An inhibitor of SUMO-activating enzyme
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COH000

Item No. 34906

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(1R,4S)-1-[(1R)-2-(4-methylphenyl)-1-(phenylamino)ethyl]-7-oxabicyclo[2.2.1]hepta-2,5-diene-2,3-dicarboxylic acid, 2,3-dimethyl ester
CAS Number
1534358-79-6
Molecular Formula
C25H25NO5
Formula Weight
419.5
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: 11 mg/mLDMSO: 13 mg/mLEthanol: Slightly SolublePBS (pH 7.2): 0.04 mg/mL
λmax
244 nm
SMILES
CC(C=C1)=CC=C1C[C@H]([C@@]23C(C(OC)=O)=C([C@H](C=C3)O2)C(OC)=O)NC4=CC=CC=C4
InChi Code
InChI=1S/C25H25NO5/c1-16-9-11-17(12-10-16)15-20(26-18-7-5-4-6-8-18)25-14-13-19(31-25)21(23(27)29-2)22(25)24(28)30-3/h4-14,19-20,26H,15H2,1-3H3/t19-,20+,25-/m0/s1
InChi Key
UFPINDDCTUCUSA-DFIYOIEZSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    5 mg

    $73

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    10 mg

    $137

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    50 mg

    $395

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    100 mg

    $717

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    Cayman Chemical
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    Product Description

    COH000 is an inhibitor of SUMO-activating enzyme (SAE; IC50 = 0.2 µM), a heterodimer composed of SAE1 and SAE2.1 It is selective for SAE over ubiquitin-activating enzyme (UAE) and NEDD8-activating enzyme (NAE) at 10 µM. COH000 induces degradation of SAE2 in HCT116 human colon cancer cells. COH000 (10 mg/kg) induces intratumoral apoptosis, decreases intratumoral c-Myc expression, and reduces tumor growth in an HCT116 mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Li, Y.-J., Du, L., Wang, J., et al. Allosteric inhibition of ubiquitin-like modifications by a class of inhibitor of SUMO-activating enzyme. Cell Chem. Biol. 26(2), 278-288 (2019).