Angiogenesis

MY-1576 is a FAK inhibitor with an IC50 of 8 nM. It activates the Hippo pathway, thereby inhibiting YAP/TAZ regulation. Additionally, MY-1576 effectively suppresses tumor growth in the KYSE30 xenograft mouse model, demonstrates good safety, and efficiently downregulates FAK autophosphorylation and YAP/TAZ levels in vivo.

Desidustat is an inhibitor of HIF hydroxylase.

"Belzutifan (MK-6482) is an oral HIF-2α inhibitor for ccRCC, with enhanced potency (IC50: 9 nM)."

HIF-1 inhibitor-4 (HIF-1 inhibitor-4) is a HIF-1 inhibitor with IC50 of 560 nM.

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.

Applications Narciclasine is an antiproliferative and pro-apoptotic inducer.

Applications Tyrphostin AG 112 is an EGFR inhibitor.

Applications 6-Methylheptanoic acid is used as a reagent to synthesize analogues of Eponemycin, an antibiotic that also exhibits anti-angiogenic activity by inhibiting proteasome function. 6-Methylheptanoic acid naturally occurs as a component of the scent chemical of the brushtail possum. Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package References McLean, S., et al.: J. Chem. Ecol., 38, 1318 (2012); Oikawa, T., et al.: Biochem. Biophys. Res. Comm., 181, 1070 (1991); Sin, N., et al.: Bioorg. Med. Chem., 6, 1209 (1998)

Applications 2-Bromoethylcyclopropane is used as a reagent to synthesize 22-Hydroxycholesterol (H918010) derivatives, compounds that act as serum cholesterol lowering agents. 2-Bromoethylcyclopropane is also used to prepare pyridazinones, compounds that act as cyclooxygenase 2-inhibitors (they possess anti-inflammatory and antiangiogenic effects). References Chorvat, R., et al.: J. Med. Chem., 28, 194 (1985); Masferrer, J., et al.: Ann. New York Acad. Sci., 889, 84 (1999); Willoughby, D., et al.: Lancet, 355, 646 (2000)

Applications 2-Chloro-N-[4-(1-cyanocyclopentyl)phenyl]-3-pyridinecarboxamide is an intermediate Apatinib 25-N-Oxide (A726160), a metabolite of the antiangiogenic agent and selective VEGFR2 inhibitor Apatinib (A726150).

cSRC/BCR-ABL-IN-1 (compound 21b) is a potent inhibitor of Bcr-Abl and C-Src, with IC50 values of 56.2 nM and 101 nM, respectively. It exhibits cytotoxicity.

Applications Tyrphostin AG 1478 is a potent and selective inhibitor of EGFR.

Dual Galectin-3/EGFR-IN-1 (Compound 29) is a dual inhibitor targeting Galectin-3 and EGFR, with dissociation constants (KD) of 52.29 μM and 3.31 μM, respectively. It inhibits TGF-β-induced hepatic stellate cell (HSC) activation, induces apoptosis in LX-2 cells, and shows antifibrotic activity in the liver.

Formononetin (Flavosil) is an O-methylated isoflavone and a phytoestrogen from the root of Astragalus membranaceus.

Applications 5-[(4-Hydroxyphenyl)methylene]-2,4-thiazolidinedione is a 5-Benzylidene-2,4-thiazolidenedione derivative designed as inhibitors of angiogenesis targeting VEGFR-2. Also, it is an intermediate used in the synthesis of MSDC 0602 (M755420), which is an analogue of thiazolidinediones, exhibits low affinity for binding and activation of peroxisome proliferator-activated receptor γ (PPARγ). Thiazolidinediones are effective insulin-sensitizing drugs for treating various metabolic and inflammatory diseases. References Bhanushali, U., et al.: Bioorg. Chem., 67, 139-147 (2016); Chen, Z., et al.: J. Biol. Chem. 287, 23537 (2012); Fukunaga, T., et al.: J. Bone Miner. Res., 30, 508 (2015)

FGFR1inhibitor-15 (Compound 23) is an FGFR1 inhibitor with an IC50 value of 27 μM, useful for tumor research.

ML228 activates HIF pathway and VEGF, with EC50 of 1μM, effective in vitro.

Applications Fumagillol is an analog of Fumagillin (F862650), a compound isolated from the fungus Aspergillus fumigatus. Fumagillin is an antimicrobial agent used in the treatment of microsporidiosis. Fumagillin shows promise as both an an anti-infective and antiangiogenic agent. References Molina, J.M. et al.: N. Eng. J. Med., 346, 1963 (2002); Hou, L. et al.: Pathol. Int., 59, 448 (2009); Ingber, D. et al.: Nature, 348, 555 (1990);

Sulfatinib (KDR-IN-1) (HMPL-012) is a potent and highly selective tyrosine kinase inhibitor against VEGFR1/2/3, FGFR1 and CSF1R with IC 50 s ranging from 1 to

Naluzotan hydrochloride, a hERG K+ blocker (IC50: 3800 nM) and potent 5-HT1A agonist (IC50: ~20 nM, Ki: ~5.1 nM), is used in anxiety and depression studies.

Applications TNP-470 is a synthetic analog of Fumagillin (F862650); a compound isolated from the fungus Aspergillus fumigatus. Fumagillin is an antimicrobial agent used in the treatment of microsporidiosis and shows promise as both an anti-infective and antiangiogenic agent. References Molina, J.M. et al.: N. Eng. J. Med., 346, 1963 (2002); Hou, L. et al.: Pathol. Int., 59, 448 (2009); Ingber, D. et al.: Nature, 348, 555 (1990)

Hexylresorcinol (4-Hexylresorcinol) is a substituted dihydroxybenzene used topically as an antiseptic for the treatment of minor skin infections.