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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- CAS. Nr.: 1627962-21-3
- Formel: C14H8N4O2
- Molecular Weight:264.24
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Biologische Aktivität
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PIM1 0.07 μM (IC50) |
PIM2 ~1 μM () |
PIM3 0.02 μM (IC50) |
DYRK1 |
AMPK |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MOLM-13 | EC50 |
0.2 μM
Compound: VS-II-173
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Antiproliferative activity against human MOLM-13 cells measured after 72 hrs by WST-1 assay
Antiproliferative activity against human MOLM-13 cells measured after 72 hrs by WST-1 assay
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[PMID: 35917834] |
| MOLM-13 | EC50 |
0.8 μM
Compound: VS-II-173
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Antiproliferative activity against human MOLM-13 cells measured after 24 hrs by WST-1 assay
Antiproliferative activity against human MOLM-13 cells measured after 24 hrs by WST-1 assay
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[PMID: 35917834] |
| MOLM-13 | EC50 |
3.7 μM
Compound: VS-II-173
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Induction of apoptosis in human MOLM-13 cells incubated for 72 hrs and assessed as presence of apoptotic nuclei
Induction of apoptosis in human MOLM-13 cells incubated for 72 hrs and assessed as presence of apoptotic nuclei
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[PMID: 35917834] |
| NRK | EC50 |
>30 μM
Compound: VS-II-173
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Cytotoxicity against rat NRK cells measured after 72 hrs by WST-1 assay
Cytotoxicity against rat NRK cells measured after 72 hrs by WST-1 assay
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[PMID: 35917834] |
| PC-3 | IC50 |
2.46 μM
Compound: 7
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Antiproliferative activity against human PC3 cells after 72 hrs by MTS assay
Antiproliferative activity against human PC3 cells after 72 hrs by MTS assay
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[PMID: 25087047] |
VS-II-173 (1 μM) inhibits a range of protein kinases beyond Pim kinases, with potent activity against DYRK1A, HIPK2, PRK2, RSK1, and AMPKa1[1].
VS-II-173 (1 μM; 24 h) synergizes with Daunorubicin to induce cell death in Molm-13 AML cells, with additive effects with Etoposide (HY-13629), Emetine, Geldanamycin (HY-15230), and antagonism with high-concentration Bortezomib (HY-10227)[1].
VS-II-173 (3-12 μM; 1-6 h) modulates cell signaling in AML cell lines by downregulating Pim kinases and dephosphorylating Stat5, Bad, 4E-BP1, and MDM2[1].
VS-II-173 (EC50=3.7 μM，72 h) induces apoptosis in MOLM-13 acute myeloid leukemia cells[2].
VS-II-173 shows low cytotoxicity toward Normal Rat Kidney (NRK) epithelial cells (EC50 =>30 μM, 72 h)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human AML cell lines (Molm-13, MV4-11, OCI-AML3)
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Concentration:3, 6, 12 μM
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Incubation Time:1, 3, 6 h
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Result:Induced transient downregulation of Pim1, Pim2, and Pim3 in Molm-13 cells; dephosphorylated Stat5 in Molm-13 and MV4-11 cells; reduced phospho-Bad in MV4-11 cells; and decreased p-4E-BP1 and pMDM2 in OCI-AML3 cells.
Chemical Information
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CAS. Nr. 1627962-21-3
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Molecular Weight 264.24
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Formel C14H8N4O2
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SMILES
O=[N+]([O-])C1=C(N=CC2=C3C=CC=C2)C3=C4C=NNC4=C1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[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]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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