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Art. -Nr.: HY-189721

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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.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Formel: C₂₅H₂₁F₂N₃O₄
Molecular Weight:465.45

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

CBI-3 Chemical Structure

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

Bax

Alle Bcl-2 Family Isoform-spezifische Produkte anzeigen :

In Vitro

OthersApoptosis

Others

CBI-3 (5 μM; overnight) covalently modifies recombinant human BAX WT^[1] 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].

Apoptosis

CBI-3 (24 h) inhibits BAX-mediated apoptosis in HCT116 Bak^−/− cells; it does not reduce the viability of HCT116 WT, Bak^−/−, Bax^−/− cells or primary human RPTEC^[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.

Cell Viability Assay^[1]

Cell Line:

primary rat DRG neurons
Concentration:

10 μM CBI-3 before the addition of 10 μM ABT-737
Incubation Time:

2 h
ABT-737 for 24 h
Result:

Protected primary rat DRG neurons from ABT-737 (HY-50907)-induced apoptosis.

Immunofluorescence^[1]

Cell Line:

hiPS cell-derived motor neurons
Concentration:

5 μM CBI-3 before the addition of 5 or 10 μM ABT-737
Incubation Time:

2 h
Result:

Protected hiPS cell-derived motor neurons from healthy donor 1016A against ABT-737-induced death.

Immunofluorescence^[1]

Cell Line:

hiPS cell-derived motor neurons
Concentration:

0.5, 1, 2 μM
Incubation Time:

DIV7
Result:

Preserved survival of hiPS cell-derived motor neurons from ALS donor TDP-43 47D.

Parmacokinetics

Species	Dose	Route	T_1/2	T_max	C_max	AUC_last	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

Apoptosis

CBI-3 (10 mg/kg; i.v.; administered twice at -4 h and 0 h) protected liver histology, reduced hepatocyte apoptosis, and achieved complete survival at the experimental endpoint in anti-Fas-induced acute liver injury in Bak^−/− mice^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Alb-cre^negBax^fl/flBak^−/− (Bak^−/−) and Alb-cre^posBax^fl/flBak^−/− (liver DKO) (13-19 weeks old; both sexes used)^[1]
Dosage:

10 mg/kg (two doses; 2.16 mM CBI-3 in 5% DMSO and 95% of 10% HPβCD)
Administration:

i.v.; two doses at -4 h and 0 h
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.

Related Protocols :

Chemical Information

Molecular Weight 465.45
Formel C₂₅H₂₁F₂N₃O₄
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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Shi P, et al. An enantioselective covalent inhibitor of BAX confers cytoprotection in vivo. Nature chemical biology. 2026 Aug 28.

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

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MOQ

Minimum order quantity

100 mg

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