PROTAC BRD2/BRD4 degrader-1

PROTAC BRD2/BRD4 degrader-1 (compound 15) is a potent and selective BET protein BRD4 and BRD2 degrader. PROTAC BRD2/BRD4 degrader-1 rapidly induces reversible, long-lasting, and unexpectedly selective removal of BRD4 and BRD2 over BRD3. It effectively inhibits solid tumors with low cytotoxic effect. PROTAC BRD2/BRD4 degrader-1 is composed of the BET inhibitor, a linker, and the ligand thalidomide for cereblon (CRBN)/cullin 4A.

Product information

Molecular Weight: 766.82

Formula: C39H38N6O9S

Chemical Name: N-[4-[[2-(2, 6-dioxopiperidin-3-yl)-1, 3-dioxoisoindol-4-yl]amino]butyl]-3-[6-[(2-methoxyphenyl)sulfonylamino]-1-methyl-2-oxobenzo[cd]indol-4-yl]propanamide

Smiles: CN1C2=CC=C(NS(=O)(=O)C3=CC=CC=C3OC)C3=CC(CCC(=O)NCCCCNC4=CC=CC5=C4C(=O)N(C4CCC(=O)NC4=O)C5=O)=CC(C1=O)=C32

InChiKey: DCPKSVYPNGBDSB-UHFFFAOYSA-N

InChi: InChI=1S/C39H38N6O9S/c1-44-28-14-13-26(43-55(52,53)31-11-4-3-10-30(31)54-2)24-20-22(21-25(34(24)28)37(44)49)12-16-32(46)41-19-6-5-18-40-27-9-7-8-23-35(27)39(51)45(38(23)50)29-15-17-33(47)42-36(29)48/h3-4,7-11,13-14,20-21,29,40,43H,5-6,12,15-19H2,1-2H3,(H,41,46)(H,42,47,48)

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:

PROTAC BRD2/BRD4 degrader-1 (100 nM; ≥8 hours) shows anti-proliferation activity with IC50 value of 12.25 nM, and the BRD4 protein is reduced very efficiently at treatment time of ≥8 h in MV4-11 cells. PROTAC BRD2/BRD4 degrader-1 (100 nM; ≥8 hours) shows anti-proliferation activity with IC50 value of 12.25 nM, and the BRD4 protein is reduced very efficiently at treatment time of ≥8 h in MV4-11 cells. PROTAC BRD2/BRD4 degrader-1 (1 nM, 3 nM, 0.1 μM, 0.3 μM; 24-48 hours) induces MV4-11 apoptosis lines. PROTAC BRD2/BRD4 degrader-1 exhibits excellent anti-proliferative activity in 6 leukemia cell lines of NCI. Among them, the GI50 values of the three leukemia cell lines were lower than 50 nM, consistent with the activity of leukemia MV4-11 cells. PROTAC BRD2/BRD4 degrader-1 has good anti-proliferation activity including prostate Cancer (22RV1 IC50: 0.081 μM), colon cancer (colo-205 IC50: 0.1557 μM) and thyroid cancer(TT IC50: 0.037451 μM).

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