as 19

AS19 is a potent, selective 5-HT7 receptor agonist (IC50: 0.83 nM; Ki: 0.6 nM) with demonstrated selectivity for 5-HT7 over 5-HT1A, 5-HT1B, 5-HT1D, and 5-HT5A receptors (Kis: 89.7 nM, 490 nM, 6.6 nM, and 98.5 nM, respectively).

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

Antitumor agent-19 is a modulator of tumor-associated macrophages with EC50s of 17.18 μM and 18.87 μM in the RAW 264.7 cells and the BMDM cells.

KFM19 is a potent and selective adenosine receptor (A1-receptor) antagonist (IC50 : 50 nM) for the study of neurological disorders.

11β-HSD1 inibitor 19 shows inhibitory activities for hHSD1 and mHSD1 with IC50s of 16 nM and 10 nM.

ZX-J-19J (N-(2,3-Diphenyl-6-quinoxalinyl)octanamide), an inhibitor of Cyclophilin J (CyPJ), demonstrates remarkable inhibition of tumor cell growth, comparable to cyclosporine A but much stronger than 5-fluorouracil.

TFIIH Modulator-19 induces the dimerization of trichothiodystrophy group A protein to modulate TFIIH transcriptional activity.

2-Chloro-5-(16,18-dioxo-17-azapentacyclo[6.6.5.0~2,7~.0~9,14~.0~15,19~]nonadeca-2,4,6,9,11,13-hexaen-17-yl)benzoic acid can be used to synthesize a variety of organic compounds.

MG-T-19, a TIM-3 inhibitor (KD=0.26 μM), significantly inhibited the interaction of TIM-3 with PtdSer, CEACAM1, and Gal-9, and increased the production of TNF-α and IFN-γ in PBMCs, which reactivated the tumor-attacking ability of T cells.

CDK8/19-IN-51 is an orally active and highly effective dual inhibitor of CDK8 and CDK19, with anticancer activity. Its IC50 values for CDK8 and CDK19 are 5.1 nM and 5.6 nM, respectively. It is used in studies of colorectal and gastric cancers.

Protein Kinase C 19-31 acetate, a peptide inhibitor of protein kinase C (PKC), derived from the pseudo-substrate regulatory domain of PKCa (residues 19-31) with a serine at position 25 replacing the wild-type alanine, is used as protein kinase C substrate

S19-1035 is a potent and specific inhibitor of aldo-keto reductase 1C3 (AKR1C3), displaying an inhibitory concentration (IC50) of 3.04 nM. It is primarily utilized in tumor research.

TAT-Gap19 acetate is a specific inhibitor of connexin43 hemichannel (Cx43 HC). TAT-Gap19 acetate traverses the blood-brain barrier and alleviates liver fibrosis in mice. TAT-Gap19 acetate does not inhibit the corresponding Cx43 GJCs.

Ned 19, a selective membrane-permeant non-competitive antagonist of NAADP, strongly inhibits tumor growth, vascularization, and lung metastases in mice.

PDE4-IN-19 (compound 1) acts as a PDE4 inhibitor and exhibits potent inhibition with IC 50 values below 10 nM for PDE4B1 and between 10-100 nM for PDE4D3.

PROTAC SMARCA2 degrader-19 (Compound 46) acts as a degrader of SMARCA2, demonstrating degradation capabilities in A549 and MV411 cells with a DC50 of less than 100 nM. Additionally, this compound degrades SMARCA4 in MV411 cells, but with a significantly higher DC50 of over 1000 nM.

Casein kinase1δ-IN-19 (compound 492) is a potent inhibitor of casein kinase 1δ. It is utilized in research related to neurodegenerative disorders, such as Alzheimer's disease.

NF-κB-IN-19 (Compound 8) is an NF-κB inhibitor. It effectively induces DNA damage in tumor cells through the NF-κB signaling pathway and promotes the production of reactive oxygen species (ROS), as well as induces autophagy and apoptosis. Additionally, NF-κB-IN-19 inhibits levels of VEGF and HIF-1α, exerting antiproliferative effects in tumor cells through the PI3K/AKT and STAT-3 pathways. It is also effective in overcoming cisplatin resistance and exhibits antitumor activity.

Nrf2 activator 19 is a compound capable of crossing the blood-brain barrier and acts as an NRF2/HO-1 activator, offering potent antioxidant and neuroprotective effects. It effectively reduces brain damage and minimizes the accumulation of Reactive Oxygen Species (ROS). Additionally, Nrf2 activator 19 inhibits neuronal apoptosis, aiding in the recovery of neural function and motor skills. It has demonstrated significant potential in ischemic stroke research.

AChE/BChE-IN-19 (compound 12) is a nicotinic hydrazine derivative that acts as an inhibitor of AChE (IC50=21.45 nM) and BChE (IC50=18.42 nM), and it is applicable in Alzheimer's disease research.

LRRK2-IN-19 is a PROTAC-targeted protein ligand utilized in the synthesis of PROTAC JH-XII-03-02. JH-XII-03-02 acts as an effective and selective LRRK2 PROTAC degrader, which is applicable for research in Parkinson's disease.

SOS1-IN-19 (Compound 10i) is a potent inhibitor of SOS1 (Son of Sevenless 1) with an IC50 value of 165.2 nM. It functions by blocking the GDP/GTP exchange in the KRAS signaling pathway, thereby inhibiting KRAS activation. SOS1-IN-19 shows potential for research in cancers driven by KRAS, such as non-small cell lung cancer and colorectal cancer.

Novel oxylipins, referred to as docosanoids, have been derived from C22polyunsaturated fatty acids 7(S),17(S)-dihydroxy-8(E),10(Z),13(Z),15(E),19(Z)-Docosapentaenoic acid (7(S),17(S)-hydroxy DPA) is a DPA-derived analog of the 17(S)-dihydroxy series of docosanoids known as protectins. Protectin D1, a DHA-derived dihydroxy fatty acid, exhibits potent anti-inflammatory activities.1,2,3Potentially, 7(S),17(S)-hydroxy DPA demonstrates similar properties; however, its biological activity has yet to be determined. 1.Serhan, C.N., Gotlinger, K., Hong, S., et al.Anti-inflammatory actions of neuroprotectin D1/protectin D1 and its natural stereoisomers: Assignments of dihydroxy-containing docosatrienesJ. Immunol.176(3)1848-1859(2006) 2.Ariel, A., and Serhan, C.N.Resolvins and protectins in the termination program of acute inflammationTRENDS in Immunology28(4)176-183(2007) 3.Schwab, J.M., Chiang, N., Arita, M., et al.Resolvin E1 and protectin D1 activate inflammation-resolution programmesNature447(7146)869-874(2007)

EDHF (endothelium-derived hyperpolarizing factor) is an unidentified mediator released from vascular endothelial cells in response to acetylcholine and bradykinin which is distinct from the NOS- (nitric oxide) and COX-derived (prostacyclin) vasodilators. Cytochrome P450 (CYP450) metabolism of polyunsaturated fatty acids produces epoxides such as (±)14(15)-EpETrE which are prime candidates for the actual active mediator. However, the CYP450 metabolites of eicosapentaenoic acid and docosahexaenoic acid have been little studied relative to arachidonate epoxygenase metabolites. (±)19(20)-EpDPA is a DHA epoxygenase metabolite, derived via epoxidation of the ω-3 double bond of DHA. The EDHF activity of (±)19(20)-EpDPA has not yet been determined. The epoxygenase metabolites of DHA have also been detected in a mouse inflammation model.