AG-09/1 is a specific formyl peptide receptor 1 (FPR1) agonist. N-formyl peptide receptors (FPR) are important in host defense[1].
eIF4A3-IN-13 (compound 75) is a silvestrol (HY-13251) analogue. eIF4A3-IN-13 interferes the assembling of eIF4F translation complex with EC50s of 0.6, 15 and 0.4 nM for myc-LUC, tub-LUC and the growth inhibition for MBA-MB-231 cells. eIF4A3-IN-13 can be used for the research of human cancer pathogenesis[1].
Fosphenytoin sodium is a phenytoin prodrug with similar anticonvulsant properties.
NVX-207 is a derivative of betulinic acid with anti-cancer activity.
Iristectorin B is an isoflavone from Iris tectorum, has anti-cancer activities in breast cancer[1].
BAY 41-4109 racemate is the racemate of BAY 41-4109. BAY 41-4109 is a potent inhibitor of human hepatitis B virus (HBV) with an IC50 of 53 nM.
Masoprocol (meso-Nordihydroguaiaretic acid) is a potent and orally active lipoxygenase inhibitor. Masoprocol shows antihyperglycemic activity. Masoprocol decreases the glucose concentration and hepatic triglyceride in vivo. Masoprocol has the potential for the research of type II diabetes[1][2][3].
RUNX-IN-2 (Compound Conjugate 3) covalently binds to the RUNX-binding sequences, and inhibits the binding of RUNX proteins to their target sites. RUNX-IN-2 induces the p53-dependent apoptosis and inhibits cancer cell growth. RUNX-IN-2 inhibits tumor growth in PANC-1 xenograft mice. RUNX-IN-2 has high alkylation efficiency and specificity[1].
Caesalmin B is a furanoditerpenoid lactone isolated from Caesalpinia minax. Caesalmin B exhibits antiviral activity[1][2].
μ-Conotoxin Sx IIIA is a biological active peptide. (NaV1.4 Channels Blocker)
Glp-Trp-OEt, a pyroglutamyl-tryptophan derivative, is a dipeptide Et ester[1].
Iberin, a sulfoxide analogue of sulforaphane, is a naturally occurring member of isothiocyanate family. It inhibits cell survival with an IC50 of 2.3 μM in HL60 cell.
UM-164 is a highly potent inhibitor of c-Src with a Kd of 2.7 nM. UM-164 also potently inhibits p38α and p38β.
2-Oxo-2-phenylethyl ((benzyloxy)carbonyl)-L-alaninate is an alanine derivative[1].
Fluphenazine enanthate is the first long-acting injectable (LAI) antipsychotic for the treatment of schizophrenia[1][2].
2'-NH2-ATP (2'-Amino-2'-deoxyadenosine-5'-triphosphate), an adenosine derivative, is a weak competitive inhibitor of ATP, with a Ki of 2.3 mM. 2'-NH2-ATP can be used in nucleic acid labeling[1][2][3].
Methylene blue trihydrate (C.I. Basic Blue 9 trihydrate) is a guanylyl cyclase (sGC), monoamine oxidase A (MAO-A) and NO synthase (NOS) inhibitor. Methylene blue trihydrate is a vasopressor and is often used as a dye in several medical procedures. Methylene blue trihydrate has antinociception, antimalarial, antidepressant and anxiolytic activity effects. Methylene Blue trihydrate has the potential for methemoglobinemias, neurodegenerative disorders and ifosfamide-induced encephalopathytreatment[1][2][3].
Olprinone Hcl(Loprinone Hcl) is a selective phosphodiesterase 3 (PDE3) inhibitor. IC50 value:Target: PDE3Olprinone is used as cardiotonic agent with positive inotropic and vasodilating effects. Olprinone has been reported to improve microcirculation and attenuate inflammation. Olprinone is often used to increase cardiac output after cardiopulmonary bypass (CPB). Olprinone was infused at a rate of 0.2 μg/kg/min when weaning from CPB was started. Olprinone has also shown potent antioxidative and anti-inflammatory effects in the meconium-induced oxidative lung injury.
Isocucurbitacin D is an antitumor agent[1].
Methyl chlorogenate is an antioxidant, and has radical scavenging activity. Methyl chlorogenate is an anti-inflammatory agent. Methyl chlorogenate also inhibits hepatocellular carcinoma (HCC) cell proliferation and metastasis[1][2].
PEG3-bis-(ethyl phosphonate) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
USP7-IN-7 (compound 124) is a USP7 inhibitor with an IC50 value ＜10 nM. USP7-IN-7 shows cytotoxicity against p53-mutant cancer cell lines, p53 wild-type blood cancer and neuroblastoma cell lines with low nanomolar values. USP7-IN-7 can be used for cancer research[1].
Enalapril Maleate, the active metabolite of enalapril, is an angiotensin-converting enzyme (ACE) inhibitor.Target: ACEEnalapril is a prodrug that belongs to the angiotensin-converting enzyme (ACE) inhibitor class of medications. It is rapidly metabolized in the liver to enalaprilat following oral administration. Enalaprilat is a potent, competitive inhibitor of ACE, the enzyme responsible for the conversion of angiotensin I (ATI) to angiotensin II (ATII). ATII regulates blood pressure and is a key component of the renin-angiotensin-aldosterone system (RAAS). Enalapril may be used to treat essential or renovascular hypertension and symptomatic congestive heart failure [1].
Mapatumumab (HGS-ETR1) is a fully human IgG1 agonistic monoclonal antibody that targets tumor necrosis factor-related apoptosis-inducing ligand receptor 1 (TRAIL-R1). Mapatumumab can be used for the research of cancer[1].
Pagoclone is an active (+)-enantiomer of the racemate RP 59037. Pagoclone is a partial GABA(A) receptor agonist used for the treatment of panic and anxiety disorders.
LU-005i is a potent inhibitor of β5i subunit of immunoproteasomes (IC50 = 6.6 nM), selective over β5c subunit (IC50 = 287 nM)[1].
PI3Kγ inhibitor 7 (compound 2) is a potent and orally active PI3Kγ inhibitor with IC50 values of 4768, 878.1, 3.42, 355.2 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ, respectively. PI3Kγ inhibitor 7 shows antitumor activity[1].
Coumalic acid is a valuable platform compound which can be prepared from malic acid. Coumalic acid can be used in the flavours, fragrances and cosmetics industries, as polymer components, and as pharmaceutical scaffolds displaying anti-bronchial and -malarial activity[1].
(±)-Vesamicol hydrochloride ((±)-AH5183 hydrochloride) is a potent vesicular acetylcholine transport inhibitor with a Ki of 2 nM. (±)-Vesamicol hydrochloride also displays high affinity for σ1 and σ2 receptors with Kis of 26 nM and 34 nM, respectively[1][2].
(Rac)-Arnebin 1 ((Rac)-β,β-Dimethylacrylalkannin) is the racemate of β,β-Dimethylacrylalkannin and/or β,β-Dimethylacrylshikonin. β,β-Dimethylacrylalkannin and β,β-Dimethylacrylshikonin are napthoquinones isolated from Arnebia nobilis. β,β-Dimethylacrylshikonin has anti-tumor activity[1].