MMH409
MMH409 is a selective HDAC8 inhibitor, with an IC50 value of 23 nM and a Kd value of 3.5 nM against human HDAC8, and an IC50 value of 11.64 μM against Schistosoma mansoni HDAC8. MMH409 reduces the viability of newly transformed schistosomula and adult worms of Schistosoma mansoni in vitro. MMH409 serves as a biological probe to investigate the pharmacological knockdown effect of HDAC8 in diseased cells. MMH409 can be used in studies related to neuroblastoma and schistosomiasis.
For research use only. We do not sell to patients.
- CAS No.: 2704554-86-7
- Formula: C19H16F6N2O3
- Molecular Weight:434.33
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Parasite Isoforms
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Biological Activity
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hHDAC8 23 nM (IC50) |
hHDAC8 3.5 nM (Kd) |
HDAC8 11.64 μM (IC50) |
MMH409 inhibits purified HDAC8 protein with an IC50 of 23.4 nmol/L, adopting a predominantly cis conformation in solution that favors stable binding to the enzyme[1].
MMH409 (0.000244-1 μM; 10 μM) potently inhibits human HDAC8 with an IC50 of 23.4 nM and exhibits 410-fold selectivity for HDAC8 over other human HDAC isoforms in an enzymatic EMSA[2].
MMH409 inhibits human HDAC8 with an IC50 of 0.11 μM in a competition-based FP assay[2].
MMH409 binds full-length human HDAC8 with high affinity, exhibiting a KD of 3.5 nM in an SPR assay[2].
MMH409 has high predicted cellular permeability (-log Pe = 5.42) and a human plasma half-life of 93 minutes[2].
MMH409 (1-10 μM; 90-120 min) potently inhibits purified hHDAC8 protein with an IC50 of 28 nM[3].
MMH409 (1-10 μM; 90-120 min) weakly inhibits purified SmHDAC8 protein with an IC50 of 11.64 μM, showing a 415.7-fold loss in potency relative to hHDAC8[3].
MMH409 (50 μM (PAMPA), 1 μM (plasma stability); 16 h (PAMPA), 0-60 min (plasma stability)) has good cell permeability (-log Pe < 6) and human plasma stability (T1/2 > 1.5 h)[3].
MMH409 does not exhibit a measurable IC50 for inhibition of colony formation in human neuroblastoma BE(2)-C cells in a colony assay[2].
MMH409 (10 μM; 72 h) reduces viability of S. mansoni NTS by 18.75%[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2704554-86-7
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Molecular Weight 434.33
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Formula C19H16F6N2O3
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SMILES
O=C(C1=CC=C(N(C(C)C)C(C2=CC(C(F)(F)F)=CC(C(F)(F)F)=C2)=O)C=C1)NO
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Abdallah DI, et al. Medicinal chemistry advances in targeting class I histone deacetylases. Explor Target Antitumor Ther. 2023;4(4):757-779. [Content Brief]
[2]. Hassan MM, et al. Characterization of Conformationally Constrained Benzanilide Scaffolds for Potent and Selective HDAC8 Targeting. Journal of medicinal chemistry. 2020 Aug 13;63(15):8634-8648. [Content Brief]
[3]. Hassan MM, et al. Phenotypic Screening of Histone Deacetylase (HDAC) Inhibitors against Schistosoma mansoni. ChemMedChem. 2022 Sep 16;17(18):e202100622. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)