Home DNA Damage/DNA Repair DNA/RNA Synthesis inhibitor B02 For research use only.

B02

B02 is a small-molecule inhibitor of human RAD51 with an IC50 of 27.4 μM, but does not inhibit its E. coli homologue RecA (IC50 > 250 μM).

B02 Chemical Structure

B02 Chemical Structure

CAS: 1290541-46-6

Selleck's B02 has been cited by 15 Publications

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Purity & Quality Control

Batch: S843401 DMSO] 67 mg/mL] false] Ethanol] 20 mg/mL] false] Water] Insoluble] false Purity: 99.93%
99.93

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HEK cells Function assay 25 uM Inhibition of DNA binding to human RAD51 in irradiated HEK cells assessed as reduction in RAD51 foci formation at 25 uM by fluorescence microscopy relative to untreated control, 22380680
MEF cells Function assay 5 uM 1 h Inhibition of RAD51 in Tp53-/- MEF cells assessed as potentiation of 32 uM cisplatin-induced cytotoxicity at 5 uM incubated for 1 hr by clonogenic survival assay relative to untreated control 22380680
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Biological Activity

Description B02 is a small-molecule inhibitor of human RAD51 with an IC50 of 27.4 μM, but does not inhibit its E. coli homologue RecA (IC50 > 250 μM).
Targets
RAD51 [2]
(Cell-free assay)
27.4 μM
In vitro
In vitro B02 is a specific inhibitor of human RAD51 recombinase, blocks HR repair in human embryonic kidney (HEK) and breast cancer cells and increases their sensitivity to a wide range of DNA damaging agents. Also, B02 enhances DNA damage and apoptosis induced by decitabine in MM cells[1]. B02 shows high specificity for RAD51 and does not significantly inhibit RAD54 in the range of concentrations from 0 to 200 μM[2]. B02 shows biological effect in human and mouse cells. In human embryonic kidney (HEK) cells, B02 disrupts RAD51 foci formation in response to DNA damage and inhibited DSB repair and DSB-dependent HR. B02 can also increase the sensitivity of cancer cells to chemotherapeutic DNA damaging agents[3].
Cell Research Cell lines The human MM cell lines NCI-H929 (H929), RPMI 8226, ARP-1, U266 and MM.1S cells
Concentrations 10 μM
Incubation Time 1 h
Method Proliferation of MM-cell lines is monitored by the WST-1 colorimetric cell-count assay. MM cell lines are seeded in 96-well plates at ~8000 cells/well. The cells are treated with or without B02 (10 μM) for 1 h, followed by treatment with vehicle (DMSO) or DOX (20-160 nM) for 72 h. WST-1 reagent is added to the culture medium in each well at a 1:10 ratio, and incubation continues at 37°C for 4 h. Relative cell number is estimated from absorbance at 450 nm using a spectrophotometer.
In Vivo
In vivo B02 significantly increases the anti-tumor activity of cisplatin in vivo. B02 is tolerated by mice at doses up to 50 mg/kg without obvious body weight loss. No detectable morphological changes induced by B02 in kidneys and livers, main organs for detoxification are found[3].
Animal Research Animal Models NCR nude mice
Dosages 50 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 339.39 Formula

C22H17N3O
CAS No. 1290541-46-6 SDF Download B02 SDF
Smiles C1=CC=C(C=C1)CN2C(=NC3=CC=CC=C3C2=O)C=CC4=CN=CC=C4
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 67 mg/mL ( (197.41 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 20 mg/mL

Water : Insoluble


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In vivo
Batch:

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In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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