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首页-抗体药物偶连体和PROTACs-E3 Ligase Ligand-Z0933M
Z0933M

Chemical Structure : Z0933M

CAS No.: 1561172-42-6

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Z0933M (Z 0933M)

货号: PC-49083Not For Human Use, Lab Use Only.

Z0933M is a potent S phase kinase-associated protein 1 (Skp1) inhibitor with Kd of 54 nM, potently inhibits Skp1-F-box protein-protein interactions with Ki value of 231 nM in FP-based in vitro competition assays.

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2 mg ￥2580 In stock
5 mg ￥4280 In stock
10 mg ￥7280 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Z0933M is a potent S phase kinase-associated protein 1 (Skp1) inhibitor with Kd of 54 nM, potently inhibits Skp1-F-box protein-protein interactions with Ki value of 231 nM in FP-based in vitro competition assays.
Z0933M binds potently to Skp1WT and ΔSkp11−140, with dissociation constant (KD) values 54.7 ± 6.68 and 40.4 ± 8.2 nM, respectively, in thermal shift assay (TSA).
The direct engagement of Z0933M at the P1 region located alongside the C-terminal extension of Skp1.
Z0933M disrupts Skp1-F-box PPIs in cellulo, impairs SCF E3 ligase functioning, and increases the levels or alter the turnover of several substrate proteins.
Z0933M exhibits anti-proliferative activity against A549 cells with EC50 (48 h)of 0.58 uM, 24 times more potent than 6-OAP, and shows lower EC50 value of 0.099 and 0.066 uM for 72 and 96h treatment.
Z0933M demonstrates substantially weaker or absolutely no anti-proliferative effects against p53-deficient (null and mutant) cell lines, Z0933M elicits apoptotic cell death which is reversed by p53 inhibition and Skp1 overexpression.

物理化学性质&存储条件

分子量 309.372
分子式 C21H15N3
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-(11H-indolo[3,2-c]quinolin-6-yl)aniline

参考文献

1. Hussain M, et al. iScience. 2022 Jun 14;25(7):104591.

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