Pom-8PEG, an E3 ligase ligand-linker conjugate, incorporates a cereblon (CRBN) ligand for the E3 ubiquitin ligase and an 8-unit PEG linker. Pom-8PEG can be used in the synthesis of PROTAC, such as IDO1 PROTAC degrader[1].
IC50 & Target[1]
Cereblon
分子量
625.66
Formula
C29H43N3O12
CAS 号
2488761-03-9
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Hu M, et al. Discovery of the first potent proteolysis targeting chimera (PROTAC) degrader of indoleamine 2,3-dioxygenase 1. Acta Pharm Sin B. 2020;10(10):1943-1953.
Pom-8PEG, an E3 ligase ligand-linker conjugate, incorporates a cereblon (CRBN) ligand for the E3 ubiquitin ligase and an 8-unit PEG linker. Pom-8PEG can be used in the synthesis of PROTAC, such as IDO1 PROTAC degrader[1].
IC50 & Target[1]
Cereblon
分子量
625.66
Formula
C29H43N3O12
CAS 号
2488761-03-9
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Hu M, et al. Discovery of the first potent proteolysis targeting chimera (PROTAC) degrader of indoleamine 2,3-dioxygenase 1. Acta Pharm Sin B. 2020;10(10):1943-1953.
Pom-8PEG, an E3 ligase ligand-linker conjugate, incorporates a cereblon (CRBN) ligand for the E3 ubiquitin ligase and an 8-unit PEG linker. Pom-8PEG can be used in the synthesis of PROTAC, such as IDO1 PROTAC degrader[1].
IC50 & Target[1]
Cereblon
分子量
625.66
Formula
C29H43N3O12
CAS 号
2488761-03-9
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Hu M, et al. Discovery of the first potent proteolysis targeting chimera (PROTAC) degrader of indoleamine 2,3-dioxygenase 1. Acta Pharm Sin B. 2020;10(10):1943-1953.
SCR130 是一种基于 SCR7 的 DNA 非同源末端连接 (NHEJ) 抑制剂。SCR130 以依赖连接酶 IV 的方式抑制 DNA 的末端连接。SCR130 对连接酶 IV 具有特异性,对连接酶 III 和连接酶 I 介导的连接的影响很小或没有影响。SCR130 诱导细胞凋亡 (apoptosis),并具有抗癌活性。
SCR130 Chemical Structure
CAS No. : 2377858-38-1
规格
价格
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数量
5 mg
¥8500
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10 mg
¥13600
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询价
100 mg
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SCR130 相关产品
•相关化合物库:
Bioactive Compound Library Plus
Apoptosis Compound Library
Cell Cycle/DNA Damage Compound Library
Anti-Cancer Compound Library
Anti-Aging Compound Library
Targeted Diversity Library
生物活性
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[1].
体外研究 (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[1]. 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[1]. 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[1]. 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[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Apoptosis Analysis[1]
Cell Line:
Reh cells
Concentration:
7 μM, 14 μM, and 21 μM
Incubation Time:
48 hours
Result:
Showed a concentration-dependent increase in the number of late and early apoptotic cells.
Western Blot Analysis[1]
Cell Line:
Reh cells
Concentration:
7 μM, 14 μM, and 21 μM
Incubation Time:
48 hours
Result:
Revealed a concentration-dependent increase in levels of pATM and activation of p53 through phosphorylation.
分子量
418.30
Formula
C19H13Cl2N3O2S
CAS 号
2377858-38-1
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder
-20°C
3 years
4°C
2 years
In solvent
-80°C
6 months
-20°C
1 month
溶解性数据
In Vitro:
DMSO : 100 mg/mL (239.06 mM; Need ultrasonic and warming)
[1]. Ujjayinee Ray, et al. Identification and characterization of novel SCR7-based small-molecule inhibitor of DNA end-joining, SCR130 and its relevance in cancer therapeutics. Mol Carcinog. 2020 Jun;59(6):618-628.