BAY 61-3606 is a potent, ATP-competitive, reversible, and highly selective inhibitor of Syk tyrosine kinase activity (Ki= 7.5 nM) with no inhibitory effect against Btk, Fyn, Itk, Lyn, and Src.IC50 value: 7.5 nM (Ki) [1]Target: Sykin vitro: BAY 61-3606 inhibited not only degranulation (IC50 values between 5 and 46 nM) but also lipid mediator and cytokine synthesis in mast cells. BAY 61-3606 was highly efficacious in basophils obtained from healthy human subjects (IC50 = 10 nM) and seems to be at least as potent in basophils obtained from atopic (high serum IgE) subjects (IC50 = 8.1 nM). B cell receptor activation and receptors for Fc portion of IgG signaling in eosinophils and monocytes were also potently suppressed by BAY 61-3606 [1]. We identified BAY61-3606 as an inhibitor of proliferation in colorectal cancer cells expressing mutant forms of K-RAS, but not in isogenic cells expressing wild-type K-RAS. In addition to its anti-proliferative effects in mutant cells, BAY61-3606 exhibited a distinct biological property in wild-type cells in that it conferred sensitivity to inhibition of RAF. In this context, BAY61-3606 acted by inhibiting MAP4K2 (GCK), which normally activates NFκβ signaling in wild-type cells in response to inhibition of RAF [2].in vivo: Oral administration of BAY 61-3606 to rats significantly suppressed antigen-induced passive cutaneous anaphylactic reaction, bronchoconstriction, and bronchial edema at 3 mg/kg. Furthermore, BAY 61-3606 attenuated antigen-induced airway inflammation in rats [1].
Anti-inflammatory agent 21 (compound 9o) is an orally active and low cytotoxic anti-inflammatory agent, with an IC50 value of 0.76 μM for NO. Anti-inflammatory agent 21 acts via accumulation ROS and blocks the NF-κB/MAPK signaling pathway. Anti-inflammatory agent 21 can ameliorate cartilage destruction and inflammatory cell infiltration in arthritis rats model[1].
EGFR-IN-49 is a potent and selective EGFR inhibitor with IC50s of 65.0 nM and 13.6 nM for EGFRT790M and EGFRT790M/L858R, respectively. EGFR-IN-49 induces late apoptosis in a dose-dependent manner[1].
CSF1R-IN-7 (Formula I) is a CSF-1R inhibitor. CSF1R-IN-7 can be used for Alzheimer’s disease research[1].
Mipasetamab is an IgG1κ antibody targeting to AXL, a tyrosine kinase receptor and an TAM Receptor. Mipasetamab involves in synthesis of ADCT-601 (Mipasetamab uzoptirine), an AXL-targeted antibody-drug conjugate (ADC). ADCT-601 has anti-tumor activity[1].
AMG 925 is a potent, selective, and orally available FLT3/CDK4 dual inhibitor with IC50s of 2±1 nM and 3±1 nM, respectively.
Lapatinib-d4-1 is deuterium labeled Lapatinib. Lapatinib (GW572016) is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively[1].
IRAK4-IN-28 (compound 42) is an orally active IRAK4 inhibitor (IC50=8.9 nM). IRAK4-IN-28 has binding affinity for IRAK4 with a Kd of 0.58 nM. IRAK4-IN-28 can be used in the research of inflammation and autoimmune diseases[1].
A 419259 trihydrochloride is a Src family kinases inhibitor with IC50s of 9 nM, 3 nM and 3 nM for Src, Lck and Lyn, respectively.
FGFR-IN-6 (Compound 5) is a FGFR inhibitor[1].
JNJ 17029259 is an orally active and selective VEGF-R2 kinase inhibitor. JNJ 17029259 inhibits VEGF-mediated signal transduction. JNJ 17029259 has anti-angiogenic activity[1][2].
FGFR1 inhibitor-10 (Compound 4i) is an FGFR1 inhibitor (IC50: 28 nM). FGFR1 inhibitor-10 inhibits the phosphorylation of FGFR1. FGFR1 inhibitor-10 has anti-angiogenic, anti-invasion activity, and anti-tumor effect[1].
Tinengotinib is the modulator of one or more protein kinases such as Aurora kinase and VEGFR kinase. Tinengotinib has the potential for the research of these kinase abnormalities diseases mediated, especially cancer-related diseases (extracted from patent WO2018108079A1)[1].
OXSI-2 is a bioavailable, cell-permeable Syk inhibitor with an EC50 of 313 nM and an IC50 of 14 nM[1][2].
GW297361 is an oxindole CDK inhibitor that elicits a Pho85-selective response in cells. GW297361 inhibits yeast Cdk1 and Pho85 with IC50s of 20 nM and 400 nM in vitro, respectively[1].
Theliatinib (Xiliertinib) tartrate is a potent, ATP-competitive, orally active and highly selective EGFR inhibitor with a Ki of 0.05 nM and an IC50 of 3 nM. Theliatinib has an IC50 of 22 nM for EGFR T790M/L858R mutant. Theliatinib shows >50-fold selectivity for EGFR than other kinases[1].
8-Chloro-cAMP is a cAMP analogue that induces growth arrest, and modulates cAMP-dependent PKA activity. 8-Chloro-cAMP has anticancer activity[1].
Anticancer agent 42 (compound 10d) is an orally active anticancer agent, and shows a potent antitumor activity against MDA-MB-231 cell with an IC50 of 0.07 μM. Anticancer agent 42 can exert its anticancer activity by activating apoptotic pathway and p53 expression. Anticancer agent 42 can be used to study metastatic breast cancer[1].
SM 16 is a ALK5/ALK4 kinase inhibitor with Kis of 10 and 1.5 nM, respectively.
PKI(5-24) is a potent, competitive, and synthetic peptide inhibitor of PKA (cAMP-dependent protein kinase), with a Ki of 2.3 nM. PKI(5-24) corresponds to residues 5-24 in the naturally occurring heat-stable protein kinase inhibitor[1][2].
AZ7550-d5 is the deuterium labeled AZ7550 (HY-B0794). AZ7550, an active metabolite of AZD9291 (HY-15772), inhibits the activity of IGF1R with an IC50 of 1.6 μM[1][2].
(S)-Sunvozertinib ((S)-DZD9008), the S-enantiomer of Sunvozertinib, shows inhibitory activity against EGFR exon 20 NPH and ASV insertions, EGFR L858R/T790M mutation and Her2 exon20 YVMA insertion (IC50=51.2 nM, 51.9 nM, 1 nM, and 21.2 nM, respectively). (S)-Sunvozertinib also inhibits BTK[1].
PKA Inhibitor Fragment (6-22) amide is an inhibitor of cAMP-dependent protein kinase A (PKA), with a Ki of 2.8 nM. PKA Inhibitor Fragment (6-22) amide can significantly reverse low-level morphine antinociceptive tolerance in mice[1][2].
PRN1008 is a reversible covalent inhibitor of Bruton’s Tyrosine Kinase (BTK), with an IC50 of 1.3 nM.
Axl-IN-8 (NO.1) is a potent AXL inhibitor, with an IC50 of <1 nM. Axl-IN-8 also inhibits c-MET, with an IC50 of 1-10 nM. Axl-IN-8 shows anti-proliferative activity against BaF3/TEL-AXL, MKN45, and EBC-1 cells, with IC50 values of <10, 226.6 and 120.3 nM, respectively[1].
Canlitinib is a tyrosine kinase inhibitor, extracted from patent WO2018072614 (IV-2). Canlitinib has the potential for cancer study.
Osimertinib-13C,d3 is the deuterium and 13C labeled Osimertinib. Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M, respectively.
SU5214 is a potent VEGFR2 inhibitor extracted from patent US5834504A, SU5214, has the IC50s of 14.8 µM (FLK-1) and 36.7 µM (EGFR), respectively[1].
ANA-12 is a potent and selective TrkB antagonist with IC50s of 45.6 nM and 41.1 μM for the high and low affinity sites, respectively.
CP-547632 is a potent inhibitor of the VEGFR2 and FGF2 kinases with IC50s of 11 and 9 nM, respectively.