cpi-637
- Product Name
- cpi-637
- CAS No.
- 1884712-47-3
- Chemical Name
- cpi-637
- Synonyms
- CPI-637 >=98% (HPLC);CPI-637;CPI 637;CPI637;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
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)
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.
N-Bromosuccinimide Price
- Product number
- 23500
- Product name
- CPI-637
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $32
- Updated
- 2024/03/01
- Product number
- 23500
- Product name
- CPI-637
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $122
- Updated
- 2024/03/01
- Product number
- 23500
- Product name
- CPI-637
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $169
- Updated
- 2024/03/01
- Product number
- 23500
- Product name
- CPI-637
- Purity
- ≥98%
- Packaging
- 25mg
- Price
- $343
- Updated
- 2024/03/01
- Product number
- B7801
- Product name
- CPI-637
- Packaging
- 50mg
- Price
- $348
- Updated
- 2021/12/16
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.
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
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