VD2173 is a side chain cyclized macrocyclic peptide inhibitor of HGF-activating serine proteases. VD2173 potently inhibits matriptase and hepsin. VD2173 can be used for the research of lung cancer[1].
Tamoxifen-d5 (ICI 47699-d5) is a deuterium labeled Tamoxifen. Tamoxifen (ICI 47699) is a selective estrogen receptor modulator (SERM). Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity[1][2].
NCX899 is a NO-releasing derivative of enalapril, and shows inhibitory activity against angiotensin-converting enzyme (ACE) activity.
Roflupram is a selective, orally active and brain-penetrant PDE4 inhibitor, with an IC50 of 26.2 nM for core catalytic domains of human PDE4. Roflupram can reverse cognitive deficits and reduce the production of pro-inflammatory factors[1][2].
SNX-0723 is a selective, brain-permeable, orally acitve small-molecule inhibitor of Hsp90 (IC50=14 nM) that inhibits alpha-synuclein oligomerization with EC50 of 48 nM; induces Hsp70 (IC50=31 nM), and decreases expression of several known Hsp90 client proteins:HER2 (IC50=9.4 nM), ribosomal protein s6 (pS6) (IC50=13 nM), and PERK (IC50=5.5 nM); shows significant brain concentrations along with induction of brain Hsp70 in vivo with promising PK properties.
Rugonersen (RG6091; RO7248824) is a locked-nucleic acid (LNA)- modified antisense oligonucleotides (ASOs), and results in reduction of ubiquitin-protein ligase E3A (UBE3A) silencing. Angelman syndrome (AS) is a severe neurodevelopmental disorder caused by the loss of neuronal E3 ligase UBE3A, Rugonersen has been used for AS reasearch[1][2].
COX/5-LO-IN-1 is an inhibitor of cylooxygenase and 5-lipoxygenase, used for the research of inflammatory and allergic disease states.
Pedunculoside is a main bioactive component isolated from Jiubiying. Pedunculoside exerts lipid-lowering effects partly through the regulation of lipogenesis and fatty acid β-oxidation[1].
LTV-1 is a highly potent, cell-permeable and reversible inhibitor of lymphoid tyrosine phosphatase (LYP) (IC50 = 508 nM). IC50 value: 508 nMTarget: LYPin vitro: LTV-1 inhibits LYP in a dose-dependent manner at low- and sub-micromolar concentrations in T cells. LTV-1 enhances TCR signaling in intact cells. Exhibits competitive to mixed mode of inhibition (Ki = 384 nM). LTV-1 inhibits the mutant, disease associated LYP-Trp620 activity. LTV-1 blocks the action of the mutant LYP protein in human T cells.
RORγt inhibitor 2 (Compound 119) is a potent RORγt inhibitor with an IC50 of 9.2 nM. RORγt inhibitor 2 can be used for the research of cancer, inflammation or autoimmune diseases mediated by RORγt[1].
BT1718 is a bicyclic anticancer peptide targeting MT1-MMP. BT1718 uses MT1-MMP to target tumors and promote delivery of the cytotoxic payload Mertansine (HY-19792). BT1718 is a bicycle toxin conjugate with a KD value of 3 nM. MT1-MMP is overexpressed in a variety of advanced solid tumors, including triple-negative breast cancer (TNBC), non-small cell lung cancer[1][2].
Lycopodine, a pharmacologically important bioactive component derived from Lycopodium clavatumspores, triggers apoptosis by modulating 5-lipoxygenase, and depolarizing mitochondrial membrane potential in refractory prostate cancer cells without modulating p53 activity[1]. Lycopodine inhibits proliferation of HeLa cells through induction of apoptosis via caspase-3 activation[2].
Ac-Leu-Val-Lys-Aldehyde is a potent cathepsin B inhibitor with IC50s of 4 nM. Ac-Leu-Val-Lys-Aldehyde significantly reduces quinolinic acid (HY-100807)-induced striatal cell death and causes accumulation of LC3-II[1].
CMS-121 is a quinolone derivative and an orally active acetyl-CoA carboxylase 1 (ACC1) inhibitor. CMS-121 protects HT22 cells against ischemia and oxidative damage with EC50 values of 7 nM and 200 nM, respectively. CMS-121 has strong neuroprotective, anti-inflammatory, antioxidative and renoprotective activities[1][2][3].
4'-Methylchrysoeriol is a potent inhibitor of Cytochrome P450 enzymes, with an IC50 of 19 nM for human P450 1B1-dependent EROD.
Hemorphin-7 is a hemorphin peptide, an endogenous opioid peptide derived from the β-chain of hemoglobin. Hemorphin peptides exhibits antinociceptive and antihypertensive activities, activating opioid receptors and inhibiting angiotensin-converting enzyme (ACE).
IDH1 Inhibitor 7-d2 is the deuterium labeled IDH1 Inhibitor 7 (HY-150238). IDH1 Inhibitor 7 is an IDH1 inhibitor with an IC50 of less than 100 nM[1][2].
Spirapril (SCH 33844) hydrochloride is a potent angiotensin converting enzyme (ACE) inhibitor with antihypertensive activity. Spirapril competitively binds to ACE and prevents the conversion of angiotensin I to angiotensin II. Spirapril is an orally active prodrug of Spiraprilat and can be used for the research of hypertension, congestive heart failure[1].
PCSK9-IN-14 (compound Ia-8) is a potent PCSK9 inhibitor[1].
Phe-Pro-Ala-pNA is a chromogenic substrate of tripeptidyl peptidase. Phe-Pro-Ala-pNA can be used to test tripeptidyl peptidase activity[1].
Sephin 1 (NSC 65390) is a selective inhibitor of PPP1R15A that disrupts the PPP1R15A-PP1c complex but spares the related PPP1R15B-PP1c complex; prolongs eIF2α phosphorylation after stress, attenuates the expression of stress genes such as CHOP, and protects cells from cytotoxic ER stress; lacks any measurable α2-adrenergic agonist activity in a cell-based assay, in contrast to Guanabenz; safely prevents the motor, morphological, and molecular defects in mice.
(-)-PX20606 trans isomer is a FXR agonist with EC50s of 18 and 29 nM for FXR in FRET and M1H assay, respectively.
Cucurbitacin D is an active component in Cucurbita texana, disrupts interactions between Hsp90 and two co-chaperones, Cdc37 and p23. Cucurbitacin D prevents Hsp90 client (Her2, Raf, Cdk6, pAkt) maturation without induction of the heat shock response. Anti-cancer activity[1].
PTP1B-IN-22, a ZINC02765569 derivative, is a potent protein tyrosine phosphatase 1B (PTP1B) inhibitor. PTP1B-IN-22 has PTP1B inhibition and glucose uptake in skeletal muscle L6 myotubes[1].
Olesoxime (TRO 19622) is a mitochondrial-targeted neuroprotective compound with mean EC50 value for increasing cell survival is 3.2±0.2 µM.
ML228(CID-46742353) is an activator of the Hypoxia Inducible Factor (HIF) pathway; potently activate HIF in vitro as well as its downstream target VEGF.IC50 value: 1 uM (EC50) [1]Target: HIF activatorML228 represents a novel chemotype available to the research community for the study of HIF activation and its therapeutic potential. Not only is the compound substantially different in structure from known HIF activators, ML228 lacks the acidic functional group almost universally present in PHD inhibitors, which may be important for certain disease applications.
Fenbendazole-d3 is a deuterium labeled Fenbendazole. Fenbendazole is a benzimidazole anthelmintic. Fenbendazole is active against Giardia in vitro (IC50 = 0.3 μM). Fenbendazole (20 mg/kg) prevents infiltration of parasites into the brain in a rabbit model of E. cuniculi infection. Fenbendazole also activates HIF-1α and prevents oxidative stress-induced death in primary neurons in vitro.
PDE12-IN-3 is a phosphodiesterase 12 (PDE12) inhibitor with a pXC50 of 7.68. Antiviral activity[1].
E6446 is a potent and orally acitve TLR7 and TLR9 antagonist, used in the research of deleterious inflammatory responses.
mIDH1-IN-1 (compound 43) is a potent and selective mIDH1 (mutant isocitrate dehydrogenases 1) inhibitor, with an IC50 of 961.5 nM. mIDH1-IN-1 potently inhibits intracellular 2-HG (2-hydroxyglutarate) production in HT1080 cells, with an EC50 of 208.6 ± 8.0 nM. mIDH1-IN-1 shows a significant anti-proliferation activity on IDH1 mutant-U-87 cells, with an IC50 of 41.8 nM. mIDH1-IN-1 is an antitumor agent, and can be used for IDH1 mutated solid tumors research[1].