B02

Catalog No.S8434 Batch:S843401

Technical Data

Formula

C₂₂H₁₇N₃O

Molecular Weight

339.39

CAS No.

1290541-46-6

Solubility (25°C)*

In vitro

DMSO

67 mg/mL (197.41 mM)

Ethanol

20 mg/mL (58.92 mM)

Water

Insoluble

In vivo (Add solvents to the product individually and in order)

Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	3.3mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 66 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil	1.6mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 32 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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

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].

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].

Protocol (from reference)

Cell Assay:^{^[1]}	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.
Animal Study:^{^[3]}	Animal Models NCR nude mice Dosages 50 mg/kg Administration i.p.

Cell Assay:^{^[1]}

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.

Animal Study:^{^[3]}

Animal Models
NCR nude mice
Dosages
50 mg/kg
Administration
i.p.

References

Customer Product Validation

: Data from [Data independently produced by , , J Virol, 2018, 92(15)]

: Data from [Data independently produced by , , Sci Rep, 2018, 8(1):14421]

Selleck's B02 has been cited by 15 publications

The fragile X locus is prone to spontaneous DNA damage that is preferentially repaired by nonhomologous end-joining to preserve genome integrity [ iScience, 2024, 27(2):108814]	PubMed: 38303711
Selective utilization of non-homologous end-joining and homologous recombination for DNA repair during meiotic maturation in mouse oocytes [ Cell Prolif, 2023, 56(4):e13384]	PubMed: 36564861
Lack of impact of the ALDH2 rs671 variant on breast cancer development in Japanese BRCA1/2-mutation carriers [ Cancer Med, 2023, 12(6):6594-6602]	PubMed: 36345163
RAD52 prevents accumulation of Polα-dependent replication gaps at perturbed replication forks in human cells [ bioRxiv, 2023, 2023.04.12.536536]	PubMed: 37090680
DNA-PKcs promotes fork reversal and chemoresistance [ Mol Cell, 2022, 82-20:3932-3942.e6]	PubMed: 36130596
Targeted Inhibition of DNA-PKcs, ATM, ATR, PARP, and Rad51 Modulate Response to X Rays and Protons [ Radiat Res, 2022, 198(4):336-346]	PubMed: 35939823
cGAS guards against chromosome end-to-end fusions during mitosis and facilitates replicative senescence [ Protein Cell, 2021, 10.1007/s13238-021-00879-y 10.1126/science.abc5386]	PubMed: 34676498
Temporally distinct post-replicative repair mechanisms fill PRIMPOL-dependent ssDNA gaps in human cells [ Mol Cell, 2021, 81(19):4026-4040.e8]	PubMed: 34624216
Control of replication stress and mitosis in colorectal cancer stem cells through the interplay of PARP1, MRE11 and RAD51 [ Cell Death Differ, 2021, 10.1038/s41418-020-00733-4]	PubMed: 33531658
Loss of N-Glycanase 1 Alters Transcriptional and Translational Regulation in K562 Cell Lines [ G3 (Bethesda), 2020, 4;10(5):1585-1597]	PubMed: 32265286

RETURN POLICY
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.