For research use only. Not for therapeutic Use.
PROTAC HSP90 degrader BP3 is a potent and selective degradation of HSP90 in a CRBN-dependent fashion. PROTAC HSP90 degrader BP3 has a certain degradation effect on HSP90 protein in MCF-7 cells (DC50=0.99 μM). PROTAC HSP90 degrader BP3 inhibits the growth of breast cancer cell[1]. PROTAC HSP90 degrader BP3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
PROTAC HSP90 degrader BP3 (compound 16b) (72 h) inhibits the growth of breast cancer cells (IC50=0.63 µM in MCF-7 cells, IC50=3.53 µM in MDA-MB-231 cells, IC50=0.61 µM in 4T1 cells, IC50=2.95 µM in MDA-MB-468 cells)[1].
PROTAC HSP90 degrader BP3 (2 µM; 6 h) shows degradation activity in the MCF-7 cells (DC50=0.99 µM)[1].
PROTAC HSP90 degrader BP3 (40 mg/kg; i.p., daily for 12 days) inhibits tumor growth and the tumor inhibition rate is 76.41%[1].
| Catalog Number | I044122 |
| CAS Number | 2669072-88-0 |
| Synonyms | 4-[4-[2-amino-4-chloro-7-[(4-methoxy-3,5-dimethylpyridin-2-yl)methyl]pyrrolo[2,3-d]pyrimidin-5-yl]but-3-ynylamino]-2-(2,6-dioxopiperidin-3-yl)isoindole-1,3-dione |
| Molecular Formula | C32H29ClN8O5 |
| Purity | ≥95% |
| InChI | InChI=1S/C32H29ClN8O5/c1-16-13-36-21(17(2)26(16)46-3)15-40-14-18(24-27(33)38-32(34)39-28(24)40)7-4-5-12-35-20-9-6-8-19-25(20)31(45)41(30(19)44)22-10-11-23(42)37-29(22)43/h6,8-9,13-14,22,35H,5,10-12,15H2,1-3H3,(H2,34,38,39)(H,37,42,43) |
| InChIKey | ZSERQSKFLSKTGE-UHFFFAOYSA-N |
| SMILES | CC1=CN=C(C(=C1OC)C)CN2C=C(C3=C2N=C(N=C3Cl)N)C#CCCNC4=CC=CC5=C4C(=O)N(C5=O)C6CCC(=O)NC6=O |
| Reference | [1]. Liu Q, et al. Discovery of BP3 as an efficacious proteolysis targeting chimera (PROTAC) degrader of HSP90 for treating breast cancer. Eur J Med Chem. 2022, 228:114013. |
