SCR7 |
| Catalog No.GC12106 |
SCR7 is a small molecule inhibitor of DNA Ligase IV , which inhibits the non-homologous end-joining (NHEJ) pathway by binding to the DNA binding domain (DBD) of Ligase IV .
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Cas No.: 1533426-72-0
Sample solution is provided at 25 µL, 10mM.
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SCR7 is a small molecule inhibitor of DNA Ligase IV [1] [2], which inhibits the non-homologous end-joining (NHEJ) pathway by binding to the DNA binding domain (DBD) of Ligase IV [3]. SCR7 is commonly used in cancer therapeutic research [4] and serves as a valuable tool for improving the efficiency of genome editing [5].
SCR7 exhibits concentration- and time-dependent cytotoxicity in DLBCL cells (SUDHL8) via both extrinsic and intrinsic apoptosis pathways. In SUDHL8 cells, treatment with SCR7 at 100 and 250µM for 48 and 72 hours increases mitochondrial membrane potential, causes translocation of phosphatidylserine to the cell surface, and raises the expression of double-strand break repair proteins and apoptotic markers [6].
SCR7 (10mg/kg, every alternate day for six doses, i.p.) treatment can significantly enhance the the effect of radiation in mice with Dalton's lymphoma (DLA) liquid tumors. The combination of SCR7 and ionizing radiation (IR) can markedly reduce tumor growth and improve the survival rate of tumor-bearing mice [7].
References:
[1]. Srivastava M, Nambiar M, Sharma S, et al. An inhibitor of nonhomologous end-joining abrogates double-strand break repair and impedes cancer progression. Cell. 2012 Dec 21;151(7):1474-87. doi: 10.1016/j.cell.2012.11.054.
[2]. Gkotzamanidou M, Terpos E, Bamia C, et al. DNA repair of myeloma plasma cells correlates with clinical outcome: the effect of the nonhomologous end-joining inhibitor SCR7. Blood. 2016 Sep 1;128(9):1214-25. doi: 10.1182/blood-2016-01-691618. Epub 2016 Jul 21. PMID: 27443291; PMCID: PMC5524533.
[3]. Manjunath M, Choudhary B, Raghavan SC. SCR7, a potent cancer therapeutic agent and a biochemical inhibitor of nonhomologous DNA end-joining. Cancer Rep (Hoboken). 2021 Jun;4(3):e1341. doi: 10.1002/cnr2.1341. Epub 2021 Jan 26.
[4]. Vartak SV, Swarup HA, Gopalakrishnan V, et al. Autocyclized and oxidized forms of SCR7 induce cancer cell death by inhibiting nonhomologous DNA end joining in a Ligase IV dependent manner. FEBS J. 2018 Nov;285(21):3959-3976. doi: 10.1111/febs.14661. Epub 2018 Oct 8. PMID: 30230716.
[5]. Hu Z, Shi Z, Guo X, Jiang B, Wang G, Luo D, Chen Y, Zhu YS. Ligase IV inhibitor SCR7 enhances gene editing directed by CRISPR-Cas9 and ssODN in human cancer cells. Cell Biosci. 2018 Feb 19;8:12. doi: 10.1186/s13578-018-0200-z. PMID: 29468011; PMCID: PMC5819182.
[6]. Gopalakrishnan V, Radha G, Raghavan SC, et al. Inhibitor of nonhomologous end joining can inhibit proliferation of diffuse large B-Cell lymphoma cells and potentiate the effect of ionization radiation. J Radiat Cancer Res 2018;9:93-101. DOI: 10.4103/jrcr.jrcr_9_18
[7]. Gopalakrishnan V, Sharma S, Ray U, et al. SCR7, an inhibitor of NHEJ can sensitize tumor cells to ionization radiation. Mol Carcinog. 2021 Sep;60(9):627-643. doi: 10.1002/mc.23329. Epub 2021 Jun 30.
| Cell experiment [1]: | |
Cell lines | A549 |
Preparation Method | A549 cells were treated with an increasing concentration of SCR7 (10, 50, 100, and 250µM) for 48h. Cell proliferation was then evaluated by MTT assay. The medium was then changed with MTT solution (0.5mg/ml) in DMEM or RPMI without phenol red and FBS; cells were incubated at 37°C for 30min and violet precipitate was dissolved with isopropanol. Absorbance at 550nm was measured through a Plate reader. |
Reaction Conditions | 10, 50, 100, and 250µM, 48h |
Applications | SCR7 can induced cytotoxicity in A549 cells. |
| Animal experiment [1]: | |
Animal models | BALB/c mice bearing EAC tumors |
Preparation Method | Mice bearing EAC tumors were treated with SCR7 (10mg/kg，six doses). Ki67 (a cell proliferation marker), p21 (cell cycle regulator) and apoptotic markers such as BID and Caspase 3 were measured in treated sections by immunohistochemistry. |
Dosage form | 10mg/kg, every alternate day for six doses, i.p. |
Applications | Accumulation of DSBs upon SCR7 treatment activates p53-mediated intrinsic pathway of apoptosis in BALB/c mice. |
References: | |
| Cas No. | 1533426-72-0 | SDF | |
| Chemical Name | 5,6-bis((E)-benzylideneamino)-2-thioxo-2,3-dihydropyrimidin-4(1H)-one | ||
| Canonical SMILES | S=C(NC(/N=C/C1=CC=CC=C1)=C2/N=C/C3=CC=CC=C3)NC2=O | ||
| Formula | C18H14N4OS | M.Wt | 334.39 |
| Solubility | ≥ 16.7195mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.9905 mL | 14.9526 mL | 29.9052 mL |
| 5 mM | 0.5981 mL | 2.9905 mL | 5.981 mL |
| 10 mM | 0.2991 mL | 1.4953 mL | 2.9905 mL |
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- Purity: >98.00%
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