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KVS0001

Chemical Structure : KVS0001

CAS No.:

KVS0001 (KVS 0001, KVS-0001)

货号: PC-21705Not For Human Use, Lab Use Only.

KVS0001 is a specific and bioavailable small molecule inhibitor of SMG1 kinase, disrupts nonsense mediated decay (NMD).

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

KVS0001 is a specific and bioavailable small molecule inhibitor of SMG1 kinase, disrupts nonsense mediated decay (NMD).
KVS0001 is highly selective against the other 246 protein or lipid kinases up to 1 uM.
KVS0001 substantially decreases the amount of phosphorylated UPF1, the downstream target of SMG1 kinase activity in NCI-H358 and LS180 cells.
KVS0001 causes MHC class I display of hidden neoantigens, increases the expression of TP53 in cancer cell lines, NCI-H716 and NCI-H2228.
KVS0001 (30 mg/kg) impacts tumor growth in syngeneic models.
KVS0001 elevates the expression of transcripts and proteins resulting from truncating mutations in vivo and in vitro.

物理化学性质&存储条件

分子量 579.08
分子式 C27H27ClN8O3S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

1-(4-(4-(2-((4-chloro-3-(piperazin-1-ylsulfonyl)phenyl)amino)pyrimidin-4-yl)pyridin-2-yl)phenyl)-3-methylurea

参考文献

1. Ashley L Cook, et al. bioRxiv. 2023 Dec 29:2023.12.28.573594.

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