Antitumor agent-119 (compound 13K) is a 2-benzoxazolyl hydrazone derivative with anticancer activities. Antitumor agent-119 inhibits the cell growth of Butkitt, CCRF-CEM, HeLa, and HT-29 with IC50 values of 30 nM, 140 nM, 100 nM, and 40 nM, respectively[1].
Sch-42495 racemate is the racemate of Sch-42495. Sch-42495 is a novel neutral metalloendopeptidase (NEP) inhibitor. Sch-42495 is the orally active ethylester prodrug of SCH 42354.
PROTAC CDK9 Degrader-1 is a selective CDK9 degrader.
Phorbol 12-myristate 13-acetate (PMA), a phorbol ester, is a commonly used PKC activator.
RTICBM-189 is a potent, brain-penetrant allosteric modulator of the cannabinoid type-1 (CB1) receptor with a pIC50 of 7.54 in Ca2+ mobilization assay. RTICBM-189 has pIC50s of 5.29 and 6.25 for hCB1 and mCB1, respectively. RTICBM-189 significantly and selectively attenuates the reinstatement of the cocaine-seeking behavior in rats[1].
Saikosaponin B3 is a saikosaponin isolated from the roots of Bupleurum falcatum L., with analgesic effect. Saikosaponin B3 inhibits ACTH-induced lipolysis in the fat cells[1][2][3].
Thalidomide-O-C8-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology[1].
Boc-Aminooxy-PEG1-C2-NH2 is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Mefloquine hydrochloride is a quinoline antimalarial drug that is structurally related to the antiarrhythmic agent quinidine. IC50 Value: 1 microM ( for K+ channel) [1]Target: AntiparasiticMefloquine is widely used in both the treatment and prophylaxis of Plasmodium falciparum malaria. MQ can induces oxidative stress in vitro. Evidence indicates that reactive oxygen species (ROS) may be used as a therapeutic modality to kill cancer cells [2].in vitro: Mefloquine inhibitedKvLQT1/minK channel currents with an IC50 value of approximately 1 microM. Mefloquine slowed the activation rate of KvLQT1/minK and more block was evident at lower membrane potentials compared with higher ones. HERG channel currents were about 6-fold less sensitive to block by mefloquine (IC50 = 5.6 microM). Block of HERG displayed a positive voltage dependence with maximal inhibition obtained at more depolarized potentials [1]. MQ has a highly selective cytotoxicity that inhibits PCa cell growth. MQ-mediated ROS simultaneously downregulated Akt phosphorylation and activated extracellular signal-regulated kinase (ERK), c-Jun N-terminal kinase (JNK) and adenosine monophosphate-activated protein kinase (AMPK) signaling in PC3 cells [2]. in vivo: Pregnant rats were treated orally with AS (15 and 40 mg/kg body weight (bwt)/day), MQ (30 and 80 mg/kg bwt/day) and AS/MQ (15/30 and 40/80 mg/kg bwt/day) on days 9-11 post coitum (pc). The dams were euthanized on day 12 pc and gestational and embryos histological parameters were evaluated [3].Clinical trial: Activity of Mefloquine Against Urinary Schistosomiasis . Phase 2
NWP-0476 is BCL-2/BCL-xL inhibitor. NWP-0476 has a modified structure with fine-tuned BCL-xL activity. NWP-0476 can be used for relapsed T-acute lymphoblastic leukemia (T-ALL) research[1].
Trichorabdal A is a diterpenoid compound isolated from Rabdosia trichocarpa. Trichorabdal A has potent anti-tumor activity[1].
Dihydroartemisinic acid (Dihydroqinghao acid), isolated as a natural product from Artemisia annua, is a biosynthetic precursor to the antimalarial agent Artemisinin[1].
Dobutamine Hcl(Dobutrex) is a sympathomimetic drug used in the treatment of heart failure and cardiogenic shock. Its primary mechanism is direct stimulation of β1 receptors of the sympathetic nervous system.
Venetoclax-d8 is deuterium labeled Venetoclax. Venetoclax (ABT-199; GDC-0199) is a highly potent, selective and orally bioavailable Bcl-2 inhibitor with a Ki of less than 0.01 nM. Venetoclax induces autophagy[1][2][3].
WAY-354574 is an active molecule targeting deacetylase (Sirtuin) for the study of Huntington's disease (HD)[1].
1,1′,1′′,1′′′-[1,4-Piperazinediylbis(2,1-ethanediylnitrilo)]tetrakis[2-dodecanol] is a lipid/lipidoid used in preparation of lipid-based or lipidoid nanoparticles[1].
Pterisolic acid B (Compound 2) is an ent-Kaurane diterpenoid. Pterisolic acid B can be isolated from fern Pteris semipinnata (Pteridaceae)[1].
NAMPT activator-3, a NAT derivative, is a NAMPT activator with an EC50 of 2.6 μM and a KD of 132 nM. NAMPT activator-3 effectively protects cultured cells from FK866 (HY-50876)-mediated toxicity. NAMPT activator-3 exhibits strong neuroprotective efficacy in a chemotherapy-induced peripheral neuropathy (CIPN) mouse model without any overt toxicity[1].
alpha-Boswellic acid is a natural product.
Disodium 5'-inosinate, obtained from bacterial fermentation of sugars, is as a food additive and often found in a variety of other snacks.
MOMIPP, a macropinocytosis inducer, is a PIKfyve inhibitor. MOMIPP penetrates the blood-brain barrier (BBB)[1][2].
Clavulanate potassium is a potent β-lactamase inhibitor and acts as an antibiotic[1][2].
N-tert-Butoxycarbonyl-trans-4-hydroxy-D-proline is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). N-tert-Butoxycarbonyl-trans-4-hydroxy-D-proline is also a alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1][2].
Semapimod tetrahydrochloride (CNI-1493), an inhibitor of proinflammatory cytokine production, can inhibit TNF-α, IL-1β, and IL-6. Semapimod tetrahydrochloride inhibits TLR4 signaling (IC50≈0.3 μM). Semapimod tetrahydrochloride inhibits p38 MAPK and nitric oxide production in macrophages. Semapimod tetrahydrochloride has potential in a variety of inflammatory and autoimmune disorders[1][2][3].
Clemastanin B, a lignin, has potent anti-influenza activities by inhibiting the virus multiplication, prophylaxsis and blocking the virus attachment. Clemastanin B targets viral endocytosis, uncoating or ribonucleoprotein (RNP) export from the nucleus. Clemastanin B has antioxidant and anti-inflammatory activities[1][2][3].
MD2-IN-1 is an inhibitor of Myeloid differentiation protein 2 (MD2) with a KD of 189 μM for the recombinant human MD2 (rhMD2).
sEH inhibitor-5 (compound D016) is a potent sEH (soluble epoxide hydrolase) inhibitor with an IC50 value of 0.1 nM[1].
Repinotan hydrochloride (BAY x 3702) is a potent, selective, brain-penetrant and orally active 5-HT1A receptor agonist, with Ki values of 0.19 nM (calf hippocampus), 0.25 nM (rat and human cortex), and 0.59 nM (rat hippocampus Repinotan hydrochloride has a weak affinity for other related receptors. Repinotan hydrochloride has pronounced neuroprotective effects[1].
Camylofin is an antimuscarinic, is a smooth muscle relaxant
6-Me-ATP (N6-Methyl-ATP) is a N6-modified ATP derivative. 6-Me-ATP shows excellent binding affinity to GSK3, serving as the phosphate group donor for GSK3β-catalyzed phosphorylation of its substrate peptide[1].