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MDL-800

Cat. No. M11538
MDL-800 Structure
Synonym:

MDL800

Size Price Availability Quantity
5mg USD 140  USD140 In stock
10mg USD 200  USD200 In stock
25mg USD 320  USD320 In stock
50mg USD 520  USD520 In stock
100mg USD 780  USD780 In stock
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Quality Control & Documentation
Biological Activity

Mdl-800 is a selective allosteric activator of SIRT6, a member of the SIRT deacetylase family responsible for deacetylation of histone H3K9Ac and H3K56ac, with tumor suppressive activity. Mdl-800 increased SIRT6 deacetylase activity by up to 22 times, leading to cell cycle arrest and inhibiting its proliferation. It also inhibited the growth of hepatocellular carcinoma line BEL7405 xenograft.

Chemical Information
Molecular Weight 626.3
Formula C21H16BrCl2FN2O6S2
CAS Number 2275619-53-7
Solubility (25°C) N/A
Storage 2-8°C
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] Xiaoqi Jiang, et al. Oxid Med Cell Longev. MDL-800, the SIRT6 Activator, Suppresses Inflammation via the NF- κ B Pathway and Promotes Angiogenesis to Accelerate Cutaneous Wound Healing in Mice

[2] Yu Chen, et al. Aging Cell. The SIRT6 activator MDL-800 improves genomic stability and pluripotency of old murine-derived iPS cells

[3] Jia-Lin Shang, et al. Acta Pharmacol Sin. MDL-800, an allosteric activator of SIRT6, suppresses proliferation and enhances EGFR-TKIs therapy in non-small cell lung cancer

[4] Jinhang Zhang, et al. Hepatology. Sirt6 Alleviated Liver Fibrosis by Deacetylating Conserved Lysine 54 on Smad2 in Hepatic Stellate Cells

[5] Zhimin Huang, et al. Nat Chem Biol. Identification of a cellularly active SIRT6 allosteric activator

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