CPI203 --- BET Inhibitor

Catalog No. size PriceQuantity
M60124-2S 2 mg solid $139
M60124-10S 10 mg solid $549


CPI203 is a novel potent, selective and cell permeable inhibitor of the bromodomain and extra terminal (BET) family protein BRD4 with an IC50 of ~37 nM (BRD4 α-screen assay). It has an IC50 of ~99 nM in inhibiting Myc expression in MV4-11 cells and an IC50 of ~30 nM in inhibiting IL-6 production in THP-1 cells stimulated with LPS, decreases specific Ser2 phosphorylation of the carboxyl-terminal domain (CTD) of the RNA polymerase II (Pol II) by either endogenous BRD4 or a BRD4 mutant, BRD4 FEE-AAA, that is incapable of binding PTEFb. CPI203 is an analog of JQ-1 but has shown superior bioavailability with oral or intraperitoneal (IP) administration. When mice that were transplanted with primary mouse T-ALL cells, either Fbxw7+/+ or Fbxw7mut/+, were treated with CPI203 at 5 mg/Kg orally twice per day, a significant and rapid reduction in leukemia burden was observed. CPI203 is a useful chemical probe to study the suppression of Myc-dependent cancer development.

Product information

CAS Number: 1446144-04-2

Molecular Weight: 399.90

Formula: C19H18ClN5OS

Chemical Name: (S)-2-(4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetamide

Smiles: CC1=NN=C2[C@H](CC(N)=O)N=C(C3=C(SC(C)=C3C)N12)C1C=CC(Cl)=CC=1


InChi: InChI=1S/C19H18ClN5OS/c1-9-10(2)27-19-16(9)17(12-4-6-13(20)7-5-12)22-14(8-15(21)26)18-24-23-11(3)25(18)19/h4-7,14H,8H2,1-3H3,(H2,21,26)/t14-/m0/s1

Technical Data

Appearance: Solid Power.

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

Solubility: DMSO up to 50 mM

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:

CPI203 was used at 0.5-1 µM final concentration in various in vitro assays.

In Vivo:

CPI203 could be dosed to the mice by oral administration at 5 mg/kg twice per day for 7 days.


  1. Devaiah BN, et al. BRD4 is an atypical kinase that phosphorylates serine2 of the RNA polymerase II carboxy-terminal domain. (2012) Proc Natl Acad Sci U S A. 109(18):6927-32.
  2. Bryan King, et al. The Ubiquitin Ligase Fbxw7 Modulates Leukemia-Initiating Cell Activity by Regulating Myc Stability. (2013) Cell 153(7):1552-66.
  3. Moros A, et al. Synergistic antitumor activity of lenalidomide with the BET bromodomain inhibitor CPI203 in bortezomib-resistant mantle cell lymphoma. (2014) Leukemia. In press.

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


Payment & Security

PayPal Venmo

Your payment information is processed securely. We do not store credit card details nor have access to your credit card information.

Estimate shipping

You may also like

Recently viewed