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首页-小分子抑制剂&激动剂-Autophagy-DCL1191
DCL1191

Chemical Structure : DCL1191

CAS No.:

DCL1191 (DCL-1191)

货号: PC-28575Not For Human Use, Lab Use Only.

DCL1191 is a potent, selective and orally bioavailable of transcription factor EB (TFEB) inhibitor with MST Kd of 80.5 nM for TFEB bHLHLZ domain, disrupts the TFEB-DNA interaction with IC50 of 60.5 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

DCL1191 is a potent, selective and orally bioavailable of transcription factor EB (TFEB) inhibitor with MST Kd of 80.5 nM for TFEB bHLHLZ domain, disrupts the TFEB-DNA interaction with IC50 of 60.5 nM.
The transcription factor EB (TFEB) serves as a master regulator of autophagy.
DCL1191 shows markedly enhanced selectivity over Tpo-R and MITF.
DCL1191 effectively blocks TFEB-CLEAR DNA binding, dampens autophagic signaling, and exerts synergistic effects combined with temozolomide (TMZ) in utophagy-hyperactivated U87 glioblastoma cells.
DCL1191 possesses satisfactory in vivo pharmacokinetic properties, with an oral bioavailability of 18.77% in rats.

物理化学性质&存储条件

分子量 530.44
分子式 C25H18F4N4O5
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

(Z)-5'-Fluoro-2'-hydroxy-5-methoxy-3'-(2-(3-methyl-5-oxo-1-(4-(trifluoromethyl)phenyl)-1,5-dihydro-4H-pyrazol-4-ylidene)hydrazineyl)-[1,1'-biphenyl]-3-carboxylic Acid

参考文献

1. Changle Du, et al. J Med Chem. 2026 Oct 22;69(20):24197-24218.

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