TyrphostinAG879 is a tyrosine kinase inhibitor that inhibits TrKA phosphorylation, but not TrKB and TrKC.[1] also a ErbB2 kinase inhibitor, has at least 500-fold higher selectivity to ErbB2 (IC50 = 1 μmol/L) than EGFR (IC50 >500 μmol/L).target: TrKA [1], ErbB2 [2].IC 50: ErbB2 1 μmol/L [2].In vitro: TyrphostinAG879 significantly inhibit the A-type potassium currents in the cultured hippocampus neurons.[2] TyrphostinAG879 can reduce gephyrin puncta in GABAergic neurons and PSD-95 puncta in glutamatergic neurons where ErbB4 expression was low. [3] In vivo: Treatment with TyrphostinAG879 in immunodepressed mice graft with leiomyosarcoma or promyelocytic leukemia cells result in dramatic reductions in tumor sizes. [1]
Ganoderic acid TR is a broad-spectrum inhibitor against influenza neuraminidases (NAs), particularly H5N1 and H1N1 neuraminidases. The IC50 values of 10.9 and 4.6 μM, respectively[1].
Biotin-VAD-FMK is a cell permeable, irreversible biotin-labeled caspase inhibitor, used to identify active caspases in cell lysates.
CDK7-IN-7 is a potent and selective CDK7 kinase inhibitor with an IC50 of <50 nM (Patent CN112661745A, compound T-01)[1].
(Rac)-Dalzanemdor((Rac)-SAGE-718) is an orally active and high intrinsic activity N-Methyl-d-aspartatereceptor (NMDAR) positive allosteric modulators (PAMs). (Rac)-Dalzanemdor canbe used for the research of Huntington’s disease[1].
(E/Z)-Squalene ((E/Z)-Super Squalene; (E/Z)-AddaVax) is a triterpenic compound. (E/Z)-Squalene accumulates and reduces liver cholesterol and triglycerides in the liver. (E/Z)-Squalen regulates the production of intracellular active oxidants (ROS) and induces apoptosis and necrosis in a concentration-and time-dependent manner[1].
Mastoparan, a tetradecapeptide which is a component of wasp venom, stimulates release of prolactin from cultured rat anterior pituitary cells.
Linopirdine (DuP 996) is an orally active, selective M-type K+ current (IM; Kv7; KCNQ Channels) inhibitor with an IC50 of 2.4 μM. Linopirdine is a TRPV1 agonist. Linopirdine, a putative cognition enhancing drug, increases acetylcholine release in rat brain tissue[1][2][3].
K1 peptide is a high-affinity peptide ligand for GABAA receptor-associated protein (GABARAP)[1].
Engeletin is a flavanonol glycoside isolated from hymenaea martiana, inhibits NF-κB signaling-pathway activation, and possesses anti-inflammatory, analgesic, diuresis, detumescence, and antibiosis effects.
Biotin-PEG7-thiourea is a biotin-labeled, PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Nelutroctiv is a potent cardiac troponin activator[1].
Ketanserin is a selective 5-HT receptor antagonist. Ketanserin also blocks hERG current (IhERG) in a concentration-dependent manner (IC50=0.11 μM).
BIM-23027 is a selective agonist of sst2 receptor (EC50=0.32 nM), with similar effect to somatostatin (SRIF), a cyclic tetradecapeptide. BIM-23027 stimulates dopamine release, which is mediated by a Glu-dependent mechanism[1][2].
L-γ-Glutamyl-p-nitroanilide Monohydrate is a glutamic acid derivative[1].
IRBP derived peptide, R16 is a biological active peptide. (R16 is an IRBP (Interphotoreceptor retinoid binding protein) derived peptide. Photoreceptor cell protein is capable of inducing an experimental autoimmune uveitis (EAU) in susceptible animal strains.)
Keap1-Nrf2 probe is a fluorescent Keap1-Nrf2 probe[1].
QPX7728 is a potent, ultra-broad-spectrum boronic acid beta-lactamase inhibitor. QPX7728 inhibits key serine and metallo beta-lactamases at a nano molar range[1].
DTSSP Crosslinker disodium is a protein cross-linker containing a disulfide bond. DTSSP Crosslinker disodium can react with sidechains of amino acids that are within close proximity[1][2].
Carbosulfan inhibited relatively potently CYP3A4 and moderately CYP1A1/2 and CYP2C19 in pooled HLM (human livers). Carbosulfan activation is predominantly catalyzed in humans by CYP3A4.
Gamma-Glu-D-Glu is a biologically active peptide.
RTC-5 is an optimized phenothiazine with anti-cancer potency. RTC-5 demonstrates efficacy against a xenograft model of an EGFR driven cancer, its effects is attributed to concomitant negative regulation of PI3K-AKT and RAS-ERK signaling[1].
Naphthalene-1,2-dicarbaldehyde is a fluorescent dye[1].
FGFR1 inhibitor-2 is a FGFR1 inhibitor (IC50 is 4.55 μM in MDA-MB-231 cells). FGFR1 inhibitor-2 can be used for the research of metastatic triple-negative breast cancer[1].
Enasidenib is an oral, potent, reversible, selective inhibitor of the IDH2 mutant enzymes, with IC50s of 100 and 400 nM against IDH2R140Q and IDH2R172K, respectively.
DBCO-PEG1-NH-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
R-96544 (free base) is a potent, selective and competitive 5-HT2 receptor antagonist. R-96544 (free base) inhibits platelet aggregation induced by serotonin, and inhibits 5-HT2A receptor-mediated contraction of guinea pig trachea[1].
GRK2 Inhibitor 1 (methyl 5-[2-(5-nitro-2-furyl)vinyl]-2-furoate) is a GRK2 (β-ARK1) inhibitor[1].
Pedalitin is a inhibitor of tyrosinase（IC50=0.28 mM） and α-glucosidase（IC50=0.29 mM）[1].
AZ 12216052 is a mGluR8 positive allosteric modulator, and helps mGluR8 modulate signaling inputing to retinal ganglion cells. AZ 12216052 exhibits antianxiety effect[1][2][3][4].