sk1i

BML-258 HCl was removed and discontinued.

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-8 (Compound 35) is an orally active inhibitor of apoptosis signal-regulating kinase 1 (ASK1) with an IC50 value of 1.8 nM. In a mouse liver injury model induced by Acetaminophen, ASK1-IN-8 significantly reduces plasma alanine aminotransferase (ALT) levels, offering liver protection. This compound is useful for research in liver disease-related fields.

ASK1-IN-10 (Compound 27) is an apoptosis signal-regulating kinase 1 (ASK1) inhibitor with an IC50 of less than 200 nM. It also exhibits inhibitory activity on the hERG potassium channel. ASK1-IN-10 is utilized in inflammation research.

ASK1-IN-11 (Compound 7) is an inhibitor of apoptosis signal-regulating kinase 1 (ASK1) with an IC50 of less than 200 nM. It also exhibits inhibitory activity against TNF-α, MYLK/MLCK kinase, and the hERG potassium ion channel. ASK1-IN-11 can be utilized in inflammation research.

ASK1-IN-9 (Compound 3) is an inhibitor of apoptosis signal-regulating kinase 1 (ASK1) with an IC50 of less than 200 nM. It is applicable for inflammation research.

ASK1-IN-12 is an ASK1 inhibitor with an IC50 of 6.3 nM. It effectively suppresses the activation of the ASK1-p38/JNK pathway induced by TNF-α. Additionally, ASK1-IN-12 reduces cholesterol elevation and lipid droplet accumulation induced by free fatty acids, improving hepatic steatosis. This compound is valuable for research on non-alcoholic steatohepatitis (NASH).

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-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].

TASK-1-IN-1 is a potent and selective inhibitor of TASK-1 (Potassium Channel) with an IC50 of 148 nM, and exhibits a reduced inhibitory effect on the TASK-3 channel with an IC50 of 1750 nM. TASK-1-IN-1 also demonstrates anticancer effects.

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.