Cat. No.: HY-12164

Mocetinostat

(Synonyms: MGCD0103)

25 Cited Publications

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Mocetinostat (MGCD0103) is a potent, orally active and isotype-selective HDAC (Class I/IV) inhibitor with IC₅₀s of 0.15, 0.29, 1.66 and 0.59 μM for HDAC1, HDAC2, HDAC3 and HDAC11, respectively. Mocetinostat shows no inhibition on HDAC4, HDAC5, HDAC6, HDAC7, or HDAC8.

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Pureté: 99.13%
CAS No.: 726169-73-9
Formule: C₂₃H₂₀N₆O
Masse moléculaire:396.45

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Mocetinostat Chemical Structure

CAS No.: 726169-73-9

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (25)
Solvant et solubilité
- In Vitro
- In Vivo
Protocole
Pureté et documentation
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Classifications
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Activité biologique

Description

IC₅₀ & Target^[1]

HDAC1

0.15 μM (IC₅₀)

HDAC2

0.29 μM (IC₅₀)

HDAC11

0.59 μM (IC₅₀)

HDAC3

1.66 μM (IC₅₀)

Voir tous les produits spécifiques à Isoform HDAC :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	0.9 μM Compound: 8, MGCD0103	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay Antiproliferative activity against human A549 cells after 72 hrs by MTT assay	[PMID: 18570366]
A549	IC₅₀	1.279 μM Compound: MGCD0103	Cytotoxicity against human A549 cells after 72 hrs by MTT assay Cytotoxicity against human A549 cells after 72 hrs by MTT assay	[PMID: 23206867]
A549	IC₅₀	1.73 μM Compound: MGCD0103, Mocetinostat	Cytotoxicity against human A549 cells assessed as growth inhibition by measuring cellular ATP level after 72 hrs by cell-titer glo assay Cytotoxicity against human A549 cells assessed as growth inhibition by measuring cellular ATP level after 72 hrs by cell-titer glo assay	[PMID: 23829483]
A549	IC₅₀	1.65 μM Compound: MGCD0103	Antiproliferative activity against human A549 cells assessed as cell viability after 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as cell viability after 72 hrs by MTT assay	[PMID: 24095018]
A549	IC₅₀	2.08 μM Compound: Mocetinostat	Cytotoxicity against human A549 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human A549 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 25805446]
A549	IC₅₀	1275 nM Compound: 4; MGCD0103	Antiproliferative activity against human A549 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human A549 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36934335]
A549	IC₅₀	11.87 μM Compound: MGCD0103	Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay	10.1039/C5MD00247H
A549	IC₅₀	14.57 μM Compound: MGCD0103	Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 48 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 48 hrs by MTT assay	10.1039/C5MD00247H
A549	IC₅₀	59.9 μM Compound: MGCD0103	Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 24 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 24 hrs by MTT assay	10.1039/C5MD00247H
CAKI-1	IC₅₀	265 nM Compound: 4; MGCD0103	Antiproliferative activity against human CAKI-1 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human CAKI-1 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36934335]
CT26	GI₅₀	1.8 μM Compound: 9; MGCD-0103	Antiproliferative activity against mouse CT26 cells measured after 72 hrs by CCK8 assay Antiproliferative activity against mouse CT26 cells measured after 72 hrs by CCK8 assay	[PMID: 34783558]
CT26	GI₅₀	1.77 μM Compound: 4; MGCD-0103	Antiproliferative activity against mouse CT26 cells after 72 hrs by CCK-8 assay Antiproliferative activity against mouse CT26 cells after 72 hrs by CCK-8 assay	[PMID: 35390714]
DOHH-2	IC₅₀	74 nM Compound: 4; MGCD0103	Antiproliferative activity against human DOHH-2 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human DOHH-2 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36934335]
DU-145	IC₅₀	0.67 μM Compound: 8, MGCD0103	Antiproliferative activity against human Du145 cells after 72 hrs by MTT assay Antiproliferative activity against human Du145 cells after 72 hrs by MTT assay	[PMID: 18570366]
DU-145	IC₅₀	2.06 μM Compound: MGCD0103, Mocetinostat	Cytotoxicity against human DU145 cells assessed as growth inhibition by measuring cellular ATP level after 72 hrs by cell-titer glo assay Cytotoxicity against human DU145 cells assessed as growth inhibition by measuring cellular ATP level after 72 hrs by cell-titer glo assay	[PMID: 23829483]
ES-2	IC₅₀	25 nM Compound: 4; MGCD0103	Antiproliferative activity against human ES2 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human ES2 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36934335]
HCT-116	EC₅₀	<1 μM Compound: 8, MGCD0103	Cell cycle arrest in human HCT116 cells assessed as accumulation at G2/M phase Cell cycle arrest in human HCT116 cells assessed as accumulation at G2/M phase	[PMID: 18570366]
HCT-116	EC₅₀	0.45 μM Compound: 8, MGCD0103	Induction of p21cip/waf1 protein expression in human HCT116 cells relative to MS275 Induction of p21cip/waf1 protein expression in human HCT116 cells relative to MS275	[PMID: 18570366]
HCT-116	IC₅₀	0.29 μM Compound: 8, MGCD0103	Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay	[PMID: 18570366]
HCT-116	EC₅₀	0.6 μM Compound: A, MGCD0103	Induction of p21WAF1/CIP1 expression in human HCT116 cells assessed as tubulin level after 16 hrs by luciferase assay Induction of p21WAF1/CIP1 expression in human HCT116 cells assessed as tubulin level after 16 hrs by luciferase assay	[PMID: 19114304]
HCT-116	IC₅₀	0.3 μM Compound: A, MGCD0103	Antiproliferative activity against human HCT116 cells by MTT assay Antiproliferative activity against human HCT116 cells by MTT assay	[PMID: 19114304]
HCT-116	IC₅₀	310 nM Compound: 5, MGCD0103	Antiproliferative activity against human HCT116 cells assessed as growth inhibition Antiproliferative activity against human HCT116 cells assessed as growth inhibition	[PMID: 21650221]
HCT-116	IC₅₀	0.31 μM Compound: 4, MGCD-0103	Antiproliferative activity against human HCT116 cells Antiproliferative activity against human HCT116 cells	[PMID: 21742496]
HCT-116	IC₅₀	0.327 μM Compound: MGCD0103	Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay	[PMID: 23206867]
HCT-116	IC₅₀	0.7 μM Compound: MGCD0103, Mocetinostat	Cytotoxicity against human HCT116 cells assessed as growth inhibition by measuring cellular ATP level after 72 hrs by cell-titer glo assay Cytotoxicity against human HCT116 cells assessed as growth inhibition by measuring cellular ATP level after 72 hrs by cell-titer glo assay	[PMID: 23829483]
HCT-116	IC₅₀	1.57 μM Compound: MGCD0103	Antiproliferative activity against human HCT116 cells assessed as cell viability after 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells assessed as cell viability after 72 hrs by MTT assay	[PMID: 24095018]
HCT-116	IC₅₀	0.396 μM Compound: Mocetinostat	Cytotoxicity against human HCT116 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human HCT116 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 25805446]
HCT-116	IC₅₀	0.53 μM Compound: 4; MGCD0103	Antiproliferative activity against human HCT-116 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human HCT-116 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36934335]
HCT-116	IC₅₀	1.24 μM Compound: MGCD0103	Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability after 48 hrs by MTT assay Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability after 48 hrs by MTT assay	10.1039/C5MD00247H
HCT-116	IC₅₀	29.69 μM Compound: MGCD0103	Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability after 24 hrs by MTT assay Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability after 24 hrs by MTT assay	10.1039/C5MD00247H
HCT-116	IC₅₀	3.51 μM Compound: MGCD0103	Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by MTT assay	10.1039/C5MD00247H
HEK293	IC₅₀	130 nM Compound: MGCD-0103	Inhibition of HDAC1 in HEK293 cells Inhibition of HDAC1 in HEK293 cells	[PMID: 18308563]
HEK293	IC₅₀	610 nM Compound: MGCD-0103	Inhibition of HDAC3 in HEK293 cells Inhibition of HDAC3 in HEK293 cells	[PMID: 18308563]
HEK293	IC₅₀	1338 nM Compound: 4; MGCD0103	Antiproliferative activity against human HEK293 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human HEK293 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36934335]
HeLa	IC₅₀	660 nM Compound: 4; MGCD0103	Antiproliferative activity against human HeLa cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human HeLa cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36934335]
HeLa	IC₅₀	3.32 μM Compound: MGCD0103	Antiproliferative activity against human HeLa cells assessed as reduction in cell viability after 48 hrs by MTT assay Antiproliferative activity against human HeLa cells assessed as reduction in cell viability after 48 hrs by MTT assay	10.1039/C5MD00247H
HeLa	IC₅₀	3.42 μM Compound: MGCD0103	Antiproliferative activity against human HeLa cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human HeLa cells assessed as reduction in cell viability after 72 hrs by MTT assay	10.1039/C5MD00247H
HeLa	IC₅₀	43.8 μM Compound: MGCD0103	Antiproliferative activity against human HeLa cells assessed as reduction in cell viability after 24 hrs by MTT assay Antiproliferative activity against human HeLa cells assessed as reduction in cell viability after 24 hrs by MTT assay	10.1039/C5MD00247H
Hep 3B2	IC₅₀	0.823 μM Compound: Mocetinostat	Cytotoxicity against human Hep3B cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human Hep3B cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 25805446]
HepG2	IC₅₀	0.876 μM Compound: Mocetinostat	Cytotoxicity against human HepG2 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human HepG2 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 25805446]
HepG2	IC₅₀	4.05 μM Compound: MGCD0103	Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability after 48 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability after 48 hrs by MTT assay	10.1039/C5MD00247H
HepG2	IC₅₀	4.25 μM Compound: MGCD0103	Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay	10.1039/C5MD00247H
HepG2	IC₅₀	5.79 μM Compound: MGCD0103	Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability after 24 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability after 24 hrs by MTT assay	10.1039/C5MD00247H
HL-60	IC₅₀	0.418 μM Compound: MGCD0103	Antiproliferative activity against human HL-60 cells incubated for 48 hrs Antiproliferative activity against human HL-60 cells incubated for 48 hrs	[PMID: 36549114]
HMEC	IC₅₀	20 μM Compound: 8, MGCD0103	Antiproliferative activity against HMEC after 72 hrs by MTT assay Antiproliferative activity against HMEC after 72 hrs by MTT assay	[PMID: 18570366]
HMEC	IC₅₀	21 μM Compound: A, MGCD0103	Antiproliferative activity against HMEC by MTT assay Antiproliferative activity against HMEC by MTT assay	[PMID: 19114304]
Jurkat	IC₅₀	150 nM Compound: 4; MGCD0103	Antiproliferative activity against human Jurkat cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human Jurkat cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36934335]
K562	IC₅₀	322 nM Compound: 4; MGCD0103	Antiproliferative activity against human K562 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human K562 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36934335]
KARPAS-299	IC₅₀	4.15 μM Compound: MGCD0103	Antiproliferative activity against human KARPAS-299 cells incubated for 48 hrs Antiproliferative activity against human KARPAS-299 cells incubated for 48 hrs	[PMID: 36549114]
Kasumi 1	IC₅₀	0.151 μM Compound: MGCD0103	Antiproliferative activity against human Kasumi 1 cells incubated for 48 hrs Antiproliferative activity against human Kasumi 1 cells incubated for 48 hrs	[PMID: 36549114]
MC-38	GI₅₀	21 μM Compound: 9; MGCD-0103	Antiproliferative activity against mouse MC38 cells measured after 72 hrs by CCK8 assay Antiproliferative activity against mouse MC38 cells measured after 72 hrs by CCK8 assay	[PMID: 34783558]
MC-38	GI₅₀	1.64 μM Compound: 4; MGCD-0103	Antiproliferative activity against mouse MC38 cells after 72 hrs by CCK-8 assay Antiproliferative activity against mouse MC38 cells after 72 hrs by CCK-8 assay	[PMID: 35390714]
MC-38	IC₅₀	1.84 μM Compound: 4; MGCD0103	Antiproliferative activity against mouse MC38 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against mouse MC38 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36934335]
MCF7	IC₅₀	4.807 μM Compound: MGCD0103	Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 23206867]
MCF7	IC₅₀	1.26 μM Compound: MGCD0103, Mocetinostat	Cytotoxicity against human MCF7 cells assessed as growth inhibition by measuring cellular ATP level after 72 hrs by cell-titer glo assay Cytotoxicity against human MCF7 cells assessed as growth inhibition by measuring cellular ATP level after 72 hrs by cell-titer glo assay	[PMID: 23829483]
MCF7	IC₅₀	2.49 μM Compound: MGCD0103	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay	10.1039/C5MD00247H
MCF7	IC₅₀	56.81 μM Compound: MGCD0103	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by MTT assay	10.1039/C5MD00247H
MCF7	IC₅₀	84.17 μM Compound: MGCD0103	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 24 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 24 hrs by MTT assay	10.1039/C5MD00247H
MDA-MB-231	IC₅₀	309 nM Compound: 4; MGCD0103	Antiproliferative activity against human MDA-MB-231 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human MDA-MB-231 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36934335]
MHCC97H	IC₅₀	4.563 μM Compound: Mocetinostat	Cytotoxicity against human MHCC97H cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human MHCC97H cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 25805446]
MIA PaCa-2	IC₅₀	303 nM Compound: 4; MGCD0103	Antiproliferative activity against human MIA PaCa-2 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human MIA PaCa-2 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36934335]
MKN-45	IC₅₀	0.61 μM Compound: Mocetinostat	Cytotoxicity against human MKN45 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human MKN45 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 25805446]
MV4-11	IC₅₀	0.19 μM Compound: MGCD0103	Antiproliferative activity against human MV4-11 cells incubated for 48 hrs Antiproliferative activity against human MV4-11 cells incubated for 48 hrs	[PMID: 36549114]
NB-4	IC₅₀	0.406 μM Compound: MGCD0103	Antiproliferative activity against human NB4 cells incubated for 48 hrs Antiproliferative activity against human NB4 cells incubated for 48 hrs	[PMID: 36549114]
NCI-H1299	IC₅₀	1440 nM Compound: 5, MGCD0103	Antiproliferative activity against human H1299 cells Antiproliferative activity against human H1299 cells	[PMID: 21650221]
NCI-N87	IC₅₀	606 nM Compound: 4; MGCD0103	Antiproliferative activity against human NCI-N87 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human NCI-N87 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36934335]
OCI-AML2	IC₅₀	1.56 μM Compound: MGCD0103	Antiproliferative activity against human OCI-AML2 cells incubated for 48 hrs Antiproliferative activity against human OCI-AML2 cells incubated for 48 hrs	[PMID: 36549114]
OCI-AML-3	IC₅₀	1.79 μM Compound: MGCD0103	Antiproliferative activity against human OCI-AML-3 cells incubated for 48 hrs Antiproliferative activity against human OCI-AML-3 cells incubated for 48 hrs	[PMID: 36549114]
PANC-1	IC₅₀	26.774 μM Compound: Mocetinostat	Cytotoxicity against human PANC1 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human PANC1 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 25805446]
PC-3	IC₅₀	1393 nM Compound: 4; MGCD0103	Antiproliferative activity against human PC-3 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human PC-3 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36934335]
PC-9	IC₅₀	345 nM Compound: 4; MGCD0103	Antiproliferative activity against human PC-9 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human PC-9 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36934335]
Sf9	IC₅₀	102 nM Compound: MGCD0103	Inhibition of human recombinant HDAC1 expressed in Sf9 cells incubated for 2 hrs using RHKK-Ac fluorogenic substrate Inhibition of human recombinant HDAC1 expressed in Sf9 cells incubated for 2 hrs using RHKK-Ac fluorogenic substrate	[PMID: 23009203]
Sf9	IC₅₀	>10000 nM Compound: MGCD0103	Inhibition of human recombinant HDAC6 expressed in Sf9 cells incubated for 2 hrs using RHKK-Ac fluorogenic substrate Inhibition of human recombinant HDAC6 expressed in Sf9 cells incubated for 2 hrs using RHKK-Ac fluorogenic substrate	[PMID: 23009203]
SJSA-1	IC₅₀	3.624 μM Compound: Mocetinostat	Cytotoxicity against human SJSA1 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human SJSA1 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 25805446]
SNU-16	IC₅₀	0.142 μM Compound: Mocetinostat	Cytotoxicity against human SNU16 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human SNU16 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 25805446]
SNU-5	IC₅₀	1.009 μM Compound: Mocetinostat	Cytotoxicity against human SNU5 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human SNU5 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 25805446]
SW-620	IC₅₀	0.419 μM Compound: Mocetinostat	Cytotoxicity against human SW620 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human SW620 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 25805446]
T-24	EC₅₀	1.38 μM Compound: 8, MGCD0103	Induction of H3 histone acetylation in human T24 cells relative to MS275 Induction of H3 histone acetylation in human T24 cells relative to MS275	[PMID: 18570366]
T-24	EC₅₀	<1 μM Compound: A, MGCD0103	Induction of histone H4 hyperacetylation in human T24 cells after 16 hrs by immunoblotting Induction of histone H4 hyperacetylation in human T24 cells after 16 hrs by immunoblotting	[PMID: 19114304]
U-937	IC₅₀	1.37 μM Compound: MGCD0103	Antiproliferative activity against human U-937 cells incubated for 48 hrs Antiproliferative activity against human U-937 cells incubated for 48 hrs	[PMID: 36549114]
ZR-75-1	IC₅₀	1132 nM Compound: 4; MGCD0103	Antiproliferative activity against human ZR-75-1 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human ZR-75-1 cells assessed as reduction of cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36934335]

In Vitro

Mocetinostat is a potent, orally active and isotype-selective HDAC (Class I/IV) inhibitor with IC₅₀s of 0.15, 0.29, 1.66 and 0.59 μM for HDAC1, HDAC2, HDAC3 and HDAC11, respectively. Mocetinostat shows no inhibition on HDAC4, HDAC5, HDAC6, HDAC7, or HDAC8. Mocetinostat (MGCD0103) exhibits potent and selective antiproliferative activities against a broad spectrum of human cancer cell lines in vitro, and HDAC inhibitory activity is required for these effects. In all cell lines tested, Mocetinostat (MGCD0103) partially inhibits cellular HDAC enzyme activity although the maximal inhibition of activity varies among cell lines from 75% to 85% of total activity. The IC₅₀ of Mocetinostat in intact cancer cells is independent of tissue origin. In A549 cells, MGCD0103 shows dose-dependent inhibition of HDAC activity in whole cells. At high concentrations in A549 cells, Mocetinostat inhibits a maximum of 80% of total activity. In HCT116 cells, Mocetinostat induces a significant S-phase depletion and both G₁ and G₂-M accumulation^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Mocetinostat (MGCD0103) significantly inhibits growth of human tumor xenografts in nude mice in a dose-dependent manner and the antitumor activity correlated with induction of histone acetylation in tumors. The p.o. administration of Mocetinostat (MGCD0103) (2HBr salt) significantly reduces growth of implanted advanced A549 tumors in nude mice in a dose-dependent manner after 13 days of daily administration. Mocetinostat (170 mg/kg for 2HBr salt, corresponding to 120 mg/kg of free base) significantly blocks growth of tumors compared with vehicle treatment alone (P<0.05 in post-ANOVA Dunnett's test) with no change in body weight^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 726169-73-9
Appearance Solid
Masse moléculaire 396.45
Formule C₂₃H₂₀N₆O
Color White to off-white
SMILES

O=C(C1=CC=C(C=C1)CNC2=NC=CC(C3=CC=CN=C3)=N2)NC4=CC=CC=C4N
Synonyms

MGCD0103
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (25)

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Journal Impact Factor

Exp Hematol Oncol

IHCH9033, a novel class I HDAC inhibitor, synergizes with FLT3 inhibitor and rescues quizartinib resistance in FLT3-ITD AML via enhancing DNA damage response. [Abstract]

2025 Feb 15;14(1):15. PMID: 39955584

Mocetinostat purchased from MedChemExpress. Usage Cited in: Exp Hematol Oncol. 2025 Feb 15;14(1):15. [Abstract]

The cytotoxicity of class I HDAC inhibitors (IHCH9033, MGCD0103 and Tucidinostat) in AML cell lines for 72 h were tested by MTT assay.

Mocetinostat purchased from MedChemExpress. Usage Cited in: Exp Hematol Oncol. 2025 Feb 15;14(1):15. [Abstract]

Dose-dependent effects of Mocetinostat (MGCD0103) on FLT3 signaling pathway protein expression in MV-4-11 and MOLM13 cell lines.

Mocetinostat purchased from MedChemExpress. Usage Cited in: Exp Hematol Oncol. 2025 Feb 15;14(1):15. [Abstract]

Mocetinostat (MGCD0103). The mRNA level of FLT3 in MV-4-11 and MOLM13 cells was detected by RT-qPCR.

Mocetinostat purchased from MedChemExpress. Usage Cited in: Exp Hematol Oncol. 2025 Feb 15;14(1):15. [Abstract]

In BALB/c nude mice, established MV-4-11 tumors were treated with a vector, IHCH9033, Mocetinostat (MGCD0103; 60, 120 mg/kg), or tucidinostat. Tumor volume was monitored.
J Adv Res

Targeting class I HDACs suppresses oncogenic vulnerabilities and potentiates KRAS/MAPK pathway inhibitors in KRAS-mutant cancers. [Abstract]

2026 Feb 13:S2090-1232(26)00144-X. PMID: 41692243
J Exp Clin Cancer Res

SENP1 drives glycolysis and cisplatin resistance in gastric cancer via desumoylating ENO1. [Abstract]

2025 Oct 8;44(1):285. PMID: 41063235
Cell Discov

Single-cell profiling reveals molecular basis of malignant phenotypes and tumor microenvironments in small bowel adenocarcinomas. [Abstract]

2022 Sep 14;8(1):92. PMID: 36104333

Mocetinostat purchased from MedChemExpress. Usage Cited in: Cell Discov. 2022 Sep 14;8(1):92. [Abstract]

Cell survival curve for HUTU-80 cells treated with the indicated inhibitors with a dose escalation from 0 to 100 μM.
Clin Cancer Res

Gene Expression Signatures Identify Novel Therapeutics for Metastatic Pancreatic Neuroendocrine Tumors. [Abstract]

2020 Apr 15;26(8):2011-2021. PMID: 31937620
Proc Natl Acad Sci U S A

MGMT-activated DUB3 stabilizes MCL1 and drives chemoresistance in ovarian cancer. [Abstract]

2019 Feb 19;116(8):2961-2966. PMID: 30718431
EMBO J

Acetylation of TIR domains in the TLR4-Mal-MyD88 complex regulates immune responses in sepsis. [Abstract]

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Oncogene

CUL4B functions as a tumor suppressor in KRAS-driven lung tumors by inhibiting the recruitment of myeloid-derived suppressor cells. [Abstract]

2023 Oct;42(42):3113-3126. PMID: 37653114
Virulence

The inhibitory and anti-inflammatory effects of TMP269 on peste des petits ruminants virus replication. [Abstract]

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2020 Jun;56(6):1429-1441. PMID: 32236593
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bioRxiv

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Patent

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Solvant et solubilité

In Vitro:

DMSO : 50 mg/mL (126.12 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.5224 mL

12.6118 mL

25.2236 mL

5 mM

0.5045 mL

2.5224 mL

5.0447 mL

10 mM

0.2522 mL

1.2612 mL

2.5224 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (5.25 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (5.25 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocole

Cell Assay^[1]

Cells in 96-well plates are incubated with Mocetinostat at various concentrations for 72 h at 37°C in 5% CO₂. MTT is added at a final concentration of 0.5 mg/mL and incubated with the cells for 4 h before an equal volume of solubilization buffer [50% N,N-dimethylformamide, 20% SDS (pH 4.7)] is added. After overnight incubation, solubilized dye is quantified by reading at 570 nm using a reference at 630 nm. Absorbance values are converted to cell numbers according to a standard growth curve of the relevant cell line. The concentration which reduces cell numbers to 50% relative to DMSO-treated cells is determined as MTT IC₅₀^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[1]^[2]

Mice^[1]
Female CD-1 nude mice, ages 8 to 10 wk are used. Tumor fragments (30 mg), which have been serially passaged thrice in vivo in minimal, are implanted s.c. through a small surgical incision on the flank of the mice while under general anesthesia. Mocetinostat is dissolved in vehicle (PBS acidified with 0.1 N HCl or PEG400/0.2 N HCl saline, 40:60) and dosed p.o. as solutions daily. Tumor volumes and body weight are monitored thrice weekly for at least 2 wk. Each experimental group containe six to eight animals. For pharmacokinetic study, blood is collected from animals at various time points, and plasma samples are analyzed.
Rats^[2]
Forty rats (220±20 g) are randomly divided into four different dosages of Mocetinostat groups (Low group, Medium group, High group, and control group with 10 rats in each group). Mocetinostat is dissolved in corn oil as suspension at three different concentrations (20, 40, and 80 mg/mL). Three different Mocetinostat groups (Low group, Medium group, and High group) are respectively given Mocetinostat 20, 40, and 80 mg/kg one time by intragastric administration at every morning and last for 7 days. Control group are given saline by same administration method. At 8 days morning, six probe drugs, Bupropion, Phenacetin, Tolbutamide, Metoprolol, Testosterone, and Omeprazole, are mixed in corn oil and given to the rats of three Mocetinostat groups and control group by intragastric administration at a single dosage of 10 mg/kg for Bupropion, Phenacetin, Metoprolol, Testosterone, and Omeprazole and 1 mg/kg for Tolbutamide.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (278 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[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 Apr;7(4):759-68. [Content Brief]

[2]. Cai J, et al. The Effect of MGCD0103 on CYP450 Isoforms Activity of Rats by Cocktail Method. Biomed Res Int. 2015;2015:517295. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.5224 mL	12.6118 mL	25.2236 mL	63.0590 mL
	5 mM	0.5045 mL	2.5224 mL	5.0447 mL	12.6118 mL
	10 mM	0.2522 mL	1.2612 mL	2.5224 mL	6.3059 mL
	15 mM	0.1682 mL	0.8408 mL	1.6816 mL	4.2039 mL
	20 mM	0.1261 mL	0.6306 mL	1.2612 mL	3.1530 mL
	25 mM	0.1009 mL	0.5045 mL	1.0089 mL	2.5224 mL
	30 mM	0.0841 mL	0.4204 mL	0.8408 mL	2.1020 mL
	40 mM	0.0631 mL	0.3153 mL	0.6306 mL	1.5765 mL
	50 mM	0.0504 mL	0.2522 mL	0.5045 mL	1.2612 mL
	60 mM	0.0420 mL	0.2102 mL	0.4204 mL	1.0510 mL
	80 mM	0.0315 mL	0.1576 mL	0.3153 mL	0.7882 mL
	100 mM	0.0252 mL	0.1261 mL	0.2522 mL	0.6306 mL

Keywords

Mocetinostat

25 Cited Publications

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Mocetinostat

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Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) Mocetinostat

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Activité biologique

Chemical Information

Publications (25)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Mocetinostat Related Classifications

HY-12164 Related Classifications