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BH3I-1 is a cell-permeable inhibitor that targets the Bcl-2 family of proteins, which are essential in regulating apoptosis. By blocking the binding of BH3 peptides to Bcl-xL, BH3I-1 promotes apoptosis and inhibits the interactions of BH3 domain-containing proteins with Bcl-xL, Bcl-2, and Bcl-W. BH3I-1 has demonstrated the ability to enhance radiation sensitivity in non-small cell lung cancer cells.

300817-68-9

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300817-68-9 Usage

Uses

Used in Cancer Therapy:
BH3I-1 is used as an apoptosis inducer for targeting Bcl-2 family proteins, which play a critical role in preventing cell death. By inhibiting the interactions between BH3 domain-containing proteins and Bcl-2 family members, BH3I-1 promotes apoptosis in Bcl-2 or Bcl-W expressing cells, making it a potential therapeutic agent for cancer treatment.
Used in Enhancing Radiation Sensitivity:
In the field of non-small cell lung cancer treatment, BH3I-1 is used as a radiosensitizer to enhance the effectiveness of radiation therapy. By increasing the sensitivity of cancer cells to radiation, BH3I-1 can improve treatment outcomes and potentially reduce the required dosage of radiation, thereby minimizing side effects and damage to healthy tissues.
Used in Drug Development:
BH3I-1 serves as a valuable compound in the development of new drugs targeting the Bcl-2 family of proteins. Its ability to inhibit protein-protein interactions and induce apoptosis makes it a promising candidate for the creation of novel therapeutics for various types of cancer.
Used in Research:
In the field of molecular biology and cell biology, BH3I-1 is used as a research tool to study the mechanisms of apoptosis and the role of Bcl-2 family proteins in cell death. BH3I-1 can help researchers gain a deeper understanding of the complex interactions between pro-apoptotic and anti-apoptotic proteins, ultimately contributing to the development of more effective cancer treatments.

in vitro

the bcl-2 inhibitors bh3i-1 and it analog bh3i-2 had been applied as lead compounds to find possible bcl-2 or bcl-x(l) inhibitors by using computer-assisted screening of in-house database. the identified compounds were further studied regarding their possible application as a drug. it was found that the induction of apoptosis, which was shown as number of hypodiploid cells, was increased by adding bh3i-1 and it analog bh3i-2 to bjab bcl-xl and bjab neo/mock cells. in addition, the effects of the pro-apoptotic proteins bax and bak on the induction of apoptosis via bh3i-1 and it analog bh3i-2 were investigated with a variety of knockout cell lines, and resulted showed that the presence or absence of bak or bax has no significant influence on the amount of apoptotic events induced by bh3i-1 and it analog bh3i-2 [1].

IC 50

293.95 μm

references

[1] füllbeck m,gebhardt n,hossbach j,daniel pt,preissner r. computer-assisted identification of small-molecule bcl-2 modulators. comput biol chem.2009 dec;33(6):451-6.

Check Digit Verification of cas no

The CAS Registry Mumber 300817-68-9 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 3,0,0,8,1 and 7 respectively; the second part has 2 digits, 6 and 8 respectively.
Calculate Digit Verification of CAS Registry Number 300817-68:
(8*3)+(7*0)+(6*0)+(5*8)+(4*1)+(3*7)+(2*6)+(1*8)=109
109 % 10 = 9
So 300817-68-9 is a valid CAS Registry Number.

300817-68-9 Well-known Company Product Price

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  • Sigma

  • (B8809)  BH3I-1  ≥97% (HPLC), powder, yellow

  • 300817-68-9

  • B8809-5MG

  • 2,004.21CNY

  • Detail

300817-68-9SDS

SAFETY DATA SHEETS

According to Globally Harmonized System of Classification and Labelling of Chemicals (GHS) - Sixth revised edition

Version: 1.0

Creation Date: Aug 12, 2017

Revision Date: Aug 12, 2017

1.Identification

1.1 GHS Product identifier

Product name BH3I-1

1.2 Other means of identification

Product number -
Other names 5-(P-BROMOBENZYLIDENE)-A-ISOPROPYL-4-OXO-2-THIOXO-3-THIAZOLIDINE ACETIC ACID

1.3 Recommended use of the chemical and restrictions on use

Identified uses For industry use only.
Uses advised against no data available

1.4 Supplier's details

1.5 Emergency phone number

Emergency phone number -
Service hours Monday to Friday, 9am-5pm (Standard time zone: UTC/GMT +8 hours).

More Details:300817-68-9 SDS

300817-68-9Upstream product

300817-68-9Downstream Products

300817-68-9Related news

The BH3 mimetic compound BH3I-1 (cas 300817-68-9) impairs mitochondrial dynamics and promotes stress response in addition to its pro-apoptotic key function07/15/2019

BH3 mimetics, such as BH3I-1, act as Bcl-2 antagonists, promote apoptosis and are used in basic research studies on apoptotic signaling and are currently tested as experimental anti-tumor agents. The present study addresses time- and dose-dependent responses of BH3I-1 on apoptosis, cellular stre...detailed

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