CPI-637 | CAS#1884712-47-3 | CBP/ EP300 bromodomain inhibitor

MedKoo Cat#: 407306 | Name: CPI-637

Description:

WARNING: This product is for research use only, not for human or veterinary use.

CPI-637 is a potent and selective CBP/ EP300 bromodomain inhibitor. The biochemical potency of CPI-637 translated well into cells (CBP BRET EC50 = 0.3 μM). CPI-637 demonstrated a >700-fold selectivity over the BET family of bromodomains (BRD4 IC50 = 11.0 ± 0.6 μM). CPI-637 inhibits MYC expression in AMO-1 cells (EC50 = 0.60 μM). CBP and EP300 are highly homologous, bromodomain-containing transcription coactivators involved in numerous cellular pathways relevant to oncology.

Chemical Structure

CPI-637

CAS#1884712-47-3

Theoretical Analysis

MedKoo Cat#: 407306

Name: CPI-637

CAS#: 1884712-47-3

Chemical Formula: C22H22N6O

Exact Mass: 386.1855

Molecular Weight: 386.46

Elemental Analysis: C, 68.38; H, 5.74; N, 21.75; O, 4.14

Price and Availability

Size	Price	Availability
50mg	USD 450.00	2 Weeks
100mg	USD 750.00	2 Weeks
200mg	USD 1,350.00	2 Weeks
1g	USD 3,850.00	2 Weeks
2g	USD 5,950.00	2 Weeks

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Related CAS #

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Synonym

CPI-637; CPI 637; CPI637.

IUPAC/Chemical Name

(R)-4-methyl-6-(1-methyl-3-(1-methyl-1H-pyrazol-4-yl)-1H-indazol-5-yl)-1,3,4,5-tetrahydro-2H-benzo[b][1,4]diazepin-2-one

InChi Key

BFTKDWYIRJGJCA-CYBMUJFWSA-N

InChi Code

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

SMILES Code

CN(N=C1C2=CN(C)N=C2)C3=C1C=C(C4=CC=CC(N5)=C4N[C@H](C)CC5=O)C=C3

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO, not in water

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

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.

In vitro activity:

As shown in Figures 1A–D, CPI-637 significantly increased GFP+ % in a dose- and time-dependent manner in both J-Lat A2 and J-Lat 10.6 cells. Furthermore, the reactivation by CPI-637 was confirmed in ACH2 cells chronically infected with HIV-1. Reference: Front Cell Infect Microbiol. 2021; 11: 686035. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8326664/

In vivo activity:

TBD

	Solvent	mg/mL	mM
Solubility
	DMSO	12.0	31.15
	DMSO:PBS (pH 7.2) (1:1)	0.5	1.29
	DMF	0.2	0.52
	Ethanol	0.1	0.26

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 386.46 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Zheng T, Chen P, Huang Y, Qiu J, Zhou C, Wu Z, Li L. CPI-637 as a Potential Bifunctional Latency-Reversing Agent That Targets Both the BRD4 and TIP60 Proteins. Front Cell Infect Microbiol. 2021 Jul 19;11:686035. doi: 10.3389/fcimb.2021.686035. PMID: 34350133; PMCID: PMC8326664. 2. Taylor AM, Côté A, Hewitt MC, Pastor R, Leblanc Y, Nasveschuk CG, Romero FA, Crawford TD, Cantone N, Jayaram H, Setser J, Murray J, Beresini MH, de Leon Boenig G, Chen Z, Conery AR, Cummings RT, Dakin LA, Flynn EM, Huang OW, Kaufman S, Keller PJ, Kiefer JR, Lai T, Li Y, Liao J, Liu W, Lu H, Pardo E, Tsui V, Wang J, Wang Y, Xu Z, Yan F, Yu D, Zawadzke L, Zhu X, Zhu X, Sims RJ 3rd, Cochran AG, Bellon S, Audia JE, Magnuson S, Albrecht BK. Fragment-Based Discovery of a Selective and Cell-Active Benzodiazepinone CBP/EP300 Bromodomain Inhibitor (CPI-637). ACS Med Chem Lett. 2016 Mar 15;7(5):531-6. doi: 10.1021/acsmedchemlett.6b00075. PMID: 27190605; PMCID: PMC4867486.

In vitro protocol:

In vivo protocol:

TBD

Fragment-Based Discovery of a Selective and Cell-Active Benzodiazepinone CBP/EP300 Bromodomain Inhibitor (CPI-637) Alexander M. Taylor*†, Alexandre Côté†, Michael C. Hewitt†, Richard Pastor‡, Yves Leblanc†, Christopher G. Nasveschuk†, F. Anthony Romero‡, Terry D. Crawford‡, Nico Cantone†, Hariharan Jayaram†, Jeremy Setser†, Jeremy Murray‡, Maureen H. Beresini‡, Gladys de Leon Boenig‡, Zhongguo Chen§, Andrew R. Conery†, Richard T. Cummings†, Leslie A. Dakin†, E. Megan Flynn‡, Oscar W. Huang‡, Susan Kaufman‡, Patricia J. Keller†, James R. Kiefer‡, Tommy Lai§, Yingjie Li§, Jiangpeng Liao§, Wenfeng Liu§, Henry Lu§, Eneida Pardo†, Vickie Tsui‡, Jian Wang§, Yongyun Wang§, Zhaowu Xu§, Fen Yan§, Dong Yu§, Laura Zawadzke†, Xiaoqin Zhu§, Xiaoyu Zhu§, Robert J. SimsIII†, Andrea G. Cochran‡, Steve Bellon†, James E. Audia†, Steven Magnuson‡, and Brian K. Albrecht† ACS Med. Chem. Lett., Article ASAP DOI: 10.1021/acsmedchemlett.6b00075 Publication Date (Web): March 15, 2016

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