BSJ-4-116

BSJ-4-116 is a specific degrader of cyclin-dependent kinase 12 (CDK12). BSJ-4-116 exhibits potent antiproliferative effects.

Product information

CAS Number: 2519823-34-6

Molecular Weight: 837.38

Formula: C40H49ClN8O8S

Chemical Name: N-{7-[(3R)-3-[(5-chloro-4-{[2-(propane-2-sulfonyl)phenyl]amino}pyrimidin-2-yl)amino]piperidin-1-yl]heptyl}-2-{[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl]oxy}acetamide

Smiles: CC(C)S(=O)(=O)C1=CC=CC=C1NC1=NC(N[C@H]2CN(CCCCCCCNC(=O)COC3=CC=CC4C(=O)N(C5CCC(=O)NC5=O)C(=O)C=43)CCC2)=NC=C1Cl

InChiKey: YJOJMGTVKMABKQ-FIQOPJFZSA-N

InChi: InChI=1S/C40H49ClN8O8S/c1-25(2)58(55,56)32-16-7-6-14-29(32)45-36-28(41)22-43-40(47-36)44-26-12-11-21-48(23-26)20-9-5-3-4-8-19-42-34(51)24-57-31-15-10-13-27-35(31)39(54)49(38(27)53)30-17-18-33(50)46-37(30)52/h6-7,10,13-16,22,25-26,30H,3-5,8-9,11-12,17-21,23-24H2,1-2H3,(H,42,51)(H,46,50,52)(H2,43,44,45,47)/t26-,30?/m1/s1

Technical Data

Appearance: Solid Power

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

Solubility: Solubility (25°C). DMSO: 100 mg/mL(119.42 mM). Water: Insoluble.

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:

BSJ-4-116 selectively degrads CDK12 as assessed through quantitative proteomics. BSJ-4-116 downregulates the expression of DDR genes and exhibits antiproliferative activity in cancer cells. BSJ-4-116 also substantially suppresses the phosphorylation of Pol II Ser2 and Thr4.

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