Chemical Structure : DCL1191
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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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.
| 分子量 | 530.44 | |
| 分子式 | C25H18F4N4O5 | |
| 外观性状 | Solid | |
| 储存条件 |
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| Solubility |
10 mM in DMSO |
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1. Changle Du, et al. J Med Chem. 2026 Oct 22;69(20):24197-24218.
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