Isovaleramide is an active principle on central nervous system from Valeriana pavonii, as an anticonvulsant.Target：in vitro: Isovaleramide (300 μM) exhibits a 42% of inhibition of the binding of 3H-FNZ to its sites.in vivo: Isovaleramide at 100 mg/Kg, p.o, evidences a 90% index protection against the maximal electroshock seizure in mice (MES).
EPZ020411 is a potent and selective inhibitor of PRMT6 with IC50 of 10 nM, has ＞10 fold selectivity for PRMT6 over PRMT1 and PRMT8.IC50 value: 10 nMTarget: PRMT6in vitro: EPZ020411 inhibits methylation of PRMT6 substrates in cells. EPZ020411 does-dependently inhibits H3R2 methylation in PRMT6-overexpressing cells.in vivo: EPZ020411 shows good bioavailability following subcutaneous (SC) dosing in rats making it a suitable tool for in vivo studies.
A potent and specific BET bromodomain inhibitor with Ki of 3.2-24.7 nM for BD1 and BD2 domains of BRD2, BRD3, and BRD4; shows an excellent selectivity over other non-BET bromodomain-containing proteins with the exception of CREBBP (Kd=670 nM); potently and selectively inhibits cell growth in human acute leukemia cell lines harboring the rearranged MLL1 gene (IC50=20 nM for MV4;11 cells).
Ergtoxin-1 is a potassium channel blocker.Ergtoxin-1 is isolated from the venom of the Mexican scorpionCentruroides noxius. Ergtoxin 1 can blockERG-K+ channels in nerve, heart and endocrine cells[1].
Biotin-bis-amido-SS-NHS is an Alkyl/ether-based PROTAC linker can be used in the synthesis of PROTACs.
JS25 is a potent, selective, covalent TEC family of non-receptor tyrosine kinases (BTK, ITK, TXK and BMX) inhibitor with IC50 of 3.5 and 5.8 nM for BMX and BTK, respectively.JS25 displays a strong binding affinity against all the members of TEC family, covalently inhibits BMX at Cys496. JS25 demonstrates intracellular target engagement in HEK293 cells (IC50=44.8 nM), 10 times greater than BMX-IN-1.JS25 inhibits androgen-receptor positive prostate-cancer cells with GI50 of 6.6 uM.JS25 shows synergistic anti-proliferative activity in LNCaP cells in combination with AKT1/2 (AKT inhibitor), Flutamide (androgen receptor antagonist) and LY293002 (PI3K inhibitor).
RORγt agonist 3 is a potent agonist of RORγt. RORγt agonist 3 promotes the differentiation of Th17 cells and enhances the levels of pro-inflammatory cytokines, thereby increasing the cytotoxicity of lymphocytes. RORγt agonist 3 inhibits the production of regulatory T cells, which suppresses the immune response (extracted from patent WO2021136326A1, compound 23)[1].
Vin-F03 is a potent pancreatic β-cells protective agent with an EC50 of 0.27 µM. Vin-F03 effectively promotes β-cell survival and protects β-cells from STZ-induced apoptosis. Vin-F03 can be used for type 2 diabetes mellitus research[1].
Bay 65-1942 hydrochloride is an ATP-competitive and selective IKKβ inhibitor.
Ms-PEG3-CH2CH2COOH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
β-Casomorphin (1-6), bovine is a opioid-like bioactive peptide of β-Casomorphin.
RO5203648 is a potent and highly selective partial agonist of TAAR1 (Trace amine-associated receptor 1) with high affinity. RO5203648 demonstrates a novel paradigm for neuropsychiatric therapeutics[1].
Pangelin is a coumarin that can be found in Ducrosia anethifolia. Pangelin exhibits anti-mycobacterial and anti-tumor activities[1][2].
HAEGTFTSDVS is the first N-terminal 1-11 residues of GLP-1 peptide.
BIMU 8 is a potent and selective 5-HT4 agonist with EC50s of 18 nM, 77 nM, and 540 nM for wild type 5HT4 receptor, T3.36A, and W6.48A mutant 5-HT4 receptors[1][2].
Zinpentraxin alfa (PRM-151) is a recombinant human pentraxin-2, also known as serum amyloid hSAP, a highly conserved serum protein and soluble pattern recognition receptor (PRR) of the innate immune system that regulates monocyte activation and differentiation. Zinpentraxin alfa inhibits the differentiation of circulating monocytes into fibroblasts and pro-fibroblastic macrophages and suppresses myofibroblast production[1].
Azido-PEG6-NHS ester is a cleavable 6 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1]. Azido-PEG6-NHS ester is also a PEG- and Alkyl/ether based PROTAC linker that can be used in the synthesis of PROTACs[2].
Galanin (1-30), human is a 30-amino acid neuropeptide, and acts as an agonist of GalR1 and GalR2 receptors, with Kis of both 1 nM.
Retrocyclin-101 is an antimicrobial peptide against of bacterial and viral[1].
4-Methylsyringol is a natural product that can be isolated from hardwood[1].
m-PEG24-alcohol is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Trelagliptin(SYR-472) is a long acting dipeptidyl peptidase-4 (DPP-4) inhibitor that is being developed for the treatment of type 2 diabetes (T2D). IC50 value:Target: DPP4Two Phase II clinical studies have been completed with Efficacy and Safety of SYR-472 in Subjects With Type 2 Diabetes Mellitus. Phase III clinical studies with trelagliptin in Japan to evaluate its safety and efficacy in a once-weekly oral treatment regimen. Currently, all available DPP-4 inhibitors are dosed once-daily. A once-weekly treatment, such as trelagliptin, would provide patients with a convenient treatment alternative and has the potential to improve treatment compliance.
Captopril-d3 is deuterium labeled Captopril. Captopril (SQ 14225), antihypertensive agent, is a thiol-containing competitive, orally active angiotensin-converting enzyme (ACE) inhibitor (IC50=0.025 μM) and has been widely used for research of hypertension and congestive heart failure. Captopril is also a New Delhi metallo-β-lactamase-1 (NDM-1) inhibitor with an IC50 of 7.9 μM[1][2][3].
RUNX-IN-1 (Compound Conjugate 1) covalently binds to the RUNX-binding sequences, and inhibits the binding of RUNX proteins to their target sites. RUNX-IN-1 induces the p53-dependent apoptosis and inhibits cancer cell growth. RUNX-IN-1 inhibits tumor growth in PANC-1 xenograft mice[1].
BRD4 degrader AT1 is a highly selective Brd4 degrader based on PROTAC technology, with a Kd of 44 nM for Brd4BD2 in cells.
LY191704, as a benzoquinolinone, is a potent, nonsteroidal, noncompetitive and selective human type I 5α-reductase inhibitor. LY191704 is a racemic mixture of the compounds LY300502 and LY300503. LY191704 may be useful in the research of human endocrine disorders associated with overproduction of dihydrotestosterone (DHT) by 5α-reductase type 1[1][2].
Paucinervin A (Compound 1) is a type of bittern.Paucinervin A inhibits the growth of HeLa cells (IC50=29.5μM). Paucinervin A is isolated from the natural Garcinia paucinervis [1].
2,2-Dimethylbutanoic acid-d11 is the deuterium labeled 2,2-Dimethylbutanoic acid[1].
Geniposide is an iridoid glucoside extracted from Gardenia jasminoides Ellis fruits; exhibits a varity of biological activities such as anti-diabetic, antioxidative, antiproliferative and neuroprotective activities.
Nav1.7-IN-8 is a potent blockage of NaV1.7 with high selectivity for the inhibition of NaV1.7 over the subtypes hNaV1.1 and hNaV1.5. Nav1.7-IN-8 inhibits CYP2C9 and CYP3A4 with an IC50 of 0.17 μM and 0.077 μM, respectively. Nav1.7-IN-8 displays significant analgesic effects in rodent models of acute and inflammatory pain[1].