MCB-613

stimulator of steroid receptor coactivator (SRC) CAS# 1162656-22-5

MCB-613

Catalog No. BCC3982----Order now to get a substantial discount!

Product Name & Size Price Stock
MCB-613: 5mg $115 In Stock
MCB-613: 10mg Please Inquire In Stock
MCB-613: 20mg Please Inquire Please Inquire
MCB-613: 50mg Please Inquire Please Inquire
MCB-613: 100mg Please Inquire Please Inquire
MCB-613: 200mg Please Inquire Please Inquire
MCB-613: 500mg Please Inquire Please Inquire
MCB-613: 1000mg Please Inquire Please Inquire
Related Products
  • C646

    Catalog No.:BCC4546
    CAS No.:328968-36-1

Quality Control of MCB-613

Number of papers citing our products

Chemical structure

MCB-613

3D structure

Chemical Properties of MCB-613

Cas No. 1162656-22-5 SDF Download SDF
PubChem ID 2175947 Appearance Powder
Formula C19H19N3O M.Wt 305.37
Type of Compound N/A Storage Desiccate at -20°C
Solubility >13.2mg/mL in DMSO
Chemical Name (2E,6E)-4-ethyl-2,6-bis(pyridin-3-ylmethylidene)cyclohexan-1-one
SMILES CCC1CC(=CC2=CN=CC=C2)C(=O)C(=CC3=CN=CC=C3)C1
Standard InChIKey MMBSCBVEHMETSA-GDAWTGGTSA-N
Standard InChI 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+
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of MCB-613

DescriptionMCB-613 is a potent, pan steroid receptor coactivator (SRC) stimulator. Target: SRC in vitro: MCB-613 exerts the greatest activation of SRC-1 in the primary screen, is confirmed to be a strong activator of all three SRCs. 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 and reversibly binds to the RID of SRC-3, and selectively kills cancer cells including MCF-7 (breast), PC-3 (prostate), H1299 (lung), and HepG2 (liver) cells, without toxicity to mouse primary hepatocytes and mouse embryonic fibroblasts (MEFs). MCB-613 also increases SRCs' interactions with other coactivators and markedly induces ER stress coupled to the generation of reactive oxygen species (ROS). [1] in vivo: In an MCF-7 breast cancer mouse xenograft model, MCB-613 (20 mg/kg, i.p.) significantly and dramatically inhibits the growth of the tumor while causing no obvious animal toxicity and body weight less. [1]

References:
[1]. Wang L, et al. 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.

MCB-613 Dilution Calculator

Concentration (start)
x
Volume (start)
=
Concentration (final)
x
Volume (final)
 
 
 
C1
V1
C2
V2

calculate

MCB-613 Molarity Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
g/mol

calculate

Preparing Stock Solutions of MCB-613

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 3.2747 mL 16.3736 mL 32.7472 mL 65.4943 mL 81.8679 mL
5 mM 0.6549 mL 3.2747 mL 6.5494 mL 13.0989 mL 16.3736 mL
10 mM 0.3275 mL 1.6374 mL 3.2747 mL 6.5494 mL 8.1868 mL
50 mM 0.0655 mL 0.3275 mL 0.6549 mL 1.3099 mL 1.6374 mL
100 mM 0.0327 mL 0.1637 mL 0.3275 mL 0.6549 mL 0.8187 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

Organizitions Citing Our Products recently

 
 
 

Calcutta University

University of Minnesota

University of Maryland School of Medicine

University of Illinois at Chicago

The Ohio State University

University of Zurich

Harvard University

Colorado State University

Auburn University

Yale University

Worcester Polytechnic Institute

Washington State University

Stanford University

University of Leipzig

Universidade da Beira Interior

The Institute of Cancer Research

Heidelberg University

University of Amsterdam

University of Auckland
TsingHua University
TsingHua University
The University of Michigan
The University of Michigan
Miami University
Miami University
DRURY University
DRURY University
Jilin University
Jilin University
Fudan University
Fudan University
Wuhan University
Wuhan University
Sun Yat-sen University
Sun Yat-sen University
Universite de Paris
Universite de Paris
Deemed University
Deemed University
Auckland University
Auckland University
The University of Tokyo
The University of Tokyo
Korea University
Korea University

Background on MCB-613

MCB-613, 4-ethyl-2,6-bis-pyridin-3-ylmethylene-cyclohexanone, is a novel and potent stimulator of p160 steroid receptor coactivators (SRCs). It is a Pan-SRCs stimulator. MCB-613 is confirmed to be a strong activator of all three SRCs family proteins [1].

Members of the SRCs family interact with nuclear receptors and other transcription factors to drive target gene expression while also functioning as integrators of upstream cell signaling pathways. Three factors share homology with each other, they have distinct and important roles in multiple physiological processes, including growth and development, reproduction, and metabolism. All of them have been found to be broadly involved in different tumorigenesis. [2, 3]

MCB-613 can super-activate transcriptional activity of SRCs. MCB-613 markedly increases SRCs’ interactions with other coactivators. Coactivation of MMP2 or MMP13 promoter-driven luciferase reporter with SRC-3 was greatly enhanced by MCB-613. MCB-613 increased SRC-3’s interaction with CBP and CARM1 robustly in a dose-dependent manner. [1]

MCB-613 is cytotoxic. It can efficiently kill a variety of human cancer cell lines, including PC-3 (prostate), MCF-7 (breast), HepG2 (liver), and H1299 (lung)cells. Cancer cells overexpress SRCs and rely on them for cell growth, MCB-613 can selectively induce excessive ER stress coupled to the generation of reactive oxygen species (ROS) in cancer cells. [1]

MCB-613 treatment probably leads to a distinct phosphorylation pattern on SRC-3, which will be interesting to pursue in future studies. [1]

Reference:
Wang L, Yu Y, Chow DC et al.  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.
Lonard, D. M., and O’malley, B.W. Nuclear receptor coregulators: judges, juries, and executioners of cellular regulation. 2007. Mol. Cell 27, 691–700.
Anzick, S. L., Kononen, J., Walker, R.L.et al. AIB1, a steroid receptor coactivator amplified in breast and ovarian cancer. 1997, Science 277, 965–968.

Featured Products
  • Levobetaxolol HCl

    Catalog No.:BCC4671
    CAS No.:116209-55-3
  • Aflatoxin B1

    Catalog No.:BCC9212
    CAS No.:1162-65-8
  • Complanatoside

    Catalog No.:BCN8213
    CAS No.:116183-66-5
  • Alexine

    Catalog No.:BCN2054
    CAS No.:116174-63-1
  • Brevicolline

    Catalog No.:BCN2459
    CAS No.:20069-02-7
  • VU 0361737

    Catalog No.:BCC4596
    CAS No.:1161205-04-4
  • G-15

    Catalog No.:BCC6058
    CAS No.:1161002-05-6
  • Phenamil

    Catalog No.:BCC7673
    CAS No.:1161-94-0
  • Z-Phe-OH

    Catalog No.:BCC2756
    CAS No.:1161-13-3
  • RETF-4NA

    Catalog No.:BCC6073
    CAS No.:1160928-63-1
  • IDE 1

    Catalog No.:BCC7841
    CAS No.:1160927-48-9
  • Dehydromiltirone

    Catalog No.:BCN5357
    CAS No.:116064-77-8
New Products
 

References on MCB-613

Molecular Pathways: Targeting Steroid Receptor Coactivators in Cancer.[Pubmed:27654711]

Clin Cancer Res. 2016 Nov 15;22(22):5403-5407.

Coactivators represent a large class of proteins that partner with nuclear receptors and other transcription factors to regulate gene expression. Given their pleiotropic roles in the control of transcription, coactivators have been implicated in a broad range of human disease states, including cancer. This is best typified by the three members of the steroid receptor coactivator (SRC) family, each of which integrates steroid hormone signaling and growth factor pathways to drive oncogenic gene expression programs in breast, endometrial, ovarian, prostate, and other cancers. Because of this, coactivators represent emerging targets for cancer therapeutics, and efforts are now being made to develop SRC-targeting agents, such as the SI-2 inhibitor and the novel SRC stimulator, MCB-613, that are able to block cancer growth in cell culture and animal model systems. Here, we will discuss the mechanisms through which coactivators drive cancer progression and how targeting coactivators represent a novel conceptual approach to combat tumor growth that is distinct from the use of other targeted therapeutic agents. We also will describe efforts to develop next-generation SRC inhibitors and stimulators that can be taken into the clinic for the treatment of recurrent, drug-resistant cancers. Clin Cancer Res; 22(22); 5403-7. (c)2016 AACR.

Characterization of a Steroid Receptor Coactivator Small Molecule Stimulator that Overstimulates Cancer Cells and Leads to Cell Stress and Death.[Pubmed:26267537]

Cancer Cell. 2015 Aug 10;28(2):240-52.

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. High-throughput screening for SRC small molecule inhibitors (SMIs) uncovered MCB-613 as a potent SRC small molecule "stimulator" (SMS). We demonstrate that MCB-613 can super-stimulate SRCs' transcriptional activity. Further investigation revealed that MCB-613 increases SRCs' interactions with other coactivators and markedly induces ER stress coupled to the generation of reactive oxygen species (ROS). Because cancer cells overexpress SRCs and rely on them for growth, we show that we can exploit MCB-613 to selectively induce excessive stress in cancer cells. This suggests that over-stimulating the SRC oncogenic program can be an effective strategy to kill cancer cells.

Description

MCB-613 is a potent Steroid receptor coactivator SRC small molecule ‘stimulator’ (SMS), super-stimulates 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 is a SMS that target oncogenes can be exploited as anti-cancer agents by over-stimulating the SRC oncogenic program.

Keywords:

MCB-613,1162656-22-5,Natural Products,Histone Acetyltransferases, buy MCB-613 , MCB-613 supplier , purchase MCB-613 , MCB-613 cost , MCB-613 manufacturer , order MCB-613 , high purity MCB-613

Online Inquiry for:

      Fill out the information below

      • Size:Qty: - +

      * Required Fields

                                      Result: