Angiogénese

Lirucitinib is a JAK inhibitor known for its anti-inflammatory properties.

JAK3 Covalent Inhibitor-1 is a compound characterized by its potent and selective inhibition of Janus kinase 3 (JAK3), possessing an IC50 of 11 nM and

LNK01004 is a JAK inhibitor that exhibits potent inhibitory effects on JAK1 (IC50: 10 nM), JAK2 (IC50: ＜0.51 nM), and TYK2 (IC50: 1.0 nM). It can concurrently inhibit multiple cytokine-induced p-STAT signaling pathways and is applicable for research on diseases such as atopic dermatitis.

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.

JAK3-IN-7 is a potent and selective JAK3 inhibitor (IC50<0.01 μM) for the treatment of rejection in organ transplantation, graft-versus-host reaction after

TQ-3959 is an orally active BTKPROTAC degrader, with a DC50 of 14.6 nM. It exhibits antiproliferative activity against both wild-type BTK and BTK C481S mutant cell lines. TQ-3959 demonstrates tumor growth inhibition in female NOD-SCID mice with TMD-8 xenografts. This compound is applicable in the study of B-cell malignancies, such as lymphoma.

mG2N001, a negative allosteric modulator (NAM) of the metabotropic glutamate receptor mGluR2, has an IC50 of 93 nM and binds to mGluR2 as an antagonist with a Ki of 63 nM. This compound is microparticle- and plasma-stable, and its radioisotope [11C] mG2N001 can be utilized in PET imaging. [11C] mG2N001 exhibits good brain heterogeneity and penetration, selectively accumulating in mGluR2-rich regions to produce high-contrast brain images [1].

DHFR-IN-4 is a potent dihydrofolate reductase (DHFR) inhibitor with anti-tumour activity, inhibits EGFR and HER2 and can be used to study pancreatic cancer.

VEGFR-2-IN-38 (compound 3) acts as a potential inhibitor of the vascular endothelial growth factor receptor-2 [1].

WS-11 is a non-covalent reversible inhibitor of BTK, with IC50 values of 3.9 nM for the wild-type and 2.2 nM for the C481S mutant BTK. In addition to strong hydrogen bonding, WS-11 also forms robust π-π interactions with PHE540, and p-π interactions with LYS430 within the active pocket.

EGFR-IN-125 (example 37) is a potent EGFR inhibitor with IC50 values of <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).

Tuspetinib (HM43239) dihydrochloride is a selective FLT3 inhibitor with oral bioactivity, exhibiting IC50 values of 1.1 nM for FLT3 wild type, 1.8 nM for FLT3ITD mutant type, and 1.0 nM for FLT3D835Y mutant type. As a reversible type I inhibitor, it directly suppresses FLT3 kinase activity and modulates p-STAT5, p-ERK, SYK, JAK1/2, and TAK1. Tuspetinib dihydrochloride inhibits the proliferation of leukemia cells and induces apoptosis (apoptosis).

(Rac)-Ibrutinib alkyne (Compound 8) is a Btk inhibitor with an IC50 of 0.72 nM. This compound effectively inhibits B cell receptor signaling functions, with an IC50 of 9 nM for calcium flux inhibition in Ramos cells. (Rac)-Ibrutinib alkyne is applicable in research on diseases such as rheumatoid arthritis.

FLT3-IN-32 is a potent FLT3 inhibitor with high selectivity, effectively suppressing FLT3 activating mutations and inducing apoptosis. It demonstrates good tolerance in non-tumor-bearing mice. In NOD/SCID mice loaded with MV4-11 cells, FLT3-IN-32 exhibits outstanding antitumor efficacy, significantly extending mouse survival. FLT3-IN-32 is applicable for acute myeloid leukemia research.

Pred17 is an effective EGFR inhibitor with potential applications in lung cancer research.

7PPD-Q is a substituted p-phenylenediamine antioxidant derivative. It exhibits toxicity towards the bacterium V. fischeri (EC50= 14.9 mg/L).

D-69491 hydrochloride is an inhibitor of HER-2 tyrosine kinase activity, blocking the phosphorylation of HER-2 and inhibiting the proliferation of SKOV-3 cells. It exhibits antitumor activity.

ALK ligand-Linker Conjugate 1 is an ALK ligand-connector conjugate used for the synthesis of PROTACALK degrader-4.

RET-IN-14 inhibits RET (IC50: <0.51-9.3 nM) & BTK (C481S) (IC50: 9.2-15 nM), promising for tumor research.

UNC9750 is an inhibitor of inositol phosphate multikinase (IPMK), with IC50 values of 31.6 nM for IPMK and 374 nM for IP6K2. It effectively suppresses the accumulation of InsP5, a direct product of IPMK kinase activity, without affecting InsP6 or InsP7 levels. Additionally, UNC9750 inhibits over 75% of the activity of four kinases: DAPK1, DYRK1B, PDGFR, and KDR. This compound is applicable in glioblastoma research.