ire1α

IRE1α kinase-IN-1 is a highly selective IRE1α (ERN1) inhibitor, with an IC50 of 77 nM, displaying 100-fold selectivity over the IRE1β isoform. It inhibits ER stress-induced IRE1α oligomerization and autophosphorylation, as well as IRE1α RNase activity (IC50=80 nM).

GSK2850163 is a novel inhibitor of inositol-requiring enzyme-1 alpha (IRE1α), effectively inhibiting both its RNase activity and IRE1α kinase activity (IC50s: 200 and 20 nM).

6-Bromo-2-hydroxy-3-methoxybenzaldehyde (NSC-95682) is an inhibitor of IRE-1α with an IC50 value of 0.08 μM.

Kira8 Hydrochloride is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC50 of 5.9 nM.

Kira8 (AMG-18) is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC50 of 5.9 nM.

MKC9989 is an inhibitor of Hydroxy aryl aldehydes (HAA). MKC9989 also inhibits IRE1α with an IC50 of 0.23 to 44 μM.

APY29 is an allosteric modulator of IRE1α; inhibits IRE1α autophosphorylation (IC50 = 280 nM) and activates IRE1α RNase activity.

IRE1α kinase-IN-2 is a highly potent inhibitor of IRE1α kinase, demonstrating an EC50 of 0.82 μM and impeding IRE1α kinase autophosphorylation with an IC50 of 3.12 μM. It also effectively inhibits the splicing of XBP1 mRNA in wild-type cell lines.

IRE1α kinase-IN-6 is a potent IRE1α inhibitor with an IC50 value of 4.4 nM.

STF-083010 is a selective inhibitor of the IRE1α endonuclease.

IRE1α kinase-IN-8, a benzoheterocyclecarboxaldehyde derivative, is a potent inhibitor of IRE-1α used in research on diseases related to the unfolded protein response and regulated IRE1-dependent decay (RIDD) [1].

IRE1α kinase-IN-9 (compound 2) is a potent inhibitor of IRE-1α with an average IC50 value of less than 0.1 μM, and it is suitable for research into diseases related to the unfolded protein response or regulated IRE1-dependent decay (RIDD) [1].

KIRA6 is an effective inhibitor of IRE1α RNase kinase (IC50: 0.6 μM). It can trigger an apoptotic response.

MKC3946 is an effective and soluble IRE1α inhibitor which triggered modest growth inhibition in multiple myeloma cell lines.

IRE1α kinase-IN-4 (compound 6) is a potent IRE1α inhibitor with a Ki value of 140 nM, functioning as an ATP-competitive ligand for IRE1α [1].

IRE1α kinase-IN-5 (compound 7) is a potent ATP-competitive inhibitor of IRE1α with a Ki value of 98 nM.

IRE1α kinase-IN-3 is a potent, ATP-competitive inhibitor of IRE1α (Ki: 480 nM).

IRE1α kinase-IN-7 is a chemical compound functioning as an inhibitor of IRE1α kinase, primarily utilized in the research of diseases related to endoplasmic reticulum stress.

D-F07 is a novel fluorescent IRE-1 RNase inhibitor and a tricyclic chromone with potential anticancer activity.

3,6-DMAD dihydrochloride is an acridine derivative and a potent inhibitor of the IRE1α-XBP1s pathway. 3,6-DMAD dihydrochloride can induce IL-6 secretion by exploiting the IRE1α-XBP1s pathway. 3,6-DMAD dihydrochloride is a potent inhibitor of the IRE1α-XBP1s pathway. 3,6-DMAD dihydrochloride has inhibitory effects on IRE1α oligomerization and RNase activity. 3,6-DMAD dihydrochloride can be used in cancer research.

B I09, an IRE-1 RNase inhibitor with an IC50 of 1230 nM, inhibits splicing of XBP1 mRNA in human WaC3 cells and expression of xbp-1 in LPS-stimulated B cells. B I09 can be used to simulate the defects of XBP-1 in CLL cells., an IRE-1 RNase inhibitor with an IC50 of 1230 nM, inhibits splicing of XBP1 mRNA in human WaC3 cells and expression of xbp-1 in LPS-stimulated B cells. B I09 can be used to simulate the defects of XBP-1 in CLL cells., an IRE-1 RNase inhibitor with an IC50 of 1230 nM, inhibits splicing of XBP1 mRNA in human WaC3 cells and expression of xbp-1 in LPS-stimulated B cells. B I09 can be used to simulate the defects of XBP-1 in CLL cells.

GSK2850163 (S enantiomer) is the inactive enantiomer of GSK2850163. GSK2850163 is an novel inhibitor of inositol-requiring enzyme-1 alpha (IRE1a).

Sunitinib Malate (Sunitinib) is an indolinone-based tyrosine kinase inhibitor. It blocks the tyrosine kinase activities of VEGFR2, PDGFRβ (IC50: 80/2 nM), and c-kit.

Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase (RTK) inhibitor that inhibits VEGFR2 and PDGFRβ (IC50=80/2 nM). It exhibits antitumor activity and is used for treating kidney cancer and gastrointestinal tumors.