vegfr-2-in-29

VEGFR-2-IN-29 is a VEGFR2 inhibitor.

VEGFR-2-IN-9 (KDR-in-4) is a potent KDR VEGFR2 inhibitor with an IC50 of 7 nM, suitable for breast cancer research.

TIE-2 VEGFR-2 kinase-IN-5 (TIE-2 and VEGFR-2 tyrosine kinase receptor inhibitor) is a potent agent with anti-angiogenic activity, commonly used in biomedical research focused on angiogenesis.

VEGFR-2-IN-5 (UNC0064-12), multikinase inhibitor and has a -NH2 terminal linker for further synthesis.

TIE-2 VEGFR-2 kinase-IN-4, a benzimidazole derivative, is a potent inhibitor of the tyrosine kinase receptors TIE-2 and VEGFR-2, with IC50 values of 5.2 nM and 5.1 nM, respectively. This compound is utilized in angiogenesis research [1].

VEGFR-2 DHFR-IN-2 (compound 5b) is a dual inhibitor targeting VEGFR-2 and DHFR, with respective IC50 values of 0.623 μM and 9.085 μM. It demonstrates potent cytotoxicity against C26, HepG2, and MCF7 cancer cell lines, with IC50 values ranging from 3.59 μM to 8.38 μM. VEGFR-2 DHFR-IN-2 holds promise for cancer research [1].

VEGFR-2-IN-18 (Compound 15d) is a high-potency inhibitor of VEGFR-2, exhibiting an IC50 value of 60 nM. This compound effectively induces cell apoptosis and demonstrates significant antitumor properties [1].

VEGFR-2/BRAF-IN-1, a dual inhibitor of VEGFR-2 and BRAF kinases, demonstrates potent inhibitory activity with IC50 values of 0.049 µM for VEGFR-2, 0.063 µM for BRAF V600E, and 0.005 µM for BRAF WT. It effectively induces apoptosis and arrests the cell cycle primarily at the G1/S phase.

SARS-CoV-2-IN-29 disodium, a diphosphate ester featuring a benzene system and molecular tweezers architecture, demonstrates antiviral efficacy by targeting SARS-CoV-2 with half-maximal inhibitory concentrations (IC50s) of 1.5 μM for virus activity and 1.6 μM for spike pseudoparticle transduction. Additionally, it disrupts liposomal membranes, evidenced by a half-maximal effective concentration (EC50) of 3.0 μM [1].

VEGFR-2 DHFR-IN-1 (compound 8b) is a chemical inhibitor of VEGFR-2 and DHFR, with IC50 values of 0.384 μM and 7.881 μM, respectively. It possesses effective antibacterial activity against pathogens including Escherichia coli, Streptococcus faecalis, Salmonella enterica, MSSA, and MRSA, with MIC values ranging from 8 to 16 μg mL. Additionally, it exhibits potent cytotoxicity against cancer cell lines C26, HepG2, and MCF7, with IC50 values between 2.97 and 7.12 μM, making it a valuable tool for cancer research [1].

VEGFR-2-IN-27 (compound 7a) is a potent VEGFR-2 inhibitor (IC50: 14.8 nM) suitable for anticancer research.

VEGFR-2-IN-19 (Compound 15b) is a highly efficacious inhibitor of VEGFR2, a receptor involved in angiogenesis, and induces cellular apoptosis while elevating intracellular reactive oxygen species, making it a promising anticancer agent [1].

VEGFR-2-IN-26 (compound 5h) is a potent VEGFR-2 inhibitor (IC50: 15.5 nM) that exhibits significant anti-proliferative effects on leukemia, CNS, non-small lung, ovarian, renal, prostate, and breast cancer cells.

VEGFR-2 c-Met-IN-1 is a dual inhibitor of VEGFR-2 and c-Met, with IC50 values of 138 nM and 74 nM, respectively, demonstrating antitumor activity [1].

VEGFR-2-IN-31 (compound 3i), a potent VEGFR-2 inhibitor (IC50=8.93 nM), functions as an anti-prostate cancer agent by arresting the cell cycle at the S-phase and inducing apoptosis.

Compound 8g (hCA/VEGFR-2-IN-2) is an indolinonylbenzenesulfonamide identified as a potential dual inhibitor targeting cancer-associated isozymes hCA IX/XII and the angiogenic receptor VEGFR-2. It demonstrates VEGFR-2 inhibition with an IC50 of 204 nM and high affinity for hCAs, exhibiting Kis of 3.6 nM for hCA IX, 16.1 nM for hCA II, 16.7 nM for hCA XII, and 75.3 nM for hCA I. Furthermore, compound 8g exhibits antiproliferative effects on breast cancer cells overexpressing VEGFR-2 [1].

VEGFR-2-IN-13 (Compound 19a) is a potent VEGFR-2 inhibitor (IC50: 3.4 nM) that arrests the HepG2 cell cycle in the G2 M phase and induces apoptosis.

VEGFR-2-IN-11 is a potent inhibitor of VEGFR-2 (IC50: 60.27 nM) with an IC50 value of 60.27 nM, which induces apoptosis and has anticancer activity.

VEGFR-2-IN-28 is a potent inhibitor of VEGFR-2 (IC50: 0.83 μM). VEGFR-2-IN-28 induces apoptosis and exhibits antitumor effects.

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

VEGFR-2-IN-21 is a potent inhibitor of VEGFR-2 (IC50: 0.10 μM) and exhibits anticancer effects.

VEGFR-2-IN-37 (compound 12), a VEGFR-2 inhibitor, demonstrates an inhibition rate of approximately 56.9 μM at 200 μM concentration and is identified as a potential inhibitor of human umbilical vein endothelial cell (HUVEC) proliferation [1].

VEGFR-2-IN-32 (Comp 3a) is an inhibitor of VEGFR-2 with an inhibitory concentration (IC50) of 8.93 nM, exhibiting cytotoxic activity towards PC-3 cells with an IC50 of 1.22 μM, indicating its potential in anti-prostate cancer research [1].

hCA VEGFR-2-IN-3 (compound 8j) is an indolinonylbenzenesulfonamide with potential as a dual inhibitor of cancer-associated hCA IX XII and VEGFR-2. It inhibits VEGFR-2 with an IC50 of 358 nM and exhibits high affinity for hCAs, with Ki values of 4.2 nM for hCA IX, 22.9 nM for hCA II, 25.1 nM for hCA I, and 28.0 nM for hCA XII. Furthermore, it demonstrates specific antiproliferative activity against breast cancer cells that overexpress VEGFR-2 [1].

VEGFR-2-IN-36 (compound 15) is a potent VEGFR-2 inhibitor with an IC50 value of 0.067 μM and acts as an apoptosis inducer with demonstrated anticancer efficacy, modulating apoptotic pathways by upregulating BAX and downregulating Bcl-2, leading to cytotoxic effects on cancer cell lines, including MCF-7 (IC50 = 0.42 μM) and HepG2 (IC50 = 0.22 μM) [1].

TIE-2 VEGFR-2 kinase-IN-3, a benzimidazole derivative, is a potent inhibitor of tyrosine kinase receptors TIE-2 and VEGFR-2, with IC50 values of 6.9 nM and 3.5 nM, respectively. This compound is useful for angiogenesis research [1].

VEGFR-2/BRAF-IN-2, as a dual VEGFR-2 and BRAF kinase inhibitor, exhibits potent IC50 values of 0.111 µM, 0.089 µM, and 0.071 µM against VEGFR-2, BRAF V600E, and BRAF WT, respectively. This compound effectively induces apoptosis and predominantly arrests the cell cycle in the G1 phase.

PROTAC VEGFR-2 Degrader-1 (PROTAC-1), a specific degrader of PROTAC VEGFR-2, demonstrates minimal inhibition of VEGFR-2 (IC50 > 1 μM) and exhibits low anti-proliferative effects on EA.hy926 cells (IC50 > 100 μM) [1].

PROTAC VEGFR-2 degrader-2 (PROTAC-4), a specific degrader of VEGFR-2, demonstrates minimal inhibition of VEGFR-2 (IC50 > 1 μM) and low anti-proliferative activity towards EA.hy926 cells (IC50 > 100 μM) [1].

SARS-CoV-2-IN-29, a two-armed diphosphate ester featuring a benzene system and molecular tweezers, demonstrates antiviral efficacy with IC50 values of 1.5 μM for SARS-CoV-2 activity and 1.6 μM against spike pseudoparticle transduction. Additionally, it disrupts liposomal membranes, as indicated by an EC50 of 3.0 μM [1].

TIE-2 VEGFR-2 kinase-IN-2 is a potent inhibitor of both VEGFR2 and Tie-2 kinases, with significant pIC50 values of 8.61 and 8.56, respectively. This compound functions as an anti-angiogenic agent, making it highly relevant for cancer research.

VEGFR-2-IN-15 (Compound 14b) is a potent VEGFR-2 inhibitor that inhibits the growth of HepG2 cells in the Pre-G1 phase and induces apoptosis.

VEGFR-2-IN-25 (compound 5d) is a potent inhibitor of VEGFR-2 with an IC50 of 12.1 nM.

Peptide agonist for galanin receptors

VEGFR-2-IN-33 (Compound 4d), a potent VEGFR inhibitor with an IC50 value of 61.04 nM, demonstrates significant inhibition of HepG2 cell proliferation with an IC50 of 4.31 nM, and is utilized for hepatocellular carcinoma (HCC) research [1].

VEGFR-2-IN-35 (compound 7) is a potent VEGFR-2 inhibitor with an IC50 of 37 nM, and it also inhibits MCF-7 and HCT 116 cancer cell lines with IC50 values of 10.56 μM and 7.07 μM, respectively [1].

hCA VEGFR-2-IN-4 (compound 15b), an indolinylbenzenesulfonamide, serves as a potential dual inhibitor targeting cancer-related human carbonic anhydrases hCA IX XII and vascular endothelial growth factor receptor 2 (VEGFR-2). It exhibits an IC50 value of 0.811 µM against VEGFR-2 and shows high affinity for hCAs, with inhibition constants (Ki) of 3.8 nM for hCA XII, 6.2 nM for hCA IX, 19.8 nM for hCA II, and 35.5 nM for hCA I. Additionally, the compound demonstrates antiproliferative effects on breast cancer cells overexpressing VEGFR-2 [1].

VEGFR-2-IN-22 (Compound 25) is an inhibitor of VEGFR-2 and β-tubulin polymerization, with an IC50 of 19.82 nM for VEGFR-2, and is capable of inducing apoptosis.

VEGFR-2-IN-17 (Compound 15a) is a highly potent inhibitor of Vascular Endothelial Growth Factor Receptor 2 (VEGFR-2) with an IC50 of 67.25 nM and exhibits significant antitumor properties [1].

VEGFR-2-IN-10 has enhanced antiangiogenic potency against VEGFR2 phosphorylation induced by VEGF with an IC50 value of 0.7 μM and no cytotoxic effects.

VEGFR-2-IN-20 (Compound 7) is a potent VEGFR inhibitor with significant potential for cancer research [1].

VEGFR-2-IN-16 (Compound 15b) is a potent VEGFR-2 inhibitor with an IC50 of 86.36 nM, demonstrating significant antitumor effects.

TIE-2 VEGFR-2 kinase-IN-1 is employed in the synthesis of TIE-2 and or VEGFR-2 inhibitors for studying diseases associated with inappropriate angiogenesis [1].

VEGFR-2-IN-30, a compound acting primarily as a VEGFR-2 inhibitor (IC50: 66 nM), demonstrates additional inhibitory effects on PDGFR, EGFR, and FGFR1, with IC50 values of 180, 98, and 82 nM, respectively. It effectively arrests cancer cells in the S-phase and induces both early and late apoptosis.

VEGFR-2-IN-12 (compound 6g), a 2-oxoquinoxalinyl-1,2,4-triazole, is a potent inhibitor of VEGFR-2 with an IC50 of 0.037 μM and demonstrates anti-tumor effects.

VEGFR-2-IN-5 hydrochloride is a potent inhibitor of VEGFR2.

VEGFR-2-IN-24 is a potent VEGFR-2 inhibitor (IC50: 0.22 μM) useful for tumor research.

VEGFR-2-IN-6 (WO 02/059110, example 64) is a potent inhibitor of VEGFR2, a crucial receptor involved in the regulation of angiogenesis [1].

Non-selective galanin receptor agonist (Ki values are 0.98, 1.48 and 1.47 nM for GAL1, GAL2 and GAL3 respectively). Anticonvulsant; prevents the occurrence of full kindled seizures in rats.

Galanin (2-11) amide is a synthetic peptide fragment of the neuropeptide galanin and an agonist of the galanin-2 (GAL2) receptor (EC50= 9.32 nM in a fluorescence imaging plate reader assay).1It selectively binds to the GAL2receptor (IC50= 1.76 nM for the rat receptor) over the GAL1receptor (IC50= 879 nM for the human receptor) but does also bind to the GAL3receptor (Ki= 271 nM for the rat receptor).1,2Intracerebroventricular administration of galanin (2-11) amide (1 nmol/animal) decreases immobility in the forced swim test in rats.3It also reduces the hind paw mechanical pain threshold and increases the hind paw cold sensitivity threshold in rats.1

Galanin is a neuropeptide with diverse biological activities. [1][2][3][4][5] It binds to rat galanin (GAL) receptor subtypes GAL1-3 (IC50s = 0.339, 1.35, and 3.31 nM, respectively) and human GAL1-3 (IC50s = 0.288, 1.62, and 12.3 nM, respectively). [1] Galanin binds to and inhibits contraction of guinea pig gastric smooth muscle cells induced by carbachol . [2] In vivo, Galanin (6 nmol, i.c.v.) increases feeding behavior in rats and increases latency to hindpaw withdrawal in response to heat and mechanical stimulation in a rat model of carrageenin-induced inflammation when administered at a dose of 2 nmol injected into the nucleus accumbens.[3][4] Galanin (5 μg, i.c.v.) also inhibits acetylcholine release induced by scopolamine in the ventral hippocampus of freely moving rats. [5]

N-terminal galanin fragment used to mediate central cardiovascular effects