TAK-981 is a potent and selective SUMOylation enzymatic cascade inhibitor with potential immune-activating and antineoplastic activities. TAK-981 targets and covalently binds to the small ubiquitin-like modifier (SUMO; small ubiquitin-related modifier) protein, which prevents the transfer of SUMO from the SUMO-activating enzyme (SAE) to SUMO-conjugating enzyme UBC9. TAK-981 is able to increase the production of type 1 IFN, thereby increasing type 1 IFN-mediated signaling, activating innate effector cells and enhancing the antitumor innate immune responses.
Molecular Weight | 578.10 |
Formula | C25H28ClN5O5S2 |
CAS Number | 1858276-04-6 |
Solubility (25°C) | DMSO ≥ 50 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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.
[2] Li Du, et al. SUMOylation inhibition enhances dexamethasone sensitivity in multiple myeloma
[3] Antti Kukkula, et al. Therapeutic Potential of Targeting the SUMO Pathway in Cancer
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