8-epi-Chlorajapolide F (compound 1) a sesquiterpene that can be isolated from the aboveground part of the Chloranthus japonicus. 8-epi-Chlorajapolide has few cytotoxic to human cancer cell lines NCI-H460 and SMMC-7721 (IC50s>50 μg/mL)[1].
Piboserod (SB 207266) Hcl is a selective 5-HT(4) receptor antagonist.IC50 value:Target: 5-HT4 antagonistin vitro: Piboserod did not modify the basal contractions but concentration-dependently antagonized the ability of 5-HT to enhance bladder strip contractions to EFS. In presence of 1 and 100 nM of piboserod, the maximal 5-HT-induced potentiations were reduced to 45.0+/-7.9 and 38.7+/-8.7%, respectively [1].in vivo: Piboserod significantly increased LVEF by 1.7% vs. placebo (CI 0.3, 3.2, P = 0.020), primarily through reduced end-systolic volume from 165 to 158 mL (P = 0.060). There was a trend for greater increase in LVEF (2.7%, CI -1.1, 6.6, P = 0.15) in a small subset of patients not on chronic beta-blocker therapy. There was no significant effect on neurohormones, quality of life, or exercise tolerance. Patients on piboserod reported more adverse events, but numbers were too small to identify specific safety issues [2]. Pretreatment with potent 5-HT4 ligands dose-dependently reduced striatal SB207145 concentration and the effective dose to achieve 50% receptor occupancy (ED50 ) values were 4.8, 2.0, 7.4, 9.9, 3.8 and 0.02 mg/kg for GR113808, piboserod, prucalopride, RS67333, TD8954 and PF04995274, respectively [3].
Histamine H4 receptor antagonist-1 is an antagonist of histamine H4 receptor extracted from patent WO2010108059A1 compound 60[1].
UC-1728 is a potent rabbit soluble epoxide hydrolase (sEH) inhibitor, with an IC50 of 2 nM on rabbit liver.
X-376 is a potent and dual ALK/MET inhibitor with IC50s of 0.61 nM and 0.69 nM, respectively.
SB-218078 is a potent, selective and cell-permeable checkpoint kinase 1 (Chk1) inhibitor that inhibits Chk1 phosphorylation of cdc25C with an IC50 of 15 nM. SB-218078 is less potently inhibits Cdc2 (IC50 of 250 nM) and PKC (IC50 of 1000 nM). SB-218078 causes apoptosis by DNA damage and cell cycle arrest[1][2][3].
[Sar9,Met(O2)11]-Substance P is a tachykinin NK1 receptor selective agonist.
3-Acetamidocoumarin plays an important role in biology and medicine. 3-Acetamidocoumarin has physiological effects and has been used for many diseases such as treatment of burns, brucellosis-rheumatic diseases and cancer[1].
(±)15-HETE is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Benperidol is a relatively old antipsychotic drug. Benperidol is a butyrophenone antipsychotic, with the highest neuroleptic potency in terms of D2 receptor blockade[1].
Mal-PEG4-OH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Thr-Val-Leu is a central nervous system tripeptide[1].
Gastrodenol(Bismuth tripotassium dicitrate; De-Noltab)is a mineral that is used in treating ulcers and upset stomach.
Ac-pSar12-OH, as a linker, can be used for preparation of Ligand-Drug-Conjugate (LDC)[1][2].
6-OAU(GTPL5846; 6-n-octylaminouracil) is a surrogate agonist of GPR84; activates human GPR84 in the presence of Gqi5 chimera in HEK293 cells with an EC50 of 105 nM in the PI assay.IC50 value: 105 nM [1]Target: GPR84 agonistin vitro: 6-OAU increased [35S]GTPγS incorporated in Sf9 cell membranes expressing human GPR84-Gαi fusion protein with an EC50 of 512 nM. 6-OAU did not activate human GPR40 in HEK293 cells in the PI assay. Stimulation with 6.25 μm 6-OAU began to induce GPR84-EGFP internalization, and the extensive internalization was observed at 200 μm 6-OAU stimulation. In a Transwell assay, 3-OH-C12 and the surrogate agonist, 6-OAU, provoked chemotaxis of PMNs prepared from human peripheral blood in a concentration-dependent manner with an EC50 of 24.2 μm and 318 nm, respectively. In addition, 3-OH-C12 and 6-OAU increased the secretion of IL-8 from LPS-stimulated PMNs [1].in vivo: Injection of 6-OAU suspension in 1% rat serum into the rat jugular vein (10 mg/kg) leads to the elevation of a chemokine, CXCL1 concentration in the serum peaking at 3 h after the injection. In the rat air pouch model, 6-OAU at 1 mg/ml dissolved in 0.3% BSA attracted both PMNs and macrophages into the air pouch, peaking at 4 h after 6-OAU inoculation [1].
Licoisoflavanone is the isoflavonoid compound isolated from Sinkiang licorice root (Glycyrrhiza)[1].
A potent glucagon receptor (GCGR) negative allosteric modulator.
KRAS inhibitor-12 (compound 6-1) is a potent KRAS G12C inhibitor with an IC50 of 0.537 µM. KRAS inhibitor-12 shows p-ERK inhibition activities with IC50s of 1.3, 3.7 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-12 has the potential for the research of pancreatic, colorectal, and lung cancers[1].
DU125530 is a potent and selective5-HT1A receptor antagonist with Ki values of 0.7, 890, 1200, 240, 750, 1100 nM for 5-HT1A, 5-HT1B, 5-HT1D, 5-HT2A, 5-HT2C, 5-HT3, respectively. DU125530 shows antidepressant effects[1][2].
Papyracillic acid, a fungal metabolite, a Penicillic acid analog, is a nonselective herbicide. Papyracillic acid has anti-bacterial, anti-fungal, nematicidal, and phytotoxic effects[1].
Capzimin is a potent and moderately specific proteasome isopeptidase Rpn11 inhibitor.
Glycidyl Palmitate-d5 is the deuterium labeled Glycidyl Palmitate[1].
γ-Tocopherol (D-γ-Tocopherol) is a potent cyclooxygenase (COX) inhibitor. γ-Tocopherol is a naturally occurring form of Vitamin E in many plant seeds, such as corn oil and soybeans. γ-Tocopherol possesses antiinflammatory properties and anti-cancer activity[1].
tBID is a selective inhibitor of homeodomain–interacting protein kinase 2 (HIPK2) with an IC50 of 0.33 µM.
BIBF 1120 is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
DL-alpha-Tocopherol is a synthetic vitamin E, with antioxidation effect. DL-alpha-Tocopherol protects human skin fibroblasts against the cytotoxic effect of UVB[1].
WEHI-345 is a potent and selective inhibitor of RIPK2, with IC50 of 0.13 μM.IC50 value: 0.13 μMTarget: RIPK2in vitro: WEHI-345 is a selective RIPK2 kinase inhibitor, which delays RIPK2 ubiquitylation and NF-κB activation downstream of NOD engagement. WEHI-345 is an ATP analogue and was therefore predicted to bind in the ATP-binding pocket of RIPK2. WEHI-345 proved to be highly specific for RIPK2(Kd=46 nM) and displayed negligible activity (>10 μM) against RIPK1, RIPK4 and RIPK5.in vivo: WEHI-345 inhibits NOD signalling and has a beneficial effect on an EAE model. WEHI-345 blocks MDP-induced cytokine production. WEHI-345 ameliorates experimental autoimmune encephalomyelitis in mice. WEHI-345 also potently inhibited MDP-induced cytokine and chemokine secretion in the mouse macrophage Raw 264.7 cell line.
PD 174265 is a potent, cell-permeable, reversible, and selective inhibitor of EGFR with an IC50 of 450 pM[1].
Bamosiran is a small interfering RNA targeting β-adrenergic receptor 2, and is used to lower intraocular pressure
Camphor ((±)-Camphor) is a topical anti-infective and anti-pruritic and internally as a stimulant and carminative. However, Camphor is poisonous when ingested. Antiviral, antitussive, and anticancer activities[1]. Camphor is a TRPV3 agonist[2].