WWQ-03-012

Chemical Structure : WWQ-03-012

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货号: PC-26201Not For Human Use, Lab Use Only.

WWQ-03-012 is a potent, specific and covalent inhibitor of JAK2‐V617F complex component DESI2 with IC50 of 47.3 nM, selectively degrades mutant JAK2.

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生物&药学活性

WWQ-03-012 is a potent, specific and covalent inhibitor of JAK2‐V617F complex component DESI2 with IC50 of 47.3 nM, selectively degrades mutant JAK2.
deSUMOylases DESI2 is a novel component of the JAK2‐V617F complex, DESI2 is a critical mutation‐specific stabilizer of JAK2‐V617F.
WWQ-03-012 covalently targets Cys94 of DESI2, displays modest activity against UCHL1 (IC50 = 5956 nM) and USP30 (IC50 = 2028 nM) in a panel of purified DUBs, including UCHL1, USP30, JOSD1.
WWQ-03-012 promotes selective degradation of mutant JAK2‐V617F in HEL cells with DC50 of 543.6 nM (24 h), with minimal impact on WT JAK2 protein.
WWQ-03-012 induces JAK2 mutant leukemia cell death in preclinical models.
WWQ-03-012 (12.5 mg/kg, i.p. BID) significantly inhibits the tumor growth and myeloproliferative neoplasms (MPN) progression in JAK2V617F‐driven MPN in vivo, significantly reduces the JAK2‐V617F protein levels and downstream signal transduction in MPN mice.

物理化学性质&存储条件

分子量	392.43
分子式	C20H16N4O3S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	3-Pyrrolidinecarboxamide, N-[5-(1,3-benzodioxol-5-yl)-2-benzothiazolyl]-1-cyano-, (3S)-

参考文献

1. Husheng Mei, et al. Adv Sci (Weinh). 2026 Feb;13(7):e15127.

WWQ-03-012

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物理化学性质&存储条件

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WWQ-03-012

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