tyrosine kinase-in-1

Tyrosine kinase-IN-1 is a multi-targeted tyrosine kinase inhibitor（KDR, Flt-1, FGFR1 and PDGFRα with IC50s of 4nM, 20nM, 4nM, 2 nM ,respectively）

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.

Protein kinase inhibitors 1 hydrochlorid (Protein kinase inhibitors 1 hydrochlorid (1365986-44-2(free base))) is a novel inhibitor of HIPK2 with an IC50 of 74 nM and Kd of 9.5 nM.

can be used in research in the fields of chemistry and life sciences.

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.

Rho-Kinase-IN-1 is an inhibitor of ROCK with Kis of 30.5 nM and 3.9 nM for ROCK1 and ROCK2, respectively. Rho-Kinase-IN-1 can be used in studies about excessive cell proliferation, remodeling, edema and inflammation diseases.

EML4-ALK kinase inhibitor 1 (EML4 ALK kinase inhibitor 1) is a potent oral active inhibitor of echinoderm microtubule-associated protein-like 4-anaplastic lymphoma kinase (EML4-ALK), with an IC50 of 1 nM.

Multi-kinase inhibitor 1 (Multi-kinase inhibitor I) is a Multi-kinase inhibitor.

Pim-1 kinase inhibitor 8 is a potent Pim-1 kinase inhibitor with anticancer activity and can effectively inhibit cell migration.Pim-1 kinase inhibitor 8 is cytotoxic to MCF-7 and HepG2 cells, and is a candidate compound for breast cancer research.

Protein kinase G inhibitor-1 is a potent Protein kinase G inhibitor, IC50= 0.9 uM.

Protein Kinase C (19-31) TFA, a peptide inhibitor of protein kinase C (PKC), derived from the pseudo-substrate regulatory domain of PKCa (residues 19-31) with a serine at position 25 replacing the wild-type alanine, is used as protein kinase C substrate p

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

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

Tie2 kinase inhibitor 1 (Tie2 kinase inhibitor), an optimized compound of SB-203580, is selective to Tie2 with IC50 of 0.25 μM, which is 200-fold more effective than p38.

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

Protein kinase affinity probe 1 is a protein kinase affinity probe for the functional identification of protein kinases (PKs).

C-RAF kinase-IN-1 is a potent inhibitor of C-RAF kinase with an IC 50 of 0.193 μM. C-RAF kinase-IN-1 is a quinoline derivative. C-RAF kinase-IN-1 has the potential for the research of cancer diseases .

IRE1α kinase-IN-1 is a highly selective IRE1α (ERN1) inhibitor, with an IC50 of 77 nM. It displays 100-fold selectivity for IRE1α over the IRE1β isoform. It inhibits ER stress-induced IRE1α oligomerization and autophosphorylation, and also inhibits IRE1α RNase activity (IC50=80 nM)

Pim-1 kinase inhibitor 1 can be used in cancer research, showing anticancer activity against a variety of cancer cell lines by promoting cell apoptosis. Pim-1 kinase inhibitor 1 is an inhibitor of Pim-1 kinase with an IC 50 value of 0.11 μM [1].

TIE-2/VEGFR-2 kinase-IN-1 is used for the synthesis of TIE-2 and/or VEGFR-2 inhibitors that can be used for the study of diseases associated with inappropriate angiogenesis [1].

Multi-kinase-IN-1, a powerful kinase inhibitor, exhibits antitumor properties by inducing cell apoptosis. It is under investigation for its potential application in treating colorectal cancer.

Glutamate-5-kinase-IN-1 (compound 50) is a potent glutamate-5-kinase (G5K) inhibitor which acts by altering the ATP binding site architecture for enzyme recognition (MIC = 4.1 μM). Glutamate-5-kinase-IN-1 has the potential for anti-TB research [1].

Tpl2 Kinase Inhibitor 1 is an effective and selective Tpl2 inhibitor.

Protein Kinase Inhibitors 1 Hydrochloride effectively inhibits HIPK2, demonstrating high potency with IC50 values of 136 nM for HIPK1 and 74 nM for HIPK2, alongside a dissociation constant (Kd) of 9.5 nM for HIPK2.

EGFR kinase inhibitor 1 is a potent inhibitor of EGFR that acts on WT (IC50: 37 nM), l885R/T790M (IC50: 1.7 nM), and L858R/T790M/C797S (IC50>300 nM). EGFR kinase inhibitor 1 is capable of blocking the cell cycle in G0/G1 phase, inducing apoptosis, and showing an inhibitory effect on cell metastasis. EGFR kinase inhibitor 1 exhibits anti-proliferative and anti-tumor effects.

PDGFRα kinase inhibitor 1 is a highly selective inhibitor of type II PDGFRα kinase (PDGFRα and PDGFRβ with IC50s of 132 nM and 6115 nM , respectively).

RIP2 kinase inhibitor 1 is a potent and selective receptor interacting inhibitor of protein 2 (RIP2) kinase(RIP2 FP with an IC50 of 0.03 μM ),and is used for autoinflammatory disorders.

Pim-1 kinase inhibitor 5 (Compound 4c), with an IC50 of 0.61 μM, exhibits cytotoxicity against various cancer cell lines, including HepG2, MCF-7, PC3, and HCT-116, with IC50 values ranging from 6.95 to 20.19 μM [1].

Mitogen-activated protein kinase 1 (MAPK1) activates the p38/NF-κB pathway and regulates cellular processes in sepsis-associated diseases. Its catalytic action phosphorylates substrate proteins, serving as a regulatory switch for their activity [1].

Aurora kinase-IN-1, a potent aurora kinase inhibitor, modulates cell cycle progression and induces apoptosis by upregulating G1 cell cycle inhibitory proteins (including p21 and p27), elevating G1 progressive cyclin D1, and downregulating G1-to-S progressive cyclins, thereby arresting the cell cycle at the G1/S boundary. It stands as a promising lead compound for the development of chemotherapeutic agents.

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

Pan-RAF kinase inhibitor 1 is a potent inhibitor of the Pan-RAF kinase pair that inhibits RAF kinase and regulates MAPK signaling, thereby affecting the proliferation of RAS-mutated tumor cells. Pan-RAF kinase inhibitor 1 has shown research potential for the study of cancer diseases.

Protein kinase D inhibitor 1 (compound 17m) is a potent pan-PKD inhibitor. It exhibits inhibitory activity in the low nanomolar range, with IC50 values ranging between 17 and 35 nM. By inhibiting protein kinase D, this compound effectively suppresses cortactin phosphorylation, which is known to be PKD-dependent [1].

SAR348830 is an ALK inhibitor, targeting anaplastic lymphoma kinase.

TAO Kinase inhibitor 1 delays mitosis and induces mitotic cell death. TAO Kinase inhibitor 1 is a selective and ATP-competitive thousand-and-one amino acid kinases inhibitor (IC50s: 11 to 15 nM for TAOK1 and 2, respectively).

Protein kinase inhibitors 1 is a novel inhibitor of HIPK2 with an IC50 of 74 nM and Kd of 9.5 nM.

JAK kinase-IN-1 (Example 1) functions as a potent inhibitor targeting the JAK family, which includes TYK2, JAK1, JAK2, and JAK3, with IC50 values of 4.2 nM, 32 nM, 27 nM, and 3473 nM, respectively [1].

Casein kinase 1δ-IN-1 (WAY-643895) is an inhibitor of casein kinase 1δ (CK1δ), which inhibits CK1δ. Casein kinase 1δ-IN-1 can be used in the study of neurodegenerative diseases such as Alzheimer's disease.

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

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

Pantothenate Kinase-IN-1 (Compound 1) functions as a modulator of Pantothenate Kinase (PANK), exhibiting an inhibition concentration (IC50) value of 0.51 μM against PANK3. It demonstrates notable ligand efficiency with a LipE value of 2.8 [1].

RIP1 kinase inhibitor 1 is an orally available and brain-penetrating inhibitor of RIP1 kinase with pKi of 9.04.

Pim-1 kinase inhibitor 3 (Compound H5) is a potent inhibitor of Pim-1 kinase, demonstrating an inhibitory concentration (IC50) of 35.13 nM [1].

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

Aurora/LIM kinase-IN-1 (Compound F114) is a potent aurora and lim kinase dual inhibitor. Aurora/LIM kinase-IN-1 inhibits the proliferation and invasion of GBM that may be used in drug development efforts for GBM, furthermore other cancers. Aurora kinases and lim kinases are the kinases which involved in neoplastic cell division and cell motility, respectively [1].

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

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].

hRIO2 kinase ligand-1 is a potent ligand for hRIO2 kinase (Kd: 520 nM).

Gilteritinib (ASP2215) is a potent inhibitor at the FMS-related tyrosine kinase 3 (FLT3) and AXL tyrosine kinase receptors (IC50 = 0.29 nM and <1 nM, respectively). In preClinicalal studies, gilteritinib showed strong antileukemic and antitumor effects. Gilteritinib is currently in several Phase 3 Clinicalal trials for acute myeloid leukemia.

BI-4020 is a fourth-generation, orally active, and non-covalent inhibitor of EGFR tyrosine kinase. BI-4020 exhibits activity agains the triple mutant EGFR del19 T790M C797S variant (IC50=0.2 nM in BaF3 cell lines), the double mutant EGFR del19 T790M and primary mutant EGFR del19 (IC50=1 nM) and EGFR wt (IC50=190 nM). BI-4020 exhibits high kinome selectivity and good DMPK properties.