CRISPR-Cas9-Agonists-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/CRISPR_Cas9.html CRISPR/Cas9The CRISPR/Cas9 system derived from bacterial adaptive immune systems is one of the most powerful genome editing technology.It is an RNA-guided genome editing tool that consists of a Cas9 nuclease and a single-guide RNA (sgRNA). By b

2、ase-pairing with aDNA target sequence, the sgRNA enables Cas9 to recognize and cut a specific target DNA sequence, generating double strandbreaks (DSBs) that trigger cell repair mechanisms and mutations at or near the DSBs sites. CRISPR/Cas9 technology has beenstudied extensively and its application

3、 has been expanded from the modification of the gene in cells to organisms. The potentialrole of CRISPR/Cas9 in gene therapy has made it to become one of the hottest pots in cancer treatment. Different concepts ofCRISPR/Cas9-mediated cancer therapy, including tumor-related genes manipulating, tumor

4、immunotherapy, tumor researchmodelling and anti-cancer drug resistance overcoming are established in various cancer types.The greatest advantages of the CRISPR-Cas9 system are its simplicity and wide applicability in genome manipulations of almost allbiological systems tested to date, including cell

5、 lines, stem cells, yeasts, worms, insects, rodents, and mammals. For a targetableDNA site, only a corresponding 20 nucleotide gRNA is needed to guide the CRISPR-Cas9 to cut the target DNA at the desiredlocation. The repair of the broken DNA ends occurs either through NHEJ to generate indels, which

6、has been used to generaterandom genomic mutations or through HDR in the presence of donor oligonucleotides or DNA fragments containing homologoussequences flanking the DSB sites to generate precise site-directed nucleotide or large gene replacements, leading to generation oftargeted gene mutations o

7、r corrections.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/CRISPR/Cas9.html CRISPR/Cas9 HYPERLINK https:/www.MedChemE/Targets/CRISPR/Cas9.html HYPERLINK https:/www.MedChemE/Targets/CRISPR/Cas9.html Inhibitors, HYPERLINK https:/www.MedChemE/Targets/CRISPR/Cas9.html HYPERLINK https:/www.MedChe

8、mE/Targets/CRISPR/Cas9.html Agonists HYPERLINK https:/www.MedChemE/Targets/CRISPR/Cas9.html HYPERLINK https:/www.MedChemE/Targets/CRISPR/Cas9.html & HYPERLINK https:/www.MedChemE/Targets/CRISPR/Cas9.html HYPERLINK https:/www.MedChemE/Targets/CRISPR/Cas9.html Activators HYPERLINK https:/www.MedChemE/

9、brd0539.html BRD0539Cat. No.: HY-136251 HYPERLINK https:/www.MedChemE/Brefeldin-A.html Brefeldin HYPERLINK https:/www.MedChemE/Brefeldin-A.html HYPERLINK https:/www.MedChemE/Brefeldin-A.html A(BFA; Cyanein; Decumbin) Cat. No.: HY-16592BRD0539 is a cell-permeable and non-toxicinhibitor of CRISPR-Cas9

10、. BRD0539 inhibitsStreptococcus pyogenes Cas9 (SpCas9) (apparentIC =22 M) in an in vitro DNA cleavage assay.50Brefeldin A (BFA) is a lactone antibiotic and aspecific inhibitor of protein trafficking. BrefeldinA blocks the transport of secreted and membraneproteins from endoplasmic reticulum to Golgi

11、apparatus. Brefeldin A is also an autophagy andmitophagy inhibitor.Purity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.87%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/cas9-in-1.html Cas

12、9-IN-1 HYPERLINK https:/www.MedChemE/cas9-in-1.html HYPERLINK https:/www.MedChemE/cas9-in-2.html Cas9-IN-2Cat. No.: HY-144118 Cat. No.: HY-144119Cas9-IN-1 is a potent Cas9 inhibitor (IC =7.0250M), acting by binding to apo-Cas9 to preventCas9:gRNA complex formation.Cas9-IN-2 is a potent Cas9 inhibito

13、r (IC =24650M), Cas9-IN-2 acts by binding to apo-Cas9 toprevent Cas9:gRNA complex formation, which canpotentially be applied to modulate and controlCas9 activity in various applications.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development Reported

14、Size: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/cas9-in-3.html Cas9-IN-3 HYPERLINK https:/www.MedChemE/cas9-in-3.html HYPERLINK https:/www.MedChemE/cem114.html CEM114Cat. No.: HY-145692 Cat. No.: HY-136572Cas9-IN-3 is a potent Cas9 inhibitor (IC =2850M). CRISPR/Cas systems have revolutionized geneedi

15、ting in various species.CEM114 is an effective chemical epigenetic modifier(CEM) that recruits endogenous chromatin machinerythrough CRISPR-Cas9 systems.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:

16、/www.MedChemE/KU-57788.html KU-57788 HYPERLINK https:/www.MedChemE/KU-57788.html HYPERLINK https:/www.MedChemE/L755507.html L755507(NU7441) Cat. No.: HY-11006Cat. No.: HY-19334KU-57788 (NU7441) is a highly potent and selectiveDNA-PK inhibitor with an IC of 14 nM. KU-5778850is an NHEJ pathway inhibit

17、or. KU-57788 alsoinhibits PI3K and mTOR with IC s of 5.0 and 1.750M, respectively.L755507 is a potent, selective agonist of -AR3with an IC of 35 nM. L755507 enhances the50homology-directed repair (HDR)-mediated genomeediting in CRISPR/Cas9 nickase system.Purity: 99.35%Clinical Data: No Development R

18、eportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98.33%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg HYPERLINK https:/www.MedChemE/Nocodazole.html Nocodazole HYPERLINK https:/www.MedChemE/Nocodazole.html HYPERLINK https:/www.MedChemE/RS-1.html RS-1(Oncodazole; R17934) Cat. N

19、o.: HY-13520Cat. No.: HY-19793Nocodazole (Oncodazole) is a rapidly-reversibleinhibitor of microtubule. Nocodazole binds to-tubulin and disrupts microtubuleassembly/disassembly dynamics, which preventsmitosis and induces apoptosis in tumor cells.RS-1 is a RAD51 activator, and also increasesCRISPR/Cas

20、9-mediated knock-in efficiencies.Purity: 99.66%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mgPurity: 98.95%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.M

21、edChemE/SCR7.html SCR7 HYPERLINK https:/www.MedChemE/SCR7.html HYPERLINK https:/www.MedChemE/scr7-pyrazine.html SCR7 HYPERLINK https:/www.MedChemE/scr7-pyrazine.html HYPERLINK https:/www.MedChemE/scr7-pyrazine.html pyrazineCat. No.: HY-12742 Cat. No.: HY-107845SCR7 is an unstable form that can be au

22、tocyclizedinto a stable form SCR7 pyrazine. SCR7 pyrazine isa DNA ligase IV inhibitor that blocksnonhomologous end-joining (NHEJ) in a ligaseIV-dependent manner.SCR7 pyrazine is a DNA ligase IV inhibitor thatblocks nonhomologous end-joining (NHEJ) in aligase IV-dependent manner. SCR7 pyrazine is als

23、oa CRISPR/Cas9 enhancer which increases theefficiency of Cas9-mediated homology-directedrepair (HDR).Purity: 98.22%Clinical Data: No Development ReportedSize: 5 mgPurity: 98.70%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg HYPERLINK https:/www.MedChemE/Zidovudine.

24、html Zidovudine(Azidothymidine; AZT; ZDV) Cat. No.: HY-17413 HYPERLINK https:/www.MedChemE/zidovudine-13c-d3.html Zidovudine-13C,d3(Azidothymidine-13C,d3; AZT-13C,d3; ZDV-13C,d3) Cat. No.: HY-17413S1Zidovudine is a nucleoside reverse transcriptaseinhibitor (NRTI), widely used to treat HIVinfection. Zidovudine increasesCRISPR/Ca