MCB-613 | CAS#296792-62-6 | stimulator of steroid receptor coactivator

MedKoo Cat#: 407170 | Name: MCB-613

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Description:

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

MCB-613 is a potent Steroid Receptor Coactivator Stimulator that Overstimulates Cancer Cells and Leads to Cell Stress and Death. MCB-613 can super-stimulate SRCs' transcriptional activity. MCB-613 increases SRCs' interactions with other coactivators and markedly induces ER stress coupled to the generation of reactive oxygen species (ROS). MCB-613 selectively induce excessive stress in cancer cells. Over-stimulating the SRC oncogenic program can be an effective strategy to kill cancer cells. By integrating growth pathways on which cancer cells rely, steroid receptor coactivators (SRC-1, SRC-2, and SRC-3) represent emerging targets in cancer therapeutics.

Chemical Structure

MCB-613

CAS#296792-62-6

Theoretical Analysis

MedKoo Cat#: 407170

Name: MCB-613

CAS#: 296792-62-6

Chemical Formula: C20H20N2O

Exact Mass: 304.1576

Molecular Weight: 304.39

Elemental Analysis: C, 78.92; H, 6.62; N, 9.20; O, 5.26

Price and Availability

Size	Price	Availability	Quantity
5mg	USD 350.00	2 Weeks
25mg	USD 950.00	2 Weeks

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Related CAS #

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Synonym

MCB-613; MCB 613; MCB613.

IUPAC/Chemical Name

4-ethyl-2,6-bis(3-pyridinylmethylene)-cyclohexanone

InChi Key

MMBSCBVEHMETSA-GDAWTGGTSA-N

InChi Code

InChI=1S/C20H20N2O/c1-2-15-9-18(11-16-5-3-7-21-13-16)20(23)19(10-15)12-17-6-4-8-22-14-17/h3-8,11-15H,2,9-10H2,1H3/b18-11+,19-12+

SMILES Code

O=C1/C(CC(CC)C/C1=C\C2=CC=CN=C2)=C/C3=CC=CN=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:

MCB-613 is a potent Steroid Receptor Coactivator Stimulator.

In vitro activity:

This study identified a small molecule called MCB-613 to cause rapid ubiquitination, nuclear export, and degradation of p53-R175H through a lysosome-mediated pathway, leading to catastrophic cancer cell death. In contrast to its effect on the p53-R175H mutant, MCB-613 causes slight stabilization of p53-WT and has weaker effects on other p53 gain-of-function mutants. Reference: Nat Commun. 2018 Mar 28;9(1):1270. https://pubmed.ncbi.nlm.nih.gov/29593334/

In vivo activity:

MCB-613 decreases mouse infarct size, apoptosis, hypertrophy, and fibrosis while maintaining significant cardiac function. MCB-613, when given within hours post MI, induces lasting protection from adverse remodeling concomitant with: 1) inhibition of macrophage inflammatory signaling and interleukin 1 (IL-1) signaling, which attenuates the acute inflammatory response, 2) attenuation of fibroblast differentiation, and 3) promotion of Tsc22d3-expressing macrophages-all of which may limit inflammatory damage. Reference: Proc Natl Acad Sci U S A. 2020 Dec 8;117(49):31353-31364. https://pubmed.ncbi.nlm.nih.gov/33229578/

	Solvent	mg/mL	mM
Solubility
	DMSO	2.0	6.57
	Ethanol	2.0	6.57
	DMF	2.0	6.57

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 304.39 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. Padmanabhan A, Candelaria N, Wong KK, Nikolai BC, Lonard DM, O'Malley BW, Richards JS. USP15-dependent lysosomal pathway controls p53-R175H turnover in ovarian cancer cells. Nat Commun. 2018 Mar 28;9(1):1270. doi: 10.1038/s41467-018-03599-w. PMID: 29593334; PMCID: PMC5871815. 2. Hossain MM, Barua D, Arabkari V, Islam N, Gupta A, Gupta S. Hyperactivation of nuclear receptor coactivators induces PERK-dependent cell death. Oncotarget. 2018 Feb 8;9(14):11707-11721. doi: 10.18632/oncotarget.24451. PMID: 29545931; PMCID: PMC5837751. 3. Mullany LK, Rohira AD, Leach JP, Kim JH, Monroe TO, Ortiz AR, Stork B, Gaber MW, Sarkar P, Sikora AG, Rosengart TK, York B, Song Y, Dacso CC, Lonard DM, Martin JF, O'Malley BW. A steroid receptor coactivator stimulator (MCB-613) attenuates adverse remodeling after myocardial infarction. Proc Natl Acad Sci U S A. 2020 Dec 8;117(49):31353-31364. doi: 10.1073/pnas.2011614117. Epub 2020 Nov 23. PMID: 33229578; PMCID: PMC7733826.

In vitro protocol:

In vivo protocol:

1. Mullany LK, Rohira AD, Leach JP, Kim JH, Monroe TO, Ortiz AR, Stork B, Gaber MW, Sarkar P, Sikora AG, Rosengart TK, York B, Song Y, Dacso CC, Lonard DM, Martin JF, O'Malley BW. A steroid receptor coactivator stimulator (MCB-613) attenuates adverse remodeling after myocardial infarction. Proc Natl Acad Sci U S A. 2020 Dec 8;117(49):31353-31364. doi: 10.1073/pnas.2011614117. Epub 2020 Nov 23. PMID: 33229578; PMCID: PMC7733826.

1: Overstimulation Fatal for Cancer Cells. Cancer Discov. 2015 Aug 19. [Epub ahead of print] PubMed PMID: 26290253. 2: Wang L, Yu Y, Chow DC, Yan F, Hsu CC, Stossi F, Mancini MA, Palzkill T, Liao L, Zhou S, Xu J, Lonard DM, O'Malley BW. Characterization of a Steroid Receptor Coactivator Small Molecule Stimulator that Overstimulates Cancer Cells and Leads to Cell Stress and Death. Cancer Cell. 2015 Aug 10;28(2):240-52. doi: 10.1016/j.ccell.2015.07.005. PubMed PMID: 26267537; PubMed Central PMCID: PMC4536575.