glutaminyl cyclase inhibitor 4

Glutaminyl Cyclase Inhibitor 4 is a potent, selective glutaminyl cyclase (QC) inhibitor (IC50: 6.1 nM). It is a potent anti-Alzheimer’s agent.

Prolyl-4-hydroxylase Inhibitor 11, a novel proline 4-hydroxylase inhibitor, shows protective effects against oxidative stress and Cu(II) toxicity in Chlorella vulgaris.

p53-Mdm2 inhibitor 4 inhibits the p53-MDM2 protein-protein interaction.

p38α inhibitor 4 is a selective MAPK p38α inhibitor, which is used to study diabetes, pain and chronic inflammation.

Pim-1 kinase inhibitor 4 is a potent Pim-1 kinase inhibitor with an IC50 value of 17.01 nM.Pim-1 kinase inhibitor 4 also possesses antioxidant activity and potential anticancer activity, and inhibits DPPH.Pim-1 kinase inhibitor 4 promotes apoptosis and inhibits the growth of PC-3 cells with an IC50 value of 16 nM. Pim-1 kinase inhibitor 4 promotes apoptosis and inhibits PC-3 cell growth with an IC50 of 16 nM. Pim-1 kinase inhibitor 4 can be used in prostate cancer research.

GSK-3 inhibitor 4 is an orally active and brain-permeable triple inhibitor of GSK-3, CDK2 and CDK5 with inhibitory effects on GSK-3β, GSK-3α, CDK2 and CDK5, with IC50 values of 0.56 nM, 0.45 nM, 0.47 μM, 0.68 μM, respectively.GSK-3 inhibitor 4 can effectively reduce Tau protein levels. GSK-3 inhibitor 4 can effectively reduce the level of Tau protein.GSK-3 inhibitor 4 can be used in the study of Alzheimer's disease.

Chitin synthase inhibitor 4 is a chitin synthase (CHS) inhibitor with antimicrobial activity.Chitin synthase inhibitor 4 is a CHS-based compound and a candidate fungicide.

IL-4 inhibitor is an inhibitor of IL-4.1It binds to IL-4 with a Kdvalue of 1.8 μM and inhibits IL-4 activity in a cell-based reporter assay (EC50= 1.81 μM). It is selective for IL-4 over IL-13 (EC50= 18.2 μM). IL-4 inhibitor inhibits IL-4-induced STAT6 phosphorylation in THP-1 monocytes (EC50= 3.1 μM), indicating inhibition of the IL-4-JAK1-STAT6 signaling pathway.

Glutaminyl Cyclase Inhibitor 1 is a glutaminyl cyclase inhibitor (IC50: 0.5 μM) that can be used to study neurological disorders.

WRN Inhibitor 4 (Example 107), a cyclic vinyl sulfone-based compound, serves as an inhibitor of the Werner Syndrome ATP-dependent helicase enzyme (WRN). This inhibitor is applicable in cancer research [1].

ChoKα Inhibitor-4 is a bioisosteric agent that effectively inhibits human choline kinase α1 (HChoK α1) with an IC50 of 0.66 μM. It demonstrates both inhibitory and antiproliferative effects on cancer cells, induces apoptosis through the mitochondrial pathway, and diminishes the expression of anti-apoptotic proteins [1].

JNK3 Inhibitor-4, a potent 2-aryl-1-pyrimidinyl-1H-imidazole-5-yl acetonitrile derivative, demonstrates a strong inhibitory effect on JNK3 with an IC 50 value of 1.0 nM. It exhibits exceptional selectivity against JNK3 when compared to other protein kinases, including isoforms JNK1 (IC 50 = 143.9 nM) and JNK2 (IC 50 = 298.2 nM). Additionally, JNK3 Inhibitor-4 benefits from neuroprotective properties and is predicted to permeate the blood-brain barrier effectively.

Angiogenesis Inhibitor 4 is a potent agent for inhibiting angiogenesis, with potential applications in cancer research [1].

IRAK-4 protein kinase inhibitor 2 is a potent interleukin-1 receptor-associated kinase-4 (IRAK-4) inhibitor(IC50 = 4 μM).

Wnt pathway inhibitor 4 is a small molecule antimicrobial agent with antibacterial and antiproliferative activity against cancer cells.

Sodium Channel Inhibitor 4 is a compound that functions as a sodium channel inhibitor [1].

MARK4 inhibitor 4, with an IC50 value of 1.49 μM, serves as an agent targeting MARK4 for potential use in research related to cancer and tauopathies [1].

RIP2 Kinase Inhibitor 4 is a highly potent and selective RIPK2 PROTAC compound that efficiently degrades RIPK2 (with a pIC50 value of 8) and effectively inhibits the release of TNF-α.

MAT2A inhibitor 4 is an inhibitor of the catalytic subunit of methionine S-adenosyltransferase-2, which is used in cancer research.

Cav 3.2 Inhibitor 4 (Compound 21) is a selective and potent inhibitor of the T-type calcium channel (Ca v 3.2), demonstrating peripheral restriction with an IC50 value of 0.6 μM. It is utilized in atrial fibrillation research [1].

Glyoxalase I inhibitor 4 is a potent inhibitor of glyoxalase I (GLO1) (Ki: 10 nM).

PI3Kγ inhibitor 4 is a selective, potent, orally active PI3Kγ inhibitor (IC50: 40 nM). PI3Kγ inhibitor 4 is ~7-fold more selective for PI3Kγ than the α subtype, 43-fold more selective than the β subtype and 18-fold more selective than the δ subtype. inflammation.

BRM/BRG1 ATP Inhibitor-4, a potent inhibitor of BRG1/BRM, is utilized in the research of cancers and BAF complex-related disorders.

URAT1 Inhibitor 4, derived from Lesinurad, is a potent, orally active inhibitor of URAT1 with an IC50 value of 7.56 μM, demonstrating greater in vivo urate-lowering efficacy than Lesinurad [1].

ERK1/2 Inhibitor 5, a potent suppressant of the ERK1/2 pathway, is instrumental in the mitogen-activated protein kinase (MAPK) signal transduction pathway, where extracellular signal-regulated kinase (ERK) serves as a critical component of the MAPK family. This compound holds promise for the investigation or mitigation of cancer, inflammation, or various proliferative diseases[1].

IRAK inhibitor 4 is a compound that functions as an inhibitor of interleukin-1 receptor-associated kinase 4 (IRAK4). It specifically targets and inhibits the activity of IRAK4. The (trans) form of IRAK inhibitor 4 refers to its specific molecular configuration.

SLLK, Control Peptide for TSP1 Inhibitor (TFA) is a control peptide for LSKL, which is a Thrombospondin (TSP-1) inhibitor.

HIF-1 inhibitor-4 (HIF-1 inhibitor-4) is a HIF-1 inhibitor with IC50 of 560 nM. HIF-1 inhibitor-4 reduces the HIF-1α protein level without affecting its mRNA level.

Topoisomerase II inhibitor 4 (compound E17) is a potent inhibitor of topoisomerase II. Topoisomerase II inhibitor 4 has antitumour effects, blocking the cell cycle in the G2/M phase, inhibiting the proliferation of cancer cells and exhibiting cytotoxicity. It inhibits the proliferation of cancer cells and exhibits cytotoxicity.

Glutaminyl Cyclase Inhibitor 3, a designed anti-Alzheimer’s compound, is a potent human Glutaminyl Cyclase (GC) inhibitor (IC50: 4.5 nM). It significantly reduced the brain concentrations of pyroform Aβ and total Aβ and restored cognitive functions.

PI3K/mTOR Inhibitor-4 is an orally active pan-I PI3K/mTOR inhibitor. PI3K/mTOR Inhibitor-4 is an enzyme inhibitor that acts on PI3Kα (IC50: 0.63 nM), PI3Kγ (IC50: 22 nM), PI3Kδ (IC50: 9.2 nM) and mTOR (IC50: 13.85 nM). PI3K/mTOR Inhibitor-4 can be used to study cancer.

Menin-MLL inhibitor 4 has antitumor activity.Menin-MLL inhibitor 4 is an inhibitor of Menin- MLL (mixed-lineage leukemia protein) interaction .

KRas G12C inhibitor 4 is a compound that inhibits KRas G12C.

Tuberculosis inhibitor 4 (compound 16) is a spirothiazolidinone based on mandelic acid that exhibits potent antimycobacterial action. The inhibitor inhibited 98% of Mycobacterium tuberculosis strain H37Rv at concentrations below 6 μg mL.

Compound 5a, also known as DPP-4 inhibitor 3, is a powerful dipeptidyl peptidase IV (DPP-IV) inhibitor, demonstrating an IC50 value of 0.75 nM. It exhibits outstanding antioxidant and insulinotropic activity [1].

PKCα (C2-4) inhibitor peptide is a specific antagonist to PKCα that impedes the α1A-adrenoreceptor agonist A-61603 [1] from inhibiting I_Kr.

RIP1 Kinase Inhibitor 4 (Compound 3) is an effective inhibitor of RIP1K, exhibiting an EC50 of ≤ 1000 nM [1].

sEH inhibitor-4 (compound B15) has been identified as a potent soluble epoxide hydrolase (SEH) inhibitor with a remarkable inhibitory potency of 0.03 ± 0.01 nm. Intensive structural modification efforts led to the discovery of this compound for its ability to decrease inflammation and alleviate pain in the presence of SEH.

HIV-1 integrase inhibitor 4 is an HIV-1 integrase strand transfer (INST) inhibitor (IC50: 3.7 nM).

Topoisomerase I inhibitor 4 (compound 7a) is a potent inhibitor of topoisomerase I activity. It effectively inhibits the proliferation of various cancer cell lines including HepG2, A549, MCF-7, and HeLa, with IC50 values of 1.20 μM, 2.09 μM, 1.56 μM, and 1.92 μM, respectively. Thus, Topoisomerase I inhibitor 4 holds promise for cancer research applications [1].

c-Myc inhibitor 4 is a potent, orally active c-Myc-reducing compound. c-Myc is an important proto-oncogene, which is closely associated with the development of many tumors.

KRAS inhibitor-4 developed as anticancer agents, is a potent KRAS inhibitor.

SCD1 inhibitor-4 is stearoylCoA desaturase-1 (SCD1) inhibitor. SCD1 inhibitor-4 can be used for the research of diabetes.

EGFR/ErbB-2/ErbB-4 inhibitor-2 (EGFR/ErbB2 Inhibitor) is a cell-permeable inhibitor of EGFR and c-ErbB2 (IC50s = 20 and 79 nM, respectively)

Microtubule inhibitor 4 (compound 2) is a potent inhibitor of microtubule and inhibits microtubule protein polymerization, HT-29 cells (IC50: 2.1 nM) exhibited cytotoxicity.

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.

ATM Inhibitor -4 is a selective and potent ATM inhibitor (IC50: 0.32 nM) that strongly inhibits the activity of the PI3K kinase family and exhibits good metabolic stability. ATM Inhibitor -4 completely inhibits mTOR at 1 μM.

P-gp inhibitor 4 is a selective P-glycoprotein modulator with an EC 50 of 94 nM. P-gp inhibitor 4 increases drug transport across gastro-intestinal barrier and recovers doxorubicin toxicity in multidrug resistant cancer cells .

GLS1 Inhibitor-4 (compound 41e) is a powerful GLS1 inhibitor, demonstrating an IC50 of 11.86 nM. It exhibits antiproliferative effects, substantial metabolic stability, and strong GLS1 binding affinity. Furthermore, it interrupts glutamine metabolism, induces ROS production, and triggers apoptosis, culminating in notable antitumor activity [1].

Phosphodiesterase 4 (PDE4) inhibitor is an inhibitor of PDE4 with an IC50 value of 0.10 μM for the human recombinant enzyme.