1. Cell Cycle/DNA Damage
    Cytoskeleton
  2. Microtubule/Tubulin
  3. S-methyl DM1

S-methyl DM1 

Cat. No.: HY-100504
Handling Instructions

S-methyl DM1 is a thiomethyl derivative of Maytansine. S-methyl DM1 binds to tubulin with a Kd of 0.93 μM and inhibts microtubule polymerization. S-methyl DM1 potently suppresses microtubule dynamic instability and has anticancer effects.

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S-methyl DM1 Chemical Structure

S-methyl DM1 Chemical Structure

CAS No. : 912569-84-7

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Description

S-methyl DM1 is a thiomethyl derivative of Maytansine. S-methyl DM1 binds to tubulin with a Kd of 0.93 μM and inhibts microtubule polymerization. S-methyl DM1 potently suppresses microtubule dynamic instability and has anticancer effects[1][2].

IC50 & Target

Kd: 0.93 μM (Tubulin)[1]

In Vitro

S-methyl DM1 is the primary cellular or liver metabolite of antibody-maytansinoid conjugates prepared with thiol-containing maytansinoids DM1[1].
The half-maximal concentration for inhibition of microtubule assembly for for S-methyl DM1 is 4 μM. At 100 nM S-methyl-DM1 (84%) suppresses dynamic instability more strongly than Maytansine (45%). Tritiated S-methyl-DM1 bound to 37 high-affinity sites per microtubule (Kd of 0.1 μM)[1].
The concentration dependence curves for the inhibition of cell proliferation by S-methyl DM1 is sigmoidal in shape in MCF7 cells. Minimal inhibition occurred at 200 pM S-methyl DM1, and inhibition is maximal at 3 nM. S-methyl DM1 (IC50 of 330 pM) is slightly more potent than Maytansine (IC50 of 710 pM)[2].
S-methyl DM1 induces maxima of 80% accumulation of cells in G2/M as compared with only 30% in controls in MCF7 cells[2].

Molecular Weight

752.31

Formula

C₃₆H₅₀ClN₃O₁₀S

CAS No.

912569-84-7

SMILES

C[[email protected]]1([[email protected]@](CC(N(C2=CC3=CC(OC)=C2Cl)C)=O)([H])OC([[email protected]](C)N(C)C(CCSC)=O)=O)[[email protected]]([[email protected]@H]([[email protected]](OC4=O)([H])C[[email protected]]([[email protected]](/C=C/C=C(C)/C3)([H])OC)(N4)O)C)O1

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Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

S-methyl DM1Microtubule/TubulinMaytansinethiomethylmetabolitemicrotubulepoisonsmaytansinoidsdynamicinstabilityanticancerInhibitorinhibitorinhibit

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S-methyl DM1
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HY-100504
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