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GPR120 (free fatty acid receptor 4/FFAR4) is a G protein-coupled receptor expressed in intestine, adipocytes, and pro-inflammatory macrophages that is activated by long-chain free fatty acids. It has been linked to the ability of fatty acids to produce anti-inflammatory effects and to acutely potentiate insulin secretion. Grifolic acid is a selective partial agonist of GPR120 that induces ERK activation and intracellular calcium responses in mouse enteroendocrine STC-1 cells that express GPR120 endogenously, but not those expressing GPR40.{31125}
Brand:CaymanSKU:-Available on backorder
Griseofulvin is a natural bacterial product used, in certain formulations, as an oral antibiotic for fungal infections of the skin.{31420} It alters microtubule dynamics, resulting in metaphase arrest.{31421} Antimicrotubule agents, including griseofulvin, have potential applications in cancer therapy, particularly when combined with other chemotherapeutic compounds.{31422,31419}
Brand:CaymanSKU:-Available on backorder
Griseofulvin is a natural bacterial product used, in certain formulations, as an oral antibiotic for fungal infections of the skin.{31420} It alters microtubule dynamics, resulting in metaphase arrest.{31421} Antimicrotubule agents, including griseofulvin, have potential applications in cancer therapy, particularly when combined with other chemotherapeutic compounds.{31422,31419}
Brand:CaymanSKU:-Available on backorder
Griseofulvin is a natural bacterial product used, in certain formulations, as an oral antibiotic for fungal infections of the skin.{31420} It alters microtubule dynamics, resulting in metaphase arrest.{31421} Antimicrotubule agents, including griseofulvin, have potential applications in cancer therapy, particularly when combined with other chemotherapeutic compounds.{31422,31419}
Brand:CaymanSKU:-Available on backorder
GH is a polypeptide hormone with a molecular weight of 23 kDa released from somatotropes of the anterior pituitary. It is regulated by several neurotransmitters and neuropeptides. Among other functions it plays an essential role in regulating body growth. Plasma GH levels in humans are markedly elevated in the perinatal period, in the range of 50 ng/ml, but decline to near-adult levels of 0.5-1.0 ng/ml within a few weeks. GH levels are slightly higher in women than in men, and are increased in both sexes in response to exercise. [Bertin Catalog No. A05104]
Brand:CaymanSKU:589601 - 96 wellsAvailable on backorder
Brand:CaymanSKU:32755 - 25 µLAvailable on backorder
Brand:CaymanSKU:32755- 25 µLAvailable on backorder
Brand:CaymanSKU:32755- 25 µL
Glucose-regulated protein 78 kDa (GRP78), also known as heat shock 70 kDa protein 5 (HspA5) and immunoglobulin heavy chain-binding protein (BiP), is a glucose-regulated protein that is constitutively expressed in the lumen of the endoplasmic reticulum (ER).{36130,36131,36132} It is composed of two functional domains, an N-terminal nucleotide-binding domain that contains an ATP catalytic site and a C-terminal substrate binding domain that binds hydrophobic polypeptides.{36134} GRP78 functions as a molecular chaperone, assisting in the translocation of polypeptides from the cytosol into the ER, folding of nascent polypeptides, as well as refolding and preventing aggregation of misfolded proteins. It also plays a role in the ER-assisted degradation (ERAD) and unfolded protein response (UPR) pathways.{36137,36136} GRP78 chaperone activity is driven by an ATPase cycle that is regulated by ER-localized DnaJ-like protein co-factors and nuclear exchange factors.{36133,36135} Expression of GRP78 is upregulated in response to ER stress caused by viral and bacterial infections as well as various cancers.{36139} ER stress can also promote extracellular secretion of GRP78 leading to its anti-inflammatory functions in immunity.{36138} Cayman’s GRP78 Monoclonal Antibody can be used for Western blot and ELISA applications. The antibody recognizes GRP78 at ~72 kDa from human, mouse, and rat samples.
Brand:CaymanSKU:25690 - 100 µgAvailable on backorder
Immunogen: Full length human recombinant GRP78 protein • Host: Mouse • Species reactivity: (+) Human, Mouse, Rat • Cross reactivity: (-) Hsp70 • Applications: ELISA,IHC, WB
Brand:CaymanSKU:25690- 100 µgAvailable on backorder
Immunogen: Full length human recombinant GRP78 protein • Host: Mouse • Species reactivity: (+) Human, Mouse, Rat • Cross reactivity: (-) Hsp70 • Applications: ELISA,IHC, WB
Brand:CaymanSKU:25690- 100 µg
Glucose-regulated protein 78 kDa (GRP78), also known as heat shock 70 kDa protein 5 (HspA5) and immunoglobulin heavy chain-binding protein (BiP), is a glucose-regulated protein that is constitutively expressed in the lumen of the endoplasmic reticulum (ER).{36130,36131,36132} It is composed of two functional domains, an N-terminal nucleotide-binding domain that contains an ATP catalytic site and a C-terminal substrate binding domain that binds hydrophobic polypeptides.{36134} GRP78 functions as a molecular chaperone, assisting in the translocation of polypeptides from the cytosol into the ER, folding of nascent polypeptides, as well as refolding and preventing aggregation of misfolded proteins. It also plays a role in the ER-assisted degradation (ERAD) and unfolded protein response (UPR) pathways.{36137,36136} GRP78 chaperone activity is driven by an ATPase cycle that is regulated by ER-localized DnaJ-like protein co-factors and nuclear exchange factors.{36133,36135} Expression of GRP78 is upregulated in response to ER stress caused by viral and bacterial infections as well as various cancers.{36139} ER stress can also promote extracellular secretion of GRP78 leading to its anti-inflammatory functions in immunity.{36138} Cayman’s GRP78 Polyclonal Antibody can be used for Western blot and ELISA applications. The antibody recognizes GRP78 at ~72 kDa from human samples.
Brand:CaymanSKU:24533 - 500 µgAvailable on backorder
Immunogen: Human recombinant GRP78 protein (full length) • Host: Rabbit • Species reactivity: (+) Human • Applications: ELISA, IHC, WB
Brand:CaymanSKU:24533- 500 µgAvailable on backorder
Immunogen: Human recombinant GRP78 protein (full length) • Host: Rabbit • Species reactivity: (+) Human • Applications: ELISA, IHC, WB
Brand:CaymanSKU:24533- 500 µg Immunogen: Purified GRP94 isolated from chicken oviducts · Host: rat, clone 9G10 · Species Reactivity: (+) Human, African clawed frog (X. laevis), bovine, chicken, dog, guinea pig (C. porcellus), hamster, horse, monkey, mouse, pig, rabbit, rat, and sheep GPR94 · Applications: FC, ICC/IF, IP, and WB · Isotype: IgG2a
Brand:CaymanSKU:10011424- 200 µg Glucose regulated protein 94 (GRP94) is a constitutively expressed endoplasmic reticulum (ER) lumenal protein that is up-regulated in response to cellular stress such as heat shock, oxidative stress or glucose depletion. GRP94 is thought to play a role in protein translocation to the ER, in their subsequent folding and assembly, and in regulating protein secretion.{15669} GRP94 also plays a role in antigen presentation by accessing the endogenous pathway and eliciting specific cytotoxic T lymphocyte (CTL) responses to chaperone bound peptides via the major histocompatibility complex (MHC) class I pathway.{15670} GRP94 is a member of the Hsp90 family of stress proteins and shares sequence homology with its cytosolic equivalent, Hsp90.{15671} Both Hsp90 and GRP94 are calcium binding proteins.{15672} Despite sharing 50% sequence homology over its N domains and complete conservation in its ligand binding domains with Hsp90, GRP94, and Hsp90 differ in their interactions with regulatory ligands as GRP94 has weak ATP binding and hydrolysis activity.{15673} GRP94 exists as a homodimer and the two subunits interact at two distinct intermolecular sites, C-terminal dimerization domains and the N-terminal interacts with the middle domain of opposing subunits.{15674} GRP94 contains a carboxy terminal KDEL (Lys-Asp-Glu-Leu) sequence which is believed to aid in its retention in the ER.{15675}
Brand:CaymanSKU:10011424 - 200 µgAvailable on backorder
Immunogen: Purified GRP94 isolated from chicken oviducts · Host: rat, clone 9G10 · Species Reactivity: (+) Human, African clawed frog (X. laevis), bovine, chicken, dog, guinea pig (C. porcellus), hamster, horse, monkey, mouse, pig, rabbit, rat, and sheep GPR94 · Applications: FC, ICC/IF, IP, and WB · Isotype: IgG2a
Brand:CaymanSKU:10011424- 200 µgAvailable on backorder
Immunogen: Purified GRP94 isolated from chicken oviducts · Host: rat, clone 9G10 · Species Reactivity: (+) Human, African clawed frog (X. laevis), bovine, chicken, dog, guinea pig (C. porcellus), hamster, horse, monkey, mouse, pig, rabbit, rat, and sheep GPR94 · Applications: FC, ICC/IF, IP, and WB · Isotype: IgG2a
Brand:CaymanSKU:10011424- 50 µg Glucose regulated protein 94 (GRP94) is a constitutively expressed endoplasmic reticulum (ER) lumenal protein that is up-regulated in response to cellular stress such as heat shock, oxidative stress or glucose depletion. GRP94 is thought to play a role in protein translocation to the ER, in their subsequent folding and assembly, and in regulating protein secretion.{15669} GRP94 also plays a role in antigen presentation by accessing the endogenous pathway and eliciting specific cytotoxic T lymphocyte (CTL) responses to chaperone bound peptides via the major histocompatibility complex (MHC) class I pathway.{15670} GRP94 is a member of the Hsp90 family of stress proteins and shares sequence homology with its cytosolic equivalent, Hsp90.{15671} Both Hsp90 and GRP94 are calcium binding proteins.{15672} Despite sharing 50% sequence homology over its N domains and complete conservation in its ligand binding domains with Hsp90, GRP94, and Hsp90 differ in their interactions with regulatory ligands as GRP94 has weak ATP binding and hydrolysis activity.{15673} GRP94 exists as a homodimer and the two subunits interact at two distinct intermolecular sites, C-terminal dimerization domains and the N-terminal interacts with the middle domain of opposing subunits.{15674} GRP94 contains a carboxy terminal KDEL (Lys-Asp-Glu-Leu) sequence which is believed to aid in its retention in the ER.{15675}
Brand:CaymanSKU:10011424 - 50 µgAvailable on backorder
Immunogen: Purified GRP94 isolated from chicken oviducts · Host: rat, clone 9G10 · Species Reactivity: (+) Human, African clawed frog (X. laevis), bovine, chicken, dog, guinea pig (C. porcellus), hamster, horse, monkey, mouse, pig, rabbit, rat, and sheep GPR94 · Applications: FC, ICC/IF, IP, and WB · Isotype: IgG2a
Brand:CaymanSKU:10011424- 50 µgAvailable on backorder
GS-143 is an inhibitor of IκBα ubiquitylation.{45272} It inhibits ubiquitylation of phosphorylated IκBα mediated by the SCFβTrCP1 E3 ubiquitin ligase complex in vitro (IC50 = 5.2 μM) and reduces TNF-α-induced degradation of phosphorylated IκBα, but not β-catenin, another SCFβTrCP1 substrate, in HeLa S3 cells. GS-143 inhibits LPS-induced expression of TNF-α, IL-6, IL-12, ICAM-1, and NF-κB in THP-1 cells in a concentration-dependent manner. Intranasal administration of GS-143 (32 μg/animal) reduces the number of eosinophils, lymphocytes, and total cells in bronchoalveolar lavage fluid (BALF) in an ovalbumin-sensitized mouse model of allergic asthma.{45273}
Brand:CaymanSKU:26138 - 10 mgAvailable on backorder
GS-143 is an inhibitor of IκBα ubiquitylation.{45272} It inhibits ubiquitylation of phosphorylated IκBα mediated by the SCFβTrCP1 E3 ubiquitin ligase complex in vitro (IC50 = 5.2 μM) and reduces TNF-α-induced degradation of phosphorylated IκBα, but not β-catenin, another SCFβTrCP1 substrate, in HeLa S3 cells. GS-143 inhibits LPS-induced expression of TNF-α, IL-6, IL-12, ICAM-1, and NF-κB in THP-1 cells in a concentration-dependent manner. Intranasal administration of GS-143 (32 μg/animal) reduces the number of eosinophils, lymphocytes, and total cells in bronchoalveolar lavage fluid (BALF) in an ovalbumin-sensitized mouse model of allergic asthma.{45273}
Brand:CaymanSKU:26138 - 25 mgAvailable on backorder
GS-143 is an inhibitor of IκBα ubiquitylation.{45272} It inhibits ubiquitylation of phosphorylated IκBα mediated by the SCFβTrCP1 E3 ubiquitin ligase complex in vitro (IC50 = 5.2 μM) and reduces TNF-α-induced degradation of phosphorylated IκBα, but not β-catenin, another SCFβTrCP1 substrate, in HeLa S3 cells. GS-143 inhibits LPS-induced expression of TNF-α, IL-6, IL-12, ICAM-1, and NF-κB in THP-1 cells in a concentration-dependent manner. Intranasal administration of GS-143 (32 μg/animal) reduces the number of eosinophils, lymphocytes, and total cells in bronchoalveolar lavage fluid (BALF) in an ovalbumin-sensitized mouse model of allergic asthma.{45273}
Brand:CaymanSKU:26138 - 5 mgAvailable on backorder
GS-143 is an inhibitor of IκBα ubiquitylation.{45272} It inhibits ubiquitylation of phosphorylated IκBα mediated by the SCFβTrCP1 E3 ubiquitin ligase complex in vitro (IC50 = 5.2 μM) and reduces TNF-α-induced degradation of phosphorylated IκBα, but not β-catenin, another SCFβTrCP1 substrate, in HeLa S3 cells. GS-143 inhibits LPS-induced expression of TNF-α, IL-6, IL-12, ICAM-1, and NF-κB in THP-1 cells in a concentration-dependent manner. Intranasal administration of GS-143 (32 μg/animal) reduces the number of eosinophils, lymphocytes, and total cells in bronchoalveolar lavage fluid (BALF) in an ovalbumin-sensitized mouse model of allergic asthma.{45273}
Brand:CaymanSKU:26138 - 50 mgAvailable on backorder
![A positive allosteric modulator of GABAB receptors; potentiates GABA-stimulated [35S]GTPγS binding to recombinant human GABAB receptors and rat cortical membranes (EC50s = 2.1 and 3.1 μM](https://interpriseusa.com/wp-content/uploads/2021/06/29482.png)
GS-39783 is a positive allosteric modulator of GABAB receptors that potentiates GABA-stimulated [35S]GTPγS binding to recombinant human GABAB receptors and rat cortical membranes (EC50s = 2.1 and 3.1 μM, respectively).{53122} It amplifies GABAB receptor-mediated transient calcium signaling in HEK293 cells expressing human receptors (EC50 = 2.4 μM). GS-39783 (25-100 mg/kg) suppresses alcohol self-administration, but has no effect on lever-responding for food, in Indiana alcohol-preferring, Sardinian alcohol-preferring, and Alko Alcohol rats.{53123} It reduces amphetamine- or MK-801-induced hyperactivity in rats and the number of DOI-induced head twitches in mice, indicating antipsychotic-like activity.{53124} GS-39783 also reduces the incidence of sound-induced tonic convulsions in juvenile mice (ED50 = 55.38 mg/kg).{53125}
Brand:CaymanSKU:29482 - 10 mgAvailable on backorder
GS-39783 is a positive allosteric modulator of GABAB receptors that potentiates GABA-stimulated [35S]GTPγS binding to recombinant human GABAB receptors and rat cortical membranes (EC50s = 2.1 and 3.1 μM, respectively).{53122} It amplifies GABAB receptor-mediated transient calcium signaling in HEK293 cells expressing human receptors (EC50 = 2.4 μM). GS-39783 (25-100 mg/kg) suppresses alcohol self-administration, but has no effect on lever-responding for food, in Indiana alcohol-preferring, Sardinian alcohol-preferring, and Alko Alcohol rats.{53123} It reduces amphetamine- or MK-801-induced hyperactivity in rats and the number of DOI-induced head twitches in mice, indicating antipsychotic-like activity.{53124} GS-39783 also reduces the incidence of sound-induced tonic convulsions in juvenile mice (ED50 = 55.38 mg/kg).{53125}
Brand:CaymanSKU:29482 - 25 mgAvailable on backorder
GS-39783 is a positive allosteric modulator of GABAB receptors that potentiates GABA-stimulated [35S]GTPγS binding to recombinant human GABAB receptors and rat cortical membranes (EC50s = 2.1 and 3.1 μM, respectively).{53122} It amplifies GABAB receptor-mediated transient calcium signaling in HEK293 cells expressing human receptors (EC50 = 2.4 μM). GS-39783 (25-100 mg/kg) suppresses alcohol self-administration, but has no effect on lever-responding for food, in Indiana alcohol-preferring, Sardinian alcohol-preferring, and Alko Alcohol rats.{53123} It reduces amphetamine- or MK-801-induced hyperactivity in rats and the number of DOI-induced head twitches in mice, indicating antipsychotic-like activity.{53124} GS-39783 also reduces the incidence of sound-induced tonic convulsions in juvenile mice (ED50 = 55.38 mg/kg).{53125}
Brand:CaymanSKU:29482 - 5 mgAvailable on backorder
GS-39783 is a positive allosteric modulator of GABAB receptors that potentiates GABA-stimulated [35S]GTPγS binding to recombinant human GABAB receptors and rat cortical membranes (EC50s = 2.1 and 3.1 μM, respectively).{53122} It amplifies GABAB receptor-mediated transient calcium signaling in HEK293 cells expressing human receptors (EC50 = 2.4 μM). GS-39783 (25-100 mg/kg) suppresses alcohol self-administration, but has no effect on lever-responding for food, in Indiana alcohol-preferring, Sardinian alcohol-preferring, and Alko Alcohol rats.{53123} It reduces amphetamine- or MK-801-induced hyperactivity in rats and the number of DOI-induced head twitches in mice, indicating antipsychotic-like activity.{53124} GS-39783 also reduces the incidence of sound-induced tonic convulsions in juvenile mice (ED50 = 55.38 mg/kg).{53125}
Brand:CaymanSKU:29482 - 50 mgAvailable on backorder
GS-441524 is an antiviral nucleoside analog and a metabolite of remdesivir (Item No. 30354).{45842} Upon entry into cells, GS-441524 is metabolized to an active triphosphate form that induces RNA chain termination and inhibits viral polymerases. It is active against Middle East respiratory syndrome coronavirus (MERS-CoV) and severe acute respiratory syndrome CoV (SARS-CoV) in infected primary human airway epithelial (HAE) cells (EC50s = 0.86 and 0.18 µM, respectively). GS-441524 reduces viral plaque formation in SARS-CoV-2-infected Vero E6 and Calu-3 2B4 cells (EC50s = 0.42 and 0.62 mM, respectively).{61140} It is cytoprotective against hepatitis C virus (HCV), yellow fever virus (YFV), dengue virus type 2 (DENV-2), influenza A, and parainfluenza 3 in cell-based assays (EC50s = 4.1, 11, 9.46, 27.9, and 1.71 µM, respectively).{53439}
Brand:CaymanSKU:30469 - 1 mgAvailable on backorder
GS-441524 is an antiviral nucleoside analog and a metabolite of remdesivir (Item No. 30354).{45842} Upon entry into cells, GS-441524 is metabolized to an active triphosphate form that induces RNA chain termination and inhibits viral polymerases. It is active against Middle East respiratory syndrome coronavirus (MERS-CoV) and severe acute respiratory syndrome CoV (SARS-CoV) in infected primary human airway epithelial (HAE) cells (EC50s = 0.86 and 0.18 µM, respectively). GS-441524 reduces viral plaque formation in SARS-CoV-2-infected Vero E6 and Calu-3 2B4 cells (EC50s = 0.42 and 0.62 mM, respectively).{61140} It is cytoprotective against hepatitis C virus (HCV), yellow fever virus (YFV), dengue virus type 2 (DENV-2), influenza A, and parainfluenza 3 in cell-based assays (EC50s = 4.1, 11, 9.46, 27.9, and 1.71 µM, respectively).{53439}
Brand:CaymanSKU:30469 - 10 mgAvailable on backorder
GS-441524 is an antiviral nucleoside analog and a metabolite of remdesivir (Item No. 30354).{45842} Upon entry into cells, GS-441524 is metabolized to an active triphosphate form that induces RNA chain termination and inhibits viral polymerases. It is active against Middle East respiratory syndrome coronavirus (MERS-CoV) and severe acute respiratory syndrome CoV (SARS-CoV) in infected primary human airway epithelial (HAE) cells (EC50s = 0.86 and 0.18 µM, respectively). GS-441524 reduces viral plaque formation in SARS-CoV-2-infected Vero E6 and Calu-3 2B4 cells (EC50s = 0.42 and 0.62 mM, respectively).{61140} It is cytoprotective against hepatitis C virus (HCV), yellow fever virus (YFV), dengue virus type 2 (DENV-2), influenza A, and parainfluenza 3 in cell-based assays (EC50s = 4.1, 11, 9.46, 27.9, and 1.71 µM, respectively).{53439}
Brand:CaymanSKU:30469 - 25 mgAvailable on backorder
GS-441524 is an antiviral nucleoside analog and a metabolite of remdesivir (Item No. 30354).{45842} Upon entry into cells, GS-441524 is metabolized to an active triphosphate form that induces RNA chain termination and inhibits viral polymerases. It is active against Middle East respiratory syndrome coronavirus (MERS-CoV) and severe acute respiratory syndrome CoV (SARS-CoV) in infected primary human airway epithelial (HAE) cells (EC50s = 0.86 and 0.18 µM, respectively). GS-441524 reduces viral plaque formation in SARS-CoV-2-infected Vero E6 and Calu-3 2B4 cells (EC50s = 0.42 and 0.62 mM, respectively).{61140} It is cytoprotective against hepatitis C virus (HCV), yellow fever virus (YFV), dengue virus type 2 (DENV-2), influenza A, and parainfluenza 3 in cell-based assays (EC50s = 4.1, 11, 9.46, 27.9, and 1.71 µM, respectively).{53439}
Brand:CaymanSKU:30469 - 5 mgAvailable on backorder
Brand:CaymanSKU:9003635 - 1 mgAvailable on backorder
Brand:CaymanSKU:9003635 - 5 mgAvailable on backorder
GS-704277 is an intermediate alanine metabolite of the antiviral prodrug remdesivir (Item No. 30354).{52858,52859} It is formed from remdesivir via intracellular hydrolysis. GS-704277 is further metabolized to the nucleoside monophosphate form and then to the nucleoside analog GS-441524 (Item No. 30469) or active nucleoside triphosphate GS-443902.
Brand:CaymanSKU:9003569 - 1 mgAvailable on backorder
GS-704277 is an intermediate alanine metabolite of the antiviral prodrug remdesivir (Item No. 30354).{52858,52859} It is formed from remdesivir via intracellular hydrolysis. GS-704277 is further metabolized to the nucleoside monophosphate form and then to the nucleoside analog GS-441524 (Item No. 30469) or active nucleoside triphosphate GS-443902.
Brand:CaymanSKU:9003569 - 500 µgAvailable on backorder
GS-7340 is a prodrug form of the antiviral adenosine analog tenofovir (Item No. 13874).{42639} It reduces HIV-1 viral replication in MT-2 cells with an EC50 value of 5 nM.
Brand:CaymanSKU:26214 - 10 mgAvailable on backorder
GS-7340 is a prodrug form of the antiviral adenosine analog tenofovir (Item No. 13874).{42639} It reduces HIV-1 viral replication in MT-2 cells with an EC50 value of 5 nM.
Brand:CaymanSKU:26214 - 100 mgAvailable on backorder
GS-7340 is a prodrug form of the antiviral adenosine analog tenofovir (Item No. 13874).{42639} It reduces HIV-1 viral replication in MT-2 cells with an EC50 value of 5 nM.
Brand:CaymanSKU:26214 - 5 mgAvailable on backorder
GS-7340 is a prodrug form of the antiviral adenosine analog tenofovir (Item No. 13874).{42639} It reduces HIV-1 viral replication in MT-2 cells with an EC50 value of 5 nM.
Brand:CaymanSKU:26214 - 50 mgAvailable on backorder
GS-9620 is an orally available agonist of toll-like receptor 7 (TLR7; EC50 = 291 nM) with 30-fold selectivity over TLR8 (EC50 = 9 µM).{32637} It has been shown to stimulate a TLR7 immune response in two different animal models of chronic hepatitis B infection and to inhibit HIV-1 infection in human peripheral blood mononuclear cells.{32636,32635,32634}
Brand:CaymanSKU:19628 -Available on backorder
GS-9620 is an orally available agonist of toll-like receptor 7 (TLR7; EC50 = 291 nM) with 30-fold selectivity over TLR8 (EC50 = 9 µM).{32637} It has been shown to stimulate a TLR7 immune response in two different animal models of chronic hepatitis B infection and to inhibit HIV-1 infection in human peripheral blood mononuclear cells.{32636,32635,32634}
Brand:CaymanSKU:19628 -Available on backorder
GS-9620 is an orally available agonist of toll-like receptor 7 (TLR7; EC50 = 291 nM) with 30-fold selectivity over TLR8 (EC50 = 9 µM).{32637} It has been shown to stimulate a TLR7 immune response in two different animal models of chronic hepatitis B infection and to inhibit HIV-1 infection in human peripheral blood mononuclear cells.{32636,32635,32634}
Brand:CaymanSKU:19628 -Available on backorder
GS-9620 is an orally available agonist of toll-like receptor 7 (TLR7; EC50 = 291 nM) with 30-fold selectivity over TLR8 (EC50 = 9 µM).{32637} It has been shown to stimulate a TLR7 immune response in two different animal models of chronic hepatitis B infection and to inhibit HIV-1 infection in human peripheral blood mononuclear cells.{32636,32635,32634}
Brand:CaymanSKU:19628 -Available on backorder
Spleen tyrosine kinase (Syk) is a non-receptor tyrosine kinase that upon phosphorylation binds to immunoreceptor tyrosine-based activation motifs of FcRγ chains and mediates downstream signaling related to platelet function and inflammation.{24052} GS-9973 is a potent Syk inhibitor (IC50 = 7.7 nM) that demonstrates 10-35-fold selectivity for Syk over a panel of 359 nonmutant kinases.{28699} In conjunction with the PI3Kδ inhibitor CAL-101 (Item No. 15279), it has been used to reduce chronic lymphocytic leukemia cell survival and to disrupt chemokine signaling at nanomolar concentrations.{28700}
Brand:CaymanSKU:-Available on backorder
Spleen tyrosine kinase (Syk) is a non-receptor tyrosine kinase that upon phosphorylation binds to immunoreceptor tyrosine-based activation motifs of FcRγ chains and mediates downstream signaling related to platelet function and inflammation.{24052} GS-9973 is a potent Syk inhibitor (IC50 = 7.7 nM) that demonstrates 10-35-fold selectivity for Syk over a panel of 359 nonmutant kinases.{28699} In conjunction with the PI3Kδ inhibitor CAL-101 (Item No. 15279), it has been used to reduce chronic lymphocytic leukemia cell survival and to disrupt chemokine signaling at nanomolar concentrations.{28700}
Brand:CaymanSKU:-Available on backorder
Spleen tyrosine kinase (Syk) is a non-receptor tyrosine kinase that upon phosphorylation binds to immunoreceptor tyrosine-based activation motifs of FcRγ chains and mediates downstream signaling related to platelet function and inflammation.{24052} GS-9973 is a potent Syk inhibitor (IC50 = 7.7 nM) that demonstrates 10-35-fold selectivity for Syk over a panel of 359 nonmutant kinases.{28699} In conjunction with the PI3Kδ inhibitor CAL-101 (Item No. 15279), it has been used to reduce chronic lymphocytic leukemia cell survival and to disrupt chemokine signaling at nanomolar concentrations.{28700}
Brand:CaymanSKU:-Available on backorder
Spleen tyrosine kinase (Syk) is a non-receptor tyrosine kinase that upon phosphorylation binds to immunoreceptor tyrosine-based activation motifs of FcRγ chains and mediates downstream signaling related to platelet function and inflammation.{24052} GS-9973 is a potent Syk inhibitor (IC50 = 7.7 nM) that demonstrates 10-35-fold selectivity for Syk over a panel of 359 nonmutant kinases.{28699} In conjunction with the PI3Kδ inhibitor CAL-101 (Item No. 15279), it has been used to reduce chronic lymphocytic leukemia cell survival and to disrupt chemokine signaling at nanomolar concentrations.{28700}
Brand:CaymanSKU:-Available on backorder
Inhibition of cardiac late sodium current (late INa) is a strategy to suppress arrhythmias and sodium-dependent calcium overload associated with myocardial ischemia and heart failure. GS967 is a selective inhibitor of late INa that has been shown to suppress experimentally induced arrhythmias in rabbit myocytes and hearts.{30900} It can inhibit A. sulcata toxin II–induced late INa in ventricular myocytes and isolated hearts with IC50 values of 0.13 and 0.21 µM, respectively.{30900} GS967 causes minimal inhibition of the delayed-rectifier potassium current nor does it affect L- or T-type calcium channel currents, sodium-calcium exchanger currents, or a panel of 162 receptors, ion channels, transporters, and enzymes.{30900}
Brand:CaymanSKU:-Available on backorder
Inhibition of cardiac late sodium current (late INa) is a strategy to suppress arrhythmias and sodium-dependent calcium overload associated with myocardial ischemia and heart failure. GS967 is a selective inhibitor of late INa that has been shown to suppress experimentally induced arrhythmias in rabbit myocytes and hearts.{30900} It can inhibit A. sulcata toxin II–induced late INa in ventricular myocytes and isolated hearts with IC50 values of 0.13 and 0.21 µM, respectively.{30900} GS967 causes minimal inhibition of the delayed-rectifier potassium current nor does it affect L- or T-type calcium channel currents, sodium-calcium exchanger currents, or a panel of 162 receptors, ion channels, transporters, and enzymes.{30900}
Brand:CaymanSKU:-Available on backorder
Inhibition of cardiac late sodium current (late INa) is a strategy to suppress arrhythmias and sodium-dependent calcium overload associated with myocardial ischemia and heart failure. GS967 is a selective inhibitor of late INa that has been shown to suppress experimentally induced arrhythmias in rabbit myocytes and hearts.{30900} It can inhibit A. sulcata toxin II–induced late INa in ventricular myocytes and isolated hearts with IC50 values of 0.13 and 0.21 µM, respectively.{30900} GS967 causes minimal inhibition of the delayed-rectifier potassium current nor does it affect L- or T-type calcium channel currents, sodium-calcium exchanger currents, or a panel of 162 receptors, ion channels, transporters, and enzymes.{30900}
Brand:CaymanSKU:-Available on backorder
Smoothened (SMO) is a cell surface receptor that, with Patched, mediates hedgehog signaling to regulate gene expression through the Gli transcription factors.{21774} GSA 10 is a quinolinecarboxamide derivative that acts as an agonist of SMO.{26551} By acting at SMO, GSA 10 has been shown to promote the differentiation of multipotent mesenchymal progenitor cells into osteoblasts (EC50 = 1.2 µM).{26551} Most notably, GSA 10 does not recognize the classic cyclopamine binding site as do other SMO agonists and as such has been used to characterize a novel SMO active site.{26551}
Brand:CaymanSKU:- Smoothened (SMO) is a cell surface receptor that, with Patched, mediates hedgehog signaling to regulate gene expression through the Gli transcription factors.{21774} GSA 10 is a quinolinecarboxamide derivative that acts as an agonist of SMO.{26551} By acting at SMO, GSA 10 has been shown to promote the differentiation of multipotent mesenchymal progenitor cells into osteoblasts (EC50 = 1.2 µM).{26551} Most notably, GSA 10 does not recognize the classic cyclopamine binding site as do other SMO agonists and as such has been used to characterize a novel SMO active site.{26551}
Brand:CaymanSKU:- Smoothened (SMO) is a cell surface receptor that, with Patched, mediates hedgehog signaling to regulate gene expression through the Gli transcription factors.{21774} GSA 10 is a quinolinecarboxamide derivative that acts as an agonist of SMO.{26551} By acting at SMO, GSA 10 has been shown to promote the differentiation of multipotent mesenchymal progenitor cells into osteoblasts (EC50 = 1.2 µM).{26551} Most notably, GSA 10 does not recognize the classic cyclopamine binding site as do other SMO agonists and as such has been used to characterize a novel SMO active site.{26551}
Brand:CaymanSKU:- Smoothened (SMO) is a cell surface receptor that, with Patched, mediates hedgehog signaling to regulate gene expression through the Gli transcription factors.{21774} GSA 10 is a quinolinecarboxamide derivative that acts as an agonist of SMO.{26551} By acting at SMO, GSA 10 has been shown to promote the differentiation of multipotent mesenchymal progenitor cells into osteoblasts (EC50 = 1.2 µM).{26551} Most notably, GSA 10 does not recognize the classic cyclopamine binding site as do other SMO agonists and as such has been used to characterize a novel SMO active site.{26551}
Brand:CaymanSKU:-
The histone H3 lysine 27 (H3K27) demethylase JMJD3 plays important roles in the transcriptional regulation of cell differentiation, development, the inflammatory response, and cancer.{19496,19494} GSK-J1 is a potent inhibitor of the H3K27 histone demethylases JMJD3 and UTX (IC50s = 18 and 56 µM, respectively as measured by mass spectrometry; IC50 = 60 nM in JMJD3 antibody-based assays).{21388} It is inactive against a panel of additional JMJ family demethylases, including several variants of JMJD2 and JMJD1 and, at concentrations up to 30 μM, has no effect on more than 100 different kinases or other unrelated proteins, including other chromatin-modifying enzymes such as histone deacetylases.{21388} Since the highly polar carboxylate group of GSK-J1 restricts its cellular permeability, a prodrug ethyl ester, GSK-J4 (Item No. 12073) has also been developed. See the Structural Genomics Consortium (SGC) website for more information.
Brand:CaymanSKU:12054 - 1 mgAvailable on backorder
The histone H3 lysine 27 (H3K27) demethylase JMJD3 plays important roles in the transcriptional regulation of cell differentiation, development, the inflammatory response, and cancer.{19496,19494} GSK-J1 is a potent inhibitor of the H3K27 histone demethylases JMJD3 and UTX (IC50s = 18 and 56 µM, respectively as measured by mass spectrometry; IC50 = 60 nM in JMJD3 antibody-based assays).{21388} It is inactive against a panel of additional JMJ family demethylases, including several variants of JMJD2 and JMJD1 and, at concentrations up to 30 μM, has no effect on more than 100 different kinases or other unrelated proteins, including other chromatin-modifying enzymes such as histone deacetylases.{21388} Since the highly polar carboxylate group of GSK-J1 restricts its cellular permeability, a prodrug ethyl ester, GSK-J4 (Item No. 12073) has also been developed. See the Structural Genomics Consortium (SGC) website for more information.
Brand:CaymanSKU:12054 - 10 mgAvailable on backorder
The histone H3 lysine 27 (H3K27) demethylase JMJD3 plays important roles in the transcriptional regulation of cell differentiation, development, the inflammatory response, and cancer.{19496,19494} GSK-J1 is a potent inhibitor of the H3K27 histone demethylases JMJD3 and UTX (IC50s = 18 and 56 µM, respectively as measured by mass spectrometry; IC50 = 60 nM in JMJD3 antibody-based assays).{21388} It is inactive against a panel of additional JMJ family demethylases, including several variants of JMJD2 and JMJD1 and, at concentrations up to 30 μM, has no effect on more than 100 different kinases or other unrelated proteins, including other chromatin-modifying enzymes such as histone deacetylases.{21388} Since the highly polar carboxylate group of GSK-J1 restricts its cellular permeability, a prodrug ethyl ester, GSK-J4 (Item No. 12073) has also been developed. See the Structural Genomics Consortium (SGC) website for more information.
Brand:CaymanSKU:12054 - 5 mgAvailable on backorder
The histone H3 lysine 27 (H3K27) demethylase JMJD3 plays important roles in the transcriptional regulation of cell differentiation, development, the inflammatory response, and cancer.{19496,19494} GSK-J1 is a potent inhibitor of the H3K27 histone demethylases JMJD3 and UTX (IC50s = 18 and 56 µM, respectively as measured by mass spectrometry; IC50 = 60 nM in JMJD3 antibody-based assays).{21388} It is inactive against a panel of additional JMJ family demethylases, including several variants of JMJD2 and JMJD1 and, at concentrations up to 30 μM, has no effect on more than 100 different kinases or other unrelated proteins, including other chromatin-modifying enzymes such as histone deacetylases.{21388} Since the highly polar carboxylate group of GSK-J1 restricts its cellular permeability, a prodrug ethyl ester, GSK-J4 (Item No. 12073) has also been developed. See the Structural Genomics Consortium (SGC) website for more information.
Brand:CaymanSKU:12054 - 50 mgAvailable on backorder
The histone H3 lysine 27 (H3K27) demethylase JMJD3 plays important roles in the transcriptional regulation of cell differentiation, development, the inflammatory response, and cancer.{19496,19494} GSK-J2 is a pyridine regio-isomer of GSK-J1 which poorly inhibits JMJD3 (IC50 > 100 μM), making it an appropriate negative control for in vitro studies involving GSK-J1.{21388} For in vivo research, cell-permeable prodrug forms of GSK-J1 and GSK-J2 are available as GSK-J4 (Item No. 12073) and GSK-J5 (Item No. 12074), respectively. See the Structural Genomics Consortium (SGC) website for more information.
Brand:CaymanSKU:12056 - 1 mgAvailable on backorder
The histone H3 lysine 27 (H3K27) demethylase JMJD3 plays important roles in the transcriptional regulation of cell differentiation, development, the inflammatory response, and cancer.{19496,19494} GSK-J2 is a pyridine regio-isomer of GSK-J1 which poorly inhibits JMJD3 (IC50 > 100 μM), making it an appropriate negative control for in vitro studies involving GSK-J1.{21388} For in vivo research, cell-permeable prodrug forms of GSK-J1 and GSK-J2 are available as GSK-J4 (Item No. 12073) and GSK-J5 (Item No. 12074), respectively. See the Structural Genomics Consortium (SGC) website for more information.
Brand:CaymanSKU:12056 - 10 mgAvailable on backorder
The histone H3 lysine 27 (H3K27) demethylase JMJD3 plays important roles in the transcriptional regulation of cell differentiation, development, the inflammatory response, and cancer.{19496,19494} GSK-J2 is a pyridine regio-isomer of GSK-J1 which poorly inhibits JMJD3 (IC50 > 100 μM), making it an appropriate negative control for in vitro studies involving GSK-J1.{21388} For in vivo research, cell-permeable prodrug forms of GSK-J1 and GSK-J2 are available as GSK-J4 (Item No. 12073) and GSK-J5 (Item No. 12074), respectively. See the Structural Genomics Consortium (SGC) website for more information.
Brand:CaymanSKU:12056 - 5 mgAvailable on backorder
The histone H3 lysine 27 (H3K27) demethylase JMJD3 plays important roles in the transcriptional regulation of cell differentiation, development, the inflammatory response, and cancer.{19496,19494} GSK-J2 is a pyridine regio-isomer of GSK-J1 which poorly inhibits JMJD3 (IC50 > 100 μM), making it an appropriate negative control for in vitro studies involving GSK-J1.{21388} For in vivo research, cell-permeable prodrug forms of GSK-J1 and GSK-J2 are available as GSK-J4 (Item No. 12073) and GSK-J5 (Item No. 12074), respectively. See the Structural Genomics Consortium (SGC) website for more information.
Brand:CaymanSKU:12056 - 50 mgAvailable on backorder
The histone H3 lysine 27 (H3K27) demethylase JMJD3 plays important roles in the transcriptional regulation of cell differentiation, development, the inflammatory response, and cancer.{19496,19494} GSK-J4 (hydrochloride) is an ethyl ester derivative of the JMJD3 selective histone demethylase inhibitor GSK-J1 (Item No. 12054) with an IC50 value greater than 50 μM in vitro.{21388} Acting as a prodrug, GSK-J4 is rapidly hydrolyzed in cells to the otherwise cell impermeable GSK-J1, which exhibits an IC50 value of 60 nM for the purified enzyme. When administered to human primary macrophages, GSK-J4 can reduce LPS-induced proinflammatory cytokine production, most notably including that of TNFα (IC50 = 9 µM).{21388}
Brand:CaymanSKU:12073 - 1 mgAvailable on backorder
The histone H3 lysine 27 (H3K27) demethylase JMJD3 plays important roles in the transcriptional regulation of cell differentiation, development, the inflammatory response, and cancer.{19496,19494} GSK-J4 (hydrochloride) is an ethyl ester derivative of the JMJD3 selective histone demethylase inhibitor GSK-J1 (Item No. 12054) with an IC50 value greater than 50 μM in vitro.{21388} Acting as a prodrug, GSK-J4 is rapidly hydrolyzed in cells to the otherwise cell impermeable GSK-J1, which exhibits an IC50 value of 60 nM for the purified enzyme. When administered to human primary macrophages, GSK-J4 can reduce LPS-induced proinflammatory cytokine production, most notably including that of TNFα (IC50 = 9 µM).{21388}
Brand:CaymanSKU:12073 - 10 mgAvailable on backorder
The histone H3 lysine 27 (H3K27) demethylase JMJD3 plays important roles in the transcriptional regulation of cell differentiation, development, the inflammatory response, and cancer.{19496,19494} GSK-J4 (hydrochloride) is an ethyl ester derivative of the JMJD3 selective histone demethylase inhibitor GSK-J1 (Item No. 12054) with an IC50 value greater than 50 μM in vitro.{21388} Acting as a prodrug, GSK-J4 is rapidly hydrolyzed in cells to the otherwise cell impermeable GSK-J1, which exhibits an IC50 value of 60 nM for the purified enzyme. When administered to human primary macrophages, GSK-J4 can reduce LPS-induced proinflammatory cytokine production, most notably including that of TNFα (IC50 = 9 µM).{21388}
Brand:CaymanSKU:12073 - 5 mgAvailable on backorder
The histone H3 lysine 27 (H3K27) demethylase JMJD3 plays important roles in the transcriptional regulation of cell differentiation, development, the inflammatory response, and cancer.{19496,19494} GSK-J4 (hydrochloride) is an ethyl ester derivative of the JMJD3 selective histone demethylase inhibitor GSK-J1 (Item No. 12054) with an IC50 value greater than 50 μM in vitro.{21388} Acting as a prodrug, GSK-J4 is rapidly hydrolyzed in cells to the otherwise cell impermeable GSK-J1, which exhibits an IC50 value of 60 nM for the purified enzyme. When administered to human primary macrophages, GSK-J4 can reduce LPS-induced proinflammatory cytokine production, most notably including that of TNFα (IC50 = 9 µM).{21388}
Brand:CaymanSKU:12073 - 50 mgAvailable on backorder
The histone H3 lysine 27 (H3K27) demethylase JMJD3 plays important roles in the transcriptional regulation of cell differentiation, development, the inflammatory response, and cancer.{19496,19494} GSK-J4 (Item No. 12073) is a cell-permeable prodrug which is modified by intracellular esterases to give GSK-J1 (Item No. 12054), an inhibitor of JMJD3. GSK-J5 is a pyridine regio-isomer of GSK-J4. Like GSK-J4, this isomer is cell-permeable and hydrolyzed to a free base.{21388} However, the free base is a weak inhibitor of JMJD3 (IC50 > 100 μM), making it an ideal inactive control molecule for elucidating the functional role of JMJD3 inhibition.{21388}
Brand:CaymanSKU:12074 - 1 mgAvailable on backorder
The histone H3 lysine 27 (H3K27) demethylase JMJD3 plays important roles in the transcriptional regulation of cell differentiation, development, the inflammatory response, and cancer.{19496,19494} GSK-J4 (Item No. 12073) is a cell-permeable prodrug which is modified by intracellular esterases to give GSK-J1 (Item No. 12054), an inhibitor of JMJD3. GSK-J5 is a pyridine regio-isomer of GSK-J4. Like GSK-J4, this isomer is cell-permeable and hydrolyzed to a free base.{21388} However, the free base is a weak inhibitor of JMJD3 (IC50 > 100 μM), making it an ideal inactive control molecule for elucidating the functional role of JMJD3 inhibition.{21388}
Brand:CaymanSKU:12074 - 10 mgAvailable on backorder
The histone H3 lysine 27 (H3K27) demethylase JMJD3 plays important roles in the transcriptional regulation of cell differentiation, development, the inflammatory response, and cancer.{19496,19494} GSK-J4 (Item No. 12073) is a cell-permeable prodrug which is modified by intracellular esterases to give GSK-J1 (Item No. 12054), an inhibitor of JMJD3. GSK-J5 is a pyridine regio-isomer of GSK-J4. Like GSK-J4, this isomer is cell-permeable and hydrolyzed to a free base.{21388} However, the free base is a weak inhibitor of JMJD3 (IC50 > 100 μM), making it an ideal inactive control molecule for elucidating the functional role of JMJD3 inhibition.{21388}
Brand:CaymanSKU:12074 - 5 mgAvailable on backorder
The histone H3 lysine 27 (H3K27) demethylase JMJD3 plays important roles in the transcriptional regulation of cell differentiation, development, the inflammatory response, and cancer.{19496,19494} GSK-J4 (Item No. 12073) is a cell-permeable prodrug which is modified by intracellular esterases to give GSK-J1 (Item No. 12054), an inhibitor of JMJD3. GSK-J5 is a pyridine regio-isomer of GSK-J4. Like GSK-J4, this isomer is cell-permeable and hydrolyzed to a free base.{21388} However, the free base is a weak inhibitor of JMJD3 (IC50 > 100 μM), making it an ideal inactive control molecule for elucidating the functional role of JMJD3 inhibition.{21388}
Brand:CaymanSKU:12074 - 50 mgAvailable on backorder
Lysine-specific demethylase 1 (LSD1) belongs to the family of flavin adenine dinucleotide (FAD)-dependent amine oxidases that include monoamine oxidases (MAOs) and polyamine oxidase (PAO).{12422} LSD1 specifically demethylates mono- and dimethylated histone H3 lysine 4, resulting in transcriptional repression.{14724} It also controls the tumor suppressor activity of p53 by demethylating a specific p53 lysine residue (LYS370).{15022} GSK-LSD1 is an irreversible, mechanism-based inhibitor of LSD1 (IC50 = 16 nM) that is >1,000-fold selective over the closely related FAD-utilizing enzymes LSD2, MAO-A, and MAO-B.{27091} GSK-LSD1 induces gene expression changes in various cancer cell lines, inhibiting their proliferation (EC50s Structural Genomics Consortium (SGC) website for more information.
Brand:CaymanSKU:-Out of stock
Lysine-specific demethylase 1 (LSD1) belongs to the family of flavin adenine dinucleotide (FAD)-dependent amine oxidases that include monoamine oxidases (MAOs) and polyamine oxidase (PAO).{12422} LSD1 specifically demethylates mono- and dimethylated histone H3 lysine 4, resulting in transcriptional repression.{14724} It also controls the tumor suppressor activity of p53 by demethylating a specific p53 lysine residue (LYS370).{15022} GSK-LSD1 is an irreversible, mechanism-based inhibitor of LSD1 (IC50 = 16 nM) that is >1,000-fold selective over the closely related FAD-utilizing enzymes LSD2, MAO-A, and MAO-B.{27091} GSK-LSD1 induces gene expression changes in various cancer cell lines, inhibiting their proliferation (EC50s Structural Genomics Consortium (SGC) website for more information.
Brand:CaymanSKU:-Out of stock
Lysine-specific demethylase 1 (LSD1) belongs to the family of flavin adenine dinucleotide (FAD)-dependent amine oxidases that include monoamine oxidases (MAOs) and polyamine oxidase (PAO).{12422} LSD1 specifically demethylates mono- and dimethylated histone H3 lysine 4, resulting in transcriptional repression.{14724} It also controls the tumor suppressor activity of p53 by demethylating a specific p53 lysine residue (LYS370).{15022} GSK-LSD1 is an irreversible, mechanism-based inhibitor of LSD1 (IC50 = 16 nM) that is >1,000-fold selective over the closely related FAD-utilizing enzymes LSD2, MAO-A, and MAO-B.{27091} GSK-LSD1 induces gene expression changes in various cancer cell lines, inhibiting their proliferation (EC50s Structural Genomics Consortium (SGC) website for more information.
Brand:CaymanSKU:-Out of stock
Lysine-specific demethylase 1 (LSD1) belongs to the family of flavin adenine dinucleotide (FAD)-dependent amine oxidases that include monoamine oxidases (MAOs) and polyamine oxidase (PAO).{12422} LSD1 specifically demethylates mono- and dimethylated histone H3 lysine 4, resulting in transcriptional repression.{14724} It also controls the tumor suppressor activity of p53 by demethylating a specific p53 lysine residue (LYS370).{15022} GSK-LSD1 is an irreversible, mechanism-based inhibitor of LSD1 (IC50 = 16 nM) that is >1,000-fold selective over the closely related FAD-utilizing enzymes LSD2, MAO-A, and MAO-B.{27091} GSK-LSD1 induces gene expression changes in various cancer cell lines, inhibiting their proliferation (EC50s Structural Genomics Consortium (SGC) website for more information.
Brand:CaymanSKU:-Out of stock
GSK0660 is the first reported antagonist of PPARβ/δ (IC50 = 155 nM) with no measurable affinity for PPARα or PPARγ (IC50s ≥ 10 μM).{32576} Because of the limited bioavailability of GSK0660, the related compound GSK3787 (Item No. 15219) was developed as a selective PPARβ/δ antagonist with more suitable pharmacokinetic properties.{24665}
Brand:CaymanSKU:- GSK0660 is the first reported antagonist of PPARβ/δ (IC50 = 155 nM) with no measurable affinity for PPARα or PPARγ (IC50s ≥ 10 μM).{32576} Because of the limited bioavailability of GSK0660, the related compound GSK3787 (Item No. 15219) was developed as a selective PPARβ/δ antagonist with more suitable pharmacokinetic properties.{24665}
Brand:CaymanSKU:- GSK0660 is the first reported antagonist of PPARβ/δ (IC50 = 155 nM) with no measurable affinity for PPARα or PPARγ (IC50s ≥ 10 μM).{32576} Because of the limited bioavailability of GSK0660, the related compound GSK3787 (Item No. 15219) was developed as a selective PPARβ/δ antagonist with more suitable pharmacokinetic properties.{24665}
Brand:CaymanSKU:- GSK0660 is the first reported antagonist of PPARβ/δ (IC50 = 155 nM) with no measurable affinity for PPARα or PPARγ (IC50s ≥ 10 μM).{32576} Because of the limited bioavailability of GSK0660, the related compound GSK3787 (Item No. 15219) was developed as a selective PPARβ/δ antagonist with more suitable pharmacokinetic properties.{24665}
Brand:CaymanSKU:-
Transient receptor potential vanilloid 4 (TRPV4) is a nonselective cation channel thought to be involved in osmoregulation, hyperalgesia, and control of epithelial cell volume. GSK1016790A is a TRPV4 agonist that has been reported to elicit calcium influx in HEK cells expressing mouse or human TRPV4 (EC50s = 18 and 2.1 nM, respectively).{28187} It has been used to demonstrate a role for TRPV4 in regulating urinary bladder activity and endothelial control of vascular tone.{28187,28188,28189}
Brand:CaymanSKU:-Available on backorder
Transient receptor potential vanilloid 4 (TRPV4) is a nonselective cation channel thought to be involved in osmoregulation, hyperalgesia, and control of epithelial cell volume. GSK1016790A is a TRPV4 agonist that has been reported to elicit calcium influx in HEK cells expressing mouse or human TRPV4 (EC50s = 18 and 2.1 nM, respectively).{28187} It has been used to demonstrate a role for TRPV4 in regulating urinary bladder activity and endothelial control of vascular tone.{28187,28188,28189}
Brand:CaymanSKU:-Available on backorder