cysteine protease inhibitor 2

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.

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

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

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.

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

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.

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

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

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.

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

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

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.

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

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

IGF-1R inhibitor-2 (example 121) is a compound that inhibits the insulin-like growth factor-1 receptor (IGF-1R). By downregulating the IGF-1R, it has the potential to reverse the transformed phenotype of tumor cells and make them more susceptible to apoptosis.

Antitumor Agent-108 (Compound 5), an inhibitor of the Hyaluronic Acid (HA)-CD44 interaction, effectively disrupts cancer spheroid integrity and exhibits antiproliferative activity against cancer cells [1].

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

TAO Kinase inhibitor 2 is a TAO kinase inhibitor with an IC50 of 50-500 nM. TAO Kinase inhibitor 2 inhibits KIAA1361 and JIK with IC50s of 50-500 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.

Compound 5K (Multi-target kinase inhibitor 2) is a multi-targeted kinase inhibitor demonstrating activity against EGFR, Her2, VEGFR2, and CDK2 with IC50 values between 40 to 204 nM. It exhibits cytotoxic effects on HepG2, HeLa, MDA-MB-231, and MCF-7 cell lines, with IC50 values of 41, 57, 51, and 59 μM, respectively. Additionally, it induces cell cycle arrest and apoptosis specifically in HepG2 cells.

αvβ6 Integrin Inhibitor 2 is a potent inhibitor of αvβ6 integrin, demonstrating an inhibition concentration (IC50) of 96.5 nM.

WRN Inhibitor 2 (example 118), a potent inhibitor of the WRN (Werner Syndrome ATP-dependent helicase enzyme), exhibits a pIC50 value of 7.0 or greater [1].

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

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

NAMPT inhibitor-linker 2, a drug-linker conjugate for antibody-drug conjugates (ADCs), comprises an NAMPT inhibitor payload and a linker. When combined with an anti-c-Kit monoclonal antibody to form ADC-4, it demonstrates potent efficacy against c-Kit expressing cell lines, including GIST-T1 and NCI-H526, with IC50 values of <7 pM and 40 pM, respectively.

SORT-PGRN Interaction Inhibitor 2 is a compound that downregulates SORT1 protein expression and enhances extracellular progranulin (PGRN) secretion in various mammalian cell lines, and is utilized in the study of neurological diseases [1].

Beclin1-Bcl-2 Interaction Inhibitor 1 effectively disrupts the binding of Beclin 1 to Bcl-2, and is utilized in cancer and neurodegeneration research [1].

Cathepsin K inhibitor 2 is a potent inhibitor of cathepsin K. Cathepsin K (Cat K) is a cysteine protease expressed under the control of the CTSK gene, which is closely related to osteoporosis and hydrolyses collagen. cathepsin K inhibitor 2 has shown potential in osteoarthritis.

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

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].

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].

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].

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].

ROCK inhibitor-2 is a selective dual inhibitor of ROCK1 and ROCK2 (IC50s of 17 nM and 2 nM, respectively).

IDH1 Inhibitor 2 (compound 13) is a potent IDH1 inhibitor via direct covalent modification of His315 (IC50: 110 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).

Protease-Activated Receptor-1 Antagonist 2 is an orally active antagonist of protease-activated receptor-1 (PAR-1), demonstrating significant potency with an IC 50 of 7 nM. It exhibits favorable pharmacokinetic characteristics, making it valuable in cardiovascular disease (CVD) research, including studies on atherosclerosis and restenosis [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].

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.

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

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.

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

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].

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

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

YAP/TAZ inhibitor-2 is a potent and orally active TEAD-YAP/TAZ inhibitor with an EC 50 value of 3 nM. YAP/TAZ inhibitor-2 shows anti-proliferative and antitumor activity [1].

Compound 7c, identified as carbonic anhydrase inhibitor 1, effectively inhibits carbonic anhydrase II. This inhibitor, also known as carbonic anhydrase inhibitor 3, lowers intraocular pressure in glaucomatous rabbits [1].

P38α Inhibitor 2, a potent and selective inhibitor of p38α MAPK, exhibits a pIC50 value of 9.6. It also demonstrates inhibition of the hERG ion channel (IC50=27 μM) and maintains promising selectivity, with <30% inhibition across a panel of 51 protein kinases at a 10 μM concentration and a broad specificity against 141 other biological targets[1].

Compound BDEO (URAT1&XO inhibitor 2) serves as a dual-action inhibitor targeting both xanthine oxidase (XO) and URAT1, demonstrating an IC50 value of 3.3 μM for XO inhibition. It effectively impedes uric acid uptake in HEK293 cells with URAT1 expression, evidenced by a Ki of 0.145 μM. In hyperuricemic mice models, the compound has been shown to reduce serum urate levels and uric acid excretion, indicating potential utility for hyperuricemia research [1].