Angiogenesis

TX2-121-1 targets HER3 for proteasome-mediated degradation to inhibit HER3-dependent signalling and growth.

<p>Ten01 exhibits a 5.0 nM inhibition of JAK1 kinase.</p>

<p>Tyk2-IN-3 is an inhibitor of Tyk2 pseudokinase (IC50: 485 nM).</p>

(-)-Cevimeline HCl hemihydrate, a muscarinic agonist, treats Sjogren's xerostomia. Quick absorption, species-dependent metabolism.

JAK-IN-19 inhibits JAK (pIC50: 7.2, 7.7), less so for VEGFR2 (7.0) and Aurora B (5.8).

TTT 3002: oral FLT3 inhibitor for AML research, blocks D835 mutations, potent at 0.2 nM IC50.

BTK-IN-15: Oral BTK inhibitor, IC50 0.7 nM, induces cancer cell apoptosis, selective with anti-tumor effects.

Flonoltinib maleate is an orally active dual inhibitor of JAK2/FLT3, with IC50 values of 0.7 nM for JAK2, 4 nM for FLT3, 26 nM for JAK1, and 39 nM for JAK3. It exhibits anticancer properties.

EGFR-IN-18 strongly inhibits L858R/T790M/C797S mutant EGFR (4.9 nM) and also targets wild-type EGFR (47 nM).

JAK3/BTK-IN-3: strong dual JAK3/BTK suppressor, promising for autoimmune disease research.

WDR5-MYC-IN-2 is an inhibitor of the WDR5-MYC protein-protein interaction (PPI) with an IC50 of 0.59 μM. It is utilized in research on MYC-driven cancers and in the development of other potent WDR5-MYC PPI inhibitors.

EGFR-IN-38: low-toxic acrylamide-derived EGFR inhibitor, targets NSCLC, patented for research on EGFR mutation-related diseases.

FAK-IN-2: potent oral FAK inhibitor, IC50 35 nM, reduces tumor growth, migration, and induces cell death.

ALK/PI3K/AKT-IN-1 (Compound 45) effectively inhibits the proliferation of cancer cell lines A549, H1975, and PC9, with IC50 values of 0.44, 0.83, and 1.51 μM, respectively. This compound enhances the expression of p21 and p27, and decreases the activity of CDK2 and p-Rb, causing cell cycle arrest at the G1 phase. It suppresses the ALK/PI3K/AKT signaling pathway, promotes mitochondrial membrane potential depolarization, and induces apoptosis in A549 cells. Furthermore, ALK/PI3K/AKT-IN-1 inhibits the formation and growth of A549 cell spheres.

WZH-15-125 is a potent ALK inhibitor capable of overcoming resistance, particularly with complex ALK mutations. It exhibits an IC50 of 101.7 nM against the highly recalcitrant Lorlatinib-resistant G1202R/L1196M mutation. Additionally, WZH-15-125 can serve as a PROTAC target protein ligand for synthesizing PROTACWZH-17-002. This compound is applicable in non-small cell lung cancer research.

EGFR/HER2-IN-8 inhibits EGFR, HER2, DHFR (IC50: 0.45, 0.244, 5.669 μM); useful in cancer research, safe and selective.

<p>FAK-IN-23 (Compound II) is an inhibitor of focal adhesion kinase (FAK).</p>

<p>I194496 is an effective inhibitor of cystathionine γ-lyase (CSE) with an IC50 value of 0.79 mM. It inhibits the growth of human TNBC cells by dual targeting the PI3K/Akt and Ras/Raf/ERK pathways. Additionally, I194496 suppresses the metastasis of human TNBC cells by downregulating the Anxa2/STAT3 and VEGF/FAK/Paxillin signaling pathways.</p>

<p>FGFR4-IN-7 is a covalent, reversible FGFR4 inhibitor (IC50: 0.42 μM) that blocks the FGFR4 signaling pathway, thereby inducing apoptosis.</p>

<p>BML-265 is a potent inhibitor of EGFR tyrosine kinase (EGFR tyrosine kinase). It disrupts Golgi apparatus integrity in human cells and hinders the transport of secretory proteins across various substances. In contrast, BML-265 does not affect the integrity and transport of the Golgi apparatus in rodent cells.</p>

NDI-034858 (TAK-279) is a tyrosine kinase 2 (TYK2) inhibitor (Kd<200 pM) that targets the JH2 structural domain of Tyk2 for the treatment of autoimmune diseases

JAK2-IN-7 selectively inhibits JAK2 (IC50: 3 nM), shows 14-fold selectivity over JAK1/3, FLT3, induces G0/G1 arrest, apoptosis, and has antitumor effects.

<p>XMD-17-51 Trifluoroacetate is a pyrimido-diazepinone compound that regulates protein kinases.</p>

JDTic, a 4-phenylpiperidine derivative distantly related to analgesics like meperidine and ketobemidone and more closely to the mu opioid antagonist alvimopan, exhibits a notably long duration of action, maintaining effects in animals for weeks following a single dose. This duration is not due to irreversible binding to the kappa opioid receptor but rather to altered activity of c-Jun N-terminal kinases. As a highly selective antagonist for the κ-opioid receptor, without influencing the μ- or δ-opioid receptors, JDTic has shown potential in animal studies for producing antidepressant and anxiolytic effects. It also demonstrates promise in treating addiction to substances such as cocaine and morphine, distinguishing itself structurally from other kappa antagonists like norbinaltorphimine.

Ibrutinib is a selective, irreversible Btk inhibitor (IC50: 0.5 nM). Ibrutinib Racemate is the racemate of Ibrutinib.

Tyrosine-protein kinase ABL, IC50: 1500 nM

<p>HMBD-001 is a humanized IgG1 monoclonal antibody inhibitor that targets HER3. By inhibiting the dimerization of HER3, HMBD-001 suppresses the growth and proliferation of tumor cells. It holds potential for research in cancer treatments, specifically for pancreatic cancer and non-small cell lung cancer.</p>

<p>XMU-MP-3 is a robust, non-covalent inhibitor of BTK, exhibiting exceptional potency with IC50 values of 10.7 nM and 17.0 nM for BTK WT and BTK C481S mutation, respectively, in the presence of 10 μM ATP. Moreover, XMU-MP-3 elicits apoptosis.</p>

(3R,4S)-Tofacitinib, the less active enantiomer of Tofacitinib, is a JAK3 inhibitor with an IC50 of 1 nM.

<p>Nimotuzumab (powder) is a humanized IgG1 monoclonal antibody that specifically targets the epidermal growth factor receptor (EGFR), possessing a dissociation constant (KD) of 0.21 nM. It blocks the binding to its ligand by targeting the extracellular domain of EGFR. Nimotuzumab exhibits strong antitumor activity by inducing both antibody-dependent cellular cytotoxicity (ADCC) and complement-dependent cytotoxicity (CDC), exerting cytolytic effects on target tumors.</p>

ENMD-2076 is an orally active kinase inhibitor. It also has antiangiogenic and antiproliferative mechanisms of action.

PCI 45227 is an active metabolite of the Bruton's tyrosine kinase inhibitor ibrutinib .1PCI 45227 is formed from ibrutinib by the cytochrome P450 (CYP) isoform CYP3A. 1.Veeraraghavan, S., Viswanadha, S., Thappali, S., et al.Simultaneous quantification of lenalidomide, ibrutinib and its active metabolite PCI-45227 in rat plasma by LC-MS/MS: Application to a pharmacokinetic studyJ. Pharm. Biomed. Anal.107151-158(2015)

<p>PM-8002 is a bispecific antibody that targets PD-L1 and VEGF-A. It is applicable for research on solid tumors.</p>

<p>Desidustat is an inhibitor of HIF hydroxylase.</p>

Olmutinib (BI1482694) is a Novel Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor

<p>Duligotuzumab (MEHD-7945A) is a bispecific humanised IgG-κ monoclonal antibody targeting HER3 and EGFR, solid tumours, head and neck cancer,colorectal cancer.</p>

<p>Applications 3,3',4,4'-Tetrabromobiphenyl is multi-persistent organic pollutants analyzed in breast milk of first time mothers. An environmental pollutant that affects copper and molybdenum metabolism in rats. Also, it is derived from 1-Bromo-2- nitrobenze (B686175), which is an organic building block used for the synthesis of various pharmaceutical compounds. It is an intermediate for the synthesis of novel Diarylamino-1,3,5-triazine derivatives as FAK inhibitors with anti-angiogenic activity.<br>References Tlustos, C., et al.: Organohalogen Compd., 75, 1185-1188 (2013); Salman, K. N., et al.: Environ. Sci. Pollut. R., 21, 6400-6409 (2014); Dao, P., et al.: Bioorg. Med. Chem. Lett., 23, 4552 (2013);<br></p>

<p>VEGFR inhibitor</p>

<p>KBP-7018: potent tyrosine kinase inhibitor targeting c-KIT, RET, PDGFR with IC50s of 10, 7.6, 25nM.</p>