Angiogénese

HER2-IN-12 is an HER2 inhibitor with an IC50 value of 121 nM and can be used to study cancers such as breast cancer.

JAK-2-/3-IN-3 (ST4j) is a potent JAK2/3 inhibitor for leukemia research, with IC50s: JAK2, 13 nM; JAK3, 14.86 nM; induces apoptosis.

Tofacitinib Prodrug-1: an oral prodrug reducing Tofacitinib's side effects, treats ulcerative colitis in mice effectively with low toxicity.

MM-589 TFA is a potent WD repeat domain 5 (WDR5)inhibitor and mixed lineage leukemia (MLL) protein-protein interaction.

EGFR-IN-47: strong oral EGFRL858R/T790M/C797S blocker, induces cell death; promising for NSCLC research. IC50: 0.01 μM.

VEGFR-2-IN-18 is a potent VEGFR-2 inhibitor with a 60 nM IC50, promoting cell apoptosis and anticancer effects.

AKN-028 acetate: an oral TK inhibitor for AML research, targets FLT3 with IC50 of 6 nM, inhibits autophosphorylation, and induces apoptosis.

EGFR/HER2-IN-4: oral, irreversible dual EGFR inhibitor (IC50: 0.6 nM), targets L858R/T790M mutations, potent anti-lung cancer effects in vivo.

HDAC-IN-35 (Compound 14) is an effective and selective inhibitor of VEGFR-2 and HDAC, with IC50 values of 13.2 and 0.166 μM for VEGFR-2 and HDAC6, respectively.

JAK3-IN-11: potent oral JAK3 inhibitor (IC50=1.7 nM), noncytotoxic, >588-fold selectivity, blocks T-cell growth; useful in autoimmune research.

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].

EGFR-IN-130 (compound 14b) is an EGFR inhibitor and an inducer of apoptosis (apoptoosis). It effectively kills HeLa cancer cells by inducing apoptosis.

W23-1006 is a selective covalent ALKBH5 inhibitor. It binds to the ALKBH5 C200 residue with an IC50 value of 3.848 μM. The inhibitory activity of W23-1006 is approximately 30 times stronger than that of FTO and 8 times greater than that of ALKBH3. W23-1006 is applicable for research in triple-negative breast cancer (TNBC).

Tyrosine Protein Kinase Substrate is a polypeptide molecule with the sequence RRLIEDNEYTARG.

Potent EGFR/HER2/DHFR inhibitor for MCF-7 breast cancer; IC50: 0.153/0.108/0.291 μM; arrests G1/S phase, triggers apoptosis.

VEGFR-2-IN-17 (15a) is a potent VEGFR-2 inhibitor with an IC50 of 67.25 nM, showing significant antitumor effects.

VEGFR-2/DHFR-IN-2 inhibits VEGFR-2 & DHFR (IC50: 0.623 & 9.085 μM), toxic to C26, HepG2, MCF7 cells (IC50: 3.59-8.38 μM), promising for cancer study.

SORT1-IN-5 (compound 3) is a SORT1 inhibitor capable of crossing the blood-brain barrier. The MSOH salt form of SORT1-IN-5 exhibits a certain degree of oral bioavailability.

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.

M-COPA disrupts Golgi, blocks MET & Arf1 activation, and inhibits angiogenesis via VEGFR & NF-kB pathways.