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CDK2 degrader CPS2

Chemical Structure : CDK2 degrader CPS2

CAS No.: 2756741-90-7

CDK2 degrader CPS2 (CPS2)

Catalog No.: PC-49057Not For Human Use, Lab Use Only.

CDK2 degrader CPS2 is a potent, selective CDK2 degarder (PROTAC) with IC50 of 24 nM, potently and specifically induces CDK2 degradation in various cancer cell lines (MDA-MB-231, DC50=8 nM; MV-4-11, DC50=1 nM).

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

CDK2 degrader CPS2 is a potent, selective CDK2 degarder (PROTAC) with IC50 of 24 nM, potently and specifically induces CDK2 degradation in various cancer cell lines (MDA-MB-231, DC50=8 nM; MV-4-11, DC50=1 nM).
CPS2 induced ubiquitination led to CDK2 degradation via the ubiquitin/proteasome system, this degradation required the binding of CPS2 to CDK2 and CRBN.
CPS2 did not directly perturb the other CDK proteins (such as CDK1, 4, 5, 6, 7, 8 and 9) under subnanomolar concentration conditions.
CPS2 induced AML cell differentiation, increased CD11b expression in a concentration-dependent manner in the NB4 cells, also promoted ATRA-induced CD11b upregulation in the HL60 cells.
CPS2 inhibited the proliferation of hematopoietic stem cells (HSCs) without inducing cytotoxicity, CPS2 also induced granulocytic differentiation of HSCs.

Physicochemical Properties

M.Wt 890.948
Formula C38H42N12O10S2
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-((5-amino-1-(3-methylthiophene-2-carbonyl)-1H-1,2,4-triazol-3-yl)amino)-N-(2-((1-(2-(2-(2-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)ethoxy)ethoxy)ethyl)-1H-1,2,3-triazol-4-yl)methoxy)ethyl)benzenesulfonamide

References

1. Wang L, et al. Nat Chem Biol. 2021 May;17(5):567-575.

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