Notch
抑制剂选择性比较
Notch产品
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1575 |
RO4929097RO4929097 (RG-4733)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。 |
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| 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。 |
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. |
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| S1262 |
Avagacestat (BMS-708163)Avagacestat (BMS-708163)是口服生物有效的，选择性的γ-分泌酶抑制剂，作用于Aβ40和Aβ42时，IC50分别为0.3 nM和0.27 nM，比作用于Notch选择性高193倍。Phase 2。 |
A panel of GICs lines was treated with various concentrations of γ secretase inhibitors BMS-708163. Cells were treated with increasing concentrations of γ secretase inhibitors in triplicate wells for 72 hours, and cell viability was assessed by CellTiter-Blue assay as described in Materials and Methods. The results shown are of a single experiment with three independent replicates cell viability was measured by CellTiter-Blue assay. The graph depicts cell viability at 72 hours. Cell viability in the vehicle control was considered as to be 100%. |
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| S2711 |
Dibenzazepine (YO-01027)Dibenzazepine (YO-01027, DBZ)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。 |
Tumor spheres formation assay. Images were taken at 48 h after treating the cells with various formulations of YO (scale bar 100 um).
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| S2714 |
LY411575LY411575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。 |
(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.
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| S3376 |
RBPJ Inhibitor-1 (RIN1)RBPJ Inhibitor-1 (RIN1) 是转录因子 RBPJ 的有效抑制剂，可破坏 NOTCH 和RBPJ之间的相互作用。 |
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| S8280 |
IMR-1IMR-1是靶向转录激活过程的新型Notch抑制剂，其IC50为26 μM。 |
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| S7399 |
FLI-06FLI-06 是一种靶向Notch信号通路的新型抑制剂，EC50是2.3 μM。 |
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.
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| 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。 |
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).
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| S0225 |
IMR-1AIMR-1A 是IMR-1的酸性代谢产物，是一种 Notch 的有效的抑制剂，IC50值为0.5 μM，Kd值为2.9 μM。IMR-1A 具有抗肿瘤活性。 |
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| S9719 |
CB-103CB-103 是一种口服活性的 Notch 转录激活复合物的抑制剂。CB-103 可在果蝇和小鼠中产生Notch功能丧失的表型，并抑制人类乳腺癌和白血病异种移植瘤的生长。 |
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| S1168 |
Valproic Acid (NSC 93819) sodium saltValproic Acid sodium salt (NSC 93819, Sodium valproate)是一种HDAC选择性抑制剂，也会抑制HDAC2的蛋白酶体降解，用于治疗癫痫和躁郁症，并预防偏头痛。Valproic acid 可在小细胞肺癌细胞系中诱导 Notch1 信号转导。Valproic acid (VPA) 正用于研究治疗HIV和各种癌症的方法。Valproic acid (VPA) 通过上调 BNIP3 诱导自噬和线粒体自噬，并通过上调 PGC-1α 来诱导线粒体的生物合成。 |
Western blot analysis of Acetylated Histone and Histone. 0-10μM sodium valproate was added.
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| S3944 |
Valproic acid (VPA)Valproic acid (VPA, 2-Propylvaleric Acid, Valproate)是一种具有抗惊厥性质的脂肪酸，可用于治疗癫痫。它也是一种 histone deacetylase (HDAC) 抑制剂，正用于研究治疗HIV和各种癌症的方法。Valproic acid (VPA) 通过上调 BNIP3 诱导自噬和线粒体自噬，并通过上调 PGC-1α 来诱导线粒体的生物合成。Valproic acid (VPA) 可激活 Notch-1 信号传递。 |
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| S6668 |
NVS-ZP7-4NVS-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 |
RO4929097RO4929097 (RG-4733)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。 |
|
|
| 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。 |
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. |
|
| S1262 |
Avagacestat (BMS-708163)Avagacestat (BMS-708163)是口服生物有效的，选择性的γ-分泌酶抑制剂，作用于Aβ40和Aβ42时，IC50分别为0.3 nM和0.27 nM，比作用于Notch选择性高193倍。Phase 2。 |
A panel of GICs lines was treated with various concentrations of γ secretase inhibitors BMS-708163. Cells were treated with increasing concentrations of γ secretase inhibitors in triplicate wells for 72 hours, and cell viability was assessed by CellTiter-Blue assay as described in Materials and Methods. The results shown are of a single experiment with three independent replicates cell viability was measured by CellTiter-Blue assay. The graph depicts cell viability at 72 hours. Cell viability in the vehicle control was considered as to be 100%. |
|
| S2711 |
Dibenzazepine (YO-01027)Dibenzazepine (YO-01027, DBZ)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。 |
Tumor spheres formation assay. Images were taken at 48 h after treating the cells with various formulations of YO (scale bar 100 um).
|
|
| S2714 |
LY411575LY411575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。 |
(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.
|
|
| S3376 |
RBPJ Inhibitor-1 (RIN1)RBPJ Inhibitor-1 (RIN1) 是转录因子 RBPJ 的有效抑制剂，可破坏 NOTCH 和RBPJ之间的相互作用。 |
||
| S8280 |
IMR-1IMR-1是靶向转录激活过程的新型Notch抑制剂，其IC50为26 μM。 |
||
| S7399 |
FLI-06FLI-06 是一种靶向Notch信号通路的新型抑制剂，EC50是2.3 μM。 |
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。 |
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).
|
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| S0225 |
IMR-1AIMR-1A 是IMR-1的酸性代谢产物，是一种 Notch 的有效的抑制剂，IC50值为0.5 μM，Kd值为2.9 μM。IMR-1A 具有抗肿瘤活性。 |
||
| S9719 |
CB-103CB-103 是一种口服活性的 Notch 转录激活复合物的抑制剂。CB-103 可在果蝇和小鼠中产生Notch功能丧失的表型，并抑制人类乳腺癌和白血病异种移植瘤的生长。 |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1168 |
Valproic Acid (NSC 93819) sodium saltValproic Acid sodium salt (NSC 93819, Sodium valproate)是一种HDAC选择性抑制剂，也会抑制HDAC2的蛋白酶体降解，用于治疗癫痫和躁郁症，并预防偏头痛。Valproic acid 可在小细胞肺癌细胞系中诱导 Notch1 信号转导。Valproic acid (VPA) 正用于研究治疗HIV和各种癌症的方法。Valproic acid (VPA) 通过上调 BNIP3 诱导自噬和线粒体自噬，并通过上调 PGC-1α 来诱导线粒体的生物合成。 |
Western blot analysis of Acetylated Histone and Histone. 0-10μM sodium valproate was added.
|
|
| S3944 |
Valproic acid (VPA)Valproic acid (VPA, 2-Propylvaleric Acid, Valproate)是一种具有抗惊厥性质的脂肪酸，可用于治疗癫痫。它也是一种 histone deacetylase (HDAC) 抑制剂，正用于研究治疗HIV和各种癌症的方法。Valproic acid (VPA) 通过上调 BNIP3 诱导自噬和线粒体自噬，并通过上调 PGC-1α 来诱导线粒体的生物合成。Valproic acid (VPA) 可激活 Notch-1 信号传递。 |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S6668 |
NVS-ZP7-4NVS-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。 |
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