sk1

SK1-IN-1 is an orally available and potent sphingosine kinase 1 (SPHK1) inhibitor (IC50: 58 nM), with potential anticancer activity, and can be used to study cancer and neurodegenerative diseases.

BML-258 HCl was removed and discontinued.

SK1-I hydrochloride is the salt form of SK1-I(BML-258). SK1-I is a selective and competitive sphingosine kinase 1 (SphK1) inhibitor and sphingosine analog that is inactive against SphK2 and a variety of other protein kinases, and possesses anti-leukemic potential to inhibit tumor cell growth and promote apoptosis.

SSK1 is a compound that selectively kills senescent cells and is a precursor for β-galactosidase, which can reduce the inflammatory response of the body. SSK1 can activate the phosphorylation of p38 MAPK and MKK3 MKK6 in senescent cells, and promote mitochondrial DNA damage in senescent cells.

GSK1940029 (SCD inhibitor 1) is an inhibitor of stearoyl-CoA desaturase (SCD).

GSK1904529A (GSK 4529) is a specific inhibitor of IGF-1R (IC50=27 nM) and IR(IC50=25 nM) .

HSK16149 is a novel ligand of voltage-gated calcium channel (VGCC) α 2 δ subunit with analgesic activity.

GSK126 (GSK2816126A) is a excellently specific EZH2 methyltransferase inhibitor ( IC50=9.9 nM).

GSK137647A (GSK 137647) is a selective agonist of FFA4.

GSK1016790A (GSK101) (GSK101) is a novel, potent activator of TRPV4 (transient receptor potential vanilloid 4) with EC50 of 34 nM in choroid plexus epithelial cells.

GSK1379725A is a selective BPTF ligand [Kd = 2.8 μM].

GSK1324726A (I-BET726) is a greatly specific inhibitor of BET family proteins for BRD2(IC50=41 nM), BRD3(IC50=31 nM), and BRD4 (IC50=22 nM).

ASK1-IN-4 is an ASK1 inhibitor, IC50 = 0.2 μM.

GSK199 is a selective PAD4 inhibitor(IC50 of 200 nM in the absence of calcium).

ASK1-IN-1 is an inhibitor of apoptosis signal-regulating kinase 1 which is a key mediator in the apoptotic and inflammatory cellular stress response with an IC50 of 21 nM in biochemica assays.

GSK1059865 is a potent antagonist of the orexin 1 receptor.

GSK1521498 free base (hydrochloride) is a selective μ-opioid receptor (MOR) antagonist used to treat compulsive consumption disorders involving food, alcohol, and drugs.

GSK1521498 free base is a potent and selective μ-opioid receptor antagonist with potential applications in treating disorders of compulsive consumption of food, alcohol, and drugs.

GSK1521498 is a selective antagonist of the μ-opioid receptor (MOR). It is being used for the treatment of disorders of compulsive consumption of food, alcohol, and drugs.

GSK1702934A, a selective TRPC3 agonist, modulates cardiac contractility and arrhythmogenesis through TRPC3 activation.

GSK180 is a selective competitive inhibitor of kynurenine 3-monooxygenase (KMO; IC50: ~6 nM), an enzyme involved in tryptophan metabolism.

GSK163929 (compound 122) is an orally active CCR5 antagonist with anti-HIV properties and demonstrates low inhibitory potency against hEGR. Administered at a dosage of 2000 mg kg day (i.v., 7 d), it shows no adverse effects in rats, and at 250 mg kg day (i.v., 7 d), it is similarly non-toxic in dogs.

ASK1-IN-7 (Compound 4c) is an ASK1 inhibitor and a derivative of the ASK1 inhibitor scaffold 5-(5-Phenyl-furan-2-ylmethylene)-2-thioxo-thiazolidin-4-one. This compound is potentially applicable in research involving ASK1 signaling pathways, including studies on cellular stress response, inflammatory response, neurodegenerative diseases, and cardiovascular diseases.

GSK1059615 has been used in trials studying the treatment of Lymphoma, Solid Tumours, Endometrial Cancer, Solid Tumor Cancer, and Metastatic Breast Cancer.