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Cat. No. Name Size Price Add Cart
KI0256MGCD01035 mg$272
MGCD010310 mg$432
MGCD010325 mg$752
MGCD010350 mg$1232

Chemical Characteristic

Product NameMGCD0103
SynonymsMocetinostat
CAS No.726169-73-9
Molecular Weight 396.44
FormulaC23H20N6O
Chemical NameN-(2-Aminophenyl)-4-([[4-(pyridin-3-yl)pyrimidin-2-yl]amino]methyl)benzamide
SmilesC(=O)(c1ccc(cc1)CNc1nc(ccn1)c1cnccc1)Nc1c(cccc1)N
Chemical Structure

Biological activities

MGCD0103 is an isotype-selective inhibitor of histone deacetylases (HDACs) targeted to isoforms 1, 2, 3, and 11. MGCD0103 exhibits a dose-dependent antiproliferative activity against a broad spectrum of human cancer cell lines from a variety of tissue origins, including solid tumor and hematologic malignancies. [1] At the molecular level, MGCD0103 acetylates histone 3 and upregulates the cell cycle regulatory protein p21, which is at much lower concentrations compared with vorinostat. Furthermore, MGCD0103 downregulates XIAP, activates caspases 9 and 3, and induces apoptosis. [2] In vitro, MGCD0103 exhibits most potent inhibitory activity against human HDAC1, HDAC2 HDAC3, and HDAC11 enzymes with IC50s of 0.15, 0.29, 1.66 and 0.59 µM, respectively. In intact cells, MGCD0103 inhibits only a fraction of the total HDAC activity and shows long-lasting inhibitory activity even upon drug removal. In all cell lines tested, MGCD0103 partially inhibits cellular HDAC enzyme activity although the maximal inhibition of activity varied among cell lines from 75% to 85% of total activity. MGCD0103 also induces p21 expression at the protein level in a dose-dependent manner in A549 cells??53-null T24 cells and U937 lymphoma cell lines. [1] At 7 hours of pretreatment, 5 µM MGCD0103 (~10 times the IC50) could inhibit HDAC activity without down-regulating HDAC7. MGCD0103 inhibits HCT116, Jurkat, T24 and MCF-7 with IC50 values of 0.45, 0.11, 0.22 and 0.21 µM, respectively. [3] MGCD0103 induces a delay increase in p21Waf1 and fails to induce G1-phase arrest. MGCD0103 also induces mitotic defects and mitotic slippage. [4] In vivo, p.o. administration of MGCD0103 significantly reduces growth of implanted advanced A549 tumors in nude mice in a dose dependent manner after 13 days of daily administration. MGCD0103 at 80 mg/kg almost completely blocks the growth of H1437 tumors after 13 days of daily p.o. administration with no reduction of body weight in animals. [1] MGCD0103 induces significant inhibition of HDAC activity in a dose-dependent manner in human peripheral WBC treated ex vivo for 18 hours, and the calculated IC50 of MGCD0103 is 0.35 µM. MGCD0103 also induces histone H3 hyperacetylation in SW48 tumors as early as 4 hours following acute administration of MGCD0103 free base (90 mg/kg). [3]

Protocols

MGCD0103 are dissolved in DMSO as 10 mM stock solutions. [1]

References

[1] Fournel M, et al. MGCD0103, a novel isotype-selective histone deacetylase inhibitor, has broad spectrum antitumor activity in vitro and in vivo. Mol Cancer Ther. 2008, 7(4): 759-768.
[2] Buglio D, et al. The class-I HDAC inhibitor MGCD0103 induces apoptosis in Hodgkin lymphoma cell lines and synergizes with proteasome inhibitors by an HDAC6-independent mechanism. Br J Haematol. 2010, 151(4): 387-396.
[3] Bonfils C, et al. Evaluation of the pharmacodynamic effects of MGCD0103 from preclinical models to human using a novel HDAC enzyme assay. Clin Cancer Res. 2008, 14(11): 3441-3449.
[4] Chia K, et al. The histone deacetylase inhibitor MGCD0103 has both deacetylase and microtubule inhibitory activity. Mol Pharmacol. 2010, 78(3): 436-443.

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