dapk3 inhibitor hs 148

JAK1/2/3 Inhibitor 1 is a potent protein kinase inhibitor.JAK1/2/3 Inhibitor 1 has antitumor activity that inhibits the growth of a variety of cancer cell lines. It inhibits the growth of cancer cells by binding to the cancer cell backbone and inhibiting the production of new proteins.

GSK-3 Inhibitor 5 (4-Cyanophenacyl bromide) is a ketone derivative that is used as an intermediate in pharmaceuticals and organic synthesis, and inhibits glycogen synthase kinase 3 (GSK-3).

GSK-3 inhibitor 3 is a selective, orally active, brain-permeable GSK-3 inhibitor that inhibits GSK-3α and GSK-3β with IC50s of 0.35 nM and 0.25 nM, respectively.GSK-3 inhibitor 3 reduces the phosphorylation level of tau protein S396 with an IC50 of 10 nM in a triple transgenic mouse model of Alzheimer's disease. GSK-3 inhibitor 3 reduced the phosphorylation level of tau protein S396 in a triple transgenic mouse model of Alzheimer's disease, with an IC50 of 10 nM.GSK-3 inhibitor 3 can be used for the study of neurological diseases.

Rac1 Inhibitor W56 acetate(1095179-01-3 free base) is a peptide comprising residues 45-60 of the guanine nucleotide exchange factor (GEF) recognition/activation site of Rac1. Rac1 Inhibitor W56 acetate(1095179-01-3 free base) selectively inhibits Rac1 interaction with Rac1-specific GEFs TrioN, GEF-H1 and Tiam1.

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.

GSK-3 inhibitor 1 is a GSK-3 inhibitor.

mTOR inhibitor-3 is a selective mTOR inhibitor (Ki= 1.5 nM). mTOR inhibitor-3 inhibits mTORC1 and mTORC2 in cellular and in vivo experiments.

RIP2 Kinase Inhibitor 3 is a potent and selective inhibitor of RIP2, demonstrating an IC50 of 1 nM.

GSK-3 Inhibitor XIII, an ATP-competitive GSK-3 inhibitor (Ki: 24 nM), can be used to study diabetes and obesity.

GSK 3 Inhibitor IX (6-BIO) is a selective reversible, ATP-competitive inhibitor of GSK-3α/β and CDK1-cyclinB complex. It inhibits (GSK-3α/β)/CDK1/CDK5 activity with IC50 values of 5 nM/320 nM/83 nM, respectively.

Aurora kinase inhibitor-3 (Aurora Kinase Inhibitor III) is a potent inhibitor of Aurora A kinase (IC50 = 42 nM).1 It is selective for Aurora A over BMX, BTK, IGF-1R, c-Src, TRKB, SYK, and EGFR.

MMP-3 Inhibitor acetate is a cell-permeable and potent inhibitor of human MMP-3.

JAK 3 inhibitor IV (ZM 39923 hydrochloride) is a JAK1/3 inhibitor with pIC50 of 4.4/7.1, almost no activity to JAK2 and modestly potent to EGFR; also found to be sensitive to transglutaminase.

PRL-3 Inhibitor I (BR-1) is a phosphatase of regenerating liver 3 (PRL-3) inhibitor which blocks the migration and invasion of metastatic cancer cells.

Chitin Synthase Inhibitor 3 (Compound 2d) is a potent inhibitor of chitin synthase, exhibiting an IC50 value of 0.16 mM and demonstrating antifungal activity with a minimum inhibitory concentration (MIC) of 1 μg/mL against Candida albicans [1].

JNK3 Inhibitor-3 (compound 15g) is a selective, blood-brain barrier permeable, and orally active inhibitor of c-Jun N-terminal kinase 3 (JNK3) with IC50 values of 147.8 nM, 44.0 nM, and 4.1 nM against JNK1, JNK2, and JNK3, respectively. This compound has been shown to significantly enhance memory in mouse models of dementia and is utilized in Alzheimer’s disease research [1].

ChoKα Inhibitor-3, a sulfur-containing choline kinase inhibitor, effectively inhibits HChoK α1 with an IC50 value of 0.66 μM and possesses the capability to induce apoptosis. This compound is utilized in cancer research [1].

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.

Compounds 17o (IC50: 14.0 nM, NCI-H460) and 17p (IC50: 2.9 nM, NCI-H460) with furan moieties showed potent cytotoxic effects at the nanomolar level against various human cancer cell lines.

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].

KRAS inhibitor-3, an efficacious inhibitor of both wild-type (WT) and oncogenic KRAS mutations, exhibits high-affinity binding (K D: 0.28 μM for KRAS WT, 0.63 μM for KRAS G12C, 0.37 μM for KRAS G12D, and 0.74 μM for KRAS Q61H). Additionally, it impedes the interaction between KRAS and Raf, highlighting its potential as a targeted therapeutic agent in KRAS-mutant cancers.

Schnurri-3 inhibitor-1, a potent inhibitor of schnurri-3, is an essential regulator of bone formation in adults that can be used in osteoporosis research. Schnurri-3 inhibitor-1 can inhibit Shn3 with EF1alpha promoter in osteoblast cell line Shn3FFL (AC50 = 2.09 μM) [1].

KRas G12C inhibitor 3 is a compound that specifically inhibits the KRas G12C mutation.

HIV-1 integrase inhibitor 3 is an HIV-1 integrase strand transfer (INST) inhibitor with an IC50 of 2.7 nM.

PI4KIII beta inhibitor 3 is a novel, highly effective inhibitor of PI4KIIIβ with an IC50 of 5.7 nM.

PI3K mTOR Inhibitor-3 (compound 12) is an imidazoline compound with potent dual inhibition of PI3K and mTOR, exhibiting notable anti-cancer activity [1].

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 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.

α-Synuclein inhibitor 3 (Compound 7g) is a potent inhibitor of α-synuclein (α-Syn) aggregation, with potential applications in Parkinson's disease research [1].

BET Bromodomain Inhibitor 3 is a BET bromodomain inhibitor with an inhibitory Ki value of >40 µM against BrdT. It is utilized in research related to contraception, cancer, and heart disease [1].

WRN Inhibitor 3 (example 110), a cyclic vinyl sulfone-based compound, serves as an inhibitor of the Werner Syndrome ATP-dependent helicase enzyme (WRN). It is utilized in cancer research [1].

Cathepsin K Inhibitor 3, exhibiting an IC50 value of 0.5 nM, is a highly selective inhibitor of cathepsin K, featuring a favorable pharmacokinetic profile. It holds potential for use in studies of osteoarthritis (OA).

HPGDS inhibitor 3 is a powerful oral compound that selectively inhibits the hematopoietic prostaglandin D synthase (H-PGDS). With an IC50 value of 9.4 nM and EC50 of 42 nM, it demonstrates high potency in peripherally restricting H-PGDS. Moreover, HPGDS inhibitor 3 exhibits excellent selectivity with no associated central nervous system toxicity. This compound also possesses favorable pharmacokinetic properties in mouse, rat, and dog models. Additionally, HPGDS inhibitor 3 displays noteworthy anti-inflammatory activity [1].

SPR inhibitor 3 is an effective sepiapterin reductase inhibitor. SPR inhibitor 3 decreases neuropathic and inflammatory pain through a reduction of BH4 levels. SPR inhibitor 3 shows a high binding affinity to human SPR in a cell-free assay (IC50=74 nM) an

MMP-3 Inhibitor is a peptide matrix metalloproteinase-3 (MMP-3) inhibitor with a Ki value of 95 nM.MMP-3 inhibitor has anticancer and antitumor activity.

IRAK inhibitor 3 is a modulator of interleukin-1 (IL-1) receptor-associated kinase (IRAK).

sEH inhibitor-3 (compound 35) is a potent, orally active inhibitor of soluble epoxide hydrolase (sEH), acting on human sEH with a Ki of 0.75 nM.

Cyclophilin inhibitor 3 (compound 7c), a potent inhibitor of cyclophilin A (CypA), exhibited potent anti-HCV effects with an EC50 value of 4.2 μM.

Prostaglandin E2 (PGE2) inhibitor 3 is a selective inhibitor targeting microsomal prostaglandin E synthase-1 (mPGES-1; IC50 = 0.2 µM), demonstrating greater selectivity for mPGES-1 over COX-1, COX-2, 5-lipoxygenase (5-LO), and soluble epoxide hydrolase (sEH) in assays at 10 µM. This compound effectively reduces IL-1β-induced PGE2 production in A549 cells and decreases LPS-induced IL-6 and PGE2 in J774A.1 macrophages at concentrations of 10 and 1 µM, respectively. Additionally, it blocks the production of 5-LO-derived products, including leukotriene B4 (LTB4) and 5-H(p)ETE, in response to calcium ionophore A23187 alone or combined with arachidonic acid, with IC50 values of 4.9 and 5.2 µM, respectively. When administered in vivo at doses of 10 mg/kg, PGE2 inhibitor 3 effectively prevents leukocyte infiltration in a mouse model of zymosan-induced peritonitis.

Z-DEVD-FMK, a Caspase-3 Inhibitor, is an irreversible, cell-permeable inhibitor of caspase-3/CPP32 that impedes tumor cell apoptosis. In vivo studies show it offers neuroprotection in rat hippocampi post-seizures and considerably diminishes post-traumatic apoptosis, enhancing neurological recovery in rats before and after traumatic brain injury induction.

IDH1 Inhibitor 3 is a mutant isocitric dehydrogenase 1 (IDH1) inhibitor (IC50: 45 nM for IDH1R132H).

P-gp Inhibitor 3, an effective P-glycoprotein (P-gp) inhibitor, activates P-gp ATPase to inhibit P-gp's efflux function. It demonstrates a relatively stronger multidrug resistance (MDR) reversal ability, thereby enhancing the anti-tumor efficacy of Paclitaxel.

KRAS G12D Inhibitor 3 TFA, exhibiting an inhibitory concentration (IC50) of less than 500 nM, is effective as an antitumor agent.

Topoisomerase I (Compound ZML-14) inhibitor 3 induces HepG2 cell apoptosis and arrests cell cycle at G2 M phase. Topoisomerase I inhibitor 3 is an inhibitor of topoisomerase I that interact with topoisomerase I-DNA complex [1].

UCK2 Inhibitor-3 is a non-competitive inhibitor of uridine-cytidine kinase 2 (UCK2), a pivotal enzyme in the pyrimidine salvage pathway, with an IC50 value of 16.6 μM. UCK2 can partially substitute for dihydroorotate dehydrogenase (DHODH) in infected or rapidly dividing cells, aiding uridine salvage. Additionally, UCK2 Inhibitor-3 inhibits DNA polymerase eta and kappa, with IC50 values of 56 μM and 16 μM, respectively.

BRM BRG1 ATP Inhibitor-3 is a potent inhibitor targeting both BRM and BRG1 components of the BAF complex, with IC50 values of 10.4 nM for BRM and 19.3 nM for BRG1, and holds potential for research in cancer and BAF complex-related disorders.