ire1α rnase

4μ8C (IRE1 Inhibitor III)(IC50=76 nM) is an effective and specific IRE1 Rnase inhibitor.

MKC8866 is a selective IRE1 RNase inhibitor (IC50: 0.29 μM in human vitro). MKC8866 inhibits IRE1 RNase in breast cancer cells leading to the decreased production of pro-tumorigenic factors and it can inhibit prostate cancer (PCa) tumor growth.

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.

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).

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.

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

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

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).

PAIR2 is a potent, selective partial antagonist of IRE1α RNase, effectively occupying the ATP-binding site of IRE1α in cells. This action prevents a potent KIRA from inhibiting XBP1 splicing [1].

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

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

KIRA-7 is an imidazopyrazine compound. KIRA-7 has an anti-fibrotic effect. KIRA-7 binds the IRE1α kinase (IC50: 110 nM) to allosterically inhibit its RNase activity.