IRE1
IRE1(肌醇需求酶1)
The serine/threonine-protein kinase/endoribonuclease inositol-requiring enzyme 1 (IRE1) is an enzyme that in humans is encoded by the ERN1 gene. IRE1 is an endoplasmic reticulum (ER) transmembrane sensor that activates UPR to maintain ER and cellular function. While mammalian IRE1 promotes cell survive, it can initiate apoptosis via decay of anti-apoptotic microRNAs.
IRE1 activation is initiated by homotypic interactions of the stress-sensing lumenal domain favoring transautophosphorylation of the kinase-extension nuclease (KEN) domain on the cytoplasmic side of the ER membrane.
IRE1/XBP-1 has been shown to regulate a variety of genes in various cell types in response to ER stress, mostly related to ER function and the secretory pathway, although the target genes vary depending on the cell type and nature of the stress stimuli.
IRE1 相关产品(23)
- GC32857GSK2850163CAS: 2121989-91-9纯度: >98.00%
GSK2850163是一个新型的肌醇需要酶-1α(IRE1α)抑制剂，它可抑制IRE1α的激酶活性和RNA酶活性，其IC50值分别为20和200nM。
- GC32889MKC8866 (IRE-1α inhibitor 1)CAS: 1338934-59-0纯度: >98.00%
MKC8866 (IRE1-IN-8866), a salicylaldehyde analog, is a specific IRE1α RNase inhibitor with IC50 of 0.29?μM for human IRE1α in vitro.
- GC34111NSC95682 (6-Bromo-2-hydroxy-3-methoxybenzaldehyde)CAS: 20035-41-0纯度: >99.50%
6-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.
- GC34205GSK2850163 hydrochlorideCAS: 2319838-09-8
GSK2850163hydrochloride是一个新型的肌醇需要酶-1α(IRE1α)抑制剂，它可抑制IRE1α的激酶活性和RNA酶活性，其IC50值分别为20和200nM。
- GC48118Sunitinib-d10CAS: 1126721-82-1纯度: >99.00%
An internal standard for the quantification of sunitinib
- GC50366AMG 18 hydrochlorideCAS: 2250019-92-0
AMG 18 hydrochloride (AMG-18 Hydrochloride) 是单选择性 IRE1α；变构减弱IRE1α的抑制剂； RNase 活性，IC50 为 5.9 nM。
- GC63513IRE1α kinase-IN-1CAS: 2328097-41-0
IRE1α kinase-IN-1 是一种高度选择性的 IRE1α (ERN1) 抑制剂，IC50 为 77 nM。IRE1α kinase-IN-1 对 IRE1α 的选择性比 IRE1β 亚型高 100 倍。IRE1α kinase-IN-1 抑制内质网诱导的 IRE1α 寡聚和自磷酸化，并抑制 IRE1α RNase 活性 (IC50=80 nM)。
- GC64232IRE1α kinase-IN-2CAS: 1414938-21-8
IRE1α kinase-IN-2 是一种有效的 IRE1α 激酶抑制剂，EC50 为 0.82 μM。IRE1α kinase-IN-2 抑制 IRE1α 激酶自磷酸化 (IC50=3.12 μM)。IRE1α kinase-IN-2 抑制 WT 细胞系 XBP1 mRNA 剪接。
| 货号 | 产品名称 | CAS号 | 纯度 | 结构 |
|---|---|---|---|---|
| GC11805 | Toyocamycin | 606-58-6 | >98.00% | |
Toyocamycin是一种腺苷类似物,是XBP1的抑制剂。 | ||||
| GC12937 | STF 083010 | 307543-71-1 | >98.00% | |
An inhibitor of IRE1 endonuclease activity | ||||
| GC14493 | 4μ8C | 14003-96-4 | >98.50% | |
4μ8C（7-Hydroxy-4-methyl-2-oxo-2H-1-benzopyran8-carboxaldehyde）是肌醇需求酶1α（IRE1α）RNAse的小分子抑制剂。 | ||||
| GC14683 | Sunitinib malate | 341031-54-7 | >99.00% | |
A multi-kinase inhibitor | ||||
| GC17139 | APY29 | 1216665-49-4 | >99.50% | |
A modulator of IRE1α function | ||||
| GC17651 | Sunitinib | 557795-19-4 | >99.00% / >98.00% | |
舒尼替尼Sunitinib（SU 11248）是一种具口服活性的多靶点受体酪氨酸激酶抑制剂，对血管内皮生长因子受体（VEGFR2）和血小板衍生生长因子受体（PDGFRβ）的IC 50 分别为80nM和2nM。 | ||||
| GC18303 | MKC-3946 | 1093119-54-0 | >99.50% | |
An inhibitor of IRE1α | ||||
| GC19212 | KIRA6 | 1589527-65-0 | >99.50% | |
An IRE1α RNase inhibitor | ||||
| GC31879 | Kira8 | 1630086-20-2 | >99.50% | |
Kira8 (Ire-1 inhibitor, AMG-18) is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC50 of 5.9 nM. | ||||
| GC32857 | GSK2850163 | 2121989-91-9 | >98.00% | |
GSK2850163是一个新型的肌醇需要酶-1α(IRE1α)抑制剂，它可抑制IRE1α的激酶活性和RNA酶活性，其IC50值分别为20和200nM。 | ||||
| GC32889 | MKC8866 (IRE-1α inhibitor 1) | 1338934-59-0 | >98.00% | |
MKC8866 (IRE1-IN-8866), a salicylaldehyde analog, is a specific IRE1α RNase inhibitor with IC50 of 0.29?μM for human IRE1α in vitro. | ||||
| GC32910 | MKC9989 | 1338934-20-5 | >98.00% | |
MKC9989是一种HAA抑制剂，且能抑制IRE1α其IC50值在0.23μM至44μM的范围之间。 | ||||
| GC33406 | B I09 | 1607803-67-7 | >99.50% | |
BI09是IRE-1核糖核酸酶的一个抑制剂，其IC50值为1230nM。 | ||||
| GC34111 | NSC95682 (6-Bromo-2-hydroxy-3-methoxybenzaldehyde) | 20035-41-0 | >99.50% | |
6-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. | ||||
| GC34205 | GSK2850163 hydrochloride | 2319838-09-8 | - | |
GSK2850163hydrochloride是一个新型的肌醇需要酶-1α(IRE1α)抑制剂，它可抑制IRE1α的激酶活性和RNA酶活性，其IC50值分别为20和200nM。 | ||||
| GC34384 | 3,6-DMAD hydrochloride | - | >99.00% | |
3,6-DMADhydrochloride是未折叠蛋白质应答(IRE1α-XBP1)通路的抑制剂。 | ||||
| GC48118 | Sunitinib-d10 | 1126721-82-1 | >99.00% | |
An internal standard for the quantification of sunitinib | ||||
| GC50366 | AMG 18 hydrochloride | 2250019-92-0 | - | |
AMG 18 hydrochloride (AMG-18 Hydrochloride) 是单选择性 IRE1α；变构减弱IRE1α的抑制剂； RNase 活性，IC50 为 5.9 nM。 | ||||
| GC63513 | IRE1α kinase-IN-1 | 2328097-41-0 | - | |
IRE1α kinase-IN-1 是一种高度选择性的 IRE1α (ERN1) 抑制剂，IC50 为 77 nM。IRE1α kinase-IN-1 对 IRE1α 的选择性比 IRE1β 亚型高 100 倍。IRE1α kinase-IN-1 抑制内质网诱导的 IRE1α 寡聚和自磷酸化，并抑制 IRE1α RNase 活性 (IC50=80 nM)。 | ||||
| GC63785 | IXA4 | 1185329-96-7 | >98.00% | |
IXA4是一种高选择性、无毒的IRE1/XBP1s激活剂，可诱导内质网（ER）蛋白质稳态重塑。 | ||||
| GC64232 | IRE1α kinase-IN-2 | 1414938-21-8 | - | |
IRE1α kinase-IN-2 是一种有效的 IRE1α 激酶抑制剂，EC50 为 0.82 μM。IRE1α kinase-IN-2 抑制 IRE1α 激酶自磷酸化 (IC50=3.12 μM)。IRE1α kinase-IN-2 抑制 WT 细胞系 XBP1 mRNA 剪接。 | ||||
| GC64238 | KIRA-7 | 1937235-76-1 | - | |
KIRA-7 是一种咪唑并吡嗪化合物，可与 IRE1α 激酶结合 (IC50 为 110 nM) 以变构方式抑制其 RNase 活性。KIRA-7 具有抗纤维化作用。 | ||||
| GC73484 | Z4P | 2361760-87-2 | >99.00% | |
Z4P是一种可渗透bbb的IRE1抑制剂（IC50: 1.11 μM）。 | ||||