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Z0933M

Chemical Structure : Z0933M

CAS No.: 1561172-42-6

Z0933M (Z 0933M)

Catalog No.: 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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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

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.

Physicochemical Properties

M.Wt 309.372
Formula C21H15N3
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

4-(11H-indolo[3,2-c]quinolin-6-yl)aniline

References

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

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