Mcl-1-Puma inhibitor 8

Research use only, not for human use.

Mcl-1-Puma inhibitor 8 is a small-molecule dual-acting compound that targets the apoptotic Mcl-1-PUMA interface with Ki of 0.3 uM (Mcl-1, FPA).

Mcl-1-Puma inhibitor 8 is a small-molecule dual-acting compound that targets the apoptotic Mcl-1-PUMA interface with Ki of 0.3 uM (Mcl-1, FPA), reduces multiple cancer cells and inhibits PUMA-mediated apoptosis; a useful chemical probe to achieve safer cancer therapies by modulating Mcl-1-PUMA interaction.

CLZ-8 (Compound 8) (0-160 μM, 48 h) significantly inhibits PUMA-dependent apoptosis.CLZ-8 (0-1 μM, 2 h) significantly enhance the irradiated cell viability in a dose-dependent manner, provides significant protection for HUVECs, and inhibits overexpressed PUMA.CLZ-8 (0-1 μM, 24 h) attenuates the radiation-induced apoptosis.CLZ-8 (1 μM, 2 h) protects HUVECs from DNA breaks. Apoptosis Analysis Cell Line:DLD-1 cells or HUVEC cellsConcentration:0-160 μM (DLD-1) or 0.01, 0.1 and 1 μM (HUVECs)Incubation Time:48 h (DLD-1) or 24 h (HUVECs)Result:Significantly inhibited PUMA-dependent apoptosis with an IC50 of 38.93 ± 0.91 μM. Attenuated the radiation-induced apoptosis.Western Blot Analysis Cell Line:HUVEC cells Concentration:0.001, 0.01, 0.1 and 1 μM Incubation Time:2 h Result:Suppressed induction of PUMA after radiation, significantly decreased the level of p53. Significantly decreased the level of MCL-1 and increased the level of Bcl-XL.

CLZ-8 (0-400 mg/kg; i.g.; once) shows powerful anti-radiation effects in mice. Animal Model:6-8 week-old male BALB/c mice Dosage:100, 200 and 400 mg/kg Administration:Intragastric administration, once, 30 min prior to irradiation Result:Increased the survival rate of irradiated mice.

Mcl-1-PUMA modulator-8

Angiogenesis

Bcl-2

Bcl-2

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678158-55-9

393.505

C22H23N3O2S

>98% (HPLC)

In Vitro:?DMSO : 50 mg/mL (127.06 mM)

O=C1N=C(N2CCN(CCO)CC2)S/C1=C\C3=CC=C(C4=CC=CC=C4)C=C3

5-([1,1'-biphenyl]-4-ylmethylene)-2-(4-(2-hydroxyethyl)piperazin-1-yl)thiazol-4(5H)-one

(-20℃)

With Ice Pack

≥ 2 years