type ii inhibitor

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].

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].

The impact of spleen tyrosine kinase (Syk) signaling might be prominent in lupus because (i) Syk is a shared downstream signaling molecule among circulating immune complex, LPS, and (1→3)-β-D-glucan (BG), and (ii) all of these factors are detectable in the serum of Fc gamma receptor IIb-deficient (FcgRIIb-/-) mice with sepsis. Syk inhibition downregulated several inflammatory pathways in FcgRIIb-/- macrophages activated with BG + LPS suggesting the potential anti-inflammatory impact of Syk inhibitors in lupus. Indeed, administration of a Syk inhibitor prior to cecal ligation and puncture (CLP) sepsis in FcgRIIb-/- mice reduced baseline lupus-induced proinflammatory cytokines and attenuated sepsis severity as evaluated by mortality, organ injury, serum LPS, and post-sepsis serum cytokines.

CaM kinase II inhibitor TFA salt (Autocamtide-2-related inhibitory peptide (TFA)) is a highly specific and potent inhibitor of CaMKII with an IC50 of 40 nM.

Topoisomerase II inhibitor 14 is a potent topoisomerase II inhibitor with anticancer and antioxidant activities.Topoisomerase II inhibitor 14 induces apoptosis and blocks the cell cycle in S phase.Topoisomerase II inhibitor 14 reduces the amount of GSH, MDA and NO. Topoisomerase II inhibitor 14 reduces the amount of GSH, MDA and NO.

Casein Kinase II Inhibitor IV is an inducer of epidermal keratinocyte differentiation.

Cdk2 Inhibitor II is a selective and potent CDK2 inhibitor50 at 60 nM.

cFMS Receptor Inhibitor II is a CSF1R kinase (FMS Receptor; colony stimulating factor 1 receptor; Macrophage colony-stimulating factor receptor) inhibitor with an IC50 of 2.8 nM, demonstrating significant selectivity over other kinases. This compound also exhibits notable CSF1R inhibition with an IC50 of 1.4 μM in cellular assays.

Histone Acetyltransferase Inhibitor II is a selective and cell permeable inhibitor of p300 histone acetyltransferase(IC50 : 5 μM).with anti-acetylase activity in mammalian cells.

Topoisomerase II inhibitor 3 (Compound 6 h) is an acridone derivative acting as a Type II DNA topoisomerase (topo II) inhibitor. It specifically targets topo IIα β subtypes, with IC50 values of 0.17 μM for topo IIα and 0.23 μM for topo IIβ, causing significant DNA damage and inducing apoptosis by triggering the loss of mitochondrial membrane potential [1].

Topoisomerase II Inhibitor 16 (compound CT3) is a selective, orally bioavailable, and irreversible inhibitor of trypanosomal topoisomerase II, possessing the ability to penetrate the brain and stabilize double-stranded DNA-enzyme cleavage complexes. It shows promise for research into Chagas disease [1].

Topoisomerase II inhibitor 5 (Compound E24) is a DNA topoisomerase II inhibitor with anticancer properties.

Spleen tyrosine kinase (Syk) is a non-receptor tyrosine kinase that, upon phosphorylation, binds to immunoreceptor tyrosine-based activation motifs of FcRγ chains and mediates downstream signaling related to platelet function and inflammation. Syk inhibit

T-Type calcium channel inhibitor 2 (compound 6g) is a potent inhibitor of the T-type calcium channel, specifically acting on Cav3.1 (α1G) with an IC50 of 31.0 μM, Cav3.2 (α1H) with an IC50 of 83.1 μM, and Cav3.3 (α1I) (α1H). T-Type calcium channel inhibitor 2 exhibited cytotoxicity against A549 and HCT-116 cells with IC50s of 5.0 μM and 6.4 μM, respectively.

Topoisomerase I II inhibitor 3 (compound 7) is a potent dual inhibitor of topoisomerase I (Topo I) and II (Topo II) that inhibits the PI3K Akt mTOR signaling pathway, subsequently inhibiting cell proliferation, invasion, and migration, and inducing apoptosis. This compound has research value in liver cancer.

Topoisomerase II inhibitor 4 (compound E17) is a potent topoisomerase II inhibitor with antitumor effects, blocking the cell cycle in the G2 M phase, inhibiting cancer cell proliferation, and exhibiting cytotoxicity.

Topoisomerase II inhibitor 9 is a Topo II inhibitor (IC50: 0.97 μM) and DNA embedding agent (IC50: 43.51 μM) that blocks the Hep G-2 cell cycle in the G2/M phase and induces apoptosis.

Human PD-L1 inhibitor II, a potent PD-L1 inhibitor, exhibits strong anti-cancer activity.

Topoisomerase II inhibitor 8 (compound 22) is a potent inhibitor of topoisomerase II (IC50 = 0.52 μM) [1] and exhibits strong anti-proliferative activities, arresting the cell cycle at the G2 M phase.

Topoisomerase I/II inhibitor 4 is a potent dual inhibitor of topoisomerase I (Topo I) and II (Topo II) with inhibitory effects on cell proliferation, invasion and migration, and induction of apoptosis, and can be used to study hepatocellular carcinoma.

DNA topoisomerase II inhibitor 1 is a potent inhibitor of DNA topoisomerase II that arrests the cell cycle in sub-G1 phase and induces apoptosis with anti-value-added effects.

Topoisomerase II inhibitor 7, a potent inhibitor of the topoisomerase II alpha subtype, exhibits an IC50 of 3.19 μM. It effectively induces cell cycle arrest and apoptosis.

Syk Inhibitor II dihydrochloride dihydrate is a highly selective, potent, ATP-competitive Syk inhibitor (IC50: 41 nM) that exhibits anti-allergic effects.

Vascular endothelial growth factor receptor 2 (VEGFR2, also known as KDR and FLK1) is a receptor tyrosine kinase that regulates angiogenesis, vascular development, and embryonic hematopoiesis in response to VEGF isoforms A, C, and D. VEGFR2 kinase inhibitor II is a reversible, cell-permeable inhibitor of VEGFR2's kinase activity (IC50 = 70 nM). It less potently inhibits the platelet-derived growth factor receptor β (PDGFRβ; IC50 = 920 nM) and related receptor and non-receptor tyrosine kinases. VEGFR2 kinase inhibitor II blocks the growth of human umbilical vein endothelial cells stimulated with either VEGF or PDGF (IC50s = 110 nM and 2 μM, respectively).

β-Secretase Inhibitor II is a tripeptide aldehyde inhibitor of β-Secretase with an inhibitory potency of IC50 = 700 nM against total Aβ and IC50 = 2.5 μM against Aβ[1-42]. This compound, with a simple structure, is particularly useful in Alzheimer's disease research.

Topoisomerase II inhibitor 10 is a potent inhibitor of topoisomerase II (IC50: 7.45 μM). Topoisomerase II inhibitor 10 was able to arrest the cell cycle of HepG-2 cells in the G2-M phase and induce apoptosis.

GSK3β inhibitor II is a GSK3β inhibitor. GSK3β inhibitor II exhibits the research potential of Alzheimer's disease (AD).

Syk inhibitor II, a cell-permeable, ATP-competitive, pyrimidine-carboxamide compound, selectively and reversibly inhibits Syk (IC50 = 41 nM).

Topoisomerase II inhibitor 6 (Compound 5), a tryptanthrin derivative, is a potent and selective topoisomerase II inhibitor that blocks the CCRF-CEM cell cycle in the G2 phase and induces DNA double-strand breaks (DSB). It exhibits antiproliferative activity on various tumor cell lines and has potential for cancer research [1].

Wee1 Inhibitor II is an ATP-binding site-targeting Wee1 inhibitor.

Topoisomerase I II inhibitor 2 (compound 1a) is a DNA topoisomerase I II dual inhibitor that significantly reduces xenograft tumor growth in a mouse model, indicating its potential use in treating liver cancer. It is a potent topoisomerase inhibitor with IC50 values of 6.83 μM and 9.82 μM for LM9 cells and Huh7 cells [1].

Type II collagen is a protein that demonstrates considerable effectiveness in alleviating pain and inflammation associated with collagen-induced arthritis in mice, with notable application in the treatment of osteoarthritis [1].

ALK5 Inhibitor II is an ALK5 inhibitor. IC50: 4, 18, and 23 nM for ALK5 autophosphorylation, TGF-β cellular assay, and ALK5 binding in HepG2 cells, respectively.

Heat shock protein (Hsp) inhibitor II is the active form of Hsp inhibitor I and a benzylidene lactam compound that prevents the synthesis of inducible Hsps, such as Hsp105, Hsp72, and Hsp40. Hsp inhibitor II decreases Hsp72 synthesis in vivo and reduces thermotolerance of tumors in SCC VII tumor-containing mice. At 100 μM, it inhibits the development of thermotolerance in COLO 320 DM cells. Inhibition of Hsp70 with Hsp inhibitor II in combination with amphotericin B increases susceptibility of AmB-susceptible (MICs = 0.058 versus 0.27 μg/ml for combined and AmB alone, respectively) and AmB-resistant (MICs = 21.33 versus >32 μg/ml for combined and AmB alone, respectively) strains of A. fumigatus.

ERK Inhibitor II (Negative control) effectively blocks extracellular signal-regulated kinase (ERK) activity and interferes with insulin receptor activation, serving as a valuable tool in diabetes research.

Lck inhibitor II is a cell-permeable, ATP binding site-targeting, tri-substituted pyrimidine that acts as a highly potent Lck (lymphocyte specific kinase) inhibitor

Topoisomerase II inhibitor 15 (compound 2g) is a potent inducer of apoptosis, demonstrating high selectivity for head and neck tumors [1].

Topoisomerase II inhibitor 13 inhibits topoisomerase II (Topo II) that shows strong anti-proliferation activity against HL-60/MX2 cancer cells derived from HL-60 against Topo II toxicity.

Casein Kinase II Inhibitor IV Hydrochloride is a small-molecule inducer of epidermal keratinocyte differentiation, offering novel therapeutic approaches for treating skin hyperproliferative disorders.

Type II collagen is composed of a triple helix of three identical α chains. These molecules associate to form a fibril that is stabilized by intermolecular crosslinks1. Damage to the fibrillar meshwork, made up of primarily type II collagen (z 90–95%), ma

Topoisomerase II inhibitor 11 (compound 3d) is a potent inhibitor of Topoisomerase II (IC50: 2.89 μM), inhibiting cell proliferation and inducing apoptosis by arresting the cell cycle in the G2 M phase.

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.

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

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.

Quizartinib, also know as AC220 and AC010220, is an orally available FLT3 / STK1 inhibitor with potential antineoplastic activity. Class III receptor tyrosine kinase inhibitor AC220 selectively inhibits class III receptor tyrosine kinases, including FMS-related tyrosine kinase 3 (FLT3/STK1), colony-stimulating factor 1 receptor (CSF1R/FMS), stem cell factor receptor (SCFR/KIT), and platelet derived growth factor receptors (PDGFRs), resulting in inhibition of ligand-independent leukemic cell proliferation and apoptosis. Mutations in FLT3, resulting in constitutive activation, are the most frequent genetic alterations in acute myeloid leukemia (AML) and occur in approximately one-third of AML cases.