type ii inhibitor

PK68 is an effective and selective inhibitor of type II receptor-interacting kinase 1 (RIPK1, IC50 = 90 nM). PK68 can be used for research on the treatment of inflammatory disorders and cancer metastasis.

Type II topoisomerase inhibitor 1 is a potent and selective inhibitor of E. coli DNA gyrase with an IC50 value of 1.7 nM and forms hydrogen bonds with the Asp73 residue. It inhibits topoisomerase IV activity with an IC50 value of 0.98 μM and is applicable in the antibacterial area [1] [2].

Type II TRK Inhibitor 1 is a potent inhibitor targeting multiple tropomyosin receptor kinase (TRK) fusion protein variants as well as the wild type. It demonstrates notable antiproliferative effects on Ba F3 cells expressing CD74-TRKA G667C and ETV6-TRKC G696C, with half-maximal inhibitory concentrations (IC50s) of 6 nM and 1.7 nM, respectively [1].

Quizartinib (AC220) is an inhibitor of FLT3 (Kd: 1.6 nM) and demonstrates high selectivity for FLT3 when tested against a panel of 227 additional kinases.

CHZ868 is a type II JAK inhibitor with potential antitumor activity that reverses the persistence of type I JAK inhibitors and can be used to study leukemia.

RIPK1-IN-4 is a potent and selective type II kinase receptor interacting protein 1 (RIP1) kinase inhibitor and binds to a DLG-out inactive form of RIP1 (IC50s of 16 nM and 10 nM for RIP1 and ADP-Glo kinase).

Trk-IN-4 (PF-6683324) is a potent pan-Trk inhibitor with IC50 = 1.1~2.6 nM for TrkA TrkB TrkC and antinociceptive effects. It is also a selective type II PTK6 inhibitor with IC50 = 76 nM and has antitumor effects.

Izonsteride (LY320236) is a selective and potent 5alpha reductase inhibitor with dual action on the type I and type II isoforms of the enzyme.Izonsteride is used in the treatment of oncology and genitourinary disorders, and may be used in the study of prostate cancer.

IHMT-TRK-284 (Compound 34) is a potent, orally active type II TRK kinase inhibitor with IC50 values of 10.5 nM for TRKA, 0.7 nM for TRKB, and 2.6 nM for TRKC. The compound demonstrates good selectivity within the kinase group and exhibits significant anti-tumor efficacy in vivo.

PF-6689840 is a potent and selective Type II PTK6 Brk inhibitor with IC50 of 54 nM in biochemical assays; inhibits PTK6 phosphorylation at Y342 in engineered HET293T cells overexpressing PTK6 WT with IC50 of 0.25 uM; demonstrates superior kinase selectivity compared to the Type I inhibitors; inhibits tumor cell growth, which is independent of PTK6 expression levels in cells.

LI-2242 is a potent inositol hexakisphosphate kinase (IP6K) inhibitor with IC50s of 31 nM, 42 nM, 8.7 nM, and 1944 nM for IP6K1, IP6K2, IP6K3, and IPMK, respectively.LI-2242 ameliorated hepatic steatosis by reducing the expression of genes that enhance lipid uptake, lipid stabilization, and adipogenesis, and enhanced mitochondrial oxygen consumption rate (OCR) and insulin signaling in adipocytes and hepatocytes in vitro. LI-2242 ameliorated diet-induced obesity, hyperglycemia and hepatic steatosis in mice.LI-2242 can be used to study type II diabetes, obesity, metabolic complications, venous thrombosis and psychiatric disorders.

Enpp-1-IN-16 is an inhibitor targeting ENPP1 with potential anti-cancer activity.Enpp-1-IN-16 can be used to study insulin resistance in relation to type II diabetes mellitus and various ENPP1-mediated diseases in the chondrocalcinosis and osteoarthritis classes.

Mitoxantrone dihydrochloride (NSC-301739) is the hydrochloride salt of an anthracenedione antibiotic with antineoplastic activity. It is a type II topoisomerase inhibitor.

Telmisartan (BIBR 277) is an Angiotensin 2 Receptor Blocker. The mechanism of action of telmisartan is as an Angiotensin 2 Receptor Antagonist.

Irbesartan (SR-47436) is an Angiotensin 2 Receptor Blocker whose mechanism of action involves antagonizing the Angiotensin 2 Receptor.

Canagliflozin (JNJ 28431754AAA) is a selective SGLT2 inhibitor that inhibits CHO cells expressing mSGLT2, rSGLT2, and hSGLT2 (IC50=2/3.7/4.4 nM). Canagliflozin can be used for the treatment of type II diabetes mellitus (T2DM).

Buformin hydrochloride (NSC-528218) is a potent AMPK activator,an oral antidiabetic drug of the biguanide class. Buformin delays the absorption of glucose from the gastrointestinal tract increases insulin sensitivity and glucose uptake into cells and inhibits synthesis of glucose by the liver. Biguanides may antagonize the action of glucagon, thus reducing fasting glucose levels.

Pyraclostrobin is one of the most heavily used fungicides that inhibits mitochondrial complex III of fungal and mammalian cells.

LY2109761 is a novel selective TGF-β receptor type I II (TβRI II) dual inhibitor with Ki of 38 nM and 300 nM, respectively; shown to negatively affect the phosphorylation of Smad2.

AUZ 454 (K03861) is a type II CDK2 inhibitor with Kd values of 50 nM for CDK2(WT), 18.6 nM for CDK2(C118L), 15.4 nM for CDK2(A144C), and 9.7 nM for CDK2(C118L A144C).

c-Fms-IN-8 is a colony-stimulating factor-1 receptor (CSF-1R, c-FMS) Type II inhibitor (IC50: 9.1 nM). It is compound 4a in the reference.

CHMFL-ABL KIT-155 is a highly potent and orally active type II ABL c-KIT dual kinase inhibitor (IC50s: 46 nM 75 nM). It arrests cell cycle progression and induces apoptosis.

Gepotidacin is a novel triazaacenaphthylene inhibitor of bacterial type II topoisomerase.

HG-12-6 is a type II inhibitor of IRAK4, demonstrating preferential binding to unphosphorylated inactive IRAK4 (IC50: 165 nM) and modulating IRAK4 activity in autoimmunity and inflammation.