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MC1742 

Cat. No. M28849
MC1742  Structure
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Biological Activity

MC1742 is a potent HDAC inhibitor, with IC50s of 0.1 μM, 0.11 μM, 0.02 μM, 0.007 μM, 0.61 μM, 0.04 μM and 0.1 μM for HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, HDAC10 and HDAC11, respectively. MC1742 can increase acetyl-H3 and acetyl-tubulin levels and inhibits cancer stem cells growth. MC1742 can induce growth arrest, apoptosis, and differentiation in sarcoma CSC.

Chemical Information
Molecular Weight 395.47
Formula C21H21N3O3S
CAS Number 1776116-74-5
Form Solid
Solubility (25°C) DMSO 200 mg/mL (ultrasonic)
Storage 4°C, protect from light, dry, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Thomas Mouveaux, et al. Int J Antimicrob Agents. A potent HDAC inhibitor blocks Toxoplasma gondii tachyzoite growth and profoundly disrupts parasite gene expression

[2] Elleard Fw Heffern, et al. J Virus Erad. Identification of isoform-selective hydroxamic acid derivatives that potently reactivate HIV from latency

[3] Gemma Di Pompo, et al. J Med Chem. Novel histone deacetylase inhibitors induce growth arrest, apoptosis, and differentiation in sarcoma cancer stem cells

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  Catalog
Abmole Inhibitor Catalog




Keywords: MC1742  supplier, HDAC, inhibitors, activators


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