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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-VDAC-NCATS-SM0225
NCATS-SM0225

Chemical Structure : NCATS-SM0225

CAS No.: 1212623-02-3

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NCATS-SM0225

货号: PC-25985Not For Human Use, Lab Use Only.

NCATS-SM0225 is a small molecule VDAC ligand and inhibitor of Endoplasmic reticulum-associated degradation (ERAD) dislocation with IC50 of 1.02 uM in NHK-drGFP reporter assays, disrupts calcium homeostasis, triggers PERK-STIM1 axis-mediated degradation of ERAD complex proteins and induces cell death.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

NCATS-SM0225 is a small molecule VDAC ligand and inhibitor of Endoplasmic reticulum-associated degradation (ERAD) dislocation with IC50 of 1.02 uM in NHK-drGFP reporter assays, disrupts calcium homeostasis, triggers PERK-STIM1 axis-mediated degradation of ERAD complex proteins and induces cell death.
NCATS-SM0225 significantly inhibits the degradation of both null Hong Kong variant of α−1-antitrypsin (NHK) and an ER membrane substrate CD3δ.
NCATS-SM0225 significantly increases the levels of HA-ΔF508CFTR in both the ER (core-glycosylated B form) and at the cell surface (fully glycosylated mature C form).
NCATS-SM0225 increases ER protein processing, activates UPR, and induces ERAD complex destruction, induces selective degradation of HERP1, OS9, and FAM8A1 in HeLa cells.
NCATS-SM0225 selectively targets all three isoforms of VDAC (voltage-dependent anion channel).
NCATS-SM0225 directly interacts with VDAC1 (MST KD=3.13 uM) and regulates VDAC1 voltage-gating in vitro.
NCATS-SM0225 induces calcium elevation in mitochondria, ER, and cytosol, leading to HERP1 and OS9 degradation, selectively targets a subgroup of cancer cells while sparing normal cells.
NCATS-SM0225 (20 mg/kg) markedly inhibited tumor growth in A375 melanoma xenografts.
STIM1 regulates 225-induced calcium influx, and its phosphorylation mediates 225-induced ERAD complex degradation and cell death.

物理化学性质&存储条件

分子量 460.61
分子式 C23H28N2O4S2
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-phenyl-N-((3S,3aS,5aS,10S,10bS)-3,5a,10-trimethyl-2-oxo-2,3,3a,4,5,5a,6,10,10a,10b-decahydrofuro[3',2':7,8]naphtho[2,3-d]thiazol-8-yl)methanesulfonamide

参考文献

1. Wenjing Yan, et al. Nat Commun. 2026 Jan 17;17(1):1058.

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