ChemicalBook > CAS DataBase List > cpi-637

cpi-637

Product Name
cpi-637
CAS No.
1884712-47-3
Chemical Name
cpi-637
Synonyms
CPI-637 >=98% (HPLC);CPI-637, 10 mM in DMSO;CPI-637;CPI 637;CPI637;CPI-637/1884712-47-3/98%;Inhibitor,inhibit,HAT,Epigenetic Reader Domain,CPI637,CPI-637,Histone Acetyltransferase,HATs;(R)-4-Methyl-6-(1-methyl-3-(1-methyl-1H-pyrazol-4-yl)-1H-indazol-5-yl)-4,5-dihydro-1H-benzo[b][1,4]diazepin-2(3H)-one;2H-1,5-Benzodiazepin-2-one, 1,3,4,5-tetrahydro-4-methyl-6-[1-methyl-3-(1-methyl-1H-pyrazol-4-yl)-1H-indazol-5-yl]-, (4R)-
CBNumber
CB13139528
Molecular Formula
C22H22N6O
Formula Weight
386.45
MOL File
1884712-47-3.mol
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cpi-637 Property

Boiling point:
689.2±55.0 °C(Predicted)
Density 
1.38±0.1 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
insoluble in EtOH; insoluble in H2O; ≥19.3 mg/mL in DMSO with gentle warming
form 
solid
pka
14.62±0.40(Predicted)
color 
White to off-white
optical activity
[α]/D -39 to -49°, c =1.0 in chloroform-d
InChI
InChI=1S/C22H22N6O/c1-13-9-20(29)25-18-6-4-5-16(22(18)24-13)14-7-8-19-17(10-14)21(26-28(19)3)15-11-23-27(2)12-15/h4-8,10-13,24H,9H2,1-3H3,(H,25,29)/t13-/m1/s1
InChIKey
BFTKDWYIRJGJCA-CYBMUJFWSA-N
SMILES
N1C2=CC=CC(C3C=CC4=C(C=3)C(C3=CN(C)N=C3)=NN4C)=C2N[C@H](C)CC1=O
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Cayman Chemical
Product number
23500
Product name
CPI-637
Purity
≥98%
Packaging
1mg
Price
$32
Updated
2024/03/01
Cayman Chemical
Product number
23500
Product name
CPI-637
Purity
≥98%
Packaging
5mg
Price
$122
Updated
2024/03/01
Cayman Chemical
Product number
23500
Product name
CPI-637
Purity
≥98%
Packaging
10mg
Price
$169
Updated
2024/03/01
Cayman Chemical
Product number
23500
Product name
CPI-637
Purity
≥98%
Packaging
25mg
Price
$343
Updated
2024/03/01
ApexBio Technology
Product number
B7801
Product name
CPI-637
Packaging
50mg
Price
$348
Updated
2021/12/16
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cpi-637 Chemical Properties,Usage,Production

Description

CPI-637 is an inhibitor of cyclic-AMP response element binding protein (CBP) and adenoviral E1A binding protein of 300 kDa (EP300), a homologous pair of bromodomain-containing proteins (IC50s = 30 and 51 nM in a time-resolved-FRET (TR-FRET) assay). It is selective for CBP and EP300 over the BET family of bromodomains (IC50s = >10 μM), however, CPI-637 is active at bromodomain BRD9 (IC50 = 0.73 μM). CPI-637 also inhibits MYC expression (EC50 = 0.6 μM) in AMO-1 cells.

Uses

CPI-637 is a selective and potent CBP/EP300 bromodomain inhibitor with IC50 values of 0.03 μM, 0.051 μM and 11.0 μM for CBP, EP300 and BRD4 BD-1, respectively, and an EC50 of 0.3 μM for CBP[1].

in vitro

previous study found that cpi-637 was potent against ep300, and its opposite enantiomer showed a over 200-fold loss in potency. moreover, the biochemical potency of cpi-637 translated well into cells with cbp bret ec50 of 0.3 μm, and cpi-637 demonstrated a more than 700-fold selectivity over the bet family of bromodomains. in addition, cpi-637 was also highly selective against other bromodomains, showing substantial biochemical activity only against brd9. furthermore, it was found that cpi-637 was able to inhibit the expression of myc with an ec50 of 0.60 μm in a cellular assay,. [1].

IC 50

0.03 and 11.0 μm for cbp/ep300 and brd4, respectively.

References

[1] taylor, a. m. et al. fragment-based discovery of a selective and cell-active benzodiazepinone cbp/ep300 bromodomain inhibitor (cpi-637). acs medicinal chemistry letters 7, 531-536, doi:10.1021/acsmedchemlett.6b00075 (2016).

cpi-637 Preparation Products And Raw materials

Raw materials

Preparation Products

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1884712-47-3, cpi-637Related Search:


  • CPI-637;CPI 637;CPI637
  • 2H-1,5-Benzodiazepin-2-one, 1,3,4,5-tetrahydro-4-methyl-6-[1-methyl-3-(1-methyl-1H-pyrazol-4-yl)-1H-indazol-5-yl]-, (4R)-
  • CPI-637 >=98% (HPLC)
  • (R)-4-Methyl-6-(1-methyl-3-(1-methyl-1H-pyrazol-4-yl)-1H-indazol-5-yl)-4,5-dihydro-1H-benzo[b][1,4]diazepin-2(3H)-one
  • Inhibitor,inhibit,HAT,Epigenetic Reader Domain,CPI637,CPI-637,Histone Acetyltransferase,HATs
  • CPI-637, 10 mM in DMSO
  • CPI-637/1884712-47-3/98%
  • 1884712-47-3
  • API