| SKU | Size | Availability | Price | Qty |
|---|---|---|---|---|
| C655182-1ml | 1ml | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $132.90 |
| Specifications & Purity | 10mM in DMSO |
|---|---|
| Biochemical and Physiological Mechanisms | CLZ-8 (Compound 8) is an orally active Mcl-1-PUMA interface inhibitor, with a K i of 0.3 μM. CLZ-8 exhibits dual activity on reduce PUMA-dependent apoptosis while deactivating Mcl-1-mediated anti-apoptosis in cancer cells. |
| Storage Temp | Store at -80°C |
| Shipped In | Ice chest + Ice pads |
| Product Description | CLZ-8 (Compound 8) is an orally active Mcl-1-PUMA interface inhibitor, with a K i of 0.3 μM. CLZ-8 exhibits dual activity on reduce PUMA-dependent apoptosis while deactivating Mcl-1-mediated anti-apoptosis in cancer cells In Vitro 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Apoptosis Analysis Cell Line: DLD-1 cells or HUVEC cells Concentration: 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 IC 50 of 38.93 ± 0.91 μM. Attenuated the radiation-induced apoptosis. Western Blot AnalysisCell 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. In Vivo CLZ-8 (0-400 mg/kg; i.g.; once) shows powerful anti-radiation effects in mice. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: 6-8 week-old male BALB/c miceDosage: 100, 200 and 400 mg/kg Administration: Intragastric administration, once, 30 min prior to irradiation Result: Increased the survival rate of irradiated mice. IC50& Target:Mcl-1 0.3 μM (Ki) PUMA |
| Canonical SMILES | C1CN(CCN1CCO)C2=NC(=O)C(=CC3=CC=C(C=C3)C4=CC=CC=C4)S2 |
|---|---|
| Molecular Weight | 393.50 |
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