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首页-小分子抑制剂&激动剂-Proteasome/Ubiquitin-E3 Ubiquitin Ligase-DDO-4033
DDO-4033

Chemical Structure : DDO-4033

CAS No.:

DDO-4033 (DDO4033)

货号: PC-24933Not For Human Use, Lab Use Only.

DDO-4033 is a potent, selective E3 ligase speckle-type POZ protein (SPOP) inhibitor with IC50 of 16.48 uM, binds to SPOP-MATH with Kd of 15.1 uM in MST assay.

规格 价格 库存 数量
25 mg Get quote
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100 mg Get quote

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

DDO-4033 is a potent, selective E3 ligase speckle-type POZ protein (SPOP) inhibitor with IC50 of 16.48 uM, binds to SPOP-MATH with Kd of 15.1 uM in MST assay.
DDO-4033 is a potent binder for SPOP with a KD value of 4.96 μM in BLI assay.
DDO-4033 exhibits the corresponding affinity in the ITC experiment with the Kd value of 4.94 μM and no binding to the mutant SPOP-Y87A and D130A.
DDO-4033 (0.5-1 uM) inhibits SPOP-mediated ubiquitination and degradation of LATS1 in ccRCC cells.
DDO-4033 suppresses the malignancy of ccRCC through the Hippo pathway, downregulated the mRNA level of CTGF and CYR61 genes, modulates the downstream YAP/TAZ signaling in ccRCC cells.
DDO-4033 (50 mg/kg) effectively suppresses ccRCC tumor growth in A498-Luc xenograft model.

物理化学性质&存储条件

分子量 406.40
分子式 C20H18N6O4
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

4-Ethynyl-N-(3-methyl-1-(6-oxo-4-propyl-1,6-dihydropyrimidin-2-yl)-1H-pyrazol-5-yl)-3-nitrobenzamide

参考文献

1. Zhang Q, et al. J Med Chem. 2025 Jul 7. doi: 10.1021/acs.jmedchem.5c00987.

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