Glycycoumarin is a major bioactive coumarin of licorice. Glycycoumarin inhibits hepatocyte lipoapoptosis through activation of autophagy and inhibition of ER stress-mediated JNK and GSK-3-mediated mitochondrial pathway. Glycycoumarin exerts anti-liver cancer activity by directly targeting T-LAK cell-originated protein kinase [1] [2].
KRAS G12C inhibitor 22 is a KRAS G12C inhibitor extracted from patent WO2021219072A1, example 120[1].
Asn-Pro-Val-PABC-MMAE TFA (compound 8) is a potent ADC Linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
Desacetylcinobufagin is a natural compound used for microbial transformation.
PTP1B-IN-13 is a selective PTP1B inhibitor targeting the allosteric site with an IC50 value of 1.59 μM.
Diethylamine NONOate (DEA NONOate, diethylammonium salt) is a nitric oxide donor. Diethylamine NONOate is a potent antimicrobial agent, which can inhibit Escherichia coli growth. Diethylamine NONOate also can enhance preservation of the donor rat heart[1][2].
Tellimagrandin II (Eugeniin), the first intermediate in the 4C1-glucose derived series of ellagitannins, also inhibits antibiotic resistance of drug-resistant Staphylococcus aureus[1][2].
PknB-IN-2 (Compound 10) is a Mycobacterium tuberculosis protein kinase B (PknB) inhibitor with an IC50 of 12.1 μM[1].
Dioxopromethazine is an orally active antihistamine. Dioxopromethazine inhibits asthmatic symptoms[1].
STING agonist-22 (CF501) is a potent non-nucleotide STING agonist. STING agonist-22 is a adjuvant by activating STING to induce the type I interferon (IFN-I) response and proinflammatory cytokine production. STING agonist-22 can be used as an adjuvant to boost the original protein vaccine, producing potent, broad, and long-term immune protection. STING agonist-22 can be used for SARS-CoV-2 variants and sarbecovirus diseases research[1].
PDE2/PDE10-IN-1 is a phosphodiesterase 2 (PDE2) and PDE10 inhibitor with IC50s of 29 and 480 nM, respectively.
Casein Kinase inhibitor A86 (CKIα inhibitor A86) is a novel pan-specific CKI (CSNK1) inhibitor (Kd=1-10 nM, CKIα Kd=9.8 nM) that co-targets the transcriptional kinases CDK7 and CDK9, with hardly inhibition of CDK8, CDK13, CDK11a, CDK11b, and CDK19; target both CDK7 and CDK9 with low nM Kd values; induces leukemia cell apoptosis at <160 nM, in correlation to the capacity to stabilize p53; shows high and selective sensitivity against leukemic CFUs in colony-forming unit (CFU) assay, without effect on normal hematopoietic CFUs; blocking CKIα together with CDK7 and/or CDK9 synergistically stabilize p53, deprive leukemia cells of survival and proliferation-maintaining SE-driven oncogenes, induce apoptosis, abolishes the expression of MYC, MDM2, and the anti-apoptotic oncogene MCL1; demonstrates therapeutic efficacy with preserved hematopoiesis and leukemia cure potential in AML mouse models.
Z-VEID-FMK is a selective inhibitor of caspase-6. Z-VEID-FMK can be used for the research of tumor[1].
K-(D-1-Nal)-FwLL-NH2 is a high affinity and potent ghrelin receptor inverse agonist (Ki values are 4.9 and 31 nM in COS7 and HEK293T cells, respectively). K-(D-1-Nal)-FwLL-NH2 blocks ghrelin receptor-mediated Gq- and G13-dependent signaling pathways.
N,N-Dimethylacetamide-d3 is the deuterium labeled N,N-Dimethylacetamide[1]. N,N-Dimethylacetamide (DMAc) is an inexpensive, common aprotic organic solvent[2].
Pitavastatin (NK-104) is a potent HMG-CoA reductase inhibitor, Pitavastatin inhibited cholesterol synthesis from acetic acid with an IC50 of 5.8 nM in a human liver cancer cell line (HepG2).IC50 value: 5.8 nM(cholesterol synthesis from aceticacid in HepG2) [1]Target: HMG-CoA reductasein vitro: Pitavastatin inhibited cholesterol synthesis from aceticacid with an IC50 of 5.8 nM in a human liver cancer cell line (HepG2), which indicates that is 2.9 and 5.7 times as potent as simvastatin and atorvastatin, respectively. When the inhibitory activity interms of the ED50 was compared with that of simvastatin,pitavastatin showed a 3-fold stronger activity in the rat and 15-fold stronger activity in a guinea pig model.22 The inhibitory effect of pitavastatin on sterol synthesis is thought to be liver-selective [1]. pitavastatin reduces total and phosphorylated tau levels in a cellular model of tauopathy, and in primary neuronal cultures. The decrease caused by pitavastatin is reversed by the addition of mevalonate, or geranylgeranyl pyrophosphate. The maturation of small G proteins, including RhoA was disrupted by pitavastatin, as was the activity of glycogen synthase kinase 3β (GSK3β), a major tau kinase [4].in vivo: Intravenous treatment with pitavastatin-incorporated nanoparticles, but not with control nanoparticles or pitavastatin alone, inhibited plaque destabilization and rupture associated with decreased monocyte infiltration and gelatinase activity in the plaque[2].The EAM model was established in BALB/c mice by immunization with murine α-myosin heavy chain. Mice were fed pitavastatin (5 mg/kg) or vehicle once daily for 3 weeks from day 0 to day 21 after immunization [3].
AMG7703 (4-CMTB, AMG-7703) is an allosteric, selective agonist of FFAR2 (GPR43).
Misoprostol acid D5 is deuterium labeled Misoprostol acid. Misoprostol acid is an active metabolite of Misoprostol. Misoprostol is a synthetic analogue of prostaglandin E1 (PGE1), extensively absorbed, and undergoes rapid de-esterification to Misoprostol acid in the gastrointestinal tract after oral administration. Misoprostol can be used for non-steroidal anti-inflammatory drug-induced (NSAID) gastric ulcers[1]. Misoprostol is an oral agent used to induce labor[2].
1-Bromononane-d3 is the deuterium labeled 1-Bromononane[1].
PF-03622905 is a potent and ATP-competitive PKC inhibitor with IC50s of 5.6 nM, 14.5 nM, 13 nM, 37.7 nM, and 74.1 nM for PKCα, PKCβI, PKCβII, PKCγ, and PKCθ, respectively. PF-03622905 shows high specificity for PKC over other protein kinases[1].
[Nphe1]Nociceptin(1-13)NH2, a novel nociceptin/orphanin FQ (NC) endogenous ligand, is a selective and competitive ociceptin receptor antagonist without any residual agonist activity. [Nphe1]nociceptin(1-13)NH2 binds selectively to recombinant nociceptin receptors (pKi=8.4) and antagonizes the inhibitory effects of nociceptin on cyclic AMP accumulation in CHO cells (pA2=6.0). [Nphe1]Nociceptin(1-13)NH2 has the potential to act as an analgesic agent[1].
Verrucarin J (Muconomycin B) is a metabolite of the Myrothecium fungus family. Verrucarin J generates reactive oxygen species (ROS) and induces apoptosis of cancer cell lines, such as A549, HCT 116 and SW-620 cells. Verrucarin J shows activities against Candida albicans and Mucor miehei. Verrucarin J inhibits arenavirus Junin (JUNV) yield with an IC50 of 1.2 ng/mL[1][2][3][4][5].
2',3'-Dideoxyuridine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
Tetrazine-Amine is a tetrazine linker that can be used to covalently label live cells through a cycloaddition[1][2].
Glucagon exhibits marked effects on protein and amino acid metabolism. Glucagon inhibits the incorporation of amino acids into protein of liver, muscle, and pancreas, to increase excretion of nitrogen, to promote hepatic urea synthesis, and to increase the concentration of hepatic transaminases and urea cycle enzymes. Glucagon can promote the hepatic uptake of amino acids, to enhance their incorporation into liver glycogen, and to depress the concentration of amino acids in blood[1].
AC-265347 is a calcium-sensing receptor (CaSR) agonist and positive allosteric modulator (ago-PAM) with the functional affinity (pKB) of 5.1. AC-265347 can be used for the research of hyperparathyroidism and related diseases[1].
BTK-IN-12 is a potent BTK inhibitor with IC50s of 1.2 nM and 0.8 nM for wild-type BTK or mutated BTK (C481S), respectively (WO2022037649A1; compound 8)[1].
Biotinyl-ACTH (1-39) (human) is abiotinylated Adrenocorticotropic Hormone (ACTH) (1-39), human (HY-P1211).
Boc-Val-Ala-PAB is a cathepsin cleavable ADC linker that is used for making antibody-drug conjugate (ADCs)[1][2].
Bigelovin, a sesquiterpene lactone isolated from Inula helianthus-aquatica, is a selective retinoid X receptor α agonist. Bigelovin suppresses tumor growth through inducing apoptosis and autophagy via the inhibition of mTOR pathway regulated by ROS generation[1].