Molecular structure of Mocetinostat, CAS Number: 726169-73-9
Mocetinostat (CAS 726169-73-9)
See product citations (2)
Alternate Names:
MGCD0103
Application:
Mocetinostat is a potent inhibitor of HDAC1, HDAC2, HDAC3, and HDAC11
CAS Number:
726169-73-9
Purity:
≥98%
Molecular Weight:
396.44
Molecular Formula:
C23H20N6O
Supplemental Information:
This is classified as a Dangerous Good for transport and may be subject to additional shipping charges.
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
Mocetinostat is a novel small molecule inhibitor specifically targeting histone deacetylase (HDAC) enzymes. It exhibits potent inhibition against a subset of nine human recombinant HDACs, including HDAC1, HDAC2, HDAC3, and HDAC11, while not affecting class II HDACs. Notably, Mocetinostat demonstrates the highest inhibitory activity against human HDAC1 and HDAC2 enzymes in vitro. The inhibitory activity of MGCD0103 reaches a maximum plateau at 6 μM, affecting approximately 75% of the total enzyme activity in HCT116 cells. Extensively studied for its potential in treating certain cancer types, mocetinostat has proven to be a valuable compound in scientific research. Its synthesis method, mechanism of action, biological activity, biochemical and physiological effects, pharmacodynamics, advantages, limitations for lab experiments, and future directions have been investigated. By inhibiting HDAC enzymes, mocetinostat disrupts the removal of acetyl groups from histones, leading to increased histone acetylation and subsequent gene activation. The biochemical and physiological effects of mocetinostat are manifold, encompassing the inhibition of HDAC enzymes, gene activation, suppression of cell proliferation, induction of apoptosis, inhibition of angiogenesis, and mitigation of inflammation. These diverse effects underline the potential of mocetinostat as a versatile tool in both basic and applied research. Understanding its intricate mechanisms and biological outcomes enables further exploration of its therapeutic applications.
Mocetinostat (CAS 726169-73-9) References
- Liquid chromatography mass spectrometry determination of mocetinostat (MGCD0103) in rat plasma and its application to a pharmacokinetic study. | Ma, J., et al. 2014. Xenobiotica. 44: 849-54. PMID: 24588344
- HDAC class I inhibitor, Mocetinostat, reverses cardiac fibrosis in heart failure and diminishes CD90+ cardiac myofibroblast activation. | Nural-Guvener, HF., et al. 2014. Fibrogenesis Tissue Repair. 7: 10. PMID: 25024745
- ZEB1-associated drug resistance in cancer cells is reversed by the class I HDAC inhibitor mocetinostat. | Meidhof, S., et al. 2015. EMBO Mol Med. 7: 831-47. PMID: 25872941
- Anti-Fibrotic Effects of Class I HDAC Inhibitor, Mocetinostat Is Associated with IL-6/Stat3 Signaling in Ischemic Heart Failure. | Nural-Guvener, H., et al. 2015. Int J Mol Sci. 16: 11482-99. PMID: 25997003
- Metabolic changes in rats after intragastric administration of MGCD0103 (Mocetinostat), a HDAC class I inhibitor. | Zhang, Q., et al. 2015. Int J Clin Exp Pathol. 8: 9320-5. PMID: 26464683
- Histone deacetyltransferase inhibitors Trichostatin A and Mocetinostat differentially regulate MMP9, IL-18 and RECK expression, and attenuate Angiotensin II-induced cardiac fibroblast migration and proliferation. | Somanna, NK., et al. 2016. Hypertens Res. 39: 709-716. PMID: 27278287
- Class I HDAC inhibitor mocetinostat induces apoptosis by activation of miR-31 expression and suppression of E2F6. | Zhang, Q., et al. 2016. Cell Death Discov. 2: 16036. PMID: 27551526
- Prostate-Specific Membrane Antigen Targeted Polymersomes for Delivering Mocetinostat and Docetaxel to Prostate Cancer Cell Spheroids. | Karandish, F., et al. 2016. ACS Omega. 1: 952-962. PMID: 27917408
- The class I/IV HDAC inhibitor mocetinostat increases tumor antigen presentation, decreases immune suppressive cell types and augments checkpoint inhibitor therapy. | Briere, D., et al. 2018. Cancer Immunol Immunother. 67: 381-392. PMID: 29124315
- Mocetinostat combined with gemcitabine for the treatment of leiomyosarcoma: Preclinical correlates. | Lopez, G., et al. 2017. PLoS One. 12: e0188859. PMID: 29186204
- SARC018_SPORE02: Phase II Study of Mocetinostat Administered with Gemcitabine for Patients with Metastatic Leiomyosarcoma with Progression or Relapse following Prior Treatment with Gemcitabine-Containing Therapy. | Choy, E., et al. 2018. Sarcoma. 2018: 2068517. PMID: 30473623
- Mocetinostat suppresses epidural fibrosis following laminectomy by inhibiting myofibroblast activation and increasing apoptosis. | Wu, WJ., et al. 2021. Eur Rev Med Pharmacol Sci. 25: 3396. PMID: 34002805
- Histone deacetylase inhibitor, mocetinostat, regulates cardiac remodelling and renin-angiotensin system activity in rats with transverse aortic constriction-induced pressure overload cardiac hypertrophy. | Kim, GJ., et al. 2021. Rev Cardiovasc Med. 22: 1037-1045. PMID: 34565105
- Isoform-Selective HDAC Inhibitor Mocetinostat (MGCD0103) Alleviates Myocardial Ischemia/Reperfusion Injury Via Mitochondrial Protection Through the HDACs/CREB/PGC-1α Signaling Pathway. | Wang, K., et al. 2022. J Cardiovasc Pharmacol. 79: 217-228. PMID: 34983914
- In vitro anti-proliferative effect of capecitabine (Xeloda) combined with mocetinostat (MGCD0103) in 4T1 breast cancer cell line by immunoblotting. | Kaya Çakir, H. and Eroglu, O. 2021. Iran J Basic Med Sci. 24: 1515-1522. PMID: 35317122
Inhibitor of:
1200013P24Rik, 4632411B12Rik, 4930557A04Rik, A530032D15Rik, Acatin, ACTR8, Ada1, ASF1B, ASXL3, BAF53B, BAF57, BAHD1, BCoR, BCORL1, BEND7, Bles03, Blood Group H2, BORIS, BRMS1L, BRWD1, BRWD3, Btnl1, C14orf43, C5orf35, CDY2, CDYL2, CECR2, CHD (chromodomain helicase), CHD5, CHD7, CHD9, Codanin-1, Dimethyl Histone H3, Dmap1, DNHD2, Dpy30, DYDC2, Dynlt1d, EF-CBP1, Enzyme, ESCO1, EZI, FAM120AOS, FOXD4L4, GAGE, GAGE13, GAGE2A, GAGE7B, Gal11, GAS41, GATAD (GATA zinc finger domain containing), GATAD2A, H2-A, H2-M10.1, H2afb2, H2BFWT, H3.Y histone 1, H60, Hat2, HDA1, HDA2, HDA4, HDA5, HDA6, HDA7, HDAC1, HDAC10, HDAC11, HDAC2, HDAC3, HDAC5, Helios, Hils1, Histone B, Histone cluster 1 H1C, Histone cluster 1 H1D, Histone cluster 1 H1E, Histone cluster 1 H1T, Histone cluster 1 H2A, Histone cluster 1 H2AG, Histone cluster 1 H2B, Histone cluster 1 H2BD, Histone cluster 1 H3B, Histone cluster 1 H3E, Histone cluster 1 H3I, Histone cluster 1 H4, Histone cluster 1 H4G, Histone cluster 1 H4H, Histone cluster 1 H4I, Histone cluster 1 H4L, Histone cluster 2 H2AA1, Histone cluster 2 H2AA3, Histone cluster 2 H2AC, Histone cluster 2 H3A, Histone cluster 2 H3C1, Histone cluster 2 H3C2, Histone cluster 2 H4, Histone H2A, Histone H2A.Bbd, Histone H2A.V, Histone H2BM, Histone H3, Histone H3.3B, Histone Z, HLA-F`, HP1, Integrin αIIIb, JAZF1, KCNMB4, KRTAP1, KRTAP13-3, KRTAP8-2, Lacrein, LIN-35, LIN-53, LOC100039452, LOC100039631, LOC100039763, LOC100040781, LOC145783, LOC150383_2210021J22Rik, LOC390245, LOC439994, LOC665622, LOC729458, Lyl-1, MAGE-A9, MAGE-A9B, MAGE-E1, MAGE-F1, MAGE-G2, mage-k1, Mammaglobin A, MBTD1, Mi2-α, MIER1, MIER3, Morc1, Morc3, MORF, MORF4L2, MRG15, mSin3A9, MTGR1, Mxi 1, NAP1L2, NAP5, NBPF24, NIF-1, NWD1, Obox5, OCIAD1, Olr1125, Olr184, Olr559, OTTMUSG00000016789, OTTMUSG00000016790, OTTMUSG00000016887, OTTMUSG00000018481, OTTMUSG00000018888, p400, P42pop, Paf1, pan-Acetyl, PATE2, PCDH11Y, PCDHB13, PCDHGA5, PCDHGA6, PHF12, PHF2, PHF20, PHF21B, PLAC4, Plectin, PRDM10, PRDM8, PWWP2B, RAI15, RBBP1, RhD, RP2, RP23-480B19.10, Rpd3, SAMD4B, SAP 130, SAP 25_Sap25, SAP 30BP, SCMH1, SCML4, SDS3, SETD5, SFMBT2, Siglec-5, SIM2, Sin3, Sin4p, SMARCD2, SMYD2, SPIN2, SPNS2, SRRM5, STAMP2, STOX2, Sum1, TADA3L, TAF II p68, TAF II p70, TAF9A, TGIF2, TIGD3, TM6SF2, TMEM103, TOX3, TRRAP, TSPY9, TSPYL4, TSSC3, TSSC4, UBN-1, USP49, VpreB3, VSTM2A, WIZ, YEATS2, ZBTB40, ZCWPW1, ZCWPW2, ZFP57, Zfp93, ZMYM6NB, ZNF165, ZNF206, ZNF232, ZNF536, and ZNF649.Activator of:
2900008C10Rik, 4930557A04Rik, ASCL2, ASH2L, BAZ2A, BPTF, Brpf1, BRPF3, BTF3, CDR2, CENP-A, CHD2, CHRAC15, dCtBP, DPF1, EAF1, EID-1, H1T2, H2AL2, H2al2y, H2BFA, HDA5, Histone cluster 1 H1B, Histone cluster 1 H2A, Histone cluster 1 H2AG, Histone cluster 1 H2AH, Histone cluster 1 H2AM, Histone cluster 1 H2AN, Histone cluster 1 H2B, Histone cluster 1 H2BH, Histone cluster 1 H3G, Histone cluster 1 H3J, Histone cluster 2 H2AB, Histone H1B, Histone H1X, Histone H2B.S, INTS4, Khdc1b, KIAA1688, L3MBTL2, L3MBTL3, LANPL, LHFP, MacroH2A1, MBD1, Mi2-α, MORF4L1, MPc3_CBX8, MRGBP, mSin3B, MSL-1, MSL3L1, MTF-2, MYSM1, NSD1, PABPC4, PCGF6, PRAME like-3, PRAME like-6, PRAME like-7, PRDM14, RBA-1, RbAp46, RCOR2, SAP 18, SAP 30L, SCML2, Sec24, Set2, SMARCD2, SPEN, SPT16, SUV420H2, SWI/SNF-B, Swi1, Swi3, TBL1Y, TIGD4, TIGD5, Trimethyl Histone H3, WSTF, ZKSCAN4, ZNF295, ZNF33A, ZNF33B, ZNF345, ZNF408, ZNF498, ZNF553, ZNF579, and ZNF806.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
Mocetinostat, 5 mg | sc-364539 | 5 mg | $214.00 | |||
Mocetinostat, 10 mg | sc-364539B | 10 mg | $247.00 | |||
Mocetinostat, 50 mg | sc-364539A | 50 mg | $1463.00 |