PF-06726304 acetate is a potent and selective EZH2 inhibitor. PF-06726304 acetate inhibits wild-type and Y641N mutant EZH2 with Kis of 0.7 and 3.0 nM, respectively. PF-06726304 acetate displays robust antitumor growth activity[1].
Benzoyl-DL-leucine is a leucine derivative[1].
Musk ketone (MK) is a widely used artificial fragrance. Musk ketone shows mutagenic and comutagenic effects in Hep G2 cells and induces neural stem cell proliferation and differentiation in cerebral ischemia via activation of the PI3K/Akt signaling pathway. In the brain, musk ketone is neuroprotective against stroke injury through inhibition of cell apoptosis[1][2][3].
Tribenuron-methyl-d3 is a deuterated labeled Tribenuron-methyl. Tribenuron-methyl is a sulfonylurea herbicide agent, can be used as the fungicide agent. Tribenuron-methyl plays an important role in controlling the weeds and diseases in wheat field[1].
Lomardexamfetamine (KP 106) is an orally active central nervous system stimulant composed of d-amphetamine and a ligand. Lomardexamfetamine can be used for the research of attention-deficit hyperactivity disorder[1].
4-Chloro-D-phenylalanine Hydrochloride is a phenylalanine derivative[1].
BODIPY-581/591 NHS ester is a bright, red fluorescent dye (excitation: 581 nm; emission: 591 nm). BODIPY-581/591 NHS ester shows unique hydrophobic properties for staining lipids, membranes, and other lipophilic compounds[1].
JTE-151 is a RORγ inhibitor, which can suppress overactive immune response through inhibition of RORγ related to the activation of Th17 cells, making JTE-151 possible to be used in autoimmune disease research[1].
Dihydrorotenone, a natural pesticide, is a potent mitochondrial inhibitor. Dihydrorotenone probably induces Parkinsonian syndrome. Dihydrorotenone induces human plasma cell apoptosis by triggering endoplasmic reticulum stress and activating p38 signaling pathway[1].
Benidipine is a potent and orally active calcium channel antagonist[1]. Benidipine shows anti-apoptosis effects in ischaemic/reperfused myocardial cells[2]. Benidipine increases the activity of endothelial cell-type nitric oxide synthase and improves coronary circulation in hypertensive rats[3].
2-Methylthio isopentenyladenosine 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].
HO-PEG16-OH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Bemfivastatin (PPD 10558) hemicalcium is an orally active lipid-lowering agent and HMG-CoA reductase inhibitor. Bemfivastatin hemicalcium enhances the activity of liver extracts. Bemfivastatin hemicalcium has no-observed adverse effect levels (NOAEL) with dosages of ≥320 mg/kg/d (rat developmental toxicity), ≥12.5 mg/kg/d (rabbit maternal toxicity), ≥25 mg/kg/d (rabbit developmental toxicity), respectively. Bemfivastatin hemicalcium can be used in the study of statin-related hypercholesterolemic myalgia in statin-intolerant patients.
(S)-2-((tert-Butoxycarbonyl)amino)-4-(cyclohexyloxy)-4-oxobutanoic acid is an aspartic acid derivative[1].
Dihydrocapsaicin is a natural capsaicin, acts as a selective TRPV1 agonist, and also increases p-Akt levels. Dihydrocapsaicin enhances the hypothermia-induced neuroprotection[1][2].
L189 is a novel human DNA ligase inhibitor, inhibits hLigI/III/IV with IC50 of 5/9/5 μM.IC50 value: 5/9/5 μM (for hLigI/III/IV)Target: DNA ligasein vitro: L189 is a competitive inhibitor with respect to nicked DNA. L189 inhibits DNA ligases I, III and IV in DNA joining assays with purified proteins and in cell extract assays of DNA replication, base excision repair and non-homologous end joinging. L189 markedly increases killing of HCT116 colon cancer cells and the other cancer cell lines by ionizing radiation.
Anticancer agent 129 (Compound 3a), a quinoline derivative, predicting to has anti-cancer activity[1].
Bay 59-3074 is a novel, selective CB1/CB2 receptor partial agonist with Ki values of 48.3 and 45.5 nM at human CB1 and CB2 receptors respectively . Orally active CB1 agonist in vivo. target: CB1/CB2 receptor partial agonist.Ki: 48.3 and 45.5 nM (CB1 and CB2 receptors)In vitro: analgesic, antihyperalgesic, and antiallodynic properties in rat models of acute and chronic pain. The reference concentration is 10 μM. [1]In vivo: administration of BAY 59-3074 (ED50 value: 0.41 mg/kg).Orally active CB1 agonist in vivo. [2] BAY 59-3074 (0.3-3 mg/kg, p.o.) induce antihyperalgesic and antiallodynic effects against thermal or mechanical stimuli in rat models of chronic neuropathic. Antiallodynic efficacy of BAY 59-3074 (1 mg/kg, p.o.) in the spared nerve injury model was maintained after 2 weeks of daily administration. However, tolerance developed rapidly (within 5 days) for cannabinoid-related side effect. [1] BAY 59-3074 have analgesic, antihyperalgesic, and antiallodynic properties in rat models of acute and chronic pain.[1]
RIPK1-IN-8 (example 16), an aminoimidazopyridine, is a potent and selective RIPK1 inhibitor with an IC50 of 4 nM. RIPK1-IN-8 has the potential for inflammatory diseases research[1].
Scyliorhinin II is a selective neurokinin-3 receptor agonist, with a Ki of 2.5 nM for neurokinin-3 receptor in rat cerebral cortex.
Pomalidomide-PEG1-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and 1-unit PEG linker used in PROTAC technology[1].
Cbl-b-IN-9 (Compound 300) is a casitas B-lineage lymphoma-b (Cbl-b) and c-Cbl inhibitor with IC50s of 5.6 nM and 4.7 nM, respectively[1].
AZ31 is a a potent, highly selective, and orally active ATM inhibitor with an IC50 of <1.2 nM for ATM enzyme, and an IC50 of 46 nM for ATM in cell. AZ31 shows excellent selectivity over ATR (>500-fold) and excellent PIKK-family selectivity and pan-kinase selectivity. AZ31 is a potent radiosensitizer in vitro, it can be used for the research of cancer[1].
Esculentoside H (EsH) is a water-soluble saponin isolated and purified from the root extract of perennial plant Phytolacca esculenta[1]. Esculentoside H (EH) has anti-tumor activity, the mechanism is related to the capacity for TNFrelease[2].Esculentoside H (EsH) suppresses colon cancer cell migration through blockage of the JNK1/2 and NF-κB signaling-mediated matrix metalloproteinases-9 (MMP-9) expression[1].
VL-6 can be used in the synthesis of biomimetic nanomaterials which for delivery of therapeutic, diagnostic, or prophylactic agents[1].
Pomolic acid 3-acetate is an antitubercular agent with a MIC of 32 μM against Mycobacterium tuberculosis H37Rv[1].
11-Oxomogrol is a triterpene aglycon. 11-Oxomogrol inhibits epstein-Barr virus early antigen (EBV-EA) activation[1].
Pyridostatin hydrochloride is a G-quadruplexe stabilizer, with a Kd of 490 nM.
Etoxadrol is a potent N-methyl-D-aspartic acid (NMDA) antagonist with high affinity. Etoxadrol can be used for anaesthetic research[1].