Notch

抑制剂选择性比较

Notch产品

所有产品 Notch抑制剂(7)

目录号	产品描述	文献引用	实验数据
S1575	RO4929097 RO4929097是一种γ secretase抑制剂，无细胞试验中IC50为4 nM，抑制Aβ40和Notch的细胞加工，EC50分别为14 nM和5 nM。Phase 2。	Clin Cancer Res, 2020, 10.1158/1078-0432.CCR-19-3420 Theranostics, 2020, 10(6):2553-2570 Cells, 2020, 9(1)
S1594	Semagacestat (LY450139) Semagacestat (LY450139)是一种γ-分泌酶抑制剂，作用于Aβ42，Aβ40和Aβ38，IC50分别为10.9 nM，12.1 nM和12.0 nM，也抑制Notch信号通路，人神经胶质瘤细胞中IC50为14.1 nM。Phase 3。	Cancer Cell, 2020, 13;37(1):104-122e12 Sci Adv, 2019, 5(1):eaau3333 Proc Natl Acad Sci USA, 2017, 114(50):E10782-E10791	HEK/APPswe cells were either left non-treated (-) or exposed to the γ-secretase inhibitor (GSI) semagacestat (+) for 19 h prior to cell harvesting and membrane preparation (Substrate accumulation). Exposure of cells with GSI prior to membrane preparation results in higher Aβ1-42 and Aβx-42 signals as compared to membranes derived from non-GSI treated cells. Direct addition of semagacestat to the membranes in the novo Aβ production assay inhibited Aβ production (Semagacestat (1 µM)). The amount of Aβx-42 is higher than Aβ1-42 suggesting that C83 is the major substrate for the Aβ42 signal detected.
S2711	Dibenzazepine (YO-01027) Dibenzazepine (YO-01027)是一种二肽γ-secretase抑制剂，作用于APPL和Notch分裂，无细胞试验中IC50分别为2.6 nM和2.9 nM。	ACS Nano, 2020, 22 Am J Respir Cell Mol Biol, 2020, 10.1165/rcmb.2019-0069OC J Exp Clin Cancer Res, 2020, 39(1):22	Tumor spheres formation assay. Images were taken at 48 h after treating the cells with various formulations of YO (scale bar 100 um).
S2714	LY411575 LY411575是一种有效的γ-secretase抑制剂，在表达APP或NΔE的HEK293细胞中IC50为0.078 nM/0.082 nM(基于膜/细胞)，也抑制Notch分裂，IC50为0.39 nM。LY411575 可诱导凋亡。	Alzheimers Res Ther, 2020, 26;12(1):63 Biochem Biophys Res Commun, 2020, 521(4):1070-1076 Elife, 2019, 8	(E) Quantitation of lumen from A-D. (F) RNA isolated from 6d acini and expression of NOTCH1 measured by qRT-PCR in triplicate. P values are * <.01, *** <0.001.
S8280	IMR-1 IMR-1是靶向转录激活过程的新型Notch抑制剂，其IC50为26 μM。	J Infect Dis, 2019, 220(12):1977-1988 Cell Mol Neurobiol, 2019, 10.1007/s10571-019-00771-8 Int J Biochem Cell Biol, 2019, 115:105578
S7399	FLI-06 FLI-06 是一种靶向Notch信号通路的新型抑制剂，EC50是2.3 μM。	Autophagy, 2020, 16:1-24 Am J Cancer Res, 2019, 9(9):1938-1956 Onco Targets Ther, 2019, 12:7663-7674	In the presence of FLI-06 (100 nM), wound healing assay was conducted to evaluate the cell motility after transfection. Data were from three independent experiments and were Mean ± SD. values. **P < 0.01 compared to cells transfected with vector, ##P < 0.01 compared to cells transfected with ZFR. Scale bar represents 200 μm.
S7169	Crenigacestat (LY3039478) Crenigacestat (LY3039478) 是一种有效的Notch和 gamma-secretase 的抑制剂，其对Notch的IC50值为0.41 nM。	Cell Death Differ, 2020, 10.1038/s41418-020-0505-4 Mol Cancer Ther, 2020, 5 pii: molcanther Cancer Cell, 2019, 35(6):868-884.e6	Effect of LY3039478 on Hes protein in SGC7901/DDP cells. A, Protein expression of Hes-1 by Western blot. B, Expression level of Hes-1 by Western blot experiment. (p < 0.05 control with LY3039478 0 μmol/L group; *p < 0.01 control with LY3039478 0 μmol/L group).
S6668^New	NVS-ZP7-4 NVS-ZP7-4是Zinc transporter SLC39A7 (ZIP7)抑制剂，是第一个报道的、用于探测调节ER锌水平的影响并研究ZIP7作为Notch通路中的新型可药物化节点的化学工具。

目录号	产品描述	文献引用	实验数据
S1575	RO4929097 RO4929097是一种γ secretase抑制剂，无细胞试验中IC50为4 nM，抑制Aβ40和Notch的细胞加工，EC50分别为14 nM和5 nM。Phase 2。	Clin Cancer Res,2020, 10.1158/1078-0432.CCR-19-3420 Theranostics,2020, 10(6):2553-2570 Cells,2020, 9(1)
S1594	Semagacestat (LY450139) Semagacestat (LY450139)是一种γ-分泌酶抑制剂，作用于Aβ42，Aβ40和Aβ38，IC50分别为10.9 nM，12.1 nM和12.0 nM，也抑制Notch信号通路，人神经胶质瘤细胞中IC50为14.1 nM。Phase 3。	Cancer Cell,2020, 13;37(1):104-122e12 Sci Adv,2019, 5(1):eaau3333 Proc Natl Acad Sci USA,2017, 114(50):E10782-E10791	HEK/APPswe cells were either left non-treated (-) or exposed to the γ-secretase inhibitor (GSI) semagacestat (+) for 19 h prior to cell harvesting and membrane preparation (Substrate accumulation). Exposure of cells with GSI prior to membrane preparation results in higher Aβ1-42 and Aβx-42 signals as compared to membranes derived from non-GSI treated cells. Direct addition of semagacestat to the membranes in the novo Aβ production assay inhibited Aβ production (Semagacestat (1 µM)). The amount of Aβx-42 is higher than Aβ1-42 suggesting that C83 is the major substrate for the Aβ42 signal detected.
S2711	Dibenzazepine (YO-01027) Dibenzazepine (YO-01027)是一种二肽γ-secretase抑制剂，作用于APPL和Notch分裂，无细胞试验中IC50分别为2.6 nM和2.9 nM。	ACS Nano,2020, 22 Am J Respir Cell Mol Biol,2020, 10.1165/rcmb.2019-0069OC J Exp Clin Cancer Res,2020, 39(1):22	Tumor spheres formation assay. Images were taken at 48 h after treating the cells with various formulations of YO (scale bar 100 um).
S2714	LY411575 LY411575是一种有效的γ-secretase抑制剂，在表达APP或NΔE的HEK293细胞中IC50为0.078 nM/0.082 nM(基于膜/细胞)，也抑制Notch分裂，IC50为0.39 nM。LY411575 可诱导凋亡。	Alzheimers Res Ther,2020, 26;12(1):63 Biochem Biophys Res Commun,2020, 521(4):1070-1076 Elife,2019, 8	(E) Quantitation of lumen from A-D. (F) RNA isolated from 6d acini and expression of NOTCH1 measured by qRT-PCR in triplicate. P values are * <.01, *** <0.001.
S8280	IMR-1 IMR-1是靶向转录激活过程的新型Notch抑制剂，其IC50为26 μM。	J Infect Dis,2019, 220(12):1977-1988 Cell Mol Neurobiol,2019, 10.1007/s10571-019-00771-8 Int J Biochem Cell Biol,2019, 115:105578
S7399	FLI-06 FLI-06 是一种靶向Notch信号通路的新型抑制剂，EC50是2.3 μM。	Autophagy,2020, 16:1-24 Am J Cancer Res,2019, 9(9):1938-1956 Onco Targets Ther,2019, 12:7663-7674	In the presence of FLI-06 (100 nM), wound healing assay was conducted to evaluate the cell motility after transfection. Data were from three independent experiments and were Mean ± SD. values. **P < 0.01 compared to cells transfected with vector, ##P < 0.01 compared to cells transfected with ZFR. Scale bar represents 200 μm.
S7169	Crenigacestat (LY3039478) Crenigacestat (LY3039478) 是一种有效的Notch和 gamma-secretase 的抑制剂，其对Notch的IC50值为0.41 nM。	Cell Death Differ,2020, 10.1038/s41418-020-0505-4 Mol Cancer Ther,2020, 5 pii: molcanther Cancer Cell,2019, 35(6):868-884.e6	Effect of LY3039478 on Hes protein in SGC7901/DDP cells. A, Protein expression of Hes-1 by Western blot. B, Expression level of Hes-1 by Western blot experiment. (p < 0.05 control with LY3039478 0 μmol/L group; *p < 0.01 control with LY3039478 0 μmol/L group).

目录号

产品描述

文献引用

实验数据

S6668^New

NVS-ZP7-4

NVS-ZP7-4是Zinc transporter SLC39A7 (ZIP7)抑制剂，是第一个报道的、用于探测调节ER锌水平的影响并研究ZIP7作为Notch通路中的新型可药物化节点的化学工具。