目录号 | 产品详情 | 靶点 | |
---|---|---|---|
T72641 | |||
IRE1α kinase-IN-7 是一种 IRE1α抑制剂。IRE1α kinase-IN-7 能够用于内质网应激相关疾病的研究。 | |||
T63734 | |||
IRE1α kinase-IN-5 (compound 7) 是 IRE1α 的有效抑制剂 (Ki: 98 nM),是 IRE1α 的 ATP 竞争性配体。 | |||
T63511 | |||
IRE1α kinase-IN-4 (compound 6) 是一种有效的IRE1α抑制剂,Ki 为 140 nM。IRE1α kinase-IN-4 是 IRE1α 的 ATP 竞争性配体。 | |||
T62568 | IRE1 | ||
IXA6 是一种新型的IRE1/XBP1s激动剂,具有潜在的血管保护活性,可激活 IRE1-XBP1s 信号传导和 XBP1s 转录反应,可用于研究帕金森病和阿尔茨海默病等神经退行性疾病。 | |||
T14847 | Others IRE1 | ||
B I09是一种 IRE-1 RNase 抑制剂,IC50为1230 nM,对人 WaC3细胞中 XBP1 mRNA 的剪接和 LPS 刺激的 B 细胞中 xbp -1的表达有抑制作用。B I09可用于 CLL 细胞模拟XBP-1缺陷的研究。 | |||
T64049 | |||
KIRA9 是 IRE1 的有效抑制剂,对 INS-1 细胞的 IC50 值为 4.8 μM。KIRA9 可以完全结合 IRE1 的 ATP 结合位点,并阻断内质网 (ER) 定位的 mRNA 衰减和细胞凋亡 (apoptosis)。 | |||
T69410 | |||
CB5305630 is an IRE1 inhibitor. |
目录号 | 产品名/同用名 | 种属 | 表达系统 | ||
---|---|---|---|---|---|
TMPY-04753 | IRE1 Protein, Human, Recombinant (aa 465-977) | Human | Baculovirus-Insect Cells | ||
Endoplasmic reticulum stress and hypoxia are necessary components of malignant tumors growth and suppression of ERN1 (from endoplasmic reticulum to nuclei-1) signalling pathway, which is linked to the apoptosis and cell death processes, significantly decreases proliferative processes. An enhanced expression of TP53 gene in ERN1 knockdown glioma cells correlates with the decreased level of ubiquitin ligase MDM2 and increased expression level of USP7 which deubiquitinates TP53 and MDM2 and induces TP53-dependent cell growth repression and apoptosis. Thus, the expression of genes encoding TP53 and related to TP53 factors depends upon the endoplasmic reticulum stress signaling as well as on hypoxia, and correlates with suppression of glioma growth under ERN1 knockdown. The dependence of insulin-like growth binding proteins as well as IGF2BP3 and HTRA1 gene expressions in U87 glioma cells on ERN1 signaling enzyme function and hypoxia, indicating its participation in the regulation of metabolic and proliferative processes via IGF/INS receptors, because endoplasmic reticulum stress is an important component of tumor growth and metabolic diseases.
|
|||||
TMPY-04413 | IRE1 Protein, Human, Recombinant (aa 465-977, His & GST) | Human | Baculovirus-Insect Cells | ||
Endoplasmic reticulum stress and hypoxia are necessary components of malignant tumors growth and suppression of ERN1 (from endoplasmic reticulum to nuclei-1) signalling pathway, which is linked to the apoptosis and cell death processes, significantly decreases proliferative processes. An enhanced expression of TP53 gene in ERN1 knockdown glioma cells correlates with the decreased level of ubiquitin ligase MDM2 and increased expression level of USP7 which deubiquitinates TP53 and MDM2 and induces TP53-dependent cell growth repression and apoptosis. Thus, the expression of genes encoding TP53 and related to TP53 factors depends upon the endoplasmic reticulum stress signaling as well as on hypoxia, and correlates with suppression of glioma growth under ERN1 knockdown. The dependence of insulin-like growth binding proteins as well as IGF2BP3 and HTRA1 gene expressions in U87 glioma cells on ERN1 signaling enzyme function and hypoxia, indicating its participation in the regulation of metabolic and proliferative processes via IGF/INS receptors, because endoplasmic reticulum stress is an important component of tumor growth and metabolic diseases.
|
|||||
TMPH-02639 | HSPA5 Protein, Mouse, Recombinant (His) | Mouse | Yeast | ||
Endoplasmic reticulum chaperone that plays a key role in protein folding and quality control in the endoplasmic reticulum lumen. Involved in the correct folding of proteins and degradation of misfolded proteins via its interaction with DNAJC10/ERdj5, probably to facilitate the release of DNAJC10/ERdj5 from its substrate. Acts as a key repressor of the ERN1/IRE1-mediated unfolded protein response (UPR). In the unstressed endoplasmic reticulum, recruited by DNAJB9/ERdj4 to the luminal region of ERN1/IRE1, leading to disrupt the dimerization of ERN1/IRE1, thereby inactivating ERN1/IRE1. Accumulation of misfolded protein in the endoplasmic reticulum causes release of HSPA5/BiP from ERN1/IRE1, allowing homodimerization and subsequent activation of ERN1/IRE1. Plays an auxiliary role in post-translational transport of small presecretory proteins across endoplasmic reticulum (ER). May function as an allosteric modulator for SEC61 channel-forming translocon complex, likely cooperating with SEC62 to enable the productive insertion of these precursors into SEC61 channel. Appears to specifically regulate translocation of precursors having inhibitory residues in their mature region that weaken channel gating. May also play a role in apoptosis and cell proliferation.
|
|||||
TMPH-02638 | HSPA5 Protein, Mouse, Recombinant (E. coli, His) | Mouse | E. coli | ||
Endoplasmic reticulum chaperone that plays a key role in protein folding and quality control in the endoplasmic reticulum lumen. Involved in the correct folding of proteins and degradation of misfolded proteins via its interaction with DNAJC10/ERdj5, probably to facilitate the release of DNAJC10/ERdj5 from its substrate. Acts as a key repressor of the ERN1/IRE1-mediated unfolded protein response (UPR). In the unstressed endoplasmic reticulum, recruited by DNAJB9/ERdj4 to the luminal region of ERN1/IRE1, leading to disrupt the dimerization of ERN1/IRE1, thereby inactivating ERN1/IRE1. Accumulation of misfolded protein in the endoplasmic reticulum causes release of HSPA5/BiP from ERN1/IRE1, allowing homodimerization and subsequent activation of ERN1/IRE1. Plays an auxiliary role in post-translational transport of small presecretory proteins across endoplasmic reticulum (ER). May function as an allosteric modulator for SEC61 channel-forming translocon complex, likely cooperating with SEC62 to enable the productive insertion of these precursors into SEC61 channel. Appears to specifically regulate translocation of precursors having inhibitory residues in their mature region that weaken channel gating. May also play a role in apoptosis and cell proliferation.
|