cot inhibitor-2

Cot inhibitor-2 is a cot (Tpl2/MAP3K8) inhibitor (IC50: 1.6 nM) with potency, selectivity and oral activity. cot inhibitor-2 inhibits LPS-stimulated TNF-α production in human whole blood with an IC50 of 0.3 μM.

DGAT-1 inhibitor 2 is an effective DGAT-1 inhibitor and anti-obesity drug. DGAT-1 (acyl-CoA: diacylglycerol acyltransferase 1) is one of two known DGAT enzymes that catalyze the final step of triglyceride synthesis. Transgenic mice and pharmacological studies indicate that inhibiting DGAT1 is a promising strategy for treating obesity and type 2 diabetes.

Cot inhibitor-1 is a selective inhibitor of Cot protein kinase (also known as Tpl2 or MAP3K8) (IC50 at 28 nM). Cot inhibitor-1 inhibited TNF-alpha production in human whole blood with IC50 of 5.7 nM. Cot is involved in a variety of cellular signaling pathways, particularly those involved in inflammation and immune responses. Cot inactivate-1 inhibits Cot activity and may have potential therapeutic effects on rheumatoid arthritis, inflammatory bowel disease and some types of cancer.

Cdk1 2 Inhibitor III is a selective inhibitor of Cdk1 2 with an IC50 value of 2.1 μM against CDK1 cyclin B.

ERK1 2 inhibitor 1 is a potent, orally bioavailable compound that exhibits 60% inhibition at 1 nM and has an IC50 of 3.0 nM against ERK1 and ERK2, respectively.

cholesterol-absorption inhibitor Intermediate 2 is a potent and orally active cholesterol absorption inhibitor that reduces blood cholesterol levels.

TbPTR1 inhibitor 2 is identified as a new development of improved pteridine reductase-1 (PTR1) inhibitors and anti-trypanosomatidic agents[1].

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.

Cot inhibitor-1 hydrochloride is an inhibitor of tumor progression loci-2 kinase (IC50 = 28 nM) and inhibits the production of TNF-α in human whole blood (IC50 = 5.7 nM).

Edg-2 receptor inhibitor 1 (SAR-100842) is an Edg-2 receptor inhibitor extracted (IC50: <0.1 μM).

2H-Imidazo[4,5-b]pyrazin-2-one, 1,3-dihydro-6-[6-(1-hydroxy-1-methylethyl)-3-pyridinyl]-1-[(tetrahydro-2H-pyran-4-yl)methyl]- is a potent mTOR inhibitor with IC50 of 0.176 μM and >30 μM for mTOR and PI3Kα, respectively.

EGFR ErbB-2 inhibitor-1 is a selective ErbB2 HER2 inhibitor that effectively blocks ErbB2 and HER2 signaling.

IRAK inhibitor 2 (IRAK-IN-2) is a potent inhibitor of interleukin 1 receptor-associated kinase 4 (IRAK-4) for the study of inflammation-related diseases.

Cysteine protease inhibitor 2 is a cysteine protease inhibitor. Cysteine protease inhibitor 2 inhibited DCT116 and PC3 cells with GI50 values of 6.5 μM and 4.4 μM, respectively.

Menin-MLL inhibitor MI-2 (MI2) is a potent menin-MLL interaction inhibitor with IC50 of 446 nM.

ROCK inhibitor-2 is a selective dual inhibitor of ROCK1 and ROCK2, with IC50 values of 17 nM and 2 nM, respectively.

YAP TAZ inhibitor-2 is a potent, orally active TEAD-YAP TAZ inhibitor with an EC50 value of 3 nM, demonstrating anti-proliferative and antitumor activity [1].

Eph inhibitor 2 is an Eph family tyrosine kinase inhibitor targeting Eph receptors.

Protein kinase G inhibitor-2 exhibits antibacterial, antiviral, and antitumor activities.

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

Ehp-inhibitor-2 is an Eph family tyrosine kinase inhibitor targeting Eph receptors.

MI-2 (MALT1 inhibitor) is an irreversible MALT1 inhibitor.

HPGDS inhibitor 2 (GSK-2894631A) is a potent, selective hematopoietic prostaglandin D synthase (h-pgds) inhibitor, IC50 = 9.9 nm.

JAMM protein inhibitor 2 (Acetamide, 2-(2-ethylphenoxy)-N-[2-methyl-4-(1-pyrrolidinyl)phenyl]-) is an inhibitor of JAMM protease and can be used for anticancer studies. The IC50s are 10 μM, 46 μM, and 89 μM for thrombin, Rpn11, and MMP2, respectively.

Raf inhibitor 2 (CID 25014542) is novel inhibitor of Raf kinases.

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.

BCATc Inhibitor 2 exhibited an IC50 of 0.8 microM in the hBCATc assays; it is an active and selective inhibitor. BCATc Inhibitor 2 also blocked calcium influx into neuronal cells following inhibition of glutamate uptake, and demonstrated neuroprotective e

BRM BRG1 ATP Inhibitor-2 is a BRG1 BRM ATPase inhibitor, suitable for studies on the treatment of BAF-related disorders.

SEC inhibitor KL-2 (KL-2) is a potent and selective inhibitor of the super elongation complex (SEC), showing a dose-dependent inhibitory effect on the AFF4-CCNT1 interaction with a Ki of 1.50 μM.

PI3K mTOR Inhibitor-2 is a potent pan inhibitor of PI3K and mTOR with IC50s of 3.4, 34, 16.1, and 4.7 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ, and mTOR, respectively. PI3K mTOR Inhibitor-2 demonstrates antitumor activity.

Pim-1 2 Kinase Inhibitor 1, an orally active inhibitor, impedes the action of Pim kinases by preventing their ability to phosphorylate peptides. It particularly inhibits the phosphorylation of 4E-BP1 and p27 Kip1 by Pim protein kinases. This compound is valuable in cancer research, with a notable application in studying prostate cancer [1].

Aurora kinase inhibitor-2 (IUN-70219) is a cell-permeable anilinoquinazoline that inhibit the activity of Aurora A (IC50 = 0.39 M).

CK2 Inhibitor 2, characterized as a potent, selective, and orally active inhibitor of CK2, demonstrates an impressive IC50 value of 0.66 nM. It exhibits high selectivity towards Clk2 with an IC50 of 32.69 nM in comparison to CK2. Furthermore, CK2 Inhibitor 2 has been shown to possess promising antiproliferative and antitumor activities [1].

ATP Synthase Inhibitor 2 (Compound 22) TFA is a potent inhibitor of Pseudomonas aeruginosa ATP synthase with an IC50 value of 10 μg/mL. It effectively halts ATP synthesis in Pseudomonas aeruginosa at a concentration of 128 μg/mL [1].

IGF-1R inhibitor-2 (example 121) is a compound that inhibits the insulin-like growth factor-1 receptor (IGF-1R), potentially reversing the transformed phenotype of tumor cells and increasing their susceptibility to apoptosis.

TAPI-2 is a broad-spectrum inhibitor of MMP (IC50: 20 μM), tumour necrosis factorα-converting enzyme (TACE) and a disintegrin and metalloproteinase (ADAM).

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].

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.

Skp2 inhibitor 2 (14f) impedes the F-box protein S-phase kinase-associated protein 2 (Skp2), demonstrating an IC50 of 10.2 μM against Skp2-Cks1. This compound targets Skp2, a component of cullin-RING ligases that recruits and ubiquitinates substrates, playing roles in both proteolytic and non-proteolytic processes [1].

URAT1 inhibitor 2 is an orally active inhibitor of URAT1 and CYP isozyme with IC50 values of 1.36 μM, 16.97 μM, and 5.22 μM for URAT1-mediated 14C-UA uptake, CYP1A2, and CYP2C9, respectively [URAT1 inhibitor 2 is a promising drug candidate for the study of hyperuricemia and gout].

ATP Synthase Inhibitor 2, a compound targeting Pseudomonas aeruginosa (PA) ATP synthase with an IC50 of 10 μg/mL, fully inhibits the ATP synthesis activity of PA at a concentration of 128 μg/mL [1].

DDR1/2 Inhibitor-2 (Example 31) serves as an inhibitor of DDR1/DDR2, exhibiting IC50 values below 100 nM. It is applicable in cancer and fibrotic disease research [1].

QS inhibitor 2 is a novel potent inhibitor of quorum sensing (QS) pathways.

CD38 inhibitor 2 is a potent CD38 inhibitor (IC 50 = 0.01 ~ 0.1 μΜ).

Microtubule inhibitor 2 is a highly potent and selective microtubule inhibitor, which is orally active. It induces cell death via ferroptosis, and exhibits notable antitumor activity [1].

EMT Inhibitor-2, targeting both CYP3A4 testosteron and CYP2C9, exhibits inhibitory effects with IC50 values of 49.72 and 5.54 μM, respectively. Furthermore, it effectively impedes the epithelial-mesenchymal transition (EMT) process, induced by immunocyte-released agents like IL-1β and TGF-β.

PI3Kγ inhibitor 2 is an orally bioavailable inhibitor of PI3Kγ(Ki of 4 nM).

TDP1 Inhibitor-2 is a potent inhibitor of TDP1 (tyrosyl-DNA phosphodiesterase 1) (IC50: 99 nM) and inhibits SCAN1 (spinal cerebellar ataxia syndrome with axonal neuropathy) (IC50: 3.5 μM).