proline-rich tyrosine kinase 2

TIE-2 VEGFR-2 kinase-IN-5 (TIE-2 and VEGFR-2 tyrosine kinase receptor inhibitor) is a potent agent with anti-angiogenic activity, commonly used in biomedical research focused on angiogenesis.

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.

1-[(5-chlorothiophen-2-yl)sulfonyl]pyrrolidine-2-carboxylic acid has been used as a starting material for the synthesis of drugs, polymers, etc., and has also been used to synthesize bioactive compounds such as peptides, peptoids, and Other small molecules.

MET kinase-IN-2, a selective and potent MET kinase inhibitor, demonstrates oral bioavailability and exhibits an IC50 value of 7.4 nM. It also possesses antitumor activity[1].

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).

PDGFR Tyrosine Kinase Inhibitor III (PDGF Receptor Tyrosine Kinase Inhibitor III) is a multikinase inhibitor that inhibits PDGFR, EGFR, FGFR, PKA, and PKC and can be used for research on amyotrophic lateral sclerosis [1].

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).

Tyrosine kinase inhibitor is a tyrosine kinase inhibitor used in combination with fragmenting aromatic nitrogen compounds as antiproliferative agents.

TIE-2 VEGFR-2 kinase-IN-4, a benzimidazole derivative, is a potent inhibitor of the tyrosine kinase receptors TIE-2 and VEGFR-2, with IC50 values of 5.2 nM and 5.1 nM, respectively. This compound is utilized in angiogenesis research [1].

Rho-Kinase-IN-2 (Compound 23) is an orally active and selective inhibitor of Rho Kinase (ROCK) with CNS penetration, exhibiting a high affinity for ROCK2 with an IC50 of 3 nM. This compound is of potential interest for further investigations in Huntington's disease research [1].

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.

Multi-kinase-IN-2 is an orally active inhibitor of angiokinases. multi-kinase-IN-2 significantly inhibits the activity of angiokinases such as VEGFR-1/2/3, PDGFRα/β, FGFR-1, LYN and c-KIT kinases. -IN-2 significantly attenuates phosphorylation of AKT and ERK proteins, induces apoptosis and has anticancer effects.

RIP2 kinase inhibitor 2 is a compound that inhibits receptor-interacting protein-2 kinase (RIP2).

TIE-2 VEGFR-2 kinase-IN-1 is employed in the synthesis of TIE-2 and or VEGFR-2 inhibitors for studying diseases associated with inappropriate angiogenesis [1].

Casein Kinase 2 Substrate Peptide, a widely recognized CK2 substrate, is synthesized with its C-terminus conjugated to 5-[(2-aminoethyl)amino]naphthalene-1-sulfonic acid (EDANS). This peptide serves as a tool for determining protein kinase CK2 activity [1].

EGFR Protein Tyrosine Kinase Substrate is an EGFR protein tyrosine kinase substrate.

PI3-Kinase α Inhibitor 2 (hydrochloride) is a PI3-Kinase α inhibitor.

TIE-2 VEGFR-2 kinase-IN-3, a benzimidazole derivative, is a potent inhibitor of tyrosine kinase receptors TIE-2 and VEGFR-2, with IC50 values of 6.9 nM and 3.5 nM, respectively. This compound is useful for angiogenesis research [1].

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.

Glutamate-5-kinase-IN-2 (compound 54) is a potent glutamate-5-kinase (G5K) inhibitor with an MIC of 4.2 μM, exhibiting G5K inhibition by promoting conformational changes at the L-glutamate binding site. Glutamate-5-kinase-IN-2 has potential for anti-TB research [1].

Tyrosine kinase-IN-1 is a multi-targeted tyrosine kinase inhibitor that acts on KDR, Flt-1, FGFR1, and PDGFRα with IC50 values of 4 nM, 20 nM, 4 nM, and 2 nM, respectively.

Compound 5b, designated as Pim-1 2 kinase inhibitor 2, acts as a competitive inhibitor of both PIM-1 and PIM-2 kinases, demonstrating IC50 values of 1.31 μM and 0.67 μM, respectively. This compound exhibits potent in-vitro anticancer activity against various cancer cell lines, including myeloid leukemia (NFS-60), liver (HepG-2), prostate (PC-3), and colon (Caco-2), while showing low cytotoxicity to the normal human lung fibroblast Wi-38 cell line [1].

IRE1α kinase-IN-2 is a highly potent inhibitor of IRE1α kinase, demonstrating an EC50 of 0.82 μM and impeding IRE1α kinase autophosphorylation with an IC50 of 3.12 μM. It also effectively inhibits the splicing of XBP1 mRNA in wild-type cell lines.

Tyrosine Protein Kinase JAK 2 (Phospho-Tyr8, 9) is a peptide derived from mouse JAK2, consisting of amino acids 475 to 491.

Tyrosine kinase-IN-7 is a potent inhibitor of the tyrosine kinase EGFR, inhibiting EGFR(WT) and EGFR(T790M) and showing anti-cancer and anti-tumor activity in a variety of cancer cell lines. Tyrosine kinase-IN-7 has potential anti-inflammatory and antiviral activities.

Tyrosine Kinase Peptide 1 is a control substrate peptide used in c-Src assay.

Phosphatidylinositol 3-kinase (PI3K) catalyzes the phosphorylation of the 3' hydroxyl position of PIs to produce the second messengers PtdIns-(3,4)-P2 and PtdIns-(3,4,5)-P3. PI3Kα, β, and δ are class 1A enzymes composed of p110 and p85 subunits, whereas PI3Kγ is a class 1B PI3K composed of a p110 catalytic subunit and a p101 or p84 regulatory subunit. PI3Kα inhibitor 2 is a selective inhibitor of PI3Kα with IC50 values of 2, 16, 660, and 220 nM for the α, β, γ, and 2Cβ isoforms, respectively. It inhibits PKA, KDR, PKCα, and cyclin E/Cdk2 significantly less effectively (IC50 = 91, 3.4, 466, and 28 μM, respectively). PI3Kα inhibitor 2 inhibits A375 melanoma cell proliferation with an IC50 value of 580 nM.

Tyrosine kinase-IN-4 (EXAMPLE 107) is a protein tyrosine kinase inhibitor [1].

Tyrosine kinase-IN-6 is a potent inhibitor of RON splice variants, exhibiting notable anticancer and antineoplastic effects [1].

Pim-1 kinase inhibitor 2 (Compound 13) is a potent inhibitor of Pim-1 kinase with potential for cancer research due to its ability to induce apoptosis [1].

PF-431396 is a dual PYK2/FAK inhibitor (IC50: 11/2 nM).

PF-562271 is an effective ATP-competitive, reversible inhibitor of FAK(IC50=1.5 nM) and Pyk2 kinase(IC50=13 nM).

NVP-TAE 226 (TAE226) is a potent FAK inhibitor (IC50: 5.5 nM), exhibiting even greater efficacy against Pyk2 (IC50: 3.5 nM), and is 10- to 100-fold less effective against IGF-1R, InsR, c-Met, and ALK.

PF-562271 hydrochloride (PF-562271 HCl) is a potent, ATP-competitive, reversible inhibitor of FAK with IC50 of 1.5 nM in cell-free assays, ~10-fold less potent for Pyk2 than FAK and >100-fold selectivity against other protein kinases, except for some CDKs.

PF-562271 besylate (PF-00562271 Besylate) is a potent, ATP-competitive, reversible inhibitor of FAK with IC50 of 1.5 nM, ~10-fold less potent for Pyk2 than FAK and >100-fold selectivity against other protein kinases, except for some CDKs.

PF-4618433 is a dual inhibitor of focal adhesion kinase (FAK) and proline-rich tyrosine kinase 2 (PYK2).