RAD51-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/RAD51.html RAD51RAD51, an essential eukaryotic DNA recombinase, promotes homologous pairing and strand exchange during homologousrecombination (HR) and the recombinational repair of double strand breaks. RAD51 protein is recruited onto the DNA break byBRCA2 and

2、 forms homopolymeric filaments that invade the homologous chromatid and use it as a template for repair. RAD51filaments are detectable by immunofluorescence as distinct foci in the cell nucleus, and their presence is a read out of HRproficiency. RAD51 is an essential gene, protecting cells from gene

3、tic instability.RAD51 recombinase activity plays a critical role for cancer cell proliferation and survival, and often contributes to drug-resistance.Abnormally elevated RAD51 function and hyperactive homologous recombination (HR) rates have been found in a panel of cancers,including breast cancer a

4、nd chronic myeloid leukaemia (CML). Directly targeting RAD51 and attenuating the deregulated RAD51activity has therefore been proposed as an alternative and supplementary strategy for cancer treatment.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/RAD51.html RAD51 HYPERLINK https:/www.MedChemE

5、/Targets/RAD51.html HYPERLINK https:/www.MedChemE/Targets/RAD51.html Inhibitors HYPERLINK https:/www.MedChemE/Targets/RAD51.html HYPERLINK https:/www.MedChemE/Targets/RAD51.html & HYPERLINK https:/www.MedChemE/Targets/RAD51.html HYPERLINK https:/www.MedChemE/Targets/RAD51.html Activators HYPERLINK h

6、ttps:/www.MedChemE/amuvatinib.html Amuvatinib(MP470; HPK 56) Cat. No.: HY-10206 HYPERLINK https:/www.MedChemE/Amuvatinib_hydrochloride.html Amuvatinib HYPERLINK https:/www.MedChemE/Amuvatinib_hydrochloride.html HYPERLINK https:/www.MedChemE/Amuvatinib_hydrochloride.html hydrochloride(MP470 hydrochlo

7、ride; HPK 56 hydrochloride) Cat. No.: HY-10206AAmuvatinib (MP470) is an orally bioavailablemulti-targeted tyrosine kinase inhibitor withpotent activity against mutant c-Kit, PDGFR, Flt3,c-Met and c-Ret.Amuvatinib hydrochloride (MP470 hydrochloride) isan orally bioavailable multi-targeted tyrosinekin

8、ase inhibitor with potent activity againstmutant c-Kit, PDGFR, Flt3, c-Met and c-Ret.Purity: 98.07%Clinical Data: Phase 2Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98%Clinical Data: Phase 2Size: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/bractoppin.html Bractoppin HYPERLINK https:/www.MedChem

9、E/bractoppin.html HYPERLINK https:/www.MedChemE/IBR2.html IBR2Cat. No.: HY-126020 Cat. No.: HY-103710Bractoppin is a potent and selective drug-likeinhibitor of phosphopeptide recognition by thehuman BRCA1 tandem(t) BRCT domain (bindingIC : 74 nM).50IBR2 is a potent and specific RAD51 inhibitor andin

10、hibits RAD51-mediated DNA double-strand breakrepair. IBR2 disrupts RAD51 multimerization,accelerates proteasome-mediated RAD51 proteindegradation, inhibits cancer cell growth andinduces apoptosis.Purity: 99.18%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgP

11、urity: 98.60%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/RAD51_Inhibitor_B02.html RAD51 HYPERLINK https:/www.MedChemE/RAD51_Inhibitor_B02.html HYPERLINK https:/www.MedChemE/RAD51_Inhibitor_B02.html Inhibitor HYPERLINK https:/www.Me

12、dChemE/RAD51_Inhibitor_B02.html HYPERLINK https:/www.MedChemE/RAD51_Inhibitor_B02.html B02(B02) Cat. No.: HY-101462 HYPERLINK https:/www.MedChemE/rad51-in-1.html RAD51-IN-1Cat. No.: HY-122705RAD51 Inhibitor B02 (B02) is an inhibitor of humanRAD51 with an IC of 27.4 M.50RAD51-IN-1, a derivative of B0

13、2, is a potentinhibitor of RAD51. RAD51-IN-1 can be used forcancer research.Purity: 99.87%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.97%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE

14、/rad51-in-2.html RAD51-IN-2 HYPERLINK https:/www.MedChemE/rad51-in-2.html HYPERLINK https:/www.MedChemE/rad51-in-3.html RAD51-IN-3Cat. No.: HY-111887 Cat. No.: HY-136604RAD51-IN-2 (compound example 67A) is a RAD51inhibitor extracted from patent WO2019/051465A1.RAD51-IN-3 is a Rad51 inhibitor extract

15、ed frompatent WO2019051465A1, compound Example 66A.Purity: 99.79%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/ri-dl-2-tfa.html RI(dl)-2 HYPERLINK https:/www.MedChemE/ri-dl-

16、2-tfa.html HYPERLINK https:/www.MedChemE/ri-dl-2-tfa.html TFA HYPERLINK https:/www.MedChemE/ri-dl-2-tfa.html HYPERLINK https:/www.MedChemE/RI-1.html RI-1Cat. No.: HY-126972A Cat. No.: HY-15317RI(dl)-2 TFA is a potent and selectiveRAD51-mediated D-loop formation inhibitorwith an IC of 11.1 M. RI(dl)-

17、2 TFA does not50influence RAD51 binding to ssDNA and inhibitshomologous recombination (HR) activity in humancells (IC of 3.0 M).50Purity: 98.0%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mgRI-1 is a RAD51 inhibitor, with IC s ranging50from 5 to 30 M. RI-1 binds covalently to thesurface

18、 of RAD51 protein at cysteine 319. RI-1inactivates RAD51 by directly binding to a proteinsurface that serves as an interface betweenprotein subunits in RAD51 filaments.Purity: 99.83%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/RI-2.html RI-2 HYPERLINK https:/www.MedChemE/RI-2.html HYPERLINK https:/www.MedChemE/RS-1.html RS-1Cat. No.: HY-16904 Cat. No.: HY-19793RI-2 is a reversible RAD51