IRE1
抑制剂选择性比较
IRE1产品
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1042 |
Sunitinib MalateSunitinib Malate是一种多靶点RTK抑制剂，作用于VEGFR2 (Flk-1)和 PDGFRβ，在无细胞试验中IC50分别为80 nM 和2 nM，也会抑制c-Kit的活性。Sunitinib Malate 可有效地抑制 Ire1α 的自身磷酸化。Sunitinib Malate 可增加 death receptor 和 线粒体依赖的凋亡 mitochondrial-dependent apoptosis。 |
Sunitinib decreases FLT-3 and RET phosphor ylation but increases ERK phosphorylation in a time-dependent manner. H295R and SW13 cells were treated with sunitinib (10 nM) for various time points as indi-cated. Cell lysates were prepared and phospho-FLT-3, RET, and ERK levels were monitored by Western Blot-ting. Re-probing against FLT-3, RET, and ERK was done to ensure equal protein loading. |
|
| S7272 |
4μ8C4μ8C是高效的选择性IRE1 Rnase抑制剂，IC50为76 nM。 |
H Representative immunofluorescence staining of TUNEL. Scale bars, 100 µm. I Representative images of DHE staining. Scale bars, 100 µm. Data are mean ± SEM, *p < 0.05, **p < 0.01, ***p < 0.001 by unpaired Student's t-test.
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| S6623New |
APY29APY29是一种I类IRE1α抑制剂，与IRE1α的ATP结合位点相结合，抑制其自我磷酸化(IC50 = 280 nM)、增强其RNase作用(EC50 = 460 nM)。 |
||
| S6495New |
6-Bromo-2-hydroxy-3-methoxybenzaldehyde6-Bromo-2-hydroxy-3-methoxybenzaldehyde是对溴苯甲醛派生物，参与(±)-norannuradhapurine的合成。 |
||
| S7781 |
SunitinibSunitinib 是一种多靶点 RTK 抑制剂，以VEGFR2(Flk-1)和PDGFRβ为靶点，IC50为80 nM 和 2 nM，对c-Kit也有抑制作用。Sunitinib 还是 IRE1α 的自磷酸化活性的剂量依赖性抑制剂。 舒尼替尼可诱导自噬和细胞凋亡。 |
Sunitinib decreases FLT-3 and RET phosphor ylation but increases ERK phosphorylation in a time-dependent manner. H295R and SW13 cells were treated with sunitinib (10 nM) for various time points as indi-cated. Cell lysates were prepared and phospho-FLT-3, RET, and ERK levels were monitored by Western Blot-ting. Re-probing against FLT-3, RET, and ERK was done to ensure equal protein loading. |
|
| S8875New |
MKC8866MKC8866 是一种水杨醛类似物，一个具有特异性的 IRE1α RNase 抑制剂，在体外实验中对人 IRE1α 的IC50值为0.29 μM。 |
||
| S7771 |
STF-083010STF-083010是一种特异性IRE1α endonuclease抑制剂，而不影响其激酶活性。 |
The effect of TUDCA and STF-083010 on mouse decidualization.(B) The average weight of implantation sites on day 8 under TUDCA treatment.(D) The effect of TUDCA treatment on the weight of deciduoma. (F) The average weight of implantation sites on day 8 under STF-083010 treatment. (H) The effect of STF-083010 treatment on the weight of deciduoma. (I) The effect of TUDCA on the mRNA expression of Dtprp in vitro decidualization. (J) The effect of STF-083010 on the mRNA expression of Dtprp in vitro decidualization. Data are presented as the mean ± SD, *p < 0.05. |
|
| S8286 |
MKC-3946MKC3946是IRE1α endoribonuclease domain的可溶性抑制剂，在多种骨髓瘤细胞株中引起适度的生长抑制作用，而不对正常单核细胞具有毒性作用。 |
||
| S8658 |
kira6Kira6是有效的II型IRE1α激酶抑制剂，IC50为0.6 μM。它能够浓度依赖性地抑制IRE1α(WT)激酶活性、XBP1 RNA剪接、Ins2 RNA剪接和寡聚化。 |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1042 |
Sunitinib MalateSunitinib Malate是一种多靶点RTK抑制剂，作用于VEGFR2 (Flk-1)和 PDGFRβ，在无细胞试验中IC50分别为80 nM 和2 nM，也会抑制c-Kit的活性。Sunitinib Malate 可有效地抑制 Ire1α 的自身磷酸化。Sunitinib Malate 可增加 death receptor 和 线粒体依赖的凋亡 mitochondrial-dependent apoptosis。 |
Sunitinib decreases FLT-3 and RET phosphor ylation but increases ERK phosphorylation in a time-dependent manner. H295R and SW13 cells were treated with sunitinib (10 nM) for various time points as indi-cated. Cell lysates were prepared and phospho-FLT-3, RET, and ERK levels were monitored by Western Blot-ting. Re-probing against FLT-3, RET, and ERK was done to ensure equal protein loading. |
|
| S7272 |
4μ8C4μ8C是高效的选择性IRE1 Rnase抑制剂，IC50为76 nM。 |
H Representative immunofluorescence staining of TUNEL. Scale bars, 100 µm. I Representative images of DHE staining. Scale bars, 100 µm. Data are mean ± SEM, *p < 0.05, **p < 0.01, ***p < 0.001 by unpaired Student's t-test.
|
|
| S6623New |
APY29APY29是一种I类IRE1α抑制剂，与IRE1α的ATP结合位点相结合，抑制其自我磷酸化(IC50 = 280 nM)、增强其RNase作用(EC50 = 460 nM)。 |
||
| S6495New |
6-Bromo-2-hydroxy-3-methoxybenzaldehyde6-Bromo-2-hydroxy-3-methoxybenzaldehyde是对溴苯甲醛派生物，参与(±)-norannuradhapurine的合成。 |
||
| S7781 |
SunitinibSunitinib 是一种多靶点 RTK 抑制剂，以VEGFR2(Flk-1)和PDGFRβ为靶点，IC50为80 nM 和 2 nM，对c-Kit也有抑制作用。Sunitinib 还是 IRE1α 的自磷酸化活性的剂量依赖性抑制剂。 舒尼替尼可诱导自噬和细胞凋亡。 |
Sunitinib decreases FLT-3 and RET phosphor ylation but increases ERK phosphorylation in a time-dependent manner. H295R and SW13 cells were treated with sunitinib (10 nM) for various time points as indi-cated. Cell lysates were prepared and phospho-FLT-3, RET, and ERK levels were monitored by Western Blot-ting. Re-probing against FLT-3, RET, and ERK was done to ensure equal protein loading. |
|
| S8875New |
MKC8866MKC8866 是一种水杨醛类似物，一个具有特异性的 IRE1α RNase 抑制剂，在体外实验中对人 IRE1α 的IC50值为0.29 μM。 |
||
| S7771 |
STF-083010STF-083010是一种特异性IRE1α endonuclease抑制剂，而不影响其激酶活性。 |
The effect of TUDCA and STF-083010 on mouse decidualization.(B) The average weight of implantation sites on day 8 under TUDCA treatment.(D) The effect of TUDCA treatment on the weight of deciduoma. (F) The average weight of implantation sites on day 8 under STF-083010 treatment. (H) The effect of STF-083010 treatment on the weight of deciduoma. (I) The effect of TUDCA on the mRNA expression of Dtprp in vitro decidualization. (J) The effect of STF-083010 on the mRNA expression of Dtprp in vitro decidualization. Data are presented as the mean ± SD, *p < 0.05. |
|
| S8286 |
MKC-3946MKC3946是IRE1α endoribonuclease domain的可溶性抑制剂，在多种骨髓瘤细胞株中引起适度的生长抑制作用，而不对正常单核细胞具有毒性作用。 |
||
| S8658 |
kira6Kira6是有效的II型IRE1α激酶抑制剂，IC50为0.6 μM。它能够浓度依赖性地抑制IRE1α(WT)激酶活性、XBP1 RNA剪接、Ins2 RNA剪接和寡聚化。 |
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