Terfenadine is a potent open-channel blocker of hERG with a mean IC50 of 204 nM.IC50 value: 204 nMTarget: HERGTerfenadine normally undergoes extensive first-pass metabolism in the liver to produce an active acidic metabolite. Terfenadine is a widely used, over-the-counter drug to treat allergies.
Bis-(m-PEG4)-amidohexanoic acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
endo-BCN-PEG4-Boc is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
TCL1(10-24) is a encompassing the betaA strand of human TCL1. TCL1(10-24) is a Akt inhibitor. TCL1(10-24) interacts with the Akt PH domain prevented phosphoinositide binding and hence inhibits membrane translocation and activation of Akt. TCL1(10-24) inhibits cellular proliferation and anti-apoptosis. TCL1(10-24) has tumor growth in vivo[1].
N-Acetyl-D-norvaline is a valine derivative[1].
PRIMA-1 is a mutant p53 reactivator, restores the sensitivity of TP53 mutant-type thyroid cancer cells to the histone methylation inhibitor 3-Deazaneplanocin A.
Duligotuzumab (MEHD-7945A; RG 7597) is a humanized IgG-κ monoclonal antibody that specifically targets Her3 (ErbB3)[1].
TAK-615 (TAK615) is a potent, selective, negative allosteric modulator (NAM) of the LPA1 receptor, partially inhibits the LPA response with IC50 of 91 nM (60% at 10 uM) in calcium mobilisation assays.
D-erythro-Sphingosine (Erythrosphingosine) hydrochloride is a specific TRPM3 activator. D-erythro-Sphingosine also induces retinoblastoma protein dephosphorylation[1][2].
[Ser25] Protein Kinase C (19-31) is a substrate of protein kinase C (PKC) (Km: 0.3 μM). [Ser25] Protein Kinase C (19-31) is derived from the pseudo-substrate regulatory domain of PKCα (19-31) with a Serine at position 25 replacing the wild-type Alanine[1].
rU Phosphoramidite is a phosphorite monomer that can be used in the synthesis of oligonucleotides.
AMG 837 sodium salt is a potent GPR40 agonist(EC50=13 nM) with a superior pharmacokinetic profile and robust glucose-dependent stimulation of insulin secretion in rodents.IC50 value: 13 nM (EC50) [1]Target: GPR40 agonistAMG 837 displayed the expected two-fold increase in potency on GPR4 (EC50 = 13 [±7] nM) compared to the racemic compound and its activity crossed over to the rat and mouse forms of GPR40 (EC50 = 23 and 13 nM, respectively). AMG 837 was found to be a partial agonist on GPR40 with maximal activity 85% of that shown by DHA under our standard assay conditions. AMG 837 is a highly potent stimulator of insulin secretion in MIN6 cells with an EC50 comparable to that seen in the aequorin Ca2+-flux assay. showedno significant activity in cell-based assays against PPARα, δ, and γ. An external panel of 64 receptors also revealed no significant activity with the exception of weak inhibition (IC50 = 3 uM) on the a2-adrenergic receptor. Overall, AMG 837 was both highly potentand selective in vitro.
GAGGVGKSAL is a wild-type KRAS G12D 10mer peptide. GAGGVGKSAL can be used as an immunogenic neoantigen for cancer immunotherapy research[1].
DPPY (compound 6) is a potent PTK inhibitor with IC50 values of <10, <10, <10 nM for EGFR, BTK, JAK3, respectively. DPPY shows anti-proliferative activity against B-cell lymphoma cells. DPPY has the potential for the research of idiopathic pulmonary fibrosis (IPF)[1].
HG-12-6 is a small-molecule inhibitor that bind preferentially to unphosphorylated IRAK4 with IC50 of 165.1 nM, displays 15-fold selectivity over phosphorylated IRAK4 (IC50=2876 nM); binds as type II inhibitor with IRAK4 in a “DFG-out” conformation.
CA224 (Compound 1) is a selective and orally active Cdk4–cyclin D1 inhibitor with an IC50 of 6.2 µM. CA224 induces cell apoptosis and shows antitumor activity[1].
Chetomin, an active component of Chaetomium globosum, is a heat shock protein 90/hypoxia-inducible factor 1 alpha (Hsp90/HIF1α) pathway inhibitor. Chetomin is a potent, nontoxic non-small cell lung cancer cancer stem cells (NSCLC CSC)-targeting molecule[1].
Oxotremorine M iodide is a potent and selective muscarinic acetylcholine receptor (mAChR) agonist. Oxotremorine M iodide potentiates NMDA receptors by muscarinic receptor dependent and independent mechanisms[1].
endo-BCN-PEG8-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
5-O-(E)-p-Coumaroylquinic acid, a quinic acid derivative, is a potent phytochemical agent against hepatitis B virus[1].
TK4g is a Janus kinase (JAK) inhibitor with the IC50 values of 12.61 nM and 15.80 nM for JAK2 and JAK3, respectively. TK4g can be used in lymphoid-derived diseases and leukemia cancer research[1].
Boc-Asp-OH is an aspartic acid derivative[1].
1-(3,4-Dihydroxyphenyl)-7-(4-hydroxyphenyl)hept-6-en-3-ol (Compound 1) is a natural product that can be isolated from rhizomes of Curcuma comosa[1].
Cidofovir dehydrate is an injectable antiviral medication for the treatment of cytomegalovirus (CMV) retinitis, which suppresses virus replication by selective inhibition of viral DNA synthesis.Target: CMV DNA polymeraseCidofovir is an injectable antiviral medication for the treatment of cytomegalovirus (CMV) retinitis in patients with AIDS. It suppresses CMV replication by selective inhibition of viral DNA polymerase and therefore prevention of viral replication and transcription. It is an acyclic nucleoside phosphonate, and is therefore independent of phosphorylation by viral enzymes, unlike acyclovir.Cidofovir was discovered at the Institute of Organic Chemistry and Biochemistry, Prague, by Antonín Hol?, and developed by Gilead Sciences and is marketed with the brand name Vistide by Gilead in the USA, and by Pfizer elsewhere. Maintenance therapy with cidofovir involves an infusion only once every two weeks, making it a convenient treatment option. Because dosing is relatively infrequent, a permanent catheter is not necessary for infusions.
Miglustat(OGT918) is an inhibitor of glucosylceramide synthase, primarily to treat Type I Gaucher disease (GD1).Target: OthersMiglustat is an inhibitor of the ceramide-specific glycosyltransferase, which catalyzes the first step of glycosphingolipid biosynthesis and is currently approved for the oral treatment of type 1 GD [1]. Consumption of a standard high-fat breakfast within 30 minutes before administration of miglustat significantly reduced peak exposure but did not significantly affect the extent of systemic exposure to miglustat. The peak plasma concentration (C(max)) decreased by 36% on average following administration with food. Area under the plasma concentration-time curve (AUC(0-infinity)) showed a modest (14%) decrease with food, but the 90% confidence interval was within the acceptance limit of 80% to 125%. The median (min-max) time to C(max) (t(max)) was prolonged from 2.5 (1.0-4.0) hours in the fasted state to 4.5 (1.5-8.0) hours in the fed state, whereas the apparent terminal half-life was approximately 8 hours and not affected by food [2].
LG 82-4-01 is a thromboxane (TX) synthetase specific inhibitor, with an IC50 of 1.3 μM[1].
Ethyl 3,4-dihydroxybenzoate (Ethyl protocatechuate), an antioxidant, is a prolyl-hydroxylase inhibitor found in the testa of peanut seeds. Ethyl 3,4-dihydroxybenzoate protects myocardium by activating NO synthase and generating mitochondrial ROS. Ethyl 3,4-dihydroxybenzoate induces cell autophagy and apoptosis in ESCC cells. Ethyl 3,4-dihydroxybenzoate is a collagen synthesis inhibitor and has a bone protecting-effect[1][2][3][4].
2,16,19-Kauranetriol 2-O-β-D-allopyranoside is an ent-kaurane glycoside, which can be isolated from the fronds of Pteris cretica[1].
Pavinetant (MLE-4901) is a neurokinin-3 receptor (NK3R) antagonist.
Isorhamnetin 3-O-β-D-glucose-7-O-β-D-gentiobioside is a bioactive constituent that can be found in the seeds of Lepidium apetalum Willd. Isorhamnetin 3-O-β-D-glucose-7-O-β-D-gentiobioside exhibits significant triglyceride (TG)-lowering effects in HepG2 cells[1].