pde4 inhibitor

PDE4 inhibitor intermediate 1 is a PDE4 inhibitor synthesis intermediate.

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 compound that acts as a triple inhibitor of GSK-3, CDK2, and CDK5, with IC50 values of 0.56 nM (GSK-3β), 0.45 nM (GSK-3α), 0.47 μM (CDK2), and 0.68 μM (CDK5). It effectively reduces Tau protein levels and 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.

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.

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.

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 compound that inhibits EGFR and c-ErbB2 with IC50 values of 20 nM and 79 nM, respectively.

IRAK-1-4 Inhibitor I is a dual inhibitor targeting IRAK1 and IRAK4.

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

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

PDE4-IN-4 is a compound acting as both a potent M3 antagonist (p IC 50 = 10.2) and a PDE4 inhibitor (p IC 50 = 8.8), designed for inhalation-based treatment of pulmonary diseases.

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

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

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.

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 topoisomerase II inhibitor with antitumor effects, blocking the cell cycle in the G2 M phase, inhibiting cancer cell proliferation, and exhibiting cytotoxicity.

PI3K mTOR Inhibitor-4 is an orally active pan-I PI3K mTOR enzyme inhibitor, acting 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 .

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].

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

Tuberculosis inhibitor 4 (compound 16) is a spirothiazolidinone derived from mandelic acid, exhibiting potent antimycobacterial activity by inhibiting 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].

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 with an IC50 of 3.7 nM.

Topoisomerase I inhibitor 4 (compound 7a) is a potent inhibitor of topoisomerase I activity, effectively inhibiting 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].

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

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].

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

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

Microtubule inhibitor 4 (compound 2) is a potent microtubule inhibitor that prevents microtubule protein polymerization and exhibits cytotoxicity in HT-29 cells (IC50: 2.1 nM).

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 potent GLS1 inhibitor with an IC50 of 11.86 nM, exhibiting antiproliferative effects, substantial metabolic stability, and strong GLS1 binding affinity. It disrupts glutamine metabolism, induces ROS production, triggers apoptosis, and demonstrates notable antitumor activity [1].

IRAK inhibitor 4 is an inhibitor of interleukin-1 receptor-associated kinase 4 (IRAK4).

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

Neutrophil elastase inhibitor 4 (compound 4f) is a competitive inhibitor of human neutrophil elastase (HNE) with an IC50 of 42.30 nM and a Ki of 8.04 nM. It induces apoptosis in T47D cells and inhibits the proliferation of T47D, RPMI 8226, A549, and HSF cells with respective IC50 values of 21.25, 34.17, 29.93, and 99.11 nM [1].