产品
编 号：F161254
分子式：C23H17F2N3O6
分子量：469.39
分子式：C23H17F2N3O6
分子量：469.39
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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1mg
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5mg
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10mg
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结构图
CAS No: 1431280-51-1
产品详情
生物活性：
VLX1570 is a competitive inhibitor of proteasome deubiquitinases (DUBs) with an IC50 of approximate 10 μM.
体内研究：
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.
体外研究：
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 Kd of 1.5-18?μM using two different sources of recombinant protein, and the Kd 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-BZR 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.
VLX1570 is a competitive inhibitor of proteasome deubiquitinases (DUBs) with an IC50 of approximate 10 μM.
体内研究：
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.
体外研究：
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 Kd of 1.5-18?μM using two different sources of recombinant protein, and the Kd 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-BZR 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.
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