CPI203 | BET bromodomain inhibitor

CAS:
 1446144-04-2
Catalog Number:
 10-4048
CPI203 supplier | CAS 1446144-04-2 | Focus Biomolecules

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CPI203 (1446144-04-2), a JQ1 analog, is a potent and selective inhibitor of the BET bromodomain BRD4 (IC50 = 26 nM).1 It helps promote the maintenance of hematopoietic stem cells via repression of Myc expression.2 CPI203 reversibly suppressed intestinal stem cell differentiation in a mouse model.3 It enhanced the expansion of human cord blood hematopoietic stem cells without losing cell viability.4 CPI203 displays synergistic antitumor activity with various agents including lenalidomide5, bortezomib6, and PARP inhibitors7.

Refences/Citations:

  1. Devaiah et al. (2012), BRD4 is an atypical kinase that phosphorylates serine2 of the RNA polymerase II carboxy-terminal domain; Proc.  Nat. Acad. Sci. USA 109 6927
  2. Knudsen et al. (2015), ERG promotes the maintenance of hematopoietic stem cells by restricting their differentiation; Genes Dev., 29 1915
  3. Nakagawa et al. (2016), Selective and reversible suppression of intestinal stem cell differentiation by pharmacological inhibition of BET bromodomains; Sci. Rep. 6 20390
  4. Hua et al. (2020), The BET inhibitor CPI203 promotes ex vivo expansion of cord blood long-term repopulating HSCs and megakaryocytes; Blood 136 2410
  5. Diaz et al. (2017), The BET bromodomain inhibitor CPI203 improves lenalidomide and dexamethasone activity in in vitro and in vivo models of multiple myeloma by blockade of Ikaros and MYC signaling; Haematologica 102 1776
  6. Siegel et al. (2015), Small molecule inhibitor screen identifies synergistic activity of the bromodomain inhibitor CPI203 and bortezomib in drug resistant myeloma; Oncotarget 6 18921
  7. Lui et al. (2020), BET, SRC, and BCL2 family inhibitors are synergistic drug combinations with PARP inhibitors in ovarian cancer; EBioMedicine 60 102988
CAS:
1446144-04-2
Catalog Number:
10-4048
Activity:
BET bromodomain inhibitor
Chemical Names:
(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; 2-[(9S)-7-(4-Chlorophenyl)-4,5-13-trimethyl-3-thia-1,8,11,12-tetrazatricyclo[8.3.0.02,6]trideca-2(6),4,7,10,12-pentaen-9-yl]acetamide
Alternate Name:
CPI-267203
Molecular Weight:
399.90
Molecular Formula:

C19H18ClN5OS

Solubility:
Soluble in DMSO (>25 mg/ml)
Physical Properties:
White to off-white solid
Purity:

>98% HPLC
NMR (Conforms)

Storage Temperature:
-20°C
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee

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