For research use only. Not for therapeutic Use.
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[1].
CPS2 (5~333 nM; 12 hours; Ramos cells) stands out as the most potent degrader[1].
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[1].
The antileukemic effects of CPS2 are mediated by CDK2 degradation. CPS2 also induces granulocytic differentiation of HSCs, as assessed by cell morphological analysis[1].
| Catalog Number | I045250 |
| CAS Number | 2756741-90-7 |
| Synonyms | 4-[[5-amino-1-(3-methylthiophene-2-carbonyl)-1,2,4-triazol-3-yl]amino]-N-[2-[[1-[2-[2-[2-[[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]amino]ethoxy]ethoxy]ethyl]triazol-4-yl]methoxy]ethyl]benzenesulfonamide |
| Molecular Formula | C38H42N12O10S2 |
| Purity | ≥95% |
| 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) |
| InChIKey | BXCPYBFBMAWDDY-UHFFFAOYSA-N |
| SMILES | CC1=C(SC=C1)C(=O)N2C(=NC(=N2)NC3=CC=C(C=C3)S(=O)(=O)NCCOCC4=CN(N=N4)CCOCCOCCNC5=CC=CC6=C5C(=O)N(C6=O)C7CCC(=O)NC7=O)N |
| Reference | [1]. Wang L, et al. Discovery of a first-in-class CDK2 selective degrader for AML differentiation therapy. Nat Chem Biol. 2021;17(5):567-575 |
