Juglone is a yellow pigment found in black walnut (Juglans regia). Juglone also shows antimicrobial activity[1].
Calcitonin gene-related peptide (CGRP) is a neuropeptide. Calcitonin gene-related peptide can be used for the research of nociception, ingestive behaviour and modulation of the endocrine systems[1].
THP-PEG9-THP is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
3, 7-di-o-methylducheside A (Compound 2) is a ethyl acetate extract of Psittacanthus cucullaris. 3, 7-di-o-methylducheside A stimulates the formation of glycosaminoglycan chains. 3, 7-di-o-methylducheside A can be used to study the rate of glycosaminoglycan synthesis [1].
BMS-986020 is an LPA1 antagonist.target: LPA1BMS-986020 is in Phase 2 clinical development for treating idiopathic pulmonary fibrosis. BMS-986020 selectively inhibits the LPA receptor, which is involved in binding of the signaling molecule lysophosphatidic acid, which in turn is involved in a host of diverse biological functions, such as cell proliferation, platelet aggregation, smooth muscle contraction and others.
PF-05085727 is a potent, selective and brain penetrant Phosphodiesterase 2A (PDE2A) inhibitor with an IC50 of 2 nM.
Methyl methyl-D-prolinate is a proline derivative[1].
2-Caren-10-al is a major component of essential oil derived from C. cyminum L[1].
8-Hydroxyquinoline hemisulfate (8-Quinolinol hemisulfate) is a monoprotic bidentate chelating agent, exhibits antiseptic, disinfectant, and pesticide properties, functioning as a transcription inhibitor.
Dihydroethidium(Hydroethidine; PD-MY 003) is a superoxide indicator; exhibits blue-fluorescence in the cytosol until oxidized, where it intercalates within the cell's DNA, staining its nucleus a bright fluorescent red.
(E)-Crotylbarbital is the isomer of Crotylbarbital. Crotylbarbital is a barbiturate derivative. It has sedative and hypnotic effects, and can be used for the treatment of insomnia.
Amatuximab (MORab-009) is a chimeric, humanized IgG1/k MAb that targets the cell surface mesothelin (MSLN). Mesothelin is a glycosylphosphatidyl inositol (GPI)-anchored membrane glycoprotein, which is present in a restricted set of normal adult tissues such as the mesothelium[1][2].
2,3-Dihydro-3α-methoxynimbolide is a limonoid compound isolated from the extracts of bark, leaves, roots, and seeds of Azadirachta indica A. Juss. var. siamensis Valeton. 2,3-Dihydro-3α-methoxynimbolide exhibits potent cyto-toxicities against one or more cell lines. 2,3-Dihydro-3α-methoxynimbolide activates caspases-3, -8, and -9, while increases the ratio of Bax/Bcl-2. 2,3-Dihydro-3α-methoxynimbolide induces apoptosis via both mitochondrial and death receptor pathways in AZ521[1].
Chlormethiazole is an potent and orally active GABAA agonist[1]. Chlormethiazole inhibits cytochrome P450 isoforms: CYP2A6 and CYP2E1 in human liver microsomes. Chlormethiazole is an anticonvulsant agent and has the potential for treating convulsive status epilepticus[2].
VU0650786 is a potent and selective CNS penetrant negative allosteric modulator of metabotropic glutamate receptor subtype 3 (mGlu3), with an IC50 of 392 nM. VU0650786 has antidepressant and anxiolytic activity in rodents[1].
Saccharin sodium hydrate is an orally active, non-caloric artificial sweeteners (NAS). Saccharin sodium hydrate has bacteriostatic and microbiome-modulating properties[1].
Swertisin, a C-glucosylflavone isolated from Swertia japonica, is known to have antidiabetic, anti-inflammatory and antioxidant effects. Swertisin is an adenosine A1 receptor antagonist[1][2].
CNQX disodium (FG9065 disodium) is a potent and competitive AMPA/kainate receptor antagonist with IC50s of 0.3 μM and 1.5 μM, respectively. CNQX disodium is a competitive non-NMDA receptor antagonist[1]. CNQX disodium blocks the expression of fear-potentiated startle in rats[5].
Thalidomide-O-C7-acid is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology[1].
IXA4 is a highly selective, non-toxic IRE1/XBP1s activator. IXA4 activates IRE1/XBP1s signaling without globally activating the unfolded protein response (UPR) or other stress-responsive signaling pathways (e.g., the heat shock response or oxidative stress response). IXA4 reduces secretion of APP through IRE1 activation[1].
Plutavimab a humanized IgG1-κ anti-SARS-CoV-2 antibody, targeting to Spike (S) glycoprotein receptor binding domain (RBD)[1][2].
Pomalidomide-C4-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a linker used in PROTAC technology[1].
(6aR,9S)-Δ10-THC is a byproduct in Cannabis processing[1].
Cercosporamide is a highly potent, ATP-competitive Pkc1 kinase inhibitor, with an IC50 of <50 nM and a Ki of <7 nM. Cercosporamide is a unique Mnk inhibitor.
Peganumine A is a natural product that can be found in Peganum harmala. Peganumine A shows cytotoxicity with IC50s of5.8, 38.5, 40.2, 55.4 µM for HL-60, MCF-7, PC-3, and HepG2 cells ,respectively[1].
L-Glutamic acid γ-(2,2,2-trichloroethyl) ester is a glutamic acid derivative[1].
Ethacizine hydrochloride (Ethacizin; NIK-244) is a longer-lasting Class Ic antiarrhythmic agent than Flecainide[1]. Ethacizine hydrochloride (Ethacizin; NIK-244) inhibits the depolarizing current responsible for the intraatrial and His-Purkinje-ventricular conduction[2].
2-Methoxyestradiol is an angiogenesis inhibitor and apoptosis inducer with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules.
SAR405838 is a highly potent and selective MDM2 inhibitor, binds to MDM2 with Ki= 0.88 nM and has high specificity over other proteins.IC50 value: 0.88 nM (Ki) [1]Target: MDM2in vitro: SAR405838 potently inhibits cell growth in cancer cell lines, including SJSA-1 (IC50, 0.092 μM), RS4;11 (IC50, 0.089 μM), LNCaP (IC50, 0.27 μM), and HCT-116 (IC50, 0.20 μM) cells, and displays high selectivity over cancer cell lines with mutated or deleted p53, including SAOS-2 (IC50, >10 μM), PC-3 (IC50, >10 μM), SW620 (IC50, >10 μM), and HCT-116 (p53-/-) (IC50, >20 μM) cells.[1] SAR405838 effectively induces apoptosis in the RS4;11 cell line. SAR405838 potently inhibits cell growth and induces dose-dependent apoptosis in the ABTR1 and ABTR2 sublines, albeit with modestly reduced potency compared with that in the control RS4;11 cell line.[2]in vivo: At well-tolerated dose schedules, SAR405838 achieves either durable tumor regression or complete tumor growth inhibition in mouse xenograft models of SJSA-1 osteosarcoma, RS4;11 acute leukemia, LNCaP prostate cancer and HCT-116 colon cancer. Remarkably, a single oral dose of SAR405838 is sufficient to achieve complete tumor regression in the SJSA-1 model. In the SJSA-1 osteosarcoma, acute lymphoblastic leukemia RS4;11, LNCaP prostate cancer, and HCT-116 colon cancer xenograft model, MI-773 (p.o.) effectively inhibits tumor growth in a dose-dependent manner (10 mg/kg, 30 mg/kg, 50 mg/kg, 100 mg/kg, and 200 mg/kg,). [1]
5’-Deoxy-5’-iodo-2’-O-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].