SCR7 DNA/RNA Synthesis inhibitor

Cat.No.S7742

SCR7 is a specific DNA Ligase IV inhibitor, which blocks nonhomologous end-joining (NHEJ). It increases the efficiency of HDR-mediated genome editing up to 19-fold using CRISPR/Cas9 in mammalian cells and mouse embryos.
SCR7 DNA/RNA Synthesis inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 332.38

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Quality Control

Batch: Purity: 99.99%
99.99

Solubility

In vitro
Batch:

DMSO : 66 mg/mL (198.56 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 23 mg/mL

Water : Insoluble

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In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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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.

Chemical Information, Storage & Stability

Molecular Weight 332.38 Formula

C18H12N4OS

Storage (From the date of receipt)
CAS No. 14892-97-8 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles C1=CC=C(C=C1)C2=NC3=C(NC(=S)NC3=O)N=C2C4=CC=CC=C4

Mechanism of Action

Targets/IC50/Ki
DNA Ligase IV
In vitro

SCR7 effectively inhibits the formation of multimers at 200 μM and above. This compound successfully inhibits cell proliferation of MCF7, A549, HeLa, T47D, A2780, HT1080, and Nalm6 with IC50 of 40, 34, 44, 8.5, 120, 10, and 50 μM, respectively. It suppresses the NHEJ repair of CRISPR-Cas9-induced DSBs.This chemical increases the efficiency of HDR-mediated genome editing up to 19-fold using CRISPR/Cas9 in mammalian cells and mouse embryos.

Kinase Assay
Complementation of SCR7 Inhibition with Purified Ligase IV
Complementation experiment is carried out by adding increasing concentrations of purified Ligase IV/XRCC4 complex (30, 60, and 120 fmol) along with the oligomeric DNA substrates (5’ compatible and 5’-5’ noncompatible ends) to the SCR7-treated extracts. Reactions are incubated for 2 h at 25℃. The reaction products are then resolved on 8% denaturing PAGE. The gel is dried and exposed and the signal is detected with a PhosphorImager and analyzed with Multi Gauge (V3.0) software.
In vivo

SCR7 treatment (10 mg/kg, i.m.) significantly reduces breast adenocarcinoma-induced tumor, and exhibits 4-fold increase in lifespan compared with control group. However, in Swiss albino mice with Dalton’s lymphoma tumor model, this compound (20 mg/kg, i.p.) exhibits neither tumor regression nor increase in lifespan. In BALB/c mice, this chemical (20 mg/kg, i.p.) significantly enhances the cytotoxic effects of radiation, VP-16213 and 3-Aminobenzamide on tumor derived from Dalton’s lymphoma (DLA) cells.

References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03941483 Completed
Acute Kidney Injury (AKI)
Astellas Pharma Inc
November 1 2019 Phase 2

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Handling Instructions

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Frequently Asked Questions

Question 1:
What should I do if I got precipitate out of solution after a freeze thaw and cannot re-suspend it?

Answer:
Some compounds will precipitate out of solution after freeze/thaw, especially at very high concentration. You can warm it up to 45 degree and sonicate it to help it dissolve, of course, adding more DMSO will help too.

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