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首页-小分子抑制剂&激动剂-Proteasome/Ubiquitin-E3 Ubiquitin Ligase-XMU-MP-10 TFA salt
XMU-MP-10 TFA salt

Chemical Structure : XMU-MP-10 TFA salt

CAS No.: 2251132-03-1

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XMU-MP-10 TFA salt

货号: PC-25638Not For Human Use, Lab Use Only.

XMU-MP-10 TFA salt is a potent, specific, high-affinity inhibitor of HECT-type E3 ubiquitin ligase NEDD4 with MST KD of 43.92 nM, targets the HECT domain of NEDD4, significantly and selectively inhibits NEDD4 auto-ubiquitination.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

XMU-MP-10 TFA salt is a potent, specific, high-affinity inhibitor of HECT-type E3 ubiquitin ligase NEDD4 with MST KD of 43.92 nM, targets the HECT domain of NEDD4, significantly and selectively inhibits NEDD4 auto-ubiquitination.
XMU-MP-10 selectively inhibits NEDD4 auto-ubiquitination without affecting the ubiquitination activity of other E3 ligases from C2-WW-HECT subfamily, including NEDD4L, NEDL1, NEDL2, Smurf1, Smurf2, WWP1, WWP2, and ITCH.
XMU-MP-10 interacts with the HECT domain of NEDD4 at residues Y604, Y605, and Y634.
XMU-MP-10 induces the upregulation of β-TrCP, resulting in YAP degradation in a dose- and time-dependent manner in various TNBC cells, without affecting NEDD4 protein expression.
XMU-MP-10 (25 mg/kg, i.v. administration) significantly reduced the TNBC tumor growth in huPBMC-NCG mice engrafted with human TNBC cell MDA-MB-231, significantly increased intratumoral CD8+ T cell infiltration and reduced collagen deposition.
XMU-MP-10 influenced the β-TrCP-YAP-ECM axis in vivo, as decrease in YAP levels and upregulation of β-TrCP.

物理化学性质&存储条件

分子量 510.27
分子式 C20H15BrF3N5O3
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

1H-Pyrrole-3-carboxamide, N-[(4-bromophenyl)methyl]-5-(1H-pyrazolo[3,4-b]pyridin-3-yl)-, 2,2,2-trifluoroacetate (1:1)

参考文献

1. Su N, et al. Cell Rep Med. 2025 Oct 21;6(10):102420.

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