(R)-(-)-Gossypol acetic acid (AT-101 (acetic acid)) is the levorotatory isomer of a natural product Gossypol. AT-101 is determined to bind to Bcl-2, Mcl-1 and Bcl-xL proteins with Kis of 260±30 nM, 170±10 nM, and 480±40 nM, respectively.
Thalidomide-NH-PEG3-COOH is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology[1].
Lorpucitinib is a Gut-Restricted JAK Inhibitor for the research of Inflammatory Bowel Disease[1].
Ocotillone ((24S)-20,24-Epoxy-25-hydroxydammaran-3-one) is a triterpenoids that can be isolated from the fruits of Dysoxylum richii. Ocotillone has antibacterial activities against P. aeruginosa and S. typhimurium without hemolytic activity[1].
Gardenin B is a flavonoid isolated from Baccharis scandens. Gardenin B induces cell death in human leukemia cells involves multiple caspases[1].
20-(tert-Butoxy)-20-oxoicosanoic acid is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). 20-(tert-Butoxy)-20-oxoicosanoic acid is also a alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs
Metronidazole-d4 hydrochloride is the deuterium labeled Metronidazole hydrochloride[1].
MK-571 sodium salt is a selective, orally active leukotriene D4 receptor antagonist, with Kis of 0.22 and 2.1 nM in guinea pig and human lung membranes.
COG 133 is a fragment of Apolipoprotein E (APOE) peptide. COG 133 competes with the ApoE holoprotein for binding the LDL receptor, with potent anti-inflammatory and neuroprotective effects. COG 133 is also a nAChR antagonist with an IC50 of 445 nM[1][2].
Akt1/Akt2-IN-2 (compound 7) is an allosteric dual Akt1 and Akt2 inhibitor (IC50=138 nM and 212 nM, respectively). Akt1/Akt2-IN-2 increases activity of caspase-3, and inhibits viability of a number of tumor cells[1].
Hesperidin (HP) is a bioflavonoid that plays a role in plant defense and is abundant in citrus species, such as grapefruit, lemon and orange. Hesperidin is used effectively as a supplemental agent in complementary therapy protocols, since it possesses biological and pharmacological properties as an effective antioxidant, anti-inflammatory, anti-carcinogenic, and anti-hypertensive agent with lipid-lowering activity[1]IC50: hesperidin (IC50=116.68μmo/L))[4]in vitro: hesperidin and linarin are two of the main constituent of Valeriana's extract exhibiting a high affinity to KATP channel, which are related to the control of Ca++ concentration and release of GABA in synaptic nerve terminal, mainly on cells of SN[2]in vivo: Hesperidin was dissolved in 1% carboxymethyl cellulose (CMC) and administered orally at a dose of 50 mg/kg for 10 consecutive days. In the control group, rats were treated with the corn oil and 1% CMC vehicle.[1]
Anti-inflammatory agent 51 (compound 11d) is an amide/sulfonamide derivative with anti-inflammatory activities. Anti-inflammatory agent 51 inhibits NF-κB activation, has the potential for acute lung injury and ulcerative colitis research[1].
Tabituximab (OTSA101) is a humanized monoclonal antibody against frizzled class receptor 10 (FZD10)[1].
PROTAC Linker 34 is a PROTAC linker, which refers to the alkyl/ether composition. PROTAC Linker 34 can be used in the synthesis of a series of PROTACs. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins[1].
DMTr-LNA-5MeU-3-CED-phosphoramidite is a nucleoside derivative[1].
2-Aminoimidazole is a potent antibiofilm agent that can be used as an adjuvant to antimicrobial. 2-aminoimidazoles disrupts the ability of bacteria to protect themselves by inhibiting biofilm formation and genetically-encoded antibiotic resistance traits. 2-Aminoimidazole is also a weak noncompetitive inhibitor of human arginase I with a Ki of 3.6 mM[1][2][3].
Ibritumomab tiuxetan is an immunoconjugate composed of the murine IgG1κ anti-CD20 monoclonal antibody Ibritumomab that is covalently bound to the chelator Tiuxetan that permits the addition of the short-lived β-emitter radioisotope yttrium-90. Ibritumomab tiuxetan can be used for the research of non-Hodgkin's B-cell lymphomas[1][2].
GSK143 is an orally active and highly selective spleen tyrosine kinase (SYK) inhibitor with a pIC50 of 7.5. GSK143 inhibits phosphorylated Erk (pErk: pIC50=7.1)[1]. GSK143 reduces inflammation and prevents recruitment of immune cells in the intestinal muscularis in mice[2][3].
L-Glutamic acid-d3 is the deuterium labeled L-Glutamic acid. L-Glutamic acid acts as an excitatory transmitter and an agonist at all subtypes of glutamate receptors (metabotropic, kainate, NMDA, and AMPA). L-Glutamic acid shows a direct activating effect on the release of DA from dopaminergic terminals.
Velagliflozin proline is an oral sodium-glucose cotransporter 2 (SGLT2) inhibitor with antidiabetic activity. Velagliflozin proline reduces renal glucose reabsorption and stimulates glycosuria, which lowers blood sugar and insulin concentrations[1].
Methyl 3,4,5-trimethoxybenzoate can be synthesized from Gallic acid. Methyl 3,4,5-trimethoxybenzoate is mainly used in the production of Trimethoprim (TMP), Sulfa synergistic intermediates, and many other agents.
GSK-114 is a highly selective, orally active TNNI3K inhibitor (IC50= 25 nM). GSK-114 shows a 40-fold selectivity for TNNI3K over B-Raf kinase (IC50= 1 µM). Cardiac troponin I-interacting kinase (TNNI3K or CARK) is a member of the tyrosine-like kinase family that is selectively expressed in heart tissue[1].
Ancymidol is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
Cobitolimod sodium is a DNA oligonucleotide agonist of TLR-9 with anti-inflammatory activity. Cobitolimod sodium inhibits Th17 cells and induces anti-inflammatory FoxP3 and IL-10 expression, inhibiting the IL-17 signaling pathway[1].
(S)-Enzaplatovir ((S)-BTA-C585) is the S-enantiomer of Enzaplatovir. (S)-Enzaplatovir shows antiviral activities with an EC50 of 56 nM for respiratory syncytial viral (RSV) (patent WO2011094823A1 compound 77)[1].
4'-O-Methylpyridoxine, a natural compound, possesses antioxidant activity[1].
Glycine ethyl ester-13C (hydrochloride) is a 13C-labeled Mebendazole.
Tin-protoporphyrin IX (SnPPIX) is a potent Heme oxygenase-1 (HO-1) inhibitor. Tin-protoporphyrin IX (SnPPIX) sensitizes pancreatic ductal adenocarcinoma (PDAC) tumors to chemotherapy in mice model[1].
Pertuzumab (PBS), a humanized monoclonal antibody, is a HER2 dimerization inhibitor for the treatment of metastatic HER2-positive breast cancer.
BIO5192 is a selective and potent integrin α4β1 (VLA-4) inhibitor (Kd<10 pM). BIO5192 selectively binds to α4β1 (IC50=1.8 μM) over a range of other integrins. BIO5192 results in a 30-fold increase in mobilization of murine hematopoietic stem and progenitors (HSPCs) over basal levels[1][2].