COH000

SKU: orb1226137

Description

COH000 (COH-000) is a highly selective, first-in-class, irreversible, allosteric, covalent inhibitor of SUMO-Activating Enzyme E1, inhibits SUMOylation in vitro with IC50 of 0.2 uM, displays >500-fold selectivity for SUMOylation over ubiquitylation; increased the degradation of SAE2, increases the expression of miR-34b and reduces c-Myc levels in lymphoma and colorectal cancer cell lines and a colorectal cancer xenograft mouse model.(In Vitro):COH000 has over 500-fold selectivity for SUMOylation than ubiquitylation. COH000 inhibits SUMO adenylation without directly competing with ATP or SUMO1 binding. COH000 has an extremely slow off-rate and is consistent with it being covalently bound to the enzyme.

Key Properties

• CAS Number: 1534358-79-6
• MW: 419.477
• Purity: >98% (HPLC)
• Formula: C₂₅H₂₅NO₅
• SMILES: O=C(C1=C(C(OC)=O)C2C=CC1([C@H](NC3=CC=CC=C3)CC4=CC=C(C)C=C4)O2)OC
• Target: E1
• Solubility: DMSO: Soluble （ < 1 mg/ml refers to the product slightly soluble or insoluble )

Bioactivity

• In Vitro:
  COH000 has over 500-fold selectivity for SUMOylation than ubiquitylation. COH000 inhibits SUMO adenylation without directly competing with ATP or SUMO1 binding. COH000 has an extremely slow off-rate and is consistent with it being covalently bound to the enzyme.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

COH-000 | COH 000 | CID 46835111 | SID 99212997

Quick Database Links

Gene Symbol

E1