2. Apoptosis
  3. Bcl-2 Family
  4. A-371191

A-371191 is a selective Bcl-XL antagonist with a Ki <0.5 μM, and also acts as a mitochondria-targeting agent and chemosensitizer. A-371191 restores the sensitivity of cancer cells overexpressing Bcl-XL to Cisplatin (HY-17394) and Doxorubicin (HY-15142A). A-371191 reduces tumor volume in mice with intraperitoneal tumors. A-371191 can be used in the research of acute myeloid leukemia.

For research use only. We do not sell to patients.

A-371191

A-371191 Chemical Structure

CAS No. : 406228-58-8

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A-371191 Related Antibodies

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Description

A-371191 is a selective Bcl-XL antagonist with a Ki <0.5 μM, and also acts as a mitochondria-targeting agent and chemosensitizer. A-371191 restores the sensitivity of cancer cells overexpressing Bcl-XL to Cisplatin (HY-17394) and Doxorubicin (HY-15142A). A-371191 reduces tumor volume in mice with intraperitoneal tumors. A-371191 can be used in the research of acute myeloid leukemia[1].

IC50 & Target[1]

Bcl-xL

<0.5 μM (Ki)

Bcl-2

40 μM (Ki)

Bcl-W

180 μM (Ki)

Bcl-B

1300 μM (Ki)

In Vitro

A-371191 binds selectively to Bcl-XL with a Ki value of <0.5 μM, and exhibits significantly lower affinity for other anti-apoptotic Bcl-2 family proteins[1].
A-371191 accumulates and localizes to mitochondria in NIH-H460 cells[1].
Combined treatment with A-371191 (1.8-3.2 μM) restores the sensitivity of HL-60/Bcl-XL cells to Cisplatin (HY-17394) and Doxorubicin (HY-15142A), which is consistent with the response of HL-60/neo control cells[1].

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

A-371191 Related Antibodies
In Vivo

A-371191 (75-150 mg/kg; i.p.; twice daily for 7 consecutive days) reduces the average tumor volume and exhibits efficacy comparable to that of Doxorubicin in SCID mice bearing intraperitoneal HL-60/Bcl-XL tumors[1].

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

Animal Model: SCID mice[1]
Dosage: 75 mg/kg; 150 mg/kg
Administration: i.p.; twice daily; 7 days
Result: Reduced average tumor volume to 2667 mm3 at 75 mg/kg.
Reduced average tumor volume to 1742 mm3 at 150 mg/kg (control average was 2435 mm3).
Caused approximately 1% body weight gain over treatment period.
Molecular Weight

693.92

Formula

C36H47N5O5S2
CAS No.
SMILES

O=C(NS(=O)(C1=CC=C(N[C@H](CCCCN(C)C)CSC2=CC=CC=C2)C([N+]([O-])=O)=C1)=O)C3=CC=C(N(CC4)CCC54CCCC5)C=C3
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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A-371191 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

A-371191406228-58-8A371191A 371191Bcl-2 Familyacute myeloid leukemiaBcl-XLdoxorubicinHL-60/Bcl-XL cellcisplatinmitochondriaSCID miceBcl-XL-overexpressing cancer cellsNIH-H460 cellsanti-apoptotic proteinInhibitorinhibitorinhibit

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