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Chemical Structure : CDK2 degrader 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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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.
| M.Wt | 890.948 | |
| Formula | C38H42N12O10S2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Wang L, et al. Nat Chem Biol. 2021 May;17(5):567-575.
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