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TAK-981

Cat. No. M9634
TAK-981 Structure
Synonym:

Subasumstat

Size Price Availability Quantity
5mg USD 180  USD180 In stock
10mg USD 285  USD285 In stock
25mg USD 530  USD530 In stock
50mg USD 880  USD880 In stock
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Quality Control & Documentation
Biological Activity

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.

Chemical Information
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
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Sumit Kumar, et al. Targeting pancreatic cancer by TAK-981: a SUMOylation inhibitor that activates the immune system and blocks cancer cell cycle progression in a preclinical model

[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

[4] Li Du, et al. Targeting SUMOylation in cancer

[5] Steven P Langston, et al. Discovery of TAK-981, a First-in-Class Inhibitor of SUMO-Activating Enzyme for the Treatment of Cancer

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Keywords: TAK-981, Subasumstat supplier, E1/E2/E3 Enzyme, inhibitors, activators


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