Insulin Receptor Inhibitor

D-(+)-Sorbose, an active enantiomer of D-Sorbose, which inhibits disaccharidase activity and demonstrates suppressive action on postprandial blood levels of glucose and insulin in the rat. D-sorbose acts as a sweetener may contribute to the prevention of lifestyle-related diseases, such as type 2 diabetes mellitus.

Ersodetug is an anti-INSR (insulin receptor) human IgG2 κ monoclonal antibody. Recommend Isotype Controls: Human IgG2 kappa, Isotype Control (HY-P99002).

AGL-2263 is an insulin receptor and insulin-like growth factor (IGF) receptor inhibitor.

MID-1 is a disruptor of MG53-IRS-1 (Mitsugumin 53-insulin receptor substrate-1) interaction. MID-1 disrupts molecular association of MG53 with IRS-1 and abolishes MG53-induced IRS-1 ubiquitination and degradation in skeletal muscle, leading to elevated IRS-1 expression level and increased insulin signaling and glucose uptake.

Olatorepatide (Olatorepatidum) is a dual gastric inhibitory polypeptide (GIP) receptor and glucagon like peptide 1 (GLP-1) receptor agonist, with antidiabetic effect.

IMP2-IN-2 (compound 6) is a potent and selective IMP2 inhibitor, with IC₅₀s of 120.9 μM and 236.7 μM for IMP2 interaction with RNA_A and RNA_B, respectively. IMP2-IN-2 can be used for the research of cancer.

Ceritinib (LDK378)-d₇ is a deuterium labeled Ceritinib (HY-15656). Ceritinib is a selective, orally bioavailable and ATP-competitive ALK tyrosine kinase inhibitor. Ceritinib is a selective, orally bioavailable, and ATP-competitive ALK tyrosine kinase inhibitor with an IC₅₀ of 200 pM. Ceritinib also inhibits IGF-1R, InsR, and STK22D with IC₅₀ values of 8, 7, and 23 nM, respectively. Ceritinib shows great antitumor potency.

CEP-14513 is an ALK inhibitor with an IC₅₀ of 4 nM. CEP-14513 also inhibits insulin receptor, VEGFR2, TIE2 and DLK kinases, but does not inhibit MET, IKKβ, or CDK1/2/5. CEP-14513 induces cancer cell apoptosis. CEP-14513 is applicable to research related to non-small cell lung cancer, anaplastic large cell lymphoma, inflammatory myofibroblastic tumor, and diffuse large B-cell lymphoma.

NVP-AEW541 dihydrochloride (AEW541 dihydrochloride) is an orally active inhibitor of the insulin-like growth factor 1 receptor (IGF-1R) with an IC₅₀ value of 0.15 μM. NVP-AEW541 dihydrochloride also inhibits InsR, IC₅₀ with a value of 0.14 μM. NVP-AEW541 dihydrochloride has antitumor activity.

AGT-182 (HIRMab; SHP-631; TAK-531) is a brain-penetrating anti-human insulin receptor antibody and iduronate-2-sulfatase conjugation. AGT-182 can be used for the research of mucopolysaccharidosis type II (MPS II, Hunter syndrome).

ALK-IN-24 is an orally active ALK inhibitor with an IC₅₀ value of 1.7 nM. ALK-IN-24 also inhibits insulin receptor kinase with an IC₅₀ value of 6 nM. ALK-IN-24 suppresses the proliferation of lung adenocarcinoma cells. ALK-IN-24 inhibits ALK-driven tumor growth in xenograft mouse models. ALK-IN-24 can be used in research related to non-small cell lung cancer.

Glybuzole (Desaglybuzole) is an orally effective hypoglycemic agent. Glybuzole promotes insulin secretion by pancreatic β cells and inhibits glucagon secretion by pancreatic α cells. Glybuzole reduces blood glucose levels as well as arginine-stimulated plasma glucagon levels. Glybuzole can be used in diabetes-related research.

Aganirsen sodium is a 25 mer DNA antisense oligonucleotide, which silences expression of insulin receptor substrate-1 (IRS-1).

C-Peptide 2, rat, 31-amino-acid peptide, is a component of proinsulin. C-Peptide 2, rat can inhibit glucose-induced insulin secretion.

D-Galactose pentaacetate inhibits leucine-induced insulin release. D-Galactose pentaacetate can be used for the research of persistent hyperinsulinemia in childhood or insulinoma.

HNMPA is a membrane impermeable insulin receptor tyrosine kinase inhibitor. HNMPA inhibits serine and tyrosine autophosphorylation by the human insulin receptor. HNMPA has no effect on protein kinase C or cyclic AMP-dependent protein kinase activities

Pancreastatin (37-52), human is a pancreastatin fragment. Pancreastatin a CgA-derived peptide (CgA residues 250–301) with biological activity, inhibited the releasing of insulin by islet beta cells.

IMP2-IN-3 is a potent IMP2 inhibitor. IMP2-IN-3 shows anticancer effects.

Ceritinib (LDK378) mesylate is a selective, orally bioavailable, and ATP-competitive ALK tyrosine kinase inhibitor with an IC₅₀ of 200 pM. Ceritinib mesylate also inhibits IGF-1R, InsR, and STK22D with IC₅₀ values of 8, 7, and 23 nM, respectively. Ceritinib mesylate shows great antitumor potency.

GTx-134 is a dual insulin-like growth factor 1 receptor/insulin receptor (IGF-1R/IR) inhibitor with an IC₅₀ values for IGF-1R and IR of 97 and 187 nM respectively. GTx-134 inhibits the autophosphorylation of IGF-1R and its downstream signaling pathway (Akt), thereby blocking the proliferation and survival signals of tumor cells. GTx-134 has broad-spectrum inhibitory activity against multiple myeloma cell lines and can induce apoptosis in sensitive cells. GTx-134 significantly inhibits tumor growth in mice with MM1.S cell transplantation. GTx-134 works in synergy with existing therapies (such as protease preparations, immunomodulators). GTx-134 can be used in high-risk myeloma research.