CPS2

CPS2 is a first-in-class, highly potent, selective and irreversible PROTAC CDK2 degrader (IC50= 24 nM). CPS2 can be used for the research of acute myeloid leukemia.

Product information

Molecular Weight: 890.94

Formula: C38H42N12O10S2

Chemical Name: 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

Smiles: CC1C=CSC=1C(=O)N1N=C(NC2C=CC(=CC=2)S(=O)(=O)NCCOCC2=CN(CCOCCOCCNC3=CC=CC4=C3C(=O)N(C3CCC(=O)NC3=O)C4=O)N=N2)N=C1N

InChiKey: BXCPYBFBMAWDDY-UHFFFAOYSA-N

InChi: InChI=1S/C38H42N12O10S2/c1-23-11-20-61-32(23)36(55)50-37(39)44-38(46-50)42-24-5-7-26(8-6-24)62(56,57)41-13-16-60-22-25-21-48(47-45-25)14-17-59-19-18-58-15-12-40-28-4-2-3-27-31(28)35(54)49(34(27)53)29-9-10-30(51)43-33(29)52/h2-8,11,20-21,29,40-41H,9-10,12-19,22H2,1H3,(H,43,51,52)(H3,39,42,44,46)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

CPS2 (5~333 nM; 12 hours; Ramos cells) stands out as the most potent degrader. CPS2 (0.5~2 μM; HSCs) inhibits the proliferation of HSCs without inducing cytotoxicity. CPS2 (1~10000 nM; 48 hours; NB4 cells) induces potent CDK2 degradation. CPS2 (250 nM; 0~6 hours; Ramos and NB4 cells) rapidly induces the degradation of CDK2. CPS2 (10~500 nM; 6 hours; Ramos cells) induces only CDK2 degradation and does not directly perturb the other CDK proteins under subnanomolar concentration conditions. CPS2 (250 nM; 6 hours; NB4 cells) stands out as the most downregulated protein in cells treated for 6 hours with CPS2, confirming the selectivity of CPS2 for CDK2. CPS2 (0~250 nM; NB4 cells) makes the levels of CDK2 obviously decreased. CPS2 (2 μM; 3 days; HL60 cells) obviously promotes ATRA-induced CD11b upregulation. The antileukemic effects of CPS2 are mediated by CDK2 degradation. CPS2 also induces granulocytic differentiation of HSCs, as assessed by cell morphological analysis.

Products are for research use only. Not for human use.