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VLX1570

CAS No. : 1431280-51-1

MCE 国际站：VLX1570

产品活性：VLX1570是蛋白酶体脱泛素酶 (DUBs) 的竞争性抑制剂，IC₅₀ 约10 μM。

研究领域：Cell Cycle/DNA Damage

作用靶点：Deubiquitinase

In Vitro: VLX1570 inhibits USP14 and UCHL5 activity of 19S regulatory particles, and the inhibition of USP14 is more pronounced. VLX1570 (1 μM) shows inhibitory activity against USP14 in KMS-11 myeloma cells. VLX1570 exhibits an IC₅₀ of 0.58 μM on HCT116 cells. VLX1570 binds to recombinant USP14 with K_d of 1.5-18 μM using two different sources of recombinant protein, and the K_d for recombinant UCHL5 is higher (14-18 μM) compared to that of USP14. VLX1570 has potent antiproliferative activities on multiple myeloma cells, with IC₅₀s of 43 ± 2 nM, 74 ± 2 nM, 126 ± 3 nM, and 191 ± 1 nM for KMS-11, RPMI8226, OPM-2, and OPM-2-BZ^R cells, respectively. VLX1570 suppresses the viability of BCWM.1 cells, with an EC₅₀ of 20.22 nM. VLX1570 (100, 250, 500 nM) induces significant apoptosis by 12 h in a dose-dependent manner in all Waldenstrom macroglobulinemia (WM) cell lines tested, including BCWM.1/IR (IR) and BCWM.1/BR (BR) subclones. VLX1570 (100, 250, 500 nM) also causes ER stress machinery and mitochondrial damage in WM cells. VLX1570 (250 nM) downregulates BCR-signalosome components and their end effectors, as well as CXCR4 expression in WM cells.

In Vivo: VLX1570 (3 mg/kg) significantly decreases tumor growth in mice bearing KMS-11 multiple myeloma cells. VLX1570 (4.4 mg/kg, i.p.) markedly suppresses tumor growth, without obvious weight loss and other signs of systemic toxicity in the Waldenstrom macroglobulinemia (WM)-bearing mice.

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