CBI-3
CBI-3 is a BAX inhibitor that covalently modifies BAX and blocks BAX-mediated apoptosis. CBI-3 protects primary rat dorsal root ganglion neurons and human induced pluripotent stem cell-derived motor neurons from apoptosis and spontaneous loss. CBI-3 reduces hepatocyte apoptosis and protects liver histology in an anti-Fas-induced acute liver injury mouse model. CBI-3 exhibits improved metabolic stability in mouse liver microsomes. CBI-3 can be used for research on Fas-induced fulminant hepatic failure and amyotrophic lateral sclerosis.
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- Formule: C25H21F2N3O4
- Masse moléculaire:465.45
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Activité biologique
Description
IC50 & Target
[1]|
Bax |
In Vitro
CBI-3 (1 μM; 0-120 min) is metabolically stable in mouse liver microsomes relative to earlier analogs[1].
CBI-3 (0.5-2 μM; DIV7) maintains the survival of hiPS cell-derived motor neurons from ALS donor TDP-43 47D[1].
CBI-3 (24 h) blocks Cisplatin (HY-17394)-induced apoptosis in iBMK Bak−/− cells in a BAX-dependent manner[1].
CBI-3 (10 μM; 2 h) protects primary rat DRG neurons from ABT-737 (HY-50907)-induced apoptosis[1].
CBI-3 (5 μM; 2 h pre-incubation) protects hiPS cell-derived motor neurons from healthy donor 1016A against ABT-737-induced death[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:primary rat DRG neurons
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Concentration:10 μM CBI-3 before the addition of 10 μM ABT-737
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Incubation Time:2 h
ABT-737 for 24 h -
Result:Protected primary rat DRG neurons from ABT-737 (HY-50907)-induced apoptosis.
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Cell Line:hiPS cell-derived motor neurons
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Concentration:5 μM CBI-3 before the addition of 5 or 10 μM ABT-737
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Incubation Time:2 h
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Result:Protected hiPS cell-derived motor neurons from healthy donor 1016A against ABT-737-induced death.
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Cell Line:hiPS cell-derived motor neurons
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Concentration:0.5, 1, 2 μM
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Incubation Time:DIV7
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Result:Preserved survival of hiPS cell-derived motor neurons from ALS donor TDP-43 47D.
Parmacokinetics
| Species | Dose | Route | T1/2 | Tmax | Cmax | AUClast | CL_obs |
|---|---|---|---|---|---|---|---|
| Mice[1] | 3 mg/kg | i.v. | 0.59 h | 0.08 h | 4.5 μM | 1.71 μM·h | 64.07 mL/min/kg |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Alb-crenegBaxfl/flBak−/− (Bak−/−) and Alb-creposBaxfl/flBak−/− (liver DKO) (13-19 weeks old; both sexes used)[1]
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Dosage:10 mg/kg (two doses; 2.16 mM CBI-3 in 5% DMSO and 95% of 10% HPβCD)
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Administration:i.v.; two doses at -4 h and 0 h
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Result:Showed full endpoint survival for CBI‑3‑treated Bak-/- mice, while vehicle‑treated Bak-/- mice succumbed to anti‑Fas challenge; DKO mice survived without CBI‑3.
Demonstrated preserved liver gross morphology in CBI‑3‑treated Bak-/- mice versus darkened livers in vehicle‑treated Bak-/- counterparts.
Detected reduced hepatocyte apoptosis in CBI‑3‑treated Bak-/- mice using cleaved caspase‑3 immunohistochemistry and H&E morphometry.
Revealed perturbed hepatic protein profiles: repressed metabolic enzymes and elevated repair‑associated proteins upon CBI‑3 exposure.
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Annexin V plus membrane-impermeant dye apoptosis staining
- Paraffin Section
- Apoptosis Solutions
- Protocol for Hematoxylin-Eosin (H&E) Staining
- Primary Dorsal Root Ganglion Sensory Neuron Culture
- Liver Histomorphometry
- How to Choose the Right Model Animal
Chemical Information
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Masse moléculaire 465.45
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Formule C25H21F2N3O4
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SMILES
C=CC(N1[C@H](C(NC2CC2)=O)CC3=C([C@@H]1C4=CC=C5OC(F)(F)OC5=C4)NC6=C3C=CC=C6)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CBI-3 Related Classifications
HY-189721 Related Classifications
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