1627962-21-3
Chemical Structure
VS-II-173
- CAS No.: 1627962-21-3
- Formula:C14H8N4O2
- Molecular Weight:264.24
IUPAC Name: 5-nitro-3H-pyrazolo[4,3-a]phenanthridine
InChIKey: JKBYIWGVODPSLG-UHFFFAOYSA-N
SMILES: O=[N+]([O-])C1=C(N=CC2=C3C=CC=C2)C3=C4C=NNC4=C1
Biological Activity: VS-II-173 is a pan-Pim kinase inhibitor with IC50 values of 0.07 μM and 0.02 μM for Pim1 and Pim3, respectively, and a residual activity of 46% for Pim2 at 1 μM. VS-II-173 also inhibits kinases such as HIPK2, PRK2, RSK1, DYRK1a and AMPKα1, selectively inhibiting acute myeloid leukemia (AML) cells with significantly lower toxicity to non-malignant cells (EC50 > 30 μM). VS-II-173 weakens the phosphorylation of substrates such as Stat5 (Y694), MDM2 (S166), Bad (S112), and 4E-BP1 (T37/46) by inhibiting Pim kinase-mediated signaling pathways, blocking pro-survival signals in AML cells and inducing apoptosis. VS-II-173 synergistically enhances anti-AML activity when combined with Daunorubicin (HY-13062A). VS-II-173 can be used in AML research, especially for AML with FLT3-ITD mutations and NPM1 mutations [1][2].
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VS-II-173 | VS-II-173 is a pan-Pim kinase inhibitor with IC50 values of 0.07 μM and 0.02 μM for Pim1 and Pim3, respectively, and a residual activity of 46% for Pim2 at 1 μM. VS-II-173 also inhibits kinases such as HIPK2, PRK2, RSK1, DYRK1a and AMPKα1, selectively inhibiting acute myeloid leukemia (AML) cells with significantly lower toxicity to non-malignant cells (EC50 > 30 μM). VS-II-173 weakens the phosphorylation of substrates such as Stat5 (Y694), MDM2 (S166), Bad (S112), and 4E-BP1 (T37/46) by inhibiting Pim kinase-mediated signaling pathways, blocking pro-survival signals in AML cells and inducing apoptosis. VS-II-173 synergistically enhances anti-AML activity when combined with Daunorubicin (HY-13062A). VS-II-173 can be used in AML research, especially for AML with FLT3-ITD mutations and NPM1 mutations . | |||||||||||||||||||||
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References
- [1]. Bjørnstad R, et al. A Kinase Inhibitor with Anti-Pim Kinase Activity is a Potent and Selective Cytotoxic Agent Toward Acute Myeloid Leukemia. Mol Cancer Ther. 2019;18(3):567-578. [Content Brief]
- [2]. Auvert E, et al. Synthesis of new pyrazolo[4,3-a]phenanthridine Pim-1 inhibitors and evaluation of their cytotoxic activity towards the MOLM-13 acute myeloid leukemia cell line. Bioorg Med Chem Lett. 2022;73:128914. [Content Brief]
