Product description
MGCD0103 CAS 726169-73-9 is a potent HDAC inhibitor with the strongest inhibitory activity against HDAC1, exhibiting an IC50 of 0.15 μM in cell-free assays. It is 2 to 10 times more selective than HDAC2, 3, and 11, but has no inhibitory activity against HDAC4, 5, 6, 7, and 8. Mocetinostat (MGCD0103) induces apoptosis and autophagy.
In vivo studies: In nude mice, MGCD0103 significantly inhibited the growth of human xenografts and suppressed histone acetylation-induced anticancer activity in tumors.
In vitro studies: MGCD0103, at nanomolar or low micromolar concentrations, inhibited only a subset of nine recombinant human HDACs, including HDAC1, HDAC2, HDAC3, and HDAC11, in a dose-dependent manner. In vitro, MGCD0103 effectively inhibited human HDAC1 and HDAC2 enzymes but did not inhibit secondary HDACs. The exoamino group of MGCD0103 is essential for enzyme inhibition because the HDAC inhibitory activity against HDAC1 and HDAC2 has been completely eliminated by desamino analogs. MGCD0103 exhibited peak inhibitory activity at 6 μM, inhibiting up to 75% of total enzyme activity in HCT116 cells, while nearly 100% inhibition was achieved in NVP-LAQ824. MGCD0103 also showed dose-dependent inhibition of A549 cells.
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COA
| Tests | Specifications | Results |
| Appearance | White Powder | Complies |
| Identification | Retention time matches reference standard | Complies |
| Assay(HPLC) | 98.0%-102.0% | 99.69% |
| Water Content(Karl | ≤0.5% | 0.26% |
| Residue on Ignition | ≤0.1% | <0.05% |
| Heavy Metals(as Pb) | ≤20 ppm | <10 ppm |
| Sulfated Ash | ≤0.1% | <0.05% |
| Microbial Limits | Total Plate Count<1000cfu/g | <100cfug |
| Yeast &Moulds<100cfu/g | <10cfuv/g | |
| EColiNegative | Negative | |
| Salmonella Negative | Negative | |
| Conclusion | Conform with enterprise specification | |
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Density 1.3±0.1 g/cm3
Molecular Formula C23H20N6O
Molecular Weight 396.444
Exact Mass 396.169861
PSA 105.82000
LogP 1.88
InChIKey HRNLUBSXIHFDHP-UHFFFAOYSA-N
SMILES Nc1ccccc1NC(=O)c1ccc(CNc2nccc(-c3cccnc3)n2)cc1
Mechanism of Action (Target) of MGCD0103 CAS 726169-73-9
It belongs to the class I/IV HDAC selective inhibitors, exhibiting potent inhibition against the following subtypes:
HDAC1: IC₅₀ = 0.15 μM (strongest)
HDAC2: IC₅₀ = 0.29 μM
HDAC3: IC₅₀ = 1.66 μM
HDAC11: IC₅₀ = 0.59 μM
It has almost no inhibitory activity against class II HDACs (4/5/6/7/8). By inhibiting HDACs, it enhances histone acetylation, regulates tumor suppressor gene expression, and induces tumor cell cycle arrest, apoptosis, and autophagy.
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3-7 days |
DHL,Germany DHL,Germany DPD, |
Suitable for under 50kg. |
We have warehouses in Germany and California, USA, and customers in Europe and America can enjoy sending goods directly from these two places. |
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7-15 days |
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Suitable for more than 50kg. |
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15-60 days |
By Sea |
Suitable for more than 500kg. |
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FAQ
01. What are the main indications for MGCD0103 CAS 726169-73-9?
Mainly studied: Hodgkin's lymphoma, follicular lymphoma, AML, CLL, and also solid tumors such as liver cancer and breast cancer.
02. What are the main characteristics of MGCD0103 CAS 726169-73-9?
High selectivity, low off-target toxicity, and relatively low platelet toxicity.
03. Where can I buy MGCD0103 CAS 726169-73-9?
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