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製品番号: 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.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

分子式: C₂₅H₂₁F₂N₃O₄
分子量:465.45

保管条件:

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

CBI-3 構造式

価格（税別）

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

Use of MCE Products

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

生物活性
- 製品説明
- IC₅₀ & Target
- 体外実験
- Parmacokinetics
- 体内実験
化学情報
純度とドキュメンテーション
参考文献
Calculators
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target

^[1]

Bax

Bcl-2 Family アイソフォーム固有の製品をすべて表示 :

体外実験

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

体内実験

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 :

化学情報

分子量 465.45
分子式 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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

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

純度とドキュメンテーション

取扱説明書 (2659 KB)

参考文献

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

Calculators

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

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

Keywords

MOQ

Minimum order quantity

100 mg

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