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Chemical Structure : TAK-981
CAS No.: 1858276-04-6
Catalog No.: PC-72802Not For Human Use, Lab Use Only.
TAK-981 (TAK981, Subasumstat) is a first-in-class, potent, highly selective SUMO-activating enzyme (SAE) inhibitor with IC50 of 1 nM, >1000-fold selectivity against UAE and NAE.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $188 | In stock | |
| 10 mg | $278 | In stock | |
| 25 mg | $478 | In stock | |
| 50 mg | Get quote | ||
| 100 mg | Get quote |
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TAK-981 (TAK981, Subasumstat) is a first-in-class, potent, highly selective SUMO-activating enzyme (SAE) inhibitor with IC50 of 1 nM, >1000-fold selectivity against UAE and NAE.
TAK-981 also exhibits potent and prolonged cellular pathway inhibition with improved selectivity over NAE.
TAK-981 reduces SUMO2/3 conjugation in xenograft tumors following IV administration.
TAK-981 decreased SUMOylation in PDAC cells at the nanomolar range, thereby causing a G2/M cell cycle arrest, mitotic failure and chromosomal segregation defects.
TAK-981 efficiently limited tumour burden in the KPC3 syngeneic mouse model without evidence of systemic toxicity.
In vivo treatment with TAK-981 enhanced the proportions of activated CD8 T cells and natural killer (NK) cells but transiently decreased B cell numbers in tumour, peripheral blood, spleen and lymph nodes.
| M.Wt | 578.099 | |
| Formula | C25H28ClN5O5S2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO (5.8 mg/mL) |
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| Chemical Name/SMILES |
Sulfamic acid, [(1R,2S,4R)-4-[[5-[[4-[(1R)-7-chloro-1,2,3,4-tetrahydro-1-isoquinolinyl]-5-methyl-2-thienyl]carbonyl]-4-pyrimidinyl]amino]-2-hydroxycyclopentyl]methyl ester |
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1. Langston SP, et al. J Med Chem. 2021 Mar 11;64(5):2501-2520.
2. Du L, et al. J Exp Clin Cancer Res. 2022 Jan 4;41(1):8.
3. Kumar S, et al. Gut. 2022 Jan 24:gutjnl-2021-324834.
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