B02 DNA/RNA Synthesis inhibitor

Cat.No.S8434

B02 is a small-molecule inhibitor of human RAD51 with an IC50 of 27.4 μM, but this compound does not inhibit its E. coli homologue RecA (IC50 > 250 μM).
B02 DNA/RNA Synthesis inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 339.39

Quality Control

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

Cell Culture, Treatment & Working Concentration

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,
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
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight 339.39 Formula

C22H17N3O

Storage (From the date of receipt)
CAS No. 1290541-46-6 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles C1=CC=C(C=C1)CN2C(=NC3=CC=CC=C3C2=O)C=CC4=CN=CC=C4

Solubility

In vitro
Batch:

DMSO : 67 mg/mL (197.41 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 20 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

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Working concentration: mg/ml;

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.

Mechanism of Action

Targets/IC50/Ki
RAD51 [2]
(Cell-free assay)
27.4 μM
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, this compound enhances DNA damage and apoptosis induced by decitabine in MM cells[1]. It shows high specificity for RAD51 and does not significantly inhibit RAD54 in the range of concentrations from 0 to 200 μM[2]. This chemical shows biological effect in human and mouse cells. In human embryonic kidney (HEK) cells, it disrupts RAD51 foci formation in response to DNA damage and inhibited DSB repair and DSB-dependent HR. It can also increase the sensitivity of cancer cells to chemotherapeutic DNA damaging agents[3].
In vivo
B02 significantly increases the anti-tumor activity of cisplatin in vivo. This compound is tolerated by mice at doses up to 50 mg/kg without obvious body weight loss. No detectable morphological changes induced by this chemical in kidneys and livers, main organs for detoxification are found[3].
References

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