DCH36_06

DCH36_06 is a potent and selective p300/CBP inhibitor with IC50s of 0.6 μM and 3.2 μM for p300 and CBP, respectively. DCH36_06 mediated p300/CBP inhibition leading to hypoacetylation on H3K18 in leukemic cells. Anti-tumor activity.

Product information

CAS Number: 593273-05-3

Molecular Weight: 372.83

Formula: C18H13ClN2O3S

Chemical Name: (5E)-1-(3-chloro-4-methylphenyl)-5-[(2E)-3-(furan-2-yl)prop-2-en-1-ylidene]-2-sulfanylidene-1,3-diazinane-4,6-dione

Smiles: CC1=CC=C(C=C1Cl)N1C(=S)NC(=O)/C(=C\C=C\C2=CC=CO2)/C1=O

InChiKey: AYNCXNUUERDREH-FMDPHQNASA-N

InChi: InChI=1S/C18H13ClN2O3S/c1-11-7-8-12(10-15(11)19)21-17(23)14(16(22)20-18(21)25)6-2-4-13-5-3-9-24-13/h2-10H,1H3,(H,20,22,25)/b4-2+,14-6+

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:

DCH36_06 (6.7-20 μM; 24-48 hours) treatment arrests cell cycle at G1 phase and induces apotosis in a dose-dependent manner in leukemic cells. DCH36_06 (5-10 μM; 24 hours) treatment significantly activates the cleavage of pro-caspase 3, pro-caspase 9 and PARP1 at dose-dependent manner. DCH36_06 shows potent antiproliferative activity against tested leukemia cell lines (CEM, MOLT3, MOLT4, Jurkat, MV4-11, THP-1, RS4; 11, KOPN8, Kasumi-1 and K562 cells) in a dose-dependent manner with IC50 values at single-digit micromolar range.

In Vivo:

DCH36_06 (25-50 mg/kg; intraperitoneal injection; every two days; for 20 days) blocks the leukemic xenograft growth in mice.

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