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CPI-637 - 99%, high purity , CAS No.1884712-47-3

COA COA
    Grade & Purity:
  • ≥99%
In stock
Item Number
C413937
Grouped product items
SKU Size
Availability
 Price Qty
C413937-10mg
10mg
3
$141.90
C413937-50mg
50mg
3
$474.90
Wish List
Bulk Order  SDS  DATASHEET  Specification Sheet

Histone Acetyltransferase Inhibitors

View related series
Epigenetic Reader Domain (314) Epigenetics (1496) Histone Acetyltransferase (79) Histone Modification (1379)

Basic Description

Synonyms (S)-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
Specifications & Purity ≥99%
Biochemical and Physiological Mechanisms CPI-637 is a selective and cell-active benzodiazepinone CBP/EP300 bromodomain inhibitor with IC50 values of 0.03 μM and 0.051μM for CBP and EP300 respectively in TR-FRET assay. It is highly selective against other bromodomains, displaying substantial bioc
Storage Temp Store at -20°C
Shipped In
Ice chest + Ice pads
This product requires cold chain shipping. Ground and other economy services are not available.
Product Description

Information

CPI-637 CPI-637 is a selective and cell-active benzodiazepinone CBP/EP300 bromodomain inhibitor with IC50 values of 0.03 μM and 0.051μM for CBP and EP300 respectively in TR-FRET assay. It is highly selective against other bromodomains, displaying substantial biochemical activity only against BRD9.


Targets

CBP (Cell-free assay); EP300 (Cell-free assay) 0.03 μM; 0.051 μM


In vitro

CPI-637 inhibits MYC expression in AMO-1 cells (EC50=0.60 μM).


Cell Research(from reference)

Cell lines：AMO-1 cells 

Concentrations：0-5 μM 

Incubation Time：6 h 

Taxonomic Classification

Taxonomy Tree

Kingdom Organic compounds
Superclass Organoheterocyclic compounds
Class Benzodiazepines
Subclass Not available
Intermediate Tree Nodes Not available
Direct Parent Benzodiazepines
Alternative Parents Beta amino acids and derivatives  Indazoles  Secondary alkylarylamines  1,4-diazepines  Benzenoids  Pyrazoles  Heteroaromatic compounds  Secondary carboxylic acid amides  Lactams  Azacyclic compounds  Organopnictogen compounds  Organic oxides  Hydrocarbon derivatives  Carbonyl compounds  
Molecular Framework Aromatic heteropolycyclic compounds
Substituents Benzodiazepine - Beta amino acid or derivatives - Benzopyrazole - Indazole - Para-diazepine - Secondary aliphatic/aromatic amine - Benzenoid - Azole - Heteroaromatic compound - Pyrazole - Amino acid or derivatives - Secondary carboxylic acid amide - Carboxamide group - Lactam - Azacycle - Secondary amine - Carboxylic acid derivative - Organooxygen compound - Carbonyl group - Organic oxide - Organopnictogen compound - Organic oxygen compound - Amine - Organic nitrogen compound - Hydrocarbon derivative - Organonitrogen compound - Aromatic heteropolycyclic compound
Description This compound belongs to the class of organic compounds known as benzodiazepines. These are organic compounds containing a benzene ring fused to either isomers of diazepine(unsaturated seven-member heterocycle with two nitrogen atoms replacing two carbon atoms).
External Descriptors Not available

Associated Targets(Human)

EP300 Tchem Histone acetyltransferase p300 (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
CREBBP Tchem CREB-binding protein (4 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
BRD9 Tchem Bromodomain-containing protein 9 (2 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
ABL1 Tclin Tyrosine-protein kinase ABL (18331 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
GSK3B Tclin Glycogen synthase kinase-3 beta (11785 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CSNK1D Tchem Casein kinase I delta (4546 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CDK2 Tchem Cyclin-dependent kinase 2 (9050 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
AURKA Tchem Serine/threonine-protein kinase Aurora-A (10240 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
U2OS (164939 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
LNCaP (8286 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CWR22R (2180 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
EP300 Tchem Histone acetyltransferase p300 (1259 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
KAT2B Tchem Histone acetyltransferase PCAF (884 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CREBBP Tchem CREB-binding protein (1602 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
BRD4 Tchem Bromodomain-containing protein 4 (13122 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
BRD2 Tchem Bromodomain-containing protein 2 (1296 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
BAZ2B Tchem Bromodomain adjacent to zinc finger domain protein 2B (56204 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
BRDT Tchem Bromodomain testis-specific protein (576 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
BRD3 Tchem Bromodomain-containing protein 3 (1086 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PHIP Tbio PH-interacting protein (91 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
SMARCA2 Tchem Probable global transcription activator SNF2L2 (466 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
TRIM24 Tchem Transcription intermediary factor 1-alpha (2087 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CECR2 Tchem Cat eye syndrome critical region protein 2 (340 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
BRD9 Tchem Bromodomain-containing protein 9 (684 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
BRPF1 Tchem Peregrin (2217 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
HEK-293T (167025 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
EP300 Tchem CREB-binding protein/Histone acetyltransferase p300 (392 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
LNCaP C4-2B (271 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Associated Targets(non-human)

Mapk1 MAP kinase ERK2 (650 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Fgfr3 Fibroblast growth factor receptor 3 (21 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
rep Replicase polyprotein 1ab (378 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Mechanisms of Action

Mechanism of Action Action Type target ID Target Name Target Type Target Organism Binding Site Name References

Names and Identifiers

Pubchem Sid 504772939
Pubchem Sid Url https://pubchem.ncbi.nlm.nih.gov/substance/504772939
IUPAC Name (4R)-4-methyl-6-[1-methyl-3-(1-methylpyrazol-4-yl)indazol-5-yl]-1,3,4,5-tetrahydro-1,5-benzodiazepin-2-one
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 CC1CC(=O)NC2=CC=CC(=C2N1)C3=CC4=C(C=C3)N(N=C4C5=CN(N=C5)C)C
Isomeric SMILES C[C@@H]1CC(=O)NC2=CC=CC(=C2N1)C3=CC4=C(C=C3)N(N=C4C5=CN(N=C5)C)C
Molecular Weight 386.45
Reaxy-Rn 39359318
Reaxys-RN_link_address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=39359318&ln=

Certificates（CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:

Find and download the COA for your product by matching the lot number on the packaging.

3 results found

Lot Number Certificate Type Date Item
I2208707 Certificate of Analysis Jun 16, 2025 C413937
I2208706 Certificate of Analysis Jun 16, 2025 C413937
C2525404 Certificate of Analysis Jun 20, 2022 C413937

Chemical and Physical Properties

Solubility Solubility (25°C) In vitro DMSO: 26 mg/mL (67.27 mM); Water: Insoluble; Ethanol: Insoluble;
Molecular Weight 386.400 g/mol
XLogP3 2.500
Hydrogen Bond Donor Count 2
Hydrogen Bond Acceptor Count 4
Rotatable Bond Count 2
Exact Mass 386.186 Da
Monoisotopic Mass 386.186 Da
Topological Polar Surface Area 76.800 Ų
Heavy Atom Count 29
Formal Charge 0
Complexity 616.000
Isotope Atom Count 0
Defined Atom Stereocenter Count 1
Undefined Atom Stereocenter Count 0
Defined Bond Stereocenter Count 0
Undefined Bond Stereocenter Count 0
The total count of all stereochemical bonds 0
Covalently-Bonded Unit Count 1

Solution Calculators

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