IRE1
阻害剤の選択性比較
| カタログ番号 | 製品カタログ | 溶解度(25°C) | ||
|---|---|---|---|---|
| 水 | DMSO | アルコール | ||
| S1042 | Sunitinib Malate | <1 mg/mL | 15 mg/mL | <1 mg/mL |
| S7272 | 4μ8C | <1 mg/mL | 19 mg/mL | <1 mg/mL |
| S6623 | APY29 | <1 mg/mL | 32 mg/mL | '<1 mg/mL |
| S6495 | 6-Bromo-2-hydroxy-3-methoxybenzaldehyde | <1 mg/mL | 46 mg/mL | '12 mg/mL |
| S7781 | Sunitinib | <1 mg/mL | 25 mg/mL | '<1 mg/mL |
| S8875 | MKC8866 | ˂1 mg/mL | 3 mg/mL | ˂1 mg/mL |
| S7771 | STF-083010 | <1 mg/mL | 63 mg/mL | <1 mg/mL |
| S8286 | MKC-3946 | <1 mg/mL | 38 mg/mL | 3 mg/mL |
| S8658 | kira6 | <1 mg/mL | 60 mg/mL | 60 mg/mL |
IRE1製品
| 製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
|---|---|---|---|
| S1042 |
Sunitinib MalateSunitinib Malate is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM in cell-free assays, and also inhibits c-Kit. Sunitinib Malate effectively inhibits autophosphorylation of Ire1α. Sunitinib Malate increases both death receptor and 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 is a potent and selective IRE1 Rnase inhibitor with IC50 of 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.
|
|
| S6623 |
APY29APY29 is a type I kinase inhibitor of IRE1α that binds to the ATP-binding site on IRE1α and inhibits its autophosphorylation (IC50 = 280 nM) and enhances its RNase function (EC50 = 460 nM). |
||
| S6495 |
6-Bromo-2-hydroxy-3-methoxybenzaldehyde6-Bromo-2-hydroxy-3-methoxybenzaldehyde is a bromobenzaldehyde derivative that participates in the synthesis of (±)-norannuradhapurine.6-Bromo-2-hydroxy-3-methoxybenzaldehyde is an IRE-1α inhibitor with an IC50 of 0.08 μM. |
||
| S7781 |
SunitinibSunitinib (SU11248) is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM, and also inhibits c-Kit. Sunitinib is also a dose-dependent inhibitor of the autophosphorylation activity of IRE1α. Sunitinib induces autophagy and 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. |
|
| S8875新 |
MKC8866MKC8866 (IRE1-IN-8866), a salicylaldehyde analog, is a specific IRE1α RNase inhibitor with IC50 of 0.29 μM for human IRE1α in vitro. |
||
| S7771 |
STF-083010STF-083010 is a specific IRE1α endonuclease inhibitor without affecting its kinase activity. |
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 is a potent and soluble IRE1α endoribonuclease domain inhibitor which triggered modest growth inhibition in multiple myeloma cell lines, without toxicity in normal mononuclear cells. |
||
| S8658 |
kira6kira6 is a potent type II IRE1α kinase inhibitor with an IC50 of 0.6 μM. It dose-dependently inhibits IRE1α(WT) kinase activity, XBP1 RNA cleavage, Ins2 RNA cleavage and oligomerization. |
| 製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
|---|---|---|---|
| S1042 |
Sunitinib MalateSunitinib Malate is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM in cell-free assays, and also inhibits c-Kit. Sunitinib Malate effectively inhibits autophosphorylation of Ire1α. Sunitinib Malate increases both death receptor and 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 is a potent and selective IRE1 Rnase inhibitor with IC50 of 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.
|
|
| S6623 |
APY29APY29 is a type I kinase inhibitor of IRE1α that binds to the ATP-binding site on IRE1α and inhibits its autophosphorylation (IC50 = 280 nM) and enhances its RNase function (EC50 = 460 nM). |
||
| S6495 |
6-Bromo-2-hydroxy-3-methoxybenzaldehyde6-Bromo-2-hydroxy-3-methoxybenzaldehyde is a bromobenzaldehyde derivative that participates in the synthesis of (±)-norannuradhapurine.6-Bromo-2-hydroxy-3-methoxybenzaldehyde is an IRE-1α inhibitor with an IC50 of 0.08 μM. |
||
| S7781 |
SunitinibSunitinib (SU11248) is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM, and also inhibits c-Kit. Sunitinib is also a dose-dependent inhibitor of the autophosphorylation activity of IRE1α. Sunitinib induces autophagy and 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. |
|
| S8875新 |
MKC8866MKC8866 (IRE1-IN-8866), a salicylaldehyde analog, is a specific IRE1α RNase inhibitor with IC50 of 0.29 μM for human IRE1α in vitro. |
||
| S7771 |
STF-083010STF-083010 is a specific IRE1α endonuclease inhibitor without affecting its kinase activity. |
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 is a potent and soluble IRE1α endoribonuclease domain inhibitor which triggered modest growth inhibition in multiple myeloma cell lines, without toxicity in normal mononuclear cells. |
||
| S8658 |
kira6kira6 is a potent type II IRE1α kinase inhibitor with an IC50 of 0.6 μM. It dose-dependently inhibits IRE1α(WT) kinase activity, XBP1 RNA cleavage, Ins2 RNA cleavage and oligomerization. |
