Angiogenesis

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

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

Siphonaxanthin is a carotenoid found in green algae, known for targeting the death receptor 5 (DR5) on cancer cells to induce apoptosis. In human leukemia HL-60 cells, it increases DR5 expression, reduces Bcl-2 levels, and activates caspase-3. It also inhibits fibroblast growth factor receptor-1 (FGFR-1) signaling in endothelial cells. Siphonaxanthin suppresses the proliferation, migration, and tubular formation of human umbilical vein endothelial cells (HUVECs), as well as the growth of microvessels in rat aorta rings. Additionally, it has anti-inflammatory properties by blocking the translocation of high-affinity IgE receptors (FcεRI) to lipid rafts in mast cells. Siphonaxanthin shows potential for research into diseases such as cancer, diabetic retinopathy, and rheumatoid arthritis.

N-Deshydroxyethyl Dasatinib-C3-NH2 is a target protein ligand-linker conjugate, comprising an LCK ligand and a PROTAC linker, designed to recruit E3 ligase. It is utilized in the synthesis of [PROTACSJ11646].

<p>EGFR-IN-125 (example 37) is a potent EGFR inhibitor with IC50 values of &lt;0.3 nM for EGFR(d746-750/T790M/C797S), 0.52 nM for EGFR(L858R/T790M/C797S), 0.5 nM for EGFR(d746-750/C797S), 0.69 nM for EGFR(L858R/C797S), and 0.92 nM for EGFR (wild type).</p>

VEGFR/PDGFR-IN-1 (Compound 1) is an inhibitor of VEGFR with an IC50 of 0.4 μM. It can inhibit angiogenesis in HUVEC cells and holds promise for impeding tumor growth and metastasis.

VEGFR-2-IN-14 (Compound 5) is a potent inhibitor of VEGFR-2, which inhibits the growth of HepG2 cells in the Pre-G1 phase and induces apoptosis.

HBI-2375 (HYBI-084) is a selective inhibitor that penetrates the blood-brain barrier and is orally active, targeting the MLL1-WDR5 interaction. It inhibits WDR5 with an IC50 of 4.48 nM and demonstrates antiproliferative activity in MV4;11 leukemia cells with an IC50 of 3.17 µM. Furthermore, HBI-2375 disrupts histone methyltransferase activity in cancer cells and is useful for researching leukemia, glioma, and glioblastoma.

BTK-IN-10 is a potent inhibitor of BTK, acting on wild-type BTK (IC50<5 nM) or mutant BTK (C481S) (IC50<5 nM).

BTK-IN-16 is a potential inhibitor of wild-type BTK and C481S mutants.BTK-IN-16 can be used to study various autoimmune diseases and cancers caused by BTK.

ALK-IN-23 inhibits ALK (IC50: 1.6-0.71 nM), hinders cancer cell spread, forms colonies in vitro, and reduces tumors in mice with low toxicity.

EGFRLigand-Linker Conjugates 1 is a Target Protein Ligand-Linker Conjugate comprising an EGFR ligand and a PROTAC linker, designed to recruit the E3 ligase. It is used in the synthesis of PROTACEGFRdegrader 3.

<p>HER2-IN-21 (compound 657994) is an inhibitor of the human epidermal growth factor receptor 2 (HER2) with an IC50 value of 3.85 μM.</p>

PROTACHer3-binding moiety 2 is an inhibitor of Her3. It is applicable in the synthesis of PROTACHer3 Degrader-8.

FGFR1 inhibitor-6, IC50: 16.31 nM, blocks cell cycle at pro-G1/G2/M and induces apoptosis.

Protein kinase inhibitor 10 is a protein kinase inhibitor with IC50 values of 28.9 μM, 13.6 μM, and 2.41 μM for TAM receptors, FAK, and KIT, respectively. It can inhibit abnormal and excessive cell proliferation, showing potential for research in the field of cancer treatment.

DualCathepsinL/JAK-IN-1 (Compound A8) serves as a dual inhibitor of Cathepsin L (CTSL) and JAK, exhibiting IC50 values of 0.68 μM for CTSL and 337.1 nM, 5.251 nM, 27.29 nM, and 172.6 nM for JAK1/2/3 and TYK2, respectively. This compound effectively prevents the activation of MAPK, NF-κB, and JAK/STAT signaling pathways, leading to significant anti-inflammatory therapeutic effects. DualCathepsinL/JAK-IN-1 is applicable in research on acute lung injury (ALI).

PF-06463922 acetate: ALK/ROS1 inhibitor, brain- penetrable, active vs crizotinib-resistant mutants, in NSCLC trials.

EGFR-IN-62: IC50 of 10-242 nM for various EGFR mutations, blocks A549/H1975 cell cycle, induces apoptosis, and inhibits cell motility and proliferation.

NSC381467: Potent, oral EGFR-TK inhibitor with strong antiproliferative effects, promising for cancer research.