BAY 61-3606 is a potent, ATP-competitive, reversible, and highly selective inhibitor of Syk tyrosine kinase activity (Ki= 7.5 nM) with no inhibitory effect against Btk, Fyn, Itk, Lyn, and Src.IC50 value: 7.5 nM (Ki) [1]Target: Sykin vitro: BAY 61-3606 inhibited not only degranulation (IC50 values between 5 and 46 nM) but also lipid mediator and cytokine synthesis in mast cells. BAY 61-3606 was highly efficacious in basophils obtained from healthy human subjects (IC50 = 10 nM) and seems to be at least as potent in basophils obtained from atopic (high serum IgE) subjects (IC50 = 8.1 nM). B cell receptor activation and receptors for Fc portion of IgG signaling in eosinophils and monocytes were also potently suppressed by BAY 61-3606 [1]. We identified BAY61-3606 as an inhibitor of proliferation in colorectal cancer cells expressing mutant forms of K-RAS, but not in isogenic cells expressing wild-type K-RAS. In addition to its anti-proliferative effects in mutant cells, BAY61-3606 exhibited a distinct biological property in wild-type cells in that it conferred sensitivity to inhibition of RAF. In this context, BAY61-3606 acted by inhibiting MAP4K2 (GCK), which normally activates NFκβ signaling in wild-type cells in response to inhibition of RAF [2].in vivo: Oral administration of BAY 61-3606 to rats significantly suppressed antigen-induced passive cutaneous anaphylactic reaction, bronchoconstriction, and bronchial edema at 3 mg/kg. Furthermore, BAY 61-3606 attenuated antigen-induced airway inflammation in rats [1].
(2-Hydroxyethoxy)acetic acid (β-hydroxyethoxyacetic acid) is the main urinary metabolite of 1,4-Dioxane. (2-Hydroxyethoxy)acetic acid is a reliable and sensitive shortterm biomarker in urine[1].
Continentalic acid from Aralia continentalis has minimum inhibitory concentrations (MICs) of approximately 8-16 µg/mL against S. aureus, including the Methicillin susceptible Staphylococcus aureus (MSSA) and Methicillin-resistant Staphylococcus aureus (MRSA) standard strains[1].
Piperidinylaminomethyl Trifluoromethyl Cyclic Ether Compound 1 has the potential function in central nervous system disorders, respiratory, inflammatory diseases and gastrointestinal disorders.
MHY1485 is a cell-permeable mTOR activator. MHY1485 has an inhibitory effect on the autophagic process by inhibition of fusion between autophagosomes and lysosomes.
eIF4A3-IN-12 (compound 62) is a silvestrol (HY-13251) analogue. eIF4A3-IN-12 interferes the assembling of eIF4F translation complex with EC50s of 4, 70 and 5 nM for myc-LUC, tub-LUC and the growth inhibition for MBA-MB-231 cells. eIF4A3-IN-12 can be used for the research of human cancer pathogenesis[1].
Cap-dependent endonuclease-IN-23 is a potent inhibitor of cap-dependent endonuclease (CEN). Cap-dependent endonuclease-IN-23 inhibits the replication of influenza virus. ap-dependent endonuclease-IN-23 has the potential for the research of influenza virus infection (influenza A) (extracted from patent WO2021233302A1, compound 8A or 8B)[1].
SB-226552 is an aryloxypropanolamine selective beta3AR agonist.
Ferrocene-d10 is the deuterium labeled Ferrocene[1].
Human β-defensin-3 (HβD-3) is an antibiotic anti-microbial peptide produced by epithelial cells with antimicrobial activities and reduces the effect of inflammatory cytokine responses. Human β-defensin-3 is against different microbes with IC90 values of 6-25 μg/ml[1].
β-Amyloid (1-34) is a β-Amyloid peptide consists of 34 amino acid.
Longikaurin E is a diterpenoids compound isolated from the leaves of Rabdosia ternifolia (D. Don)[1].
AKT-IN-14 (Example 2) is a potent AKTinhibitor with the IC50 values of <0.01 nM, 1.06 nM and 0.66 nM for AKT1, AKT2, AKT3, respectively. AKT-IN-14 can be used in cancer research[1].
Nevanimibe (PD-132301; ATR101) is a selective and potent acyl-coenzyme A:cholesterol O-acyltransferase 1 (ACAT1) inhibitor with an EC50 of 9 nM. Nevanimibe (PD-132301; ATR101) inhibits ACAT2 with an EC50 of 368 nM[1].
(R)-Etomoxir sodium salt is the R-form of Etomoxir sodium salt, acts as an inhibitorof carnitine palmitoyltransferase I (CPT-I), and inhibits palmitate β-oxidation in human, rat and guinea pig.
Diallyl phthalate-d4 is the deuterium labeled Diallyl phthalate[1].
10-O-Methylprotosappanin B is a protosappanin[1].
(3S,5R)-Pitavastatin hemicacium is the 3-epimer of Pitavastatin. Pitavastatin is a potent HMG-CoA reductase inhibitor[1].
Phenytoin sodium is an inactive voltage-gated sodium channel stabilizer.Target: Sodium ChannelPhenytoin sodium is an antiepileptic drug. It is useful to treat partial seizures and generalized tonic-clonic seizures but not primary generalized seizures such as absence seizures or myoclonic seizures. Phenytoin is believed to protect against seizures by causing voltage-dependent block of voltage-gated sodium channels [1]. Phenytoin has low affinity for resting sodium channels at hyperpolarized membrane potentials [2]. When neurons are depolarized and the channels transition into the open and inactivated states, greater binding and block occur. The inhibitory potency is strongly use dependent, so that block accumulates with prolonged or repetitive activation, such as occurs during a seizure discharge. The blocking of sodium channels by phenytoin is of slow onset. The time course of fast sodium currents is therefore not altered in the presence of the drug and action potentials evoked by synaptic depolarizations of ordinary duration are not blocked. Thus phenytoin is able to selectively inhibit pathological hyperexcitability in epilepsy without unduly impairing ongoing activity. Phenytoin also blocks persistent sodium current and this may be of particular importance in seizure control. Phenytoin is a class 1b antiarrhythmic [3].
Wilforgine is a bioactive sesquiterpene alkaloid in Tripterygium wilfordii Hook. F. Wilforgine can induce microstructural and ultrastructural changes in the muscles of Mythimna separata larvae, and the sites of action are proposed to be calcium receptors or channels in the muscular system[1][2].
C8-Ceramide (N-Octanoyl-D-erythro-sphingosine) is a cell-permeable analog of naturally occurring ceramides. C8-Ceramide has anti-proliferation properties and acts as a potent chemotherapeutic agent. C8-Ceramide stimulates dendritic cells to promote T cell responses upon virus infections. C8-Ceramide induces slight activation of protein kinase (PKC) in vitro[1][2][3][4].
Salvianolic acid F is a synthesized polyphenolic acid[1].
CSF1R-IN-7 (Formula I) is a CSF-1R inhibitor. CSF1R-IN-7 can be used for Alzheimer’s disease research[1].
Desmethyl Sibutramine hydrochloride, the secondary metabolite of Sibutramine, is an orally active norepinephrine transporter (NET) and serotonin transporter (SERT) inhibitor. Desmethyl Sibutramine hydrochloride can be used in the research of obesity and appetite suppressant[1][2][3][4].
BCN-HS-PEG2-VA-PABC-SG3199 (Compound 4) is a pyrrolobenzodiazepine that can be used as a drug linker of antibody-drug conjugates (ADC)[1].
SCH-23390 maleate (R-(+)-SCH-23390 maleate) is a potent and selective dopamine D1-like receptor antagonist with Kis of 0.2 nM and 0.3 nM for the D1 and D5 receptor, respectively. SCH-23390 maleate is a potent and high efficacy human 5-HT2C receptor agonist with a Ki of 9.3 nM. SCH-23390 maleate also binds with high affinity to the 5-HT2 and 5-HT1C receptors. SCH-23390 maleate inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with an IC50 of 268 nM[1][2][3].
3-O-Methyl-D-glucose-13C is the 13C labeled 3-O-Methyl-D-glucose[1].
Antioxidant agent-1 is a new chalcone derivative as a potential antioxidant agent.
Metyrosine is a selective tyrosine hydroxylase enzyme inhibitor. Metyrosine exerts anti-inflammatory and anti-ulcerative effects. Metyrosine significantly inhibits high COX-2 activity[1]. Metyrosine is a very effective agent for blood pressure control[2].
SIRT1 activator 3 is a potent activator of Sirt1 and suppresses TNF-α in a dose-dependent manner. SIRT1 activator 3 has the potential for anti-obesity or anti-diabetic researches[1].