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I-CBP 112 - ≥98%(HPLC), high purity , CAS No.1640282-31-0, Inhibitor of CREB binding protein;Inhibitor of E1A binding protein p300

  • Moligand™
  • ≥98%(HPLC)
Item Number
I288434
Grouped product items
SKUSizeAvailabilityPrice Qty
I288434-1mg
1mg
In stock
$63.90
I288434-5mg
5mg
In stock
$197.90
I288434-10mg
10mg
In stock
$345.90
I288434-25mg
25mg
In stock
$778.90

Selective CBP/p300 BRD inhibitor

Basic Description

Synonyms1-[7-(3,4-Dimethoxyphenyl)-2,3-dihydro-9-[[(3S)-1-methyl-3-piperidinyl]methoxy]-1,4-benzoxazepin-4(5H)-yl]-1-propanone;1-[7-(3,4-Dimethoxyphenyl)-9-[[(3S)-1-methylpiperidin-3-yl]methoxy]-2,3,4,5-tetrahydro-1,4-benzoxazepin-4-yl]propan-1-one
Specifications & PurityMoligand™, ≥98%(HPLC)
Biochemical and Physiological MechanismsCBP/p300 bromodomain inhibitor (IC50values are 0.142-0.17 and 0.625μM for CBP and p300 respectively). Selective for CBP and p300 over ATAD2, BAZ2B, BRD2(2), BRD4(1), PB1(5), PCAF, PHIP(2) and TIF1αbromodomains in a BLI assay. Accelerates FRAP recovery in
Storage TempStore at -20°C,Desiccated
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionInhibitor of CREB binding protein;Inhibitor of E1A binding protein p300
Product Description

I-CBP112 is a potent and selective CBP/p300 inhibitor with dissociation constant (KD) of 151 ± 6 nM and 167 ± 8 nM for CBP and p300, respectively.

Associated Targets

EP300 Tchem Histone acetyltransferase p300 3 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CREBBP Tchem CREB-binding protein 7 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

BRD4 Tchem Bromodomain-containing protein 4 1 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CDK2 Tchem Cyclin-dependent kinase 2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

HDAC6 Tclin Histone deacetylase 6 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

FGFR3 Tclin Fibroblast growth factor receptor 3 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CSNK1D Tchem Casein kinase I isoform delta 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

TRIM24 Tchem Transcription intermediary factor 1-alpha 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

BRD9 Tchem Bromodomain-containing protein 9 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

BRD3 Tchem Bromodomain-containing protein 3 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

BRPF1 Tchem Peregrin 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

BRD2 Tchem Bromodomain-containing protein 2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

AURKA Tchem Aurora kinase A 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CHRM2 Tclin Muscarinic acetylcholine receptor M2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ABL1 Tclin Tyrosine-protein kinase ABL1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ADRA1A Tclin Alpha-1A adrenergic receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

GSK3B Tclin Glycogen synthase kinase-3 beta 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

MAPK1 Tchem Mitogen-activated protein kinase 1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

Names and Identifiers

IUPAC Name 1-[7-(3,4-dimethoxyphenyl)-9-[[(3S)-1-methylpiperidin-3-yl]methoxy]-3,5-dihydro-2H-1,4-benzoxazepin-4-yl]propan-1-one
INCHI InChI=1S/C27H36N2O5/c1-5-26(30)29-11-12-33-27-22(17-29)13-21(20-8-9-23(31-3)24(14-20)32-4)15-25(27)34-18-19-7-6-10-28(2)16-19/h8-9,13-15,19H,5-7,10-12,16-18H2,1-4H3/t19-/m0/s1
InChi Key YKNAKDFZAWQEEO-IBGZPJMESA-N
Canonical SMILES CCC(=O)N1CCOC2=C(C1)C=C(C=C2OCC3CCCN(C3)C)C4=CC(=C(C=C4)OC)OC
Isomeric SMILES CCC(=O)N1CCOC2=C(C1)C=C(C=C2OC[C@H]3CCCN(C3)C)C4=CC(=C(C=C4)OC)OC
PubChem CID 90488984
MeSH Entry Terms 1-(7-(3,4-Dimethoxyphenyl)-9-(((3S)-1-methyl-3-piperidinyl)methoxy)-2,3-dihydro-1,4-benzoxazepin-4(5H)-yl)-1-propanone;1-Propanone, 1-(7-(3,4-dimethoxyphenyl)-2,3-dihydro-9-(((3S)-1-methyl-3-piperidinyl)methoxy)-1,4-benzoxazepin-4(5H)-yl)-;I-CBP112
Molecular Weight 468.59

Certificates

Certificate of Analysis(COA)

Enter Lot Number to search for COA:

To view the certificate results,please click on a Lot number.For Lot numbers from past orders,please use our order status section

4 results found

Lot NumberCertificate TypeDateItem
J2130447Certificate of AnalysisAug 14, 2024 I288434
J2130448Certificate of AnalysisAug 14, 2024 I288434
J2130449Certificate of AnalysisAug 14, 2024 I288434
J2130450Certificate of AnalysisAug 14, 2024 I288434

Chemical and Physical Properties

SolubilitySoluble in DMSO, the highest concentration (mg / ml): 94, the highest concentration (mm): 200.60; Soluble in H2O, the highest concentration (mg / ml): 94, the highest concentration (mm): 200.60; Dissolved in ethanol, the highest concentration (mg / ml): 9

Safety and Hazards(GHS)

Pictogram(s) GHS07
Signal Warning
Hazard Statements

H315:Causes skin irritation

H319:Causes serious eye irritation

H335:May cause respiratory irritation

Precautionary Statements

P261:Avoid breathing dust/fume/gas/mist/vapors/spray.

P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses if present and easy to do - continue rinsing.

Related Documents

References

1. Zeng L, Zhang Q, Gerona-Navarro G, Moshkina N, Zhou MM.  (2008)  Structural basis of site-specific histone recognition by the bromodomains of human coactivators PCAF and CBP/p300..  Structure,  16  (4): (643-52).  [PMID:18400184]
2. Iyer NG, Ozdag H, Caldas C.  (2004)  p300/CBP and cancer..  Oncogene,  23  (24): (4225-31).  [PMID:15156177]
3. Kalkhoven E.  (2004)  CBP and p300: HATs for different occasions..  Biochem Pharmacol,  68  (6): (1145-55).  [PMID:15313412]

Solution Calculators