A dipeptide pan-caspase inhibitor
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MX1013

Item No. 27904

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5-fluoro-3-[[(2S)-3-methyl-1-oxo-2-[[(phenylmethoxy)carbonyl]amino]butyl]amino]-4-oxo-pentanoic acid
CAS Number
582316-00-5
Synonyms
  • Z-Val-Asp-Fluoromethyl Ketone
  • Z-VD-FMK
Molecular Formula
C18H23FN2O6
Formula Weight
382.4
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:4): 0.2 mg/mlEthanol: 10 mg/ml
SMILES
O=C(O)CC(NC([C@@H](NC(OCC1=CC=CC=C1)=O)C(C)C)=O)C(CF)=O
InChi Code
InChI=1S/C18H23FN2O6/c1-11(2)16(17(25)20-13(8-15(23)24)14(22)9-19)21-18(26)27-10-12-6-4-3-5-7-12/h3-7,11,13,16H,8-10H2,1-2H3,(H,20,25)(H,21,26)(H,23,24)/t13?,16-/m0/s1
InChi Key
LYBWGROBJJXCJJ-VYIIXAMBSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $75

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    10 mg

    $134

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    25 mg

    $295

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    Product Description

    MX1013 is a dipeptide pan-caspase inhibitor that inhibits caspase-1 (IC50 = 20 nM), caspase-3 (IC50 = 30 nM), and caspase-6, -7, -8, and -9 (IC50s = 5-18 nM).1 It is selective for caspases over calpain I, cathepsin B, cathepsin D, renin, thrombin, and Factor Xa (IC50s = >10 μM). MX1013 (0.05 μM) inhibits anti-Fas antibody-induced caspase-3 processing and poly(ADP)ribose polymerase (PARP) cleavage in Jurkat cells, indicating inhibition of apoptosis. It increases survival in a mouse model of anti-Fas antibody-induced liver failure when administered at doses of greater than or equal to 0.25 mg/kg. MX1013 reduces infarct size in rat models of acute myocardial infarction-reperfusion or transient focal brain ischemia-reperfusion injury when administered intravenously as a 20 mg/kg bolus dose followed by a 5 mg/kg per hour infusion.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Yang, W., Guastella, J., Huang, J.-C., et al. MX1013, a dipeptide caspase inhibitor with potent in vivo antiapoptotic activity. Br. J. Pharmacol. 140(2), 402-412 (2003).