5-epi-Arvestonate A is a sesquiterpenoid isolated from the whole plants of Seriphidium transiliense. 5-epi-Arvestonate A promotes melanogenic production by activating the transcription of microphthalmia-associated transcription factor (MITF) and tyrosinase family genes. 5-epi-Arvestonate A inhibits the expression of IFN-γ-chemokine through the JAK/STAT signaling pathway in immortalized human keratinocyte (HaCaT) cells[1].
(S)-2,6-Bis((tert-butoxycarbonyl)amino)hexanoic acid is a polypeptide derivative, can be used to synthesis multifunctional amphiphilic peptide dendrimer, as a nonviral gene vectors, realizes the method in cancer research. (S)-2,6-Bis((tert-butoxycarbonyl)amino)hexanoic acid also involves in the synthesis of an organic substance that increases the luminescence intensity of alkaline phosphatase substrates[1][2].
Pentagastrin (ICI-50123) meglumine is a potent, selective Cholecystokinin B (CCKB) receptor antagonists with IC50 values of 11 nM and 1100 nM for CCKB and CCKA, respectively. Pentagastrin meglumine enhances gastric mucosal defense mechanisms against acid and protects the gastric mucosa from experimental injury[1].[2].
1-Naphthyl 3,5-dinitrobenzoate is a potent 5-lipoxygenase inhibitor with IC50 values of 1.04 µM and 3.6 µM for 5-LOX and mPGES-1, respectively. 1-Naphthyl 3,5-dinitrobenzoate has strong inhibition activity in the human whole blood (HWB) assay with an IC50 value of 8.6 μM. 1-Naphthyl 3,5-dinitrobenzoate can be used in research of inflammation[1].
Parthenolide is an NF-κB inhibitor, reduces histone deacetylase 1 (HDAC-1) and DNA methyltransferase 1 independent of NF-κB inhibition.
MAPTAM is an intracellular Ca2+ chelator[1].
N3-Methyl-5-methyluridine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
Kadsuralignan A (compound 1) is a dibenzocyclooctadiene lignan isolated from the leaves and stems of Schisandra lancifolia. Kadsuralignan A has anti-HIV activity with EC50=2.23 μg/mL[1].
DBCO-Amide-PEG5-acid is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
(-)-Eseroline fumarate is a metabolic of Physostigmine (HY-N6608), an AChE inhibitor. (-)-Eseroline fumarate elicits a leakage of lactic acid dehydrogenase (LDH) from cancer cells. (-)-Eseroline fumarate also induces the release of adenine nucleotides and 5-hydroxytryptamine (5-HT) from neuronal cells, thus induce cell death. (-)-Eseroline fumarate inhibits the electrically evoked twitches of the mouse vas deferens and of the guinea-pig ileum[1][2].
Fluorescein-PEG5-acid is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
BMS-582949 (compound 7k) is an orally active and highly selective p38α MAP kinase inhibitor, with IC50 values of 13 nM for p38α, and 50 nM for cellular TNFα. BMS-582949 can be used for research on rheumatoid arthritis[1].
(22R)-33,34,35-Trinorbacteriohopan-32-oic acid (compound 2c) is a hapten that can be covalently coupled to a carrier protein. (22R)-33,34,35-Trinorbacteriohopan-32-oic acid can be used in antibody generation and immunoassay[1].
Atenolol is a selective β1 receptor antagonist.Target: Adrenergic ReceptorAtenolol is a cardioselective beta-adrenergic blocker possessing properties and potency similar to propranolol, but without a negative inotropic effect [1, 2].
Asperlactone has anti-inflammatory activity. Asperlactone inhibits superoxide anion generation. Asperlactone is a fungal metabolite that can be isolated from isolated from Aspergillus ochraceus[1].
Bis-ANS dipotassium is a fluorescent probe of hydrophobic protein. Bis-ANS binds to tubulin with a Kd of 2 μM[1]. Bis-ANS dipotassium is a potent biphasic modulator of protein liquid-liquid phase separation (LLPS). Bis-ANS dipotassium promotes LLPS at low concentrations but suppresses LLPS at high concentrations[2].
Cladosporin is a fungal metabolite produced in good yield in the mycelium of Cladosporium cladosporioid. Cladosporin completely inhibits growth of severa dermatophytes on agar medium at a concentration of 75 μg/mL[1].
Ipsapirone (TVX Q 7821), an anxiolytic compound and a 5-HT1A partial agonist, also exhibits 5-HT1A antagonistic effect, and only at high doses it can also produce an inhibitory effect on 5-HT2 and the α1-adrenergic function[1][2].
Rilpivirine (R278474; TMC278) is a type of anti-HIV medicine called a non-nucleoside reverse transcriptase inhibitor (NNRTI).
Cipralisant (GT-2331) enantiomer is the enantiomer of Cipralisant (HY-106993), Cipralisant is an orally active, potent, selective, and high affinity histamine H3 receptor antagonist (rat Ki=0.47 nM)[1][2][3][4][5].
Dodoviscin A is a pigmentation-altering agent, which can be isolated from the aerial parts of Dodonaea viscosa. Dodoviscin A inhibits melanin production in B16-F10 melanoma cells. Dodoviscin A suppresses mushroom tyrosinase activity, and tyrosinase activity induced by 3-isobutyl-1-methylxanthine. Dodoviscin A also inhibits the phorphosylation of cAMP response element binding protein, induced by 3-isobutyl-1-methylxanthine and forskolin[1].
NY-ESO-1 (87-111) is a pan-MHC class II-restricted peptide sequence. NY-ESO-1 (87-111) binds to multiple HLA-DR and HLA-DP4 molecules, and stimulates Th1-type and Th-2/Th0-type CD4+ T cells when presented in the context of HLA-DR and HLA-DP4 molecules[1].
Nifuratel(NF 113, SAP 113) is a broad antibacterial spectrum agent, which is used as an antibacterial, antifungal, and antiprotozoal (Trichomonas).IC50 Value: 0.125-1 μg/mL(MIC, A. vaginae) [1]Target: Antibacterial; Antiprotozoal in vitro: In vitro, nifuratel is able to inhibit the growth of A. vaginae, with a MIC range of 0.125-1 μg/mL; it is active against G. vaginalis and does not affect lactobacilli [1].in vivo: Patients were randomized to receive a 2-week course of bismuth subcitrate (8 mg/kg/day, q.d.s.), amoxicillin (50 mg/kg/day, q.d.s.), with either nifuratel (15 mg/kg/day, q.d.s.) or furazolidone (10 mg/kg/day, q.d.s.), plus omeprazole (0.5 mg/kg, once daily) [2].Toxicity: There were no serious adverse reactions and were no withdrawals due to any side-effects. All of side-effects were self-limiting (dark stools, urine discoloration, blackening of the tongue, and others) [3].Clinical trial: N/A
benzyl (tert-Butoxycarbonyl)-L-leucyl-L-phenylalaninate is a phenylalanine derivative[1].
7-Ketositosterol is a phytosterol isolated from the fruits of the mulberry tree (Morus alba L.). 7-Ketositosterol can significantly inhibit Cisplatin (HY-17394)-induced apoptosis in LLC-PK1 cells and has the potential to improve Cisplatin-induced nephrotoxicity[1].
Didesethyl chloroquine (Bisdesethylchloroquine) is a major metabolite of the antimalarial drug Chloroquine. Didesethyl chloroquine is a potent myocardial depressant[1][2].
J-113397 is the first potent and selective nonpeptidyl ORL1 receptor antagonist (Ki: cloned human ORL1=1.8 nM) without any agonistic effects on other opioid receptors[1].
(-)-Syringaresinol, found in stems of Annona Montana, possesses anti-cancer activity[1].
((4-(tert-Butyl)phenyl)sulfonyl)proline is a proline derivative[1].
Methylthiomcresol-succinaldehydic acid is a fenthion hapten that can be used for immunoreagent production (protein conjugates and polyclonal antibodies)[1].