sk1-i

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.

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

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.

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.

ASK1-IN-3 is a highly potent and selective inhibitor of ASK1 kinase, demonstrating an IC 50 of 33.8 nM. This compound also exhibits inhibitory effects on various cell cycle regulating kinases. ASK1-IN-3 showcases remarkable induction of apoptosis in HepG2 cancer cells and displays potent activity in arresting the cell cycle [1].

ASK1-IN-6 (Compound 32), a selective apoptosis signal-regulating kinase 1 (ASK1) inhibitor, exhibits an IC50 of 25 nM. This compound readily crosses the blood-brain barrier, as evidenced by rat pharmacokinetics showing a clearance unchanged clearance rate of 1.6 56 L h kg and an unbound partition coefficient (Kp,uu) of 0.46. Additionally, ASK1-IN-6 demonstrates anti-inflammatory activity and effectively improves symptoms in the Alzheimer's Disease Tg4510 mouse model.

ASK1-IN-2 is a potent, orally active inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with an IC50 of 32.8 nM. It has potential therapeutic applications for ulcerative colitis[1].

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.