BIIB021 is an orally available, fully synthetic inhibitor of HSP90 with Ki and EC50 of 1.7 nM and 38 nM, respectively.
2-Amino-4-(ethylthio)butanoic acid is a Methionine (HY-13694) derivative[1].
Mulberrofuran A is a natural product, that can be isolated from the root bark of mulberry tree. Mulberrofuran A inhibits the formations of 12-hydroxy-,8,10-heptadecatrienoic acid (HHT) and thromboxane B2 (cyclooxygenase products), but it increases the formation of 12-hydroxy-5,8,10,14-eicosatetraenoic acid (12-HETE) (12-lipoxygenase product)[1].
Dasatinib hydrochloride is a potent and dual AblWT/Src inhibitor IC50 of 0.6 nM/0.8 nM respectively; also inhibits c-KitWT/c-KitD816V with IC50 of 79 nM/37 nM.
Trimyristin, an active molluscicidal component of Myristica fragrans Houtt, significantly inhibits acetylcholinesterase (AChE), acid and alkaline phosphatase (ACP/ALP) activities in the nervous tissue of Lymnaea acuminata. IC50s of Trimyristin against AChE, ACP, and ALP are 0.11, 0.16 and 0.18 mM, respectively[1].
Tetrahydrofluoroene 52 is a potent and selective estrogen receptor β agonist.
Anticancer agent 143 (compound 369) is a dual PTPN2/PTP1B inhibitor with IC50 values <2.5 nM. Anticancer agent 143 can be used in cancer research[1].
Kynuramine, an endogenously occurring amine, is a fluorescent substrate and probe of plasma amine oxidase[1][2].
Fmoc-(FmocHmb)Lys(Boc)-OH is a lysine derivative[1].
PXYC1 is a ribosomal protein S1 (RpsA) antagonist with Kds of 0.81 and 0.31 μM for RpsA-CTD and RpsA-CTD Δ438A, respectively. RpsA plays an important role in the trans-translation process of Mycobacterium Tuberculosis (Mtb)[1].
Hydroxyprogesterone caproate is a synthetic, steroidal progestin; an ester derivative of 17α-hydroxyprogesterone formed from caproic acid.
(3S,5S)-Pitavastatin (hemicacium) is the enantiomer of Pitavastatin. Pitavastatin is a potent HMG-CoA reductase inhibitor[1].
Olprinone(Loprinone) 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.
GPR3 agonist-2(compound 32) is a potent full agonist of G protein-coupled receptor 3, with the IC50of 260 nM[1].
(+)-JQ1 PA is a derivative of the Bromodomain and extra-terminal (BET) inhibitor JQ1, with an IC50 of 10.4 nM.
TAE-1 is a potent inhibitor of AChE and BuChE. TAE-1 also inhibits Aβ fibril formation and aggregation. TAE-1 can be used for the researches of Alzheimer's disease[1].
Fmoc-Tyr(tBu)-Ser(psi(Me,Me)pro)-OH is a dipeptide.
20:0-20:1-20:0 TG-d5 is deuterium labeled 20:0-20:1-20:0 TG.
MSDC 0160 act as an insulin sensitizer and a modulator of mitochondrial pyruvate carrier (MPC), a key controller of cellular metabolism that influences mTOR (mammalian target of rapamycin) activation. In Vitro: MSDC-0160 acts as insulin sensitizers without activating PPARγ. MSDC-0160 (10 μM) pretreatment (1 hour) prevents the MPP+ (10 μM)-induced loss of both tyrosine hydroxylase (TH)-immunoreactive differentiated Lund human mesencephalic (LUHMES) cells. MSDC-0160 protects only TH-immunoreactive neurons, which is consistent with the selected concentration of MPP+ primarily being toxic to dopamine neurons. In addition, MSDC-0160 counteracts both MPP+-induced shortening of neurite length and reduces branching in both LUHMES cells. MSDC-0160 (10 or 100 μM) prevents the loss of GFP-fluorescent dopaminergic neurons induced by MPP+ (0.75 mM) in nematodes (P =0.0001), whereas 1 μM MSDC-0160 does not. MSDC-0160 (10 μM) blocks LPS-induced increases in iNOS expression in BV2 cell lysates. MSDC-0160 is mainly to prevent the activation of mTOR produced by the metabolic changes rather than to directly inhibit mTOR kinase activity[1]. PPARγ sparing TZD, MSDC-0160, reduces resistance in the insulin/IGF-1 signaling pathway and restores IGF-1-induced akt phosphorylation. MSDC-0160 (10-20 μM) in conbination with IGF-1 prevents the loss of insulin content and maintains insulin secretion. Treatment of human islets with MSDC-0160 (1-50 μM) activates AMPK and downregulates mTOR. MSDC-0160 (1-50 μM) treatment maintains human β-cell phenotype[2]. The combined treatment with PPARγ ligands (MSDC 0160) and γ-radiation synergistically induces caspase-dependent apoptotic cell death, and PPARγ ligands significantly enhance the γ-radiation-induced DNA damage response in a PPARγ-independent manner[3].In Vivo: MSDC-0160 (30 mg/kg per day, p.o.) can be observed in plasma and brain tissue of the mice, proving MSDC-0160 can effectively enter the brain. MSDC-0160 (30 mg/kg per day, p.o.) treatment 3 days after MPTP injection, improves motor behavior, protects nigrostriatal neurons, and suppresses disease progression in the MPTP mouse model of Parkinson’s disease (PD), improves motor behavior in the open-field and rotarod tests in the En1+/- genetic mouse model of PD, and prevents dopaminergic neurodegeneration in the En1+/- genetic mouse model of PD. MSDC-0160 (30 mg/kg, p.o.) modulates mTOR signaling in C. elegans and the MPTP mouse model of PD. MSDC-0160 down-regulates mTOR signaling and restores autophagy in the En1+/- genetic mouse model of PD[1].
Alnuctamab (EM901) is an asymmetric 2-arm, humanized IgG T-cell engager (TCE). Alnuctamab can be used for immune research[1].
Ampicillin trihydrate (D-(-)-α-Aminobenzylpenicillin trihydrate) is a broad-spectrum beta-lactam antibiotic against a variety of gram-positive and gram-negative bacteria.
OATD-02 is an orally active, competitive, reversible, noncovalent dual inhibitor of Arginase1 and 2. OATD-02 is a slow offset inhibitor, blocking intracellular arginases with IC50s of 20 nM (hARG1), 39 nM (hARG2), 39 nM (mARG1), and 28 nM (rARG1), respectively. OATD-02 abolishes tumor immunosuppression induced by both arginases. OATD-02 can be used for melanoma study[1].
Thioperamide maleate (MR-12842 maleate) is a potent, orally available, brain penetrant and selective H3 receptor antagonist with a Ki of 4.3 nM for inhibition of [3H]histamine release. Thioperamide maleate inhibits [3H]histamine synthesis with a Ki of 31 nM[1].
Momelotinib-3,3,5,5-d6 (CYT387-3,3,5,5-d6) is the deuterium labeled Momelotinib (HY-10961). Momelotinib has inhibitory activity for JAK1/JAK2[1][2].
Brombuterol hydrochloride (Bromobuterol hydrochloride) is a β-adrenergic receptor agonist[1].
SSAA09E3 is a SARS-CoV entry inhibitor that inhibits SARS/HIV pseudotyped virus entry with an EC50 of 9.7 μM in 293T cells and inhibits SARS-CoV infection of Vero cells with an EC50 of 0.15 μM[1][2].
Fasiglifam (TAK-875) hemihydrate is a potent, selective and orally active GPR40 agonist with EC50 of 72 nM. Fasiglifam enhances glucose-dependent insulin secretion and improves hyperglycemia in type 2 diabetic rats. Fasiglifam can induce liver injury[1][2][3][4].
(2E,9Z)-Octadeca-2,9-dienoic acid, a polyunsaturated fatty acid, can be used for the research of lipoxygenase-dependent metabolism[1].
R916562 is a potential and selective Axl/VEGF-R2 dual inhibitor with IC50s of 136 and 24 nM, respectively.
Tropodifene (Tropaphen) is an α-Adrenergic receptor inhibitor.