1177741-83-1
Chemical Structure
SKI II hydrochloride
- CAS No.: 1177741-83-1
- Formula:C15H12Cl2N2OS
- Molecular Weight:339.24
IUPAC Name: 4-((4-(4-chlorophenyl)thiazol-2-yl)amino)phenol hydrochloride
InChIKey: ZDRVLAOYDGQLFI-UHFFFAOYSA-N
SMILES: ClC1=CC=C(C2=CSC(NC3=CC=C(C=C3)O)=N2)C=C1.Cl
Biological Activity: SKI-II hydrochloride is an orally active dual-target inhibitor of SphK1/2 and DES1, with Ki values of 16 µM and 0.3 µM against SphK1 and DES1, respectively. SKI-II hydrochloride activates the PERK-Nrf2 antioxidant pathway by stabilizing Nrf2, and synergizes with Temozolomide (HY-17364) to induce oxidative/endoplasmic reticulum stress and cancer cell death under hypoxic conditions. SKI-II hydrochloride inhibits SphK activity, promotes ceramide accumulation and apoptosis, and synergizes with Cisplatin (HY-17394) to reverse drug resistance via the ras/MAPK pathway in vivo. SKI-II hydrochloride reduces measles virus replication by inhibiting mTORC1 activity. SKI-II hydrochloride binds to VCP to induce M1 polarization, enhances host tolerance to Staphylococcus aureus infection, and exerts radioprotective effects through Nrf2 activation and accelerated DNA repair. SKI-II hydrochloride can be used in research related to glioblastoma, acute myeloid leukemia, gastric cancer, measles virus infection, Staphylococcus aureus infection, and acute radiation syndrome[1][2][3][4][5][6][7][8].
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SKI II hydrochloride | SKI-II hydrochloride is an orally active dual-target inhibitor of SphK1/2 and DES1, with Ki values of 16 µM and 0.3 µM against SphK1 and DES1, respectively. SKI-II hydrochloride activates the PERK-Nrf2 antioxidant pathway by stabilizing Nrf2, and synergizes with Temozolomide (HY-17364) to induce oxidative/endoplasmic reticulum stress and cancer cell death under hypoxic conditions. SKI-II hydrochloride inhibits SphK activity, promotes ceramide accumulation and apoptosis, and synergizes with Cisplatin (HY-17394) to reverse drug resistance via the ras/MAPK pathway in vivo. SKI-II hydrochloride reduces measles virus replication by inhibiting mTORC1 activity. SKI-II hydrochloride binds to VCP to induce M1 polarization, enhances host tolerance to Staphylococcus aureus infection, and exerts radioprotective effects through Nrf2 activation and accelerated DNA repair. SKI-II hydrochloride can be used in research related to glioblastoma, acute myeloid leukemia, gastric cancer, measles virus infection, Staphylococcus aureus infection, and acute radiation syndrome. | |||||||||||||||||||||
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References
- [1]. Liu Y, et al. SKI-II reverses the chemoresistance of SGC7901/DDP gastric cancer cells. Oncology letters. 2014 Jul;8(1):367-373. [Content Brief]
- [2]. Chithelen J, et al. The Sphingolipid Inhibitors Ceranib-2 and SKI-II Reduce Measles Virus Replication in Primary Human Lymphocytes: Effects on mTORC1 Downstream Signaling. Frontiers in physiology. 2022;13:856143.
- [3]. Sousa N, et al. Targeting sphingolipid metabolism with the sphingosine kinase inhibitor SKI-II overcomes hypoxia-induced chemotherapy resistance in glioblastoma cells: effects on cell death, self-renewal, and invasion. BMC cancer. 2023 Aug 16;23(1):762.
- [4]. Yang L, et al. SphK1 inhibitor II (SKI-II) inhibits acute myelogenous leukemia cell growth in vitro and in vivo. Biochemical and biophysical research communications. 2015 May 15;460(4):903-8.
- [5]. Zhang L, et al. Identification of SKI-II as a host-protective immunomodulator against Staphylococcus aureus infection. mBio. 2026 Aug 10:e0155826.
- [6]. Sah DK, et al. Sphingosine kinase inhibitor, SKI-II confers protection against the ionizing radiation by maintaining redox homeostasis most likely through Nrf2 signaling. Life sciences. 2021 Aug 01;278:119543.
- [7]. French KJ, et al. Antitumor activity of sphingosine kinase inhibitors. J Pharmacol Exp Ther. 2006 Aug;318(2):596-603.
- [8]. Potì F, et al. SKI-II--a sphingosine kinase 1 inhibitor--exacerbates atherosclerosis in low-density lipoprotein receptor-deficient (LDL-R-/-) mice on high cholesterol diet. Atherosclerosis. 2015 May;240(1):212-5. [Content Brief]
