3, respectively.
Brand:CaymanSKU:27597 - 5 mgAvailable on backorder
ITD 1 is an inhibitor of TGF-β (IC50 = 0.85 µM).{40715} It is selective for TGF-β in an SBE4/Smad reporter assay, providing 83% inhibition when used at a concentration of 2.5 µM, over activin A, which is inhibited by 51% when used at the same concentration. ITD 1 inhibits TGF-β signaling by induction of TGF-β receptor type II degradation. It stimulates differentiation of mouse embryonic stem cells (mESCs) into cardiomyocytes.
Brand:CaymanSKU:23326 - 10 mgAvailable on backorder
ITD 1 is an inhibitor of TGF-β (IC50 = 0.85 µM).{40715} It is selective for TGF-β in an SBE4/Smad reporter assay, providing 83% inhibition when used at a concentration of 2.5 µM, over activin A, which is inhibited by 51% when used at the same concentration. ITD 1 inhibits TGF-β signaling by induction of TGF-β receptor type II degradation. It stimulates differentiation of mouse embryonic stem cells (mESCs) into cardiomyocytes.
Brand:CaymanSKU:23326 - 25 mgAvailable on backorder
ITD 1 is an inhibitor of TGF-β (IC50 = 0.85 µM).{40715} It is selective for TGF-β in an SBE4/Smad reporter assay, providing 83% inhibition when used at a concentration of 2.5 µM, over activin A, which is inhibited by 51% when used at the same concentration. ITD 1 inhibits TGF-β signaling by induction of TGF-β receptor type II degradation. It stimulates differentiation of mouse embryonic stem cells (mESCs) into cardiomyocytes.
Brand:CaymanSKU:23326 - 5 mgAvailable on backorder
ITD 1 is an inhibitor of TGF-β (IC50 = 0.85 µM).{40715} It is selective for TGF-β in an SBE4/Smad reporter assay, providing 83% inhibition when used at a concentration of 2.5 µM, over activin A, which is inhibited by 51% when used at the same concentration. ITD 1 inhibits TGF-β signaling by induction of TGF-β receptor type II degradation. It stimulates differentiation of mouse embryonic stem cells (mESCs) into cardiomyocytes.
Brand:CaymanSKU:23326 - 50 mgAvailable on backorder
ITE is an endogenous aryl hydrocarbon receptor (AhR) agonist.{52676} It binds to AhR (Kd = 65 nM) and induces AhR-dependent transcription in luciferase reporter assays when used at a concentration of 0.01 µM. ITE (1 µM) inhibits anti-CD40- and IL-4-induced differentiation of isolated mouse splenic B cells, as well as proliferation and migration of SKOV3 ovarian cancer cells.{52677,52678} In vivo, ITE (200 µg/animal, i.p.) reduces retinal detachment and ocular inflammatory cell infiltration in a mouse model of experimental autoimmune uveitis induced by complete Freund’s adjuvant (CFA) and M. tuberculosis.{52679} ITE (80 mg/kg, i.p.) reduces tumor growth by 39% in an OVCAR-3 mouse xenograft model.{52678}
Brand:CaymanSKU:25355 - 10 mgAvailable on backorder
ITE is an endogenous aryl hydrocarbon receptor (AhR) agonist.{52676} It binds to AhR (Kd = 65 nM) and induces AhR-dependent transcription in luciferase reporter assays when used at a concentration of 0.01 µM. ITE (1 µM) inhibits anti-CD40- and IL-4-induced differentiation of isolated mouse splenic B cells, as well as proliferation and migration of SKOV3 ovarian cancer cells.{52677,52678} In vivo, ITE (200 µg/animal, i.p.) reduces retinal detachment and ocular inflammatory cell infiltration in a mouse model of experimental autoimmune uveitis induced by complete Freund’s adjuvant (CFA) and M. tuberculosis.{52679} ITE (80 mg/kg, i.p.) reduces tumor growth by 39% in an OVCAR-3 mouse xenograft model.{52678}
Brand:CaymanSKU:25355 - 25 mgAvailable on backorder
ITE is an endogenous aryl hydrocarbon receptor (AhR) agonist.{52676} It binds to AhR (Kd = 65 nM) and induces AhR-dependent transcription in luciferase reporter assays when used at a concentration of 0.01 µM. ITE (1 µM) inhibits anti-CD40- and IL-4-induced differentiation of isolated mouse splenic B cells, as well as proliferation and migration of SKOV3 ovarian cancer cells.{52677,52678} In vivo, ITE (200 µg/animal, i.p.) reduces retinal detachment and ocular inflammatory cell infiltration in a mouse model of experimental autoimmune uveitis induced by complete Freund’s adjuvant (CFA) and M. tuberculosis.{52679} ITE (80 mg/kg, i.p.) reduces tumor growth by 39% in an OVCAR-3 mouse xenograft model.{52678}
Brand:CaymanSKU:25355 - 5 mgAvailable on backorder
ITE is an endogenous aryl hydrocarbon receptor (AhR) agonist.{52676} It binds to AhR (Kd = 65 nM) and induces AhR-dependent transcription in luciferase reporter assays when used at a concentration of 0.01 µM. ITE (1 µM) inhibits anti-CD40- and IL-4-induced differentiation of isolated mouse splenic B cells, as well as proliferation and migration of SKOV3 ovarian cancer cells.{52677,52678} In vivo, ITE (200 µg/animal, i.p.) reduces retinal detachment and ocular inflammatory cell infiltration in a mouse model of experimental autoimmune uveitis induced by complete Freund’s adjuvant (CFA) and M. tuberculosis.{52679} ITE (80 mg/kg, i.p.) reduces tumor growth by 39% in an OVCAR-3 mouse xenograft model.{52678}
Brand:CaymanSKU:25355 - 50 mgAvailable on backorder
ITF 2357 inhibits class I and class II histone deacetylases (maize HDACs: HD2, HD-1B, and HD-1A with IC50s = 7.5-16 nM) and reduces the production of several pro-inflammatory cytokines including TNFα, IL-1α, and IL-1β (IC50s = 10-22 nM).{22291} ITF 2357 also has activity against cells expressing janus kinase 2 (JAK2)V617F (IC50s = 1-10 nM), a mutated form of the JAK2 enzyme that is implicated in the pathophysiology of many myeloproliferative diseases, including polycythaemia vera.{22292}
Brand:CaymanSKU:11045 - 1 mgAvailable on backorder
ITF 2357 inhibits class I and class II histone deacetylases (maize HDACs: HD2, HD-1B, and HD-1A with IC50s = 7.5-16 nM) and reduces the production of several pro-inflammatory cytokines including TNFα, IL-1α, and IL-1β (IC50s = 10-22 nM).{22291} ITF 2357 also has activity against cells expressing janus kinase 2 (JAK2)V617F (IC50s = 1-10 nM), a mutated form of the JAK2 enzyme that is implicated in the pathophysiology of many myeloproliferative diseases, including polycythaemia vera.{22292}
Brand:CaymanSKU:11045 - 10 mgAvailable on backorder
ITF 2357 inhibits class I and class II histone deacetylases (maize HDACs: HD2, HD-1B, and HD-1A with IC50s = 7.5-16 nM) and reduces the production of several pro-inflammatory cytokines including TNFα, IL-1α, and IL-1β (IC50s = 10-22 nM).{22291} ITF 2357 also has activity against cells expressing janus kinase 2 (JAK2)V617F (IC50s = 1-10 nM), a mutated form of the JAK2 enzyme that is implicated in the pathophysiology of many myeloproliferative diseases, including polycythaemia vera.{22292}
Brand:CaymanSKU:11045 - 5 mgAvailable on backorder
ITI214 is an inhibitor of phosphodiesterase 1 (PDE1; Ki = 0.058 nM).{54039} It is selective for PDE1 over PDE2A, -3B, -4A, -5A, -6, -7B, -8A, -9A, -10A, and -11A (Kis = 0.16-18 µM). ITI214 (3 and 6 mg/kg) enhances novel object recognition in rats. It increases prefrontal cortex cAMP and cGMP levels in mice when administered at a dose of 50 mg/kg.{54040} ITI214 (0.1, 3, and 10 mg/kg) reverses MK-801-induced decreases in spontaneous alteration in the T-maze continuous alternation task in mice.
Brand:CaymanSKU:30376 - 1 mgAvailable on backorder
ITI214 is an inhibitor of phosphodiesterase 1 (PDE1; Ki = 0.058 nM).{54039} It is selective for PDE1 over PDE2A, -3B, -4A, -5A, -6, -7B, -8A, -9A, -10A, and -11A (Kis = 0.16-18 µM). ITI214 (3 and 6 mg/kg) enhances novel object recognition in rats. It increases prefrontal cortex cAMP and cGMP levels in mice when administered at a dose of 50 mg/kg.{54040} ITI214 (0.1, 3, and 10 mg/kg) reverses MK-801-induced decreases in spontaneous alteration in the T-maze continuous alternation task in mice.
Brand:CaymanSKU:30376 - 10 mgAvailable on backorder
ITI214 is an inhibitor of phosphodiesterase 1 (PDE1; Ki = 0.058 nM).{54039} It is selective for PDE1 over PDE2A, -3B, -4A, -5A, -6, -7B, -8A, -9A, -10A, and -11A (Kis = 0.16-18 µM). ITI214 (3 and 6 mg/kg) enhances novel object recognition in rats. It increases prefrontal cortex cAMP and cGMP levels in mice when administered at a dose of 50 mg/kg.{54040} ITI214 (0.1, 3, and 10 mg/kg) reverses MK-801-induced decreases in spontaneous alteration in the T-maze continuous alternation task in mice.
Brand:CaymanSKU:30376 - 5 mgAvailable on backorder
Itopride is an inhibitor of acetylcholinesterase (AChE; IC50 = 1.6 µM for rat stomach enzyme) and a prokinetic agent.{58108} It induces contractions in isolated rabbit duodenum when used at concentrations ranging from 1 to 100 µM and enhances ACh-induced contractions in isolated guinea pig stomach circular muscle strips.{58109,58110} Itopride (100 mg/kg) enhances normal gastric antral motility and improves gastric antral hypomotility and delayed gastric emptying induced by clonidine (Item No. 15949) in rats.{58108} Formulations containing itopride have been used in the treatment of functional dyspepsia.
Brand:CaymanSKU:31183 - 1 mgAvailable on backorder
Itopride is an inhibitor of acetylcholinesterase (AChE; IC50 = 1.6 µM for rat stomach enzyme) and a prokinetic agent.{58108} It induces contractions in isolated rabbit duodenum when used at concentrations ranging from 1 to 100 µM and enhances ACh-induced contractions in isolated guinea pig stomach circular muscle strips.{58109,58110} Itopride (100 mg/kg) enhances normal gastric antral motility and improves gastric antral hypomotility and delayed gastric emptying induced by clonidine (Item No. 15949) in rats.{58108} Formulations containing itopride have been used in the treatment of functional dyspepsia.
Brand:CaymanSKU:31183 - 10 mgAvailable on backorder
Itopride is an inhibitor of acetylcholinesterase (AChE; IC50 = 1.6 µM for rat stomach enzyme) and a prokinetic agent.{58108} It induces contractions in isolated rabbit duodenum when used at concentrations ranging from 1 to 100 µM and enhances ACh-induced contractions in isolated guinea pig stomach circular muscle strips.{58109,58110} Itopride (100 mg/kg) enhances normal gastric antral motility and improves gastric antral hypomotility and delayed gastric emptying induced by clonidine (Item No. 15949) in rats.{58108} Formulations containing itopride have been used in the treatment of functional dyspepsia.
Brand:CaymanSKU:31183 - 25 mgAvailable on backorder
Itopride is an inhibitor of acetylcholinesterase (AChE; IC50 = 1.6 µM for rat stomach enzyme) and a prokinetic agent.{58108} It induces contractions in isolated rabbit duodenum when used at concentrations ranging from 1 to 100 µM and enhances ACh-induced contractions in isolated guinea pig stomach circular muscle strips.{58109,58110} Itopride (100 mg/kg) enhances normal gastric antral motility and improves gastric antral hypomotility and delayed gastric emptying induced by clonidine (Item No. 15949) in rats.{58108} Formulations containing itopride have been used in the treatment of functional dyspepsia.
Brand:CaymanSKU:31183 - 5 mgAvailable on backorder
Itraconazole is an antifungal agent and inhibitor of hedgehog signaling (IC50 = 800 nM).{36692,19161} It binds to 14-α sterol demethylase/CYP51 isoform B (AF51B; Kd = 31 nM for A. fumigatus enzyme expressed in E. coli) and inhibits ergosterol biosynthesis in C. neoformans (IC50 = 6 nM after a 16-hour incubation).{36692,25587} It inhibits the growth of C. neoformans by 50% when used at a concentration of 3.2 nM. Itraconazole inhibits hedgehog signaling, reducing accumulation of Smoothened induced by sonic hedgehog (Shh) in primary cilia of NIHT-3T3 cells.{19161} It suppresses growth of medulloblastomas in a Ptch+/-p53-/- mouse allograft model when administered at a dose of 100 mg/kg twice daily. Itraconazole (1.25-100 µM) also reduces viral titers of several enteroviruses, including human rhinovirus 17, in infected cells, effects that can be reversed by overexpression of OSBP, the gene encoding oxysterol-binding protein (OSBP).{45895}
Brand:CaymanSKU:- Itraconazole is an antifungal agent and inhibitor of hedgehog signaling (IC50 = 800 nM).{36692,19161} It binds to 14-α sterol demethylase/CYP51 isoform B (AF51B; Kd = 31 nM for A. fumigatus enzyme expressed in E. coli) and inhibits ergosterol biosynthesis in C. neoformans (IC50 = 6 nM after a 16-hour incubation).{36692,25587} It inhibits the growth of C. neoformans by 50% when used at a concentration of 3.2 nM. Itraconazole inhibits hedgehog signaling, reducing accumulation of Smoothened induced by sonic hedgehog (Shh) in primary cilia of NIHT-3T3 cells.{19161} It suppresses growth of medulloblastomas in a Ptch+/-p53-/- mouse allograft model when administered at a dose of 100 mg/kg twice daily. Itraconazole (1.25-100 µM) also reduces viral titers of several enteroviruses, including human rhinovirus 17, in infected cells, effects that can be reversed by overexpression of OSBP, the gene encoding oxysterol-binding protein (OSBP).{45895}
Brand:CaymanSKU:- Itraconazole is an antifungal agent and inhibitor of hedgehog signaling (IC50 = 800 nM).{36692,19161} It binds to 14-α sterol demethylase/CYP51 isoform B (AF51B; Kd = 31 nM for A. fumigatus enzyme expressed in E. coli) and inhibits ergosterol biosynthesis in C. neoformans (IC50 = 6 nM after a 16-hour incubation).{36692,25587} It inhibits the growth of C. neoformans by 50% when used at a concentration of 3.2 nM. Itraconazole inhibits hedgehog signaling, reducing accumulation of Smoothened induced by sonic hedgehog (Shh) in primary cilia of NIHT-3T3 cells.{19161} It suppresses growth of medulloblastomas in a Ptch+/-p53-/- mouse allograft model when administered at a dose of 100 mg/kg twice daily. Itraconazole (1.25-100 µM) also reduces viral titers of several enteroviruses, including human rhinovirus 17, in infected cells, effects that can be reversed by overexpression of OSBP, the gene encoding oxysterol-binding protein (OSBP).{45895}
Brand:CaymanSKU:- Itraconazole is an antifungal agent and inhibitor of hedgehog signaling (IC50 = 800 nM).{36692,19161} It binds to 14-α sterol demethylase/CYP51 isoform B (AF51B; Kd = 31 nM for A. fumigatus enzyme expressed in E. coli) and inhibits ergosterol biosynthesis in C. neoformans (IC50 = 6 nM after a 16-hour incubation).{36692,25587} It inhibits the growth of C. neoformans by 50% when used at a concentration of 3.2 nM. Itraconazole inhibits hedgehog signaling, reducing accumulation of Smoothened induced by sonic hedgehog (Shh) in primary cilia of NIHT-3T3 cells.{19161} It suppresses growth of medulloblastomas in a Ptch+/-p53-/- mouse allograft model when administered at a dose of 100 mg/kg twice daily. Itraconazole (1.25-100 µM) also reduces viral titers of several enteroviruses, including human rhinovirus 17, in infected cells, effects that can be reversed by overexpression of OSBP, the gene encoding oxysterol-binding protein (OSBP).{45895}
Brand:CaymanSKU:-
Itraconazole-d5 is intended for use as an internal standard for the quantification of itraconazole (Item No. 13288) by GC- or LC-MS. Itraconazole is an antifungal agent and inhibitor of hedgehog signaling (IC50 = 800 nM).{36692,19161} It binds to 14-α sterol demethylase/CYP51 isoform B (AF51B; Kd = 31 nM for A. fumigatus enzyme expressed in E. coli) and inhibits ergosterol biosynthesis in C. neoformans (IC50 = 6 nM after a 16-hour incubation).{36692,25587} It inhibits the growth of C. neoformans by 50% when used at a concentration of 3.2 nM. Itraconazole inhibits hedgehog signaling, reducing accumulation of Smoothened induced by sonic hedgehog (Shh) in primary cilia of NIHT-3T3 cells.{19161} It suppresses growth of medulloblastomas in a Ptch+/-p53-/- mouse allograft model when administered at a dose of 100 mg/kg twice daily. Itraconazole (1.25-100 µM) also reduces viral titers of several enteroviruses, including human rhinovirus 17, in infected cells, effects that can be reversed by overexpression of OSBP, the gene encoding oxysterol-binding protein (OSBP).{45895}
Brand:CaymanSKU:25219 - 1 mgAvailable on backorder
Itraconazole-d5 is intended for use as an internal standard for the quantification of itraconazole (Item No. 13288) by GC- or LC-MS. Itraconazole is an antifungal agent and inhibitor of hedgehog signaling (IC50 = 800 nM).{36692,19161} It binds to 14-α sterol demethylase/CYP51 isoform B (AF51B; Kd = 31 nM for A. fumigatus enzyme expressed in E. coli) and inhibits ergosterol biosynthesis in C. neoformans (IC50 = 6 nM after a 16-hour incubation).{36692,25587} It inhibits the growth of C. neoformans by 50% when used at a concentration of 3.2 nM. Itraconazole inhibits hedgehog signaling, reducing accumulation of Smoothened induced by sonic hedgehog (Shh) in primary cilia of NIHT-3T3 cells.{19161} It suppresses growth of medulloblastomas in a Ptch+/-p53-/- mouse allograft model when administered at a dose of 100 mg/kg twice daily. Itraconazole (1.25-100 µM) also reduces viral titers of several enteroviruses, including human rhinovirus 17, in infected cells, effects that can be reversed by overexpression of OSBP, the gene encoding oxysterol-binding protein (OSBP).{45895}
Brand:CaymanSKU:25219 - 500 µgAvailable on backorder
Trichostatin A (TSA; Item No. 89730) is a potent, reversible inhibitor of histone deacetylase (HDAC) that inhibits HDAC1 (IC50 = 70 nM) in Jurkat cells, resulting in cell cycle arrest.{8150} ITSA1 is a cell-permeable benzotriazole amide that blocks TSA action, reducing TSA-induced acetylation of histone and tubulin in A549 cells when given at 50 µM.{30169} At the same concentration, ITSA1 also prevents TSA-mediated cell cycle arrest and apoptosis.{30169} It similarly blocks the action of the HDAC inhibitor SAHA (Item No. 10009929), preventing SAHA-induced hyperacetylation of tubulin in A549 cells.{30169} ITSA1 reduces TSA-regulated transcription in mouse embryonic stem cells and in zebrafish.{30169}
Brand:CaymanSKU:-Available on backorder
Trichostatin A (TSA; Item No. 89730) is a potent, reversible inhibitor of histone deacetylase (HDAC) that inhibits HDAC1 (IC50 = 70 nM) in Jurkat cells, resulting in cell cycle arrest.{8150} ITSA1 is a cell-permeable benzotriazole amide that blocks TSA action, reducing TSA-induced acetylation of histone and tubulin in A549 cells when given at 50 µM.{30169} At the same concentration, ITSA1 also prevents TSA-mediated cell cycle arrest and apoptosis.{30169} It similarly blocks the action of the HDAC inhibitor SAHA (Item No. 10009929), preventing SAHA-induced hyperacetylation of tubulin in A549 cells.{30169} ITSA1 reduces TSA-regulated transcription in mouse embryonic stem cells and in zebrafish.{30169}
Brand:CaymanSKU:-Available on backorder
Trichostatin A (TSA; Item No. 89730) is a potent, reversible inhibitor of histone deacetylase (HDAC) that inhibits HDAC1 (IC50 = 70 nM) in Jurkat cells, resulting in cell cycle arrest.{8150} ITSA1 is a cell-permeable benzotriazole amide that blocks TSA action, reducing TSA-induced acetylation of histone and tubulin in A549 cells when given at 50 µM.{30169} At the same concentration, ITSA1 also prevents TSA-mediated cell cycle arrest and apoptosis.{30169} It similarly blocks the action of the HDAC inhibitor SAHA (Item No. 10009929), preventing SAHA-induced hyperacetylation of tubulin in A549 cells.{30169} ITSA1 reduces TSA-regulated transcription in mouse embryonic stem cells and in zebrafish.{30169}
Brand:CaymanSKU:-Available on backorder
Trichostatin A (TSA; Item No. 89730) is a potent, reversible inhibitor of histone deacetylase (HDAC) that inhibits HDAC1 (IC50 = 70 nM) in Jurkat cells, resulting in cell cycle arrest.{8150} ITSA1 is a cell-permeable benzotriazole amide that blocks TSA action, reducing TSA-induced acetylation of histone and tubulin in A549 cells when given at 50 µM.{30169} At the same concentration, ITSA1 also prevents TSA-mediated cell cycle arrest and apoptosis.{30169} It similarly blocks the action of the HDAC inhibitor SAHA (Item No. 10009929), preventing SAHA-induced hyperacetylation of tubulin in A549 cells.{30169} ITSA1 reduces TSA-regulated transcription in mouse embryonic stem cells and in zebrafish.{30169}
Brand:CaymanSKU:-Available on backorder
Polybiquitinylation designates proteins for proteasomal degradation. USP14 is one of several deubiquitinating enzymes (DUBs) responsible for shortening proteasome-bound ubiquitin chains, which is known to antagonize the degradation of ubiquitin-protein conjugates.{18550} IU1 is a reversible, small molecule inhibitor of deubiquitination by USP14 that demonstrates an IC50 value of 4-5 μM.{18550} IU1 selectively stimulates ubiquitin-dependent protein degradation in vitro at 34 μM and in MEF cells at 50 μM. At 75 μM, IU1 reduces accumulation of oxidized proteins in HEK293 cells, alleviating cytotoxicity induced by oxidative stress.{18550}
Brand:CaymanSKU:10617 - 10 mgAvailable on backorder
Polybiquitinylation designates proteins for proteasomal degradation. USP14 is one of several deubiquitinating enzymes (DUBs) responsible for shortening proteasome-bound ubiquitin chains, which is known to antagonize the degradation of ubiquitin-protein conjugates.{18550} IU1 is a reversible, small molecule inhibitor of deubiquitination by USP14 that demonstrates an IC50 value of 4-5 μM.{18550} IU1 selectively stimulates ubiquitin-dependent protein degradation in vitro at 34 μM and in MEF cells at 50 μM. At 75 μM, IU1 reduces accumulation of oxidized proteins in HEK293 cells, alleviating cytotoxicity induced by oxidative stress.{18550}
Brand:CaymanSKU:10617 - 100 mgAvailable on backorder
Polybiquitinylation designates proteins for proteasomal degradation. USP14 is one of several deubiquitinating enzymes (DUBs) responsible for shortening proteasome-bound ubiquitin chains, which is known to antagonize the degradation of ubiquitin-protein conjugates.{18550} IU1 is a reversible, small molecule inhibitor of deubiquitination by USP14 that demonstrates an IC50 value of 4-5 μM.{18550} IU1 selectively stimulates ubiquitin-dependent protein degradation in vitro at 34 μM and in MEF cells at 50 μM. At 75 μM, IU1 reduces accumulation of oxidized proteins in HEK293 cells, alleviating cytotoxicity induced by oxidative stress.{18550}
Brand:CaymanSKU:10617 - 5 mgAvailable on backorder
Polybiquitinylation designates proteins for proteasomal degradation. USP14 is one of several deubiquitinating enzymes (DUBs) responsible for shortening proteasome-bound ubiquitin chains, which is known to antagonize the degradation of ubiquitin-protein conjugates.{18550} IU1 is a reversible, small molecule inhibitor of deubiquitination by USP14 that demonstrates an IC50 value of 4-5 μM.{18550} IU1 selectively stimulates ubiquitin-dependent protein degradation in vitro at 34 μM and in MEF cells at 50 μM. At 75 μM, IU1 reduces accumulation of oxidized proteins in HEK293 cells, alleviating cytotoxicity induced by oxidative stress.{18550}
Brand:CaymanSKU:10617 - 50 mgAvailable on backorder
Ivabradine is a hyperpolarization-activated cyclic nucleotide-gated (HCN) channel blocker that blocks the mixed sodium/potassium inward funny current (If) in HEK293 cells expressing mouse HCN1, human HCN2, and human HCN4 (EC50s = 4.5, 4.52, and 4.28 μM, respectively).{25789} In vivo, ivabradine (10 mg/kg per day) reduces heart rate, incidence of ventricular tachycardia and ventricular fibrillation, and arrhythmic mortality in a rat model of myocardial infarction.{37776} Formulations containing ivabradine have been used in the treatment of heart failure and angina.
Brand:CaymanSKU:- Ivabradine is a hyperpolarization-activated cyclic nucleotide-gated (HCN) channel blocker that blocks the mixed sodium/potassium inward funny current (If) in HEK293 cells expressing mouse HCN1, human HCN2, and human HCN4 (EC50s = 4.5, 4.52, and 4.28 μM, respectively).{25789} In vivo, ivabradine (10 mg/kg per day) reduces heart rate, incidence of ventricular tachycardia and ventricular fibrillation, and arrhythmic mortality in a rat model of myocardial infarction.{37776} Formulations containing ivabradine have been used in the treatment of heart failure and angina.
Brand:CaymanSKU:- Ivabradine is a hyperpolarization-activated cyclic nucleotide-gated (HCN) channel blocker that blocks the mixed sodium/potassium inward funny current (If) in HEK293 cells expressing mouse HCN1, human HCN2, and human HCN4 (EC50s = 4.5, 4.52, and 4.28 μM, respectively).{25789} In vivo, ivabradine (10 mg/kg per day) reduces heart rate, incidence of ventricular tachycardia and ventricular fibrillation, and arrhythmic mortality in a rat model of myocardial infarction.{37776} Formulations containing ivabradine have been used in the treatment of heart failure and angina.
Brand:CaymanSKU:- Ivabradine is a hyperpolarization-activated cyclic nucleotide-gated (HCN) channel blocker that blocks the mixed sodium/potassium inward funny current (If) in HEK293 cells expressing mouse HCN1, human HCN2, and human HCN4 (EC50s = 4.5, 4.52, and 4.28 μM, respectively).{25789} In vivo, ivabradine (10 mg/kg per day) reduces heart rate, incidence of ventricular tachycardia and ventricular fibrillation, and arrhythmic mortality in a rat model of myocardial infarction.{37776} Formulations containing ivabradine have been used in the treatment of heart failure and angina.
Brand:CaymanSKU:-
Ivabradine-d3 is intended for use as an internal standard for the quantification of ivabradine (Item No. 15868) by GC- or LC-MS. Ivabradine is a hyperpolarization-activated cyclic nucleotide-gated (HCN) channel blocker that blocks the mixed sodium/potassium inward funny current (If) in HEK293 cells expressing mouse HCN1, human HCN2, and human HCN4 (EC50s = 4.5, 4.52, and 4.28 μM, respectively).{25789} In vivo, ivabradine (10 mg/kg per day) reduces heart rate, incidence of ventricular tachycardia and ventricular fibrillation, and arrhythmic mortality in a rat model of myocardial infarction.{37776} Formulations containing ivabradine have been used in the treatment of heart failure and angina.
Brand:CaymanSKU:25711 - 1 mgAvailable on backorder
Ivabradine-d3 is intended for use as an internal standard for the quantification of ivabradine (Item No. 15868) by GC- or LC-MS. Ivabradine is a hyperpolarization-activated cyclic nucleotide-gated (HCN) channel blocker that blocks the mixed sodium/potassium inward funny current (If) in HEK293 cells expressing mouse HCN1, human HCN2, and human HCN4 (EC50s = 4.5, 4.52, and 4.28 μM, respectively).{25789} In vivo, ivabradine (10 mg/kg per day) reduces heart rate, incidence of ventricular tachycardia and ventricular fibrillation, and arrhythmic mortality in a rat model of myocardial infarction.{37776} Formulations containing ivabradine have been used in the treatment of heart failure and angina.
Brand:CaymanSKU:25711 - 500 µgAvailable on backorder
Ivacaftor is an orally bioavailable potentiator of the cystic fibrosis transmembrane conductance regulator (CFTR) that improves chloride transport.{25614} It increases the forskolin-induced CFTR-mediated epithelial current in cells expressing the G551D missense mutation associated with severe cystic fibrosis by approximately 4-fold (EC50 = 100 nM) but has no effect on current in the absence of forskolin.{25614} Ivacaftor increases chloride secretion in cultured human cystic fibrosis bronchial epithelial cells carrying the G551D mutation on one allele and the common ΔF508 processing mutation on the other allele.{25614} It binds CFTR directly and leads to CFTR channel opening via an ATP-independent mechanism.{25613} Formulations containing ivacaftor have been used in the treatment of cystic fibrosis in patients carrying one or more mutations in the CFTR gene.
Brand:CaymanSKU:- Ivacaftor is an orally bioavailable potentiator of the cystic fibrosis transmembrane conductance regulator (CFTR) that improves chloride transport.{25614} It increases the forskolin-induced CFTR-mediated epithelial current in cells expressing the G551D missense mutation associated with severe cystic fibrosis by approximately 4-fold (EC50 = 100 nM) but has no effect on current in the absence of forskolin.{25614} Ivacaftor increases chloride secretion in cultured human cystic fibrosis bronchial epithelial cells carrying the G551D mutation on one allele and the common ΔF508 processing mutation on the other allele.{25614} It binds CFTR directly and leads to CFTR channel opening via an ATP-independent mechanism.{25613} Formulations containing ivacaftor have been used in the treatment of cystic fibrosis in patients carrying one or more mutations in the CFTR gene.
Brand:CaymanSKU:- Ivacaftor is an orally bioavailable potentiator of the cystic fibrosis transmembrane conductance regulator (CFTR) that improves chloride transport.{25614} It increases the forskolin-induced CFTR-mediated epithelial current in cells expressing the G551D missense mutation associated with severe cystic fibrosis by approximately 4-fold (EC50 = 100 nM) but has no effect on current in the absence of forskolin.{25614} Ivacaftor increases chloride secretion in cultured human cystic fibrosis bronchial epithelial cells carrying the G551D mutation on one allele and the common ΔF508 processing mutation on the other allele.{25614} It binds CFTR directly and leads to CFTR channel opening via an ATP-independent mechanism.{25613} Formulations containing ivacaftor have been used in the treatment of cystic fibrosis in patients carrying one or more mutations in the CFTR gene.
Brand:CaymanSKU:- Ivacaftor is an orally bioavailable potentiator of the cystic fibrosis transmembrane conductance regulator (CFTR) that improves chloride transport.{25614} It increases the forskolin-induced CFTR-mediated epithelial current in cells expressing the G551D missense mutation associated with severe cystic fibrosis by approximately 4-fold (EC50 = 100 nM) but has no effect on current in the absence of forskolin.{25614} Ivacaftor increases chloride secretion in cultured human cystic fibrosis bronchial epithelial cells carrying the G551D mutation on one allele and the common ΔF508 processing mutation on the other allele.{25614} It binds CFTR directly and leads to CFTR channel opening via an ATP-independent mechanism.{25613} Formulations containing ivacaftor have been used in the treatment of cystic fibrosis in patients carrying one or more mutations in the CFTR gene.
Brand:CaymanSKU:-
Ivacaftor-d19 is intended for use as an internal standard for the quantification of ivacaftor (Item No. 15145) by GC- or LC-MS. Ivacaftor is an orally bioavailable potentiator of the cystic fibrosis transmembrane conductance regulator (CFTR) that improves chloride transport.{25614} It increases the forskolin-induced CFTR-mediated epithelial current in cells expressing the G551D missense mutation associated with severe cystic fibrosis by approximately 4-fold (EC50 = 100 nM) but has no effect on current in the absence of forskolin.{25614} Ivacaftor increases chloride secretion in cultured human cystic fibrosis bronchial epithelial cells carrying the G551D mutation on one allele and the common ΔF508 processing mutation on the other allele.{25614} It binds CFTR directly and leads to CFTR channel opening via an ATP-independent mechanism.{25613} Formulations containing ivacaftor have been used in the treatment of cystic fibrosis in patients carrying one or more mutations in the CFTR gene.
Brand:CaymanSKU:28539 - 1 mgAvailable on backorder
Ivermectin B1a is the main component (>80%) of the anthelmintic ivermectin, which also contains ivermectin B1b (23824).{39419} It produces antiparasitic activity by binding to glutamate-gated chloride channels expressed on nematode neurons and pharyngeal muscle cells, inducing irreversible channel opening and very long-lasting hyperpolarization/depolarization of the neuron/muscle cell, thereby blocking further function (EC50 = 104 nM).{30216,28250} Formulations containing ivermectin inhibit replication of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) in Vero/hSLAM cells.{55038}
Brand:CaymanSKU:-Available on backorder
Ivermectin B1a is the main component (>80%) of the anthelmintic ivermectin, which also contains ivermectin B1b (23824).{39419} It produces antiparasitic activity by binding to glutamate-gated chloride channels expressed on nematode neurons and pharyngeal muscle cells, inducing irreversible channel opening and very long-lasting hyperpolarization/depolarization of the neuron/muscle cell, thereby blocking further function (EC50 = 104 nM).{30216,28250} Formulations containing ivermectin inhibit replication of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) in Vero/hSLAM cells.{55038}
Brand:CaymanSKU:-Available on backorder
Ivermectin B1a aglycone is an acid degradation product produced by hydrolysis of the disaccharide unit of ivermectin. It can inhibit nematode larval development, but does not cause paralytic activity.{31085}
Brand:CaymanSKU:-Available on backorder
Ivermectin B1a aglycone is an acid degradation product produced by hydrolysis of the disaccharide unit of ivermectin. It can inhibit nematode larval development, but does not cause paralytic activity.{31085}
Brand:CaymanSKU:-Available on backorder
Ivermectin B1a monosaccharide is produced by selective hydrolysis of the terminal saccharide unit of ivermectin.{31087} It can inhibit nematode larval development, but does not cause paralytic activity. This compound has been used as a probe to detect some types of ivermectin resistance.{31085}
Brand:CaymanSKU:-Available on backorder
Ivermectin B1a monosaccharide is produced by selective hydrolysis of the terminal saccharide unit of ivermectin.{31087} It can inhibit nematode larval development, but does not cause paralytic activity. This compound has been used as a probe to detect some types of ivermectin resistance.{31085}
Brand:CaymanSKU:-Available on backorder
Ivermectin B1b is the minor component (1a (>80%; Item No. 18768).{39419} It produces antiparasitic activity by binding to glutamate-gated chloride channels expressed on nematode neurons and pharyngeal muscle cells, inducing irreversible channel opening and very long-lasting hyperpolarization/depolarization of the neuron/muscle cell, thereby blocking further function.{30216,28250} Formulations containing ivermectin inhibit replication of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) in Vero/hSLAM cells.{55038}
Brand:CaymanSKU:23824 - 2.5 mgAvailable on backorder
Ivermectin B1b is the minor component (1a (>80%; Item No. 18768).{39419} It produces antiparasitic activity by binding to glutamate-gated chloride channels expressed on nematode neurons and pharyngeal muscle cells, inducing irreversible channel opening and very long-lasting hyperpolarization/depolarization of the neuron/muscle cell, thereby blocking further function.{30216,28250} Formulations containing ivermectin inhibit replication of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) in Vero/hSLAM cells.{55038}
Brand:CaymanSKU:23824 - 500 µgAvailable on backorder
IWP-12 is a small molecule inhibitor of porcupine (PORCN), which is an acyltransferase that palmitoylates and activates Wnt proteins.{27202} IWP-12 inhibits cell-autonomous Wnt signaling with an IC50 value of 15 nM.
Brand:CaymanSKU:22729 -Out of stock
IWP-12 is a small molecule inhibitor of porcupine (PORCN), which is an acyltransferase that palmitoylates and activates Wnt proteins.{27202} IWP-12 inhibits cell-autonomous Wnt signaling with an IC50 value of 15 nM.
Brand:CaymanSKU:22729 -Out of stock
IWP-12 is a small molecule inhibitor of porcupine (PORCN), which is an acyltransferase that palmitoylates and activates Wnt proteins.{27202} IWP-12 inhibits cell-autonomous Wnt signaling with an IC50 value of 15 nM.
Brand:CaymanSKU:22729 -Out of stock
IWP-12 is a small molecule inhibitor of porcupine (PORCN), which is an acyltransferase that palmitoylates and activates Wnt proteins.{27202} IWP-12 inhibits cell-autonomous Wnt signaling with an IC50 value of 15 nM.
Brand:CaymanSKU:22729 -Out of stock
Wnt signaling proteins are small secreted proteins that are active in embryonic development, tissue homeostasis, and tumorigenesis.{17947,14336,13185} Wnt proteins bind to receptors on the cell surface, initiating a signaling cascade that leads to β-catenin activation of gene transcription. IWP-2 is an inhibitor of Wnt production that impairs Wnt pathway activity in vitro with an IC50 value of 27 nM.{17505} IWP-2 inactivates Porcupine, a membrane-bound O-acyltransferase responsible for palmitoylating Wnt proteins, which is essential for their signaling ability and secretion.{17505} At 5 μM, IWP-2 has been shown to block Wnt-dependent phosphorylation of the frizzled co-receptor and the scaffold protein Dishevelled, preventing the accumulation of β-catenin.{17505} This compound has been used to suppress embryonic stem cell self-renewal and to decrease cancer cell proliferation, migration, and invasion.{23268,23269}
Brand:CaymanSKU:- Wnt signaling proteins are small secreted proteins that are active in embryonic development, tissue homeostasis, and tumorigenesis.{17947,14336,13185} Wnt proteins bind to receptors on the cell surface, initiating a signaling cascade that leads to β-catenin activation of gene transcription. IWP-2 is an inhibitor of Wnt production that impairs Wnt pathway activity in vitro with an IC50 value of 27 nM.{17505} IWP-2 inactivates Porcupine, a membrane-bound O-acyltransferase responsible for palmitoylating Wnt proteins, which is essential for their signaling ability and secretion.{17505} At 5 μM, IWP-2 has been shown to block Wnt-dependent phosphorylation of the frizzled co-receptor and the scaffold protein Dishevelled, preventing the accumulation of β-catenin.{17505} This compound has been used to suppress embryonic stem cell self-renewal and to decrease cancer cell proliferation, migration, and invasion.{23268,23269}
Brand:CaymanSKU:- Wnt signaling proteins are small secreted proteins that are active in embryonic development, tissue homeostasis, and tumorigenesis.{17947,14336,13185} Wnt proteins bind to receptors on the cell surface, initiating a signaling cascade that leads to β-catenin activation of gene transcription. IWP-2 is an inhibitor of Wnt production that impairs Wnt pathway activity in vitro with an IC50 value of 27 nM.{17505} IWP-2 inactivates Porcupine, a membrane-bound O-acyltransferase responsible for palmitoylating Wnt proteins, which is essential for their signaling ability and secretion.{17505} At 5 μM, IWP-2 has been shown to block Wnt-dependent phosphorylation of the frizzled co-receptor and the scaffold protein Dishevelled, preventing the accumulation of β-catenin.{17505} This compound has been used to suppress embryonic stem cell self-renewal and to decrease cancer cell proliferation, migration, and invasion.{23268,23269}
Brand:CaymanSKU:- Wnt signaling proteins are small secreted proteins that are active in embryonic development, tissue homeostasis, and tumorigenesis.{17947,14336,13185} Wnt proteins bind to receptors on the cell surface, initiating a signaling cascade that leads to β-catenin activation of gene transcription. IWP-2 is an inhibitor of Wnt production that impairs Wnt pathway activity in vitro with an IC50 value of 27 nM.{17505} IWP-2 inactivates Porcupine, a membrane-bound O-acyltransferase responsible for palmitoylating Wnt proteins, which is essential for their signaling ability and secretion.{17505} At 5 μM, IWP-2 has been shown to block Wnt-dependent phosphorylation of the frizzled co-receptor and the scaffold protein Dishevelled, preventing the accumulation of β-catenin.{17505} This compound has been used to suppress embryonic stem cell self-renewal and to decrease cancer cell proliferation, migration, and invasion.{23268,23269}
Brand:CaymanSKU:-
Wnt signaling proteins are small secreted proteins that are active in embryonic development, tissue homeostasis, and tumorigenesis.{17947,14336,13185} Wnt proteins bind to receptors on the cell surface, initiating a signaling cascade that leads to β-catenin activation of gene transcription. IWP-2 (Item No. 13951) is an inhibitor of Wnt production (IC50 = 27 nM) that inactivates porcupine, a membrane-bound O-acyltransferase whose palmitoylation activity is essential for the signaling ability and secretion of Wnt proteins.{17505} IWP-2-V2 is a less potent IWP-2 derivative whose chemical structure retains the benzothiazole group of its parent compound.{17505} It has been used to determine which structural features of IWP-2 are essential for impairing Wnt/β-catenin pathway activity.{17505}
Brand:CaymanSKU:- Wnt signaling proteins are small secreted proteins that are active in embryonic development, tissue homeostasis, and tumorigenesis.{17947,14336,13185} Wnt proteins bind to receptors on the cell surface, initiating a signaling cascade that leads to β-catenin activation of gene transcription. IWP-2 (Item No. 13951) is an inhibitor of Wnt production (IC50 = 27 nM) that inactivates porcupine, a membrane-bound O-acyltransferase whose palmitoylation activity is essential for the signaling ability and secretion of Wnt proteins.{17505} IWP-2-V2 is a less potent IWP-2 derivative whose chemical structure retains the benzothiazole group of its parent compound.{17505} It has been used to determine which structural features of IWP-2 are essential for impairing Wnt/β-catenin pathway activity.{17505}
Brand:CaymanSKU:- Wnt signaling proteins are small secreted proteins that are active in embryonic development, tissue homeostasis, and tumorigenesis.{17947,14336,13185} Wnt proteins bind to receptors on the cell surface, initiating a signaling cascade that leads to β-catenin activation of gene transcription. IWP-2 (Item No. 13951) is an inhibitor of Wnt production (IC50 = 27 nM) that inactivates porcupine, a membrane-bound O-acyltransferase whose palmitoylation activity is essential for the signaling ability and secretion of Wnt proteins.{17505} IWP-2-V2 is a less potent IWP-2 derivative whose chemical structure retains the benzothiazole group of its parent compound.{17505} It has been used to determine which structural features of IWP-2 are essential for impairing Wnt/β-catenin pathway activity.{17505}
Brand:CaymanSKU:- Wnt signaling proteins are small secreted proteins that are active in embryonic development, tissue homeostasis, and tumorigenesis.{17947,14336,13185} Wnt proteins bind to receptors on the cell surface, initiating a signaling cascade that leads to β-catenin activation of gene transcription. IWP-2 (Item No. 13951) is an inhibitor of Wnt production (IC50 = 27 nM) that inactivates porcupine, a membrane-bound O-acyltransferase whose palmitoylation activity is essential for the signaling ability and secretion of Wnt proteins.{17505} IWP-2-V2 is a less potent IWP-2 derivative whose chemical structure retains the benzothiazole group of its parent compound.{17505} It has been used to determine which structural features of IWP-2 are essential for impairing Wnt/β-catenin pathway activity.{17505}
Brand:CaymanSKU:-
Wnt signaling proteins are small secreted proteins that are active in embryonic development, tissue homeostasis, and tumorigenesis.{17947,14336,13185} Wnt proteins bind to receptors on the cell surface, initiating a signaling cascade that leads to β-catenin activation of gene transcription. IWP-3 is an inhibitor of Wnt production that impairs Wnt pathway activity in vitro with an IC50 value of 40 nM.{17505} IWP-3 inactivates porcupine, a membrane-bound O-acyltransferase responsible for palmitoylating Wnt proteins, which is essential for their signaling ability and secretion.{17505} At 5 μM, IWP-3 has been shown to block Wnt-dependent phosphorylation of the low-density lipoprotein receptor-related protein 6 (LRP6) and the scaffold protein Dishevelled, preventing the accumulation of β-catenin.{17505} By inhibiting Wnt signaling, IWP-3 has been used to promote cardiomyocyte generation from human embryonic stem cells (EC50 = 1.2 μM).{23267}
Brand:CaymanSKU:- Wnt signaling proteins are small secreted proteins that are active in embryonic development, tissue homeostasis, and tumorigenesis.{17947,14336,13185} Wnt proteins bind to receptors on the cell surface, initiating a signaling cascade that leads to β-catenin activation of gene transcription. IWP-3 is an inhibitor of Wnt production that impairs Wnt pathway activity in vitro with an IC50 value of 40 nM.{17505} IWP-3 inactivates porcupine, a membrane-bound O-acyltransferase responsible for palmitoylating Wnt proteins, which is essential for their signaling ability and secretion.{17505} At 5 μM, IWP-3 has been shown to block Wnt-dependent phosphorylation of the low-density lipoprotein receptor-related protein 6 (LRP6) and the scaffold protein Dishevelled, preventing the accumulation of β-catenin.{17505} By inhibiting Wnt signaling, IWP-3 has been used to promote cardiomyocyte generation from human embryonic stem cells (EC50 = 1.2 μM).{23267}
Brand:CaymanSKU:- Wnt signaling proteins are small secreted proteins that are active in embryonic development, tissue homeostasis, and tumorigenesis.{17947,14336,13185} Wnt proteins bind to receptors on the cell surface, initiating a signaling cascade that leads to β-catenin activation of gene transcription. IWP-3 is an inhibitor of Wnt production that impairs Wnt pathway activity in vitro with an IC50 value of 40 nM.{17505} IWP-3 inactivates porcupine, a membrane-bound O-acyltransferase responsible for palmitoylating Wnt proteins, which is essential for their signaling ability and secretion.{17505} At 5 μM, IWP-3 has been shown to block Wnt-dependent phosphorylation of the low-density lipoprotein receptor-related protein 6 (LRP6) and the scaffold protein Dishevelled, preventing the accumulation of β-catenin.{17505} By inhibiting Wnt signaling, IWP-3 has been used to promote cardiomyocyte generation from human embryonic stem cells (EC50 = 1.2 μM).{23267}
Brand:CaymanSKU:- Wnt signaling proteins are small secreted proteins that are active in embryonic development, tissue homeostasis, and tumorigenesis.{17947,14336,13185} Wnt proteins bind to receptors on the cell surface, initiating a signaling cascade that leads to β-catenin activation of gene transcription. IWP-3 is an inhibitor of Wnt production that impairs Wnt pathway activity in vitro with an IC50 value of 40 nM.{17505} IWP-3 inactivates porcupine, a membrane-bound O-acyltransferase responsible for palmitoylating Wnt proteins, which is essential for their signaling ability and secretion.{17505} At 5 μM, IWP-3 has been shown to block Wnt-dependent phosphorylation of the low-density lipoprotein receptor-related protein 6 (LRP6) and the scaffold protein Dishevelled, preventing the accumulation of β-catenin.{17505} By inhibiting Wnt signaling, IWP-3 has been used to promote cardiomyocyte generation from human embryonic stem cells (EC50 = 1.2 μM).{23267}
Brand:CaymanSKU:-
IWP-4 is an inhibitor of Wnt production that impairs Wnt pathway activity in vitro with an IC50 value of 25 nM.{17505} IWP-4 inactivates Porcupine, a membrane-bound O-acyltransferase responsible for palmitoylating Wnt proteins, which is essential for their signaling ability and secretion.{17505} At 5 μM, IWP-4 has been shown to block Wnt-dependent phosphorylation of the low-density lipoprotein receptor-related protein 6 receptor and the scaffold protein Dishevelled, preventing the accumulation of β-catenin.{17505} This compound has been used to induce cardiomyocyte differentiation from human pluripotent stem cells.{23268}
Brand:CaymanSKU:- IWP-4 is an inhibitor of Wnt production that impairs Wnt pathway activity in vitro with an IC50 value of 25 nM.{17505} IWP-4 inactivates Porcupine, a membrane-bound O-acyltransferase responsible for palmitoylating Wnt proteins, which is essential for their signaling ability and secretion.{17505} At 5 μM, IWP-4 has been shown to block Wnt-dependent phosphorylation of the low-density lipoprotein receptor-related protein 6 receptor and the scaffold protein Dishevelled, preventing the accumulation of β-catenin.{17505} This compound has been used to induce cardiomyocyte differentiation from human pluripotent stem cells.{23268}
Brand:CaymanSKU:- IWP-4 is an inhibitor of Wnt production that impairs Wnt pathway activity in vitro with an IC50 value of 25 nM.{17505} IWP-4 inactivates Porcupine, a membrane-bound O-acyltransferase responsible for palmitoylating Wnt proteins, which is essential for their signaling ability and secretion.{17505} At 5 μM, IWP-4 has been shown to block Wnt-dependent phosphorylation of the low-density lipoprotein receptor-related protein 6 receptor and the scaffold protein Dishevelled, preventing the accumulation of β-catenin.{17505} This compound has been used to induce cardiomyocyte differentiation from human pluripotent stem cells.{23268}
Brand:CaymanSKU:- IWP-4 is an inhibitor of Wnt production that impairs Wnt pathway activity in vitro with an IC50 value of 25 nM.{17505} IWP-4 inactivates Porcupine, a membrane-bound O-acyltransferase responsible for palmitoylating Wnt proteins, which is essential for their signaling ability and secretion.{17505} At 5 μM, IWP-4 has been shown to block Wnt-dependent phosphorylation of the low-density lipoprotein receptor-related protein 6 receptor and the scaffold protein Dishevelled, preventing the accumulation of β-catenin.{17505} This compound has been used to induce cardiomyocyte differentiation from human pluripotent stem cells.{23268}
Brand:CaymanSKU:-
Porcupine (PORCN) is a membrane bound O-acyltransferase that mediates palmitoylation of Wnt family proteins.{27064} This step is required for secretion and biologic activity of Wnt proteins, which have roles in embryonic development and cancer.{27064,27062} IWP-L6 is a potent inhibitor of PORCN (EC50 = 0.5 nM).{27202} It suppresses the phosphorylation of disheveled 2 in HEK293 cells. IWP-L6 displays high stability in human plasma (t1/2 > 24 hours) and in zebrafish, but it is much less stable in plasma from mice and rats.{27202} In zebrafish, IWP-L6 blocks Wnt/β-catenin-dependent developmental processes, including tailfin regeneration and posterior axis formation.{27202} It also completely prevents branching morphogenesis in cultured mouse embryonic kidneys at doses of 50 nM and above, indicating complete inhibition of Wnt signaling.{27202}
Brand:CaymanSKU:- Porcupine (PORCN) is a membrane bound O-acyltransferase that mediates palmitoylation of Wnt family proteins.{27064} This step is required for secretion and biologic activity of Wnt proteins, which have roles in embryonic development and cancer.{27064,27062} IWP-L6 is a potent inhibitor of PORCN (EC50 = 0.5 nM).{27202} It suppresses the phosphorylation of disheveled 2 in HEK293 cells. IWP-L6 displays high stability in human plasma (t1/2 > 24 hours) and in zebrafish, but it is much less stable in plasma from mice and rats.{27202} In zebrafish, IWP-L6 blocks Wnt/β-catenin-dependent developmental processes, including tailfin regeneration and posterior axis formation.{27202} It also completely prevents branching morphogenesis in cultured mouse embryonic kidneys at doses of 50 nM and above, indicating complete inhibition of Wnt signaling.{27202}
Brand:CaymanSKU:-