B02

Catalog No.S8434

B02 Chemical Structure

Molecular Weight(MW): 339.39

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).

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Cited by 2 Publications

2 Customer Reviews

  • HEK 293T cells were transfected with a total of 6 μg of plasmid DNA (2 μg pSG-I-SceI-HA, 2 μg pcDNA-HBZ-Myc-His or empty vector, and 2 μg the pDR-GFP reporter) and treated with 20 μM B02 for 48 h where indicated. Data shown are averages of results from three independent experiments, and error bars represent SEM (*, P ≤ 0.05 by Student's t test).

    J Virol, 2018, 92(15). B02 purchased from Selleck.

    The number of RAD51 foci per nucleus were counted from at least 50 nuclei for each treatment. Following DMSO, RI-1 or B02 pre-treatment, cells were incubated in normal media or with 10 nM doxorubicin (Dox), 1 μM cisplatin (Cis), 0.1 nM vincristine (Vin) or 10 μM GDC-0152 (GDC) for 24 hours then harvested.

    Sci Rep, 2018, 8(1):14421. B02 purchased from Selleck.

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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

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 Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HEK cells MVjGeY5kfGmxbjDhd5NigQ>? M{PpXFI2KHWP MVLJcohq[mm2aX;uJI9nKESQQTDibY5lcW6pIITvJIh2dWGwIGLBSFUyKGmwIHnydoFlcWG2ZXSgTGVMKGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDSRWQ2OSCob3PpJIZwem2jdHnvckBifCB{NTD1UUBjgSCobIXvdoV{[2WwY3WgcYlkem:|Y3;wfUBz\WyjdHn2[UB1dyC3boTy[YF1\WRiY3;ueJJwdCx? MoDzNlI{QDB4OEC=
MEF cells M4nOR2Z2dmO2aX;uJIF{e2G7 NXPmT|FRPSC3TR?= MYGxJIg> MlT3TY5pcWKrdHnvckBw\iCUQVS1NUBqdiCWcEWzMU8uKE2HRjDj[YxteyCjc4Pld5Nm\CCjczDwc5RmdnSrYYTpc44hd2ZiM{KgeW0h[2m|cHzheIlvNWmwZIXj[YQh[3m2b4TvfIlkcXS7IHH0JFUhfU1iaX7jeYJifGWmIH\vdkAyKGi{IHL5JINtd26xZ3XubYMhe3W{dnn2ZYwh[XO|YYmgdoVt[XSrdnWgeI8hfW62cnXheIVlKGOxboTyc4w> NEHKd3UzOjN6ME[4NC=>

... Click to View More Cell Line Experimental Data

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

Cell Research:[1]
+ Expand
  • 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.
    (Only for Reference)
Animal Research:[3]
+ Expand
  • Animal Models: NCR nude mice
  • Formulation: cremophor/DMSO/NS (1∶1∶3)
  • Dosages: 50 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 67 mg/mL warmed (197.41 mM)
Ethanol 20 mg/mL warmed (58.92 mM)
Water 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.

Chemical Information

Molecular Weight 339.39
Formula

C22H17N3O

CAS No. 1290541-46-6
Storage powder
in solvent
Synonyms N/A

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID