IRE1

抑制剂选择性比较

IRE1产品

所有产品(9) IRE1抑制剂(9)

目录号	产品描述	文献引用	实验数据
S1042	Sunitinib Malate Sunitinib Malate (SU 11248)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。	Adv Sci (Weinh), 2021, 8(2):2001596 Drug Metab Dispos, 2021, 49(1):53-61 Mol Med Rep, 2021, 23(1)40	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	4μ8C 4μ8C (IRE1 Inhibitor III)是高效的选择性IRE1 Rnase抑制剂，IC50为76 nM。	Cancer Lett, 2020, 28;476:67-74 Front Cell Dev Biol, 2020, 8:269 Oncol Rep, 2020, 43(4):1245-1255	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	APY29 APY29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)。
S6495	6-Bromo-2-hydroxy-3-methoxybenzaldehyde 6-Bromo-2-hydroxy-3-methoxybenzaldehyde是对溴苯甲醛派生物，参与(±)-norannuradhapurine的合成。6-Bromo-2-hydroxy-3-methoxybenzaldehyde 是一种 IRE-1α 的抑制剂，其IC50值为0.08 μM。
S7781	Sunitinib Sunitinib (SU11248) 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。	Cancers (Basel), 2021, 13(2)E361 Drug Metab Dispos, 2021, 49(1):53-61 Mol Med Rep, 2021, 23(1)40	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^New	MKC8866 MKC8866 (IRE1-IN-8866)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-083010 STF-083010是一种特异性IRE1α endonuclease抑制剂，而不影响其激酶活性。	Front Oncol, 2020, 10:589112 Sci Rep, 2020, 10(1):9666 Am J Transl Res, 2020, 12(12):7885-7898	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-3946 MKC3946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	kira6 Kira6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。	Biochim Biophys Acta Mol Cell Biol Lipids, 2020, S1388-1981(20)30217-1 ACS Infect Dis, 2020, 21 Transbound Emerg Dis, 2020, 67(4):1492-1506

目录号	产品描述	文献引用	实验数据
S1042	Sunitinib Malate Sunitinib Malate (SU 11248)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。	Adv Sci (Weinh),2021, 8(2):2001596 Drug Metab Dispos,2021, 49(1):53-61 Mol Med Rep,2021, 23(1)40	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	4μ8C 4μ8C (IRE1 Inhibitor III)是高效的选择性IRE1 Rnase抑制剂，IC50为76 nM。	Cancer Lett,2020, 28;476:67-74 Front Cell Dev Biol,2020, 8:269 Oncol Rep,2020, 43(4):1245-1255	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	APY29 APY29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)。
S6495	6-Bromo-2-hydroxy-3-methoxybenzaldehyde 6-Bromo-2-hydroxy-3-methoxybenzaldehyde是对溴苯甲醛派生物，参与(±)-norannuradhapurine的合成。6-Bromo-2-hydroxy-3-methoxybenzaldehyde 是一种 IRE-1α 的抑制剂，其IC50值为0.08 μM。
S7781	Sunitinib Sunitinib (SU11248) 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。	Cancers (Basel),2021, 13(2)E361 Drug Metab Dispos,2021, 49(1):53-61 Mol Med Rep,2021, 23(1)40	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^New	MKC8866 MKC8866 (IRE1-IN-8866)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-083010 STF-083010是一种特异性IRE1α endonuclease抑制剂，而不影响其激酶活性。	Front Oncol,2020, 10:589112 Sci Rep,2020, 10(1):9666 Am J Transl Res,2020, 12(12):7885-7898	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-3946 MKC3946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	kira6 Kira6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。	Biochim Biophys Acta Mol Cell Biol Lipids,2020, S1388-1981(20)30217-1 ACS Infect Dis,2020, 21 Transbound Emerg Dis,2020, 67(4):1492-1506

Tags: IRE1 inhibitor | IRE1 modulator | IRE1 stress