CBP/p300-IN-12

CBP/p300-IN-12 is a potent and selective covalent histone acetyltransferases p300 (IC50 of 166 nM) and CBP inhibitor. CBP/p300-IN-12 decreases the levels of H3K27Ac of PC-3 cells (EC50 of 37 nM). CBP/p300-IN-12 forms a covalent adduct with C1450.

Product information

Molecular Weight: 667.61

Formula: C33H29F4N5O6

Chemical Name: N-[3-({[(1R)-4'-({[(4-fluorophenyl)methyl][(2S)-1,1,1-trifluoropropan-2-yl]carbamoyl}methyl)-3',5'-dioxo-2,3-dihydrospiro[indene-1,2'-[1,4]oxazolidin]-5-yl]carbamoyl}amino)phenyl]prop-2-enamide

Smiles: C[C@H](N(CC1=CC=C(F)C=C1)C(=O)CN1C(=O)[C@]2(CCC3C=C(C=CC2=3)NC(=O)NC2=CC(=CC=C2)NC(=O)C=C)OC1=O)C(F)(F)F

InChiKey: JUWRXRFZRKHMBP-PSTIOWGYSA-N

InChi: InChI=1S/C33H29F4N5O6/c1-3-27(43)38-23-5-4-6-24(16-23)39-30(46)40-25-11-12-26-21(15-25)13-14-32(26)29(45)42(31(47)48-32)18-28(44)41(19(2)33(35,36)37)17-20-7-9-22(34)10-8-20/h3-12,15-16,19H,1,13-14,17-18H2,2H3,(H,38,43)(H2,39,40,46)/t19-,32+/m0/s1

Technical Data

Appearance: Solid Power

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

Solubility: To be determined

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:

CBP/p300-IN-12 (Compound 2) shows antiproliferative effect against androgen receptor (AR)-positive LnCaP-FGC cells (EC50 of 87 nM), while displaying significantly less activity in the AR-negative cell line DU-145 (EC50 of 1.37 μM).

References:

1. Ait-Si-Ali, S., Polesskaya, A., Filleur, S. et al. CBP/p300 histone acetyl-transferase activity is important for the G1/S transition. Oncogene 19, 2430–2437 (2000).

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