Description
SCR130 is a SCR7-based DNA nonhomologous end-joining (NHEJ) inhibitor. SCR130 inhibits the end-joining of DNA in a Ligase IV-dependent manner. SCR130 is specific to Ligase IV, and shows minimal or no effect on Ligase III and Ligase I mediated joining. SCR130 induces cell apoptosis and has anticancer activity.
Product information
CAS Number: 2377858-38-1
Molecular Weight: 418.30
Formula: C19H13Cl2N3O2S
Chemical Name: 2, 4-bis(4-chlorophenyl)-8-sulfanylidene-1, 7, 9-triazaspiro[4.5]dec-1-ene-6, 10-dione
Smiles: O=C1NC(=S)NC(=O)C21N=C(CC2C1C=CC(Cl)=CC=1)C1C=CC(Cl)=CC=1
InChiKey: QEMQLCCYJLGAKB-UHFFFAOYSA-N
InChi: InChI=1S/C19H13Cl2N3O2S/c20-12-5-1-10(2-6-12)14-9-15(11-3-7-13(21)8-4-11)24-19(14)16(25)22-18(27)23-17(19)26/h1-8,14H,9H2,(H2,22,23,25,26,27)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
SCR130 (7-21 μM; 48 hours) increase in the number of late and early apoptotic cells. SCR130 induces apoptosis by both intrinsic and extrinsic pathways. SCR130 increases the expression of p-p53, BCL2 and MCL1, and CYTOCHROME C, BAX, and BAK also increaseed. The activation of caspase 8, increase in expression of FAS and SMAC-DIABLO proteins are also observed. SCR130 (48 hours) exhibits cytotoxicity in Reh, HeLa, CEM, Nalm6, and N114 cells with IC50 values of 14.1 μM, 5.9 μM, 6.5 μM, 2.2 μM, and 11 μM, respectively. SCR130 can potentiate the effect of radiation (0.5 and 1 Gy) by inducing enhanced cell death upon coadministration in Reh and Nalm6 cell lines. SCR130 blocks the endogenous NHEJ leading to accumulation of unrepaired DNA breaks. Treatment with SCR130 leads to inhibition of endogenous NHEJ, resulting in the accumulation of DNA double-strand breaks (DSBs) and cell death by activating apoptotic pathways.
Products are for research use only. Not for human use.
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