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1613695-14-9

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1613695-14-9 Usage

Description

SGC-CBP30 is a potent CBP/p300 bromodomain (BRD) inhibitor. SGC-CBP30 shows Kd values are 21 and 32 nM for CBP and p300 BRDs respectively. SGC-CBP30 also exhibits 40-fold and 250-fold selectivity for CBP over the first BRD of BRD4 (BRD4(1)) and BRD4(2) respectively. SGC-CBP30 accelerates FRAP recovery in cells at a concentration of 1 ?M.

Uses

SGC-CBP30 is a potent CREBBP/EP300 inhibitor.

Biochem/physiol Actions

SGC-CBP30 is a selective inhibitor of the bromodomain-containing transcription factors CREBBP (CBP) and EP300 (IC50 = 0.021 and 0.038 μM, respectively). SGC-CBP30 has little activity against other bromodomains at concentrations up to 1 mM. For full characterization details, please visit the SGC-CBP30 probe summary on the Structural Genomics Consortium (SGC) website.To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc

Check Digit Verification of cas no

The CAS Registry Mumber 1613695-14-9 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,6,1,3,6,9 and 5 respectively; the second part has 2 digits, 1 and 4 respectively.
Calculate Digit Verification of CAS Registry Number 1613695-14:
(9*1)+(8*6)+(7*1)+(6*3)+(5*6)+(4*9)+(3*5)+(2*1)+(1*4)=169
169 % 10 = 9
So 1613695-14-9 is a valid CAS Registry Number.

1613695-14-9SDS

SAFETY DATA SHEETS

According to Globally Harmonized System of Classification and Labelling of Chemicals (GHS) - Sixth revised edition

Version: 1.0

Creation Date: Aug 18, 2017

Revision Date: Aug 18, 2017

1.Identification

1.1 GHS Product identifier

Product name SGC?CBP30

1.2 Other means of identification

Product number -
Other names 2-[2-(3-chloro-4-methoxyphenyl)ethyl]-5-(3,5-dimethyl-1,2-oxazol-4-yl)-1-[(2S)-2-(morpholin-4-yl)propyl]-1H-benzimidazole

1.3 Recommended use of the chemical and restrictions on use

Identified uses For industry use only.
Uses advised against no data available

1.4 Supplier's details

1.5 Emergency phone number

Emergency phone number -
Service hours Monday to Friday, 9am-5pm (Standard time zone: UTC/GMT +8 hours).

More Details:1613695-14-9 SDS

1613695-14-9Downstream Products

1613695-14-9Relevant articles and documents

Discovery and optimization of small-molecule ligands for the CBP/p300 bromodomains

Hay, Duncan A.,Fedorov, Oleg,Martin, Sarah,Singleton, Dean C.,Tallant, Cynthia,Wells, Christopher,Picaud, Sarah,Philpott, Martin,Monteiro, Octovia P.,Rogers, Catherine M.,Conway, Stuart J.,Rooney, Timothy P. C.,Tumber, Anthony,Yapp, Clarence,Filippakopoulos, Panagis,Bunnage, Mark E.,Müller, Susanne,Knapp, Stefan,Schofield, Christopher J.,Brennan, Paul E.

, p. 9308 - 9319 (2014/07/21)

Small-molecule inhibitors that target bromodomains outside of the bromodomain and extra-terminal (BET) sub-family are lacking. Here, we describe highly potent and selective ligands for the bromodomain module of the human lysine acetyl transferase CBP/p300, developed from a series of 5-isoxazolyl-benzimidazoles. Our starting point was a fragment hit, which was optimized into a more potent and selective lead using parallel synthesis employing Suzuki couplings, benzimidazole-forming reactions, and reductive aminations. The selectivity of the lead compound against other bromodomain family members was investigated using a thermal stability assay, which revealed some inhibition of the structurally related BET family members. To address the BET selectivity issue, X-ray crystal structures of the lead compound bound to the CREB binding protein (CBP) and the first bromodomain of BRD4 (BRD4(1)) were used to guide the design of more selective compounds. The crystal structures obtained revealed two distinct binding modes. By varying the aryl substitution pattern and developing conformationally constrained analogues, selectivity for CBP over BRD4(1) was increased. The optimized compound is highly potent (K d = 21 nM) and selective, displaying 40-fold selectivity over BRD4(1). Cellular activity was demonstrated using fluorescence recovery after photo-bleaching (FRAP) and a p53 reporter assay. The optimized compounds are cell-active and have nanomolar affinity for CBP/p300; therefore, they should be useful in studies investigating the biological roles of CBP and p300 and to validate the CBP and p300 bromodomains as therapeutic targets.

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