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

VLX1570 is a competitive inhibitor of proteasome deubiquitinases (DUBs) with an IC 50 of approximate 10 μM.

Solid

IC50: appr 10?μM (Deubiquitinase)

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-BZ 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 macro

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. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Wang X, et al. Synthesis and evaluation of derivatives of the proteasome deubiquitinase inhibitor b-AP15. Chem Biol Drug Des. 2015 Nov;86(5):1036-48.
[2]. Wang X, et al. The proteasome deubiquitinase inhibitor VLX1570 shows selectivity for ubiquitin-specific protease-14 and induces apoptosis of multiple myeloma cells. Sci Rep. 2016 Jun 6;6:26979.

In Vitro: DMSO : ≥ 32 mg/mL (68.17 mM)配制储备液