EC089 is a linker used in conjugates of tubulysins and folates, and extracted from patent WO2011069116A1[1].
Momordin Ic is a principal saponin constituent of Fructus Kochiae, with with anti-cancer bioactivity. Momordin Ic induces apoptosis through oxidative stress-regulated mitochondrial dysfunction[1][2].
Sodium Channel inhibitor1, one of 3-Oxoisoindoline-1-carboxamides, is a novel and selective voltage-gated sodium channel for pain treatment. IC50 Value: 0.16 uM ( Na v1.7, V hold-90mV); 0.41 uM (Na v1.7, V hold-90mV) [1]Target: Na v1.7Sodium Channel inhibitor1 demonstrated concentration-dependent efficacy in preclinical behavioral pain models.
FA-Phe-Phe is a furylacryloyl (fa)-amino acid derivative, targeting to Angiotensin-converting Enzyme (ACE). FA-Phe-Phe is also a specific substrate of Cathepsin A[1][2].
DPP-4 inhibitor 1 (compound 5) is a potent and long acting Dipeptidyl peptidase-4 (DPP-4) inhibitor for t treatment of T2DM, with a KD of 0.177 nM[1].
Fluensulfone is a new nematicide for chemical control of plant parasitic nematodes.
Fipsomin is a natural product that can be isolated from the fruits of F. nipponica[1].
CHM-1, a microtubule-destabilizing agent, inhibits tubulin polymerization. CHM-1 is a potent and selective antimitotic antitumor activity against human hepatocellular carcinoma. CHM-1 induces growth inhibition and apoptosis via G2-M phase arrest in human hepatocellular carcinoma cells by activation of Cdc2 kinase activity[1][2][3].
Peptide C105Y, a synthetic and cell-penetrating peptide based on the amino acid sequence corresponding to residues 359-374 of α1-antitrypsin, enhances gene expression from DNA nanoparticles[1].
(R)-(−)-N-Benzyl-2-phenylglycinol is a Glycine (HY-Y0966) derivative[1].
Withasomniferolide B is a withanolide. Withasomniferolide B can be isolated from a GABAA receptor positive activator methanol extract of the roots of Withania somnifera[1].
Methisazone (Marboran) is an antiviral agent that works by inhibiting mRNA and protein synthesis. Methisazone is also a SARS-CoV-2 (COVID-19) inhibitor. Methisazone is mainly used in pox viruses[1].
Elinogrel (PRT060128) is a potent, direct acting, competitive, and reversible platelet P2Y12 antagonist (IC50=20 nM). It is orally and intravenously available and has potent antiplatelet effects[1].
MAX-40279 hemiadipate is a dual and potent inhibitor of FLT3 kinase and FGFR kinase. MAX-40279 hemiadipate has the potential for the research of acute myelogenous leukemia (AML) (extracted from patent WO2021180032)[1].
Erlotinib-13C6 (hydrochloride) is the 13C labeled Erlotinib Hydrochloride[1]. Erlotinib Hydrochloride (CP-358774 Hydrochloride) inhibits purified EGFR kinase with an IC50 of 2 nM[2].
Cephalotin (Cephalotin) is a beta-lactam antibiotic, inhibits class C β-lactamase AmpC, with an Ki of 0.32 µM[1].
(D-Trp8,D-Cys14)-Somatostatin-14 is a Somatostatin synthetic analogue. (D-Trp8,D-Cys14)-Somatostatin-14 can be used for the research of metabolic related diseases[1][2].
SR-18292 is a PPAR gamma coactivator-1α (PGC-1α) inhibitor, which increases PGC-1α acetylation, suppresses gluconeogenic gene expression and reduces glucose production in hepatocytes.
Iophendylate (Pantopaque) is a highly lipophilic substance, and can be used as a contrast medium. Iophendylate is mainly for brain and spinal cord visualization[1][2].
Deoxycytidine triphosphate-d14 (dCTP-d14 dilithium; 2′-Deoxycytidine-5′-triphosphate-d14) dilithium is deuterium labeled Deoxycytidine triphosphate (HY-101400). Deoxycytidine triphosphate (dCTP) is a nucleoside triphosphate that can be used for DNA synthesis. Deoxycytidine triphosphate has many applications, such as real-time PCR, cDNA synthesis, and DNA sequencing.
N-Nitroso-N-methyl-4-aminobutyric acid-d3 is the deuterium labeled N-Nitroso-N-methyl-4-aminobutyric acid[1].
Valtropine is an alkaloid. Valtropine can be isolated from the leaves of Duboisia myoporoides[1].
GNE0877 is a highly potent, selective, and brain-penetrant aminopyrazole leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitor with an IC50 of 3 nM.IC50 value: 3 nM [1]Target: LRRK2Invitrogen kinase-selectivity profiling(188 kinases) of aminopyrazole GNE0877 at 0.1 μM (145-fold overLRRK2 Ki) resulted in only four kinases showing greater than 50% inhibition (Aurora B = 51%, RSK2 = 52%, RSK4 = 62%, and RSK3 = 68%) and suggested that GNE0877 is a highly selective LRRK2 inhibitor. Furthermore, GNE0877 possessed a 212-fold biochemical-selectivity index over TTK (Ki= 150 nM), which was previously highlighted as an off-target kinase of concern because of the suggested role of TTK in themaintenance of chromosomal stability. The in vivo rat clearance for inhibitor GNE0877 was within 2-fold of measured in vitro stability, and good oral bioavailability (88%) was achieved at 50 mg/kg following administration of a methylcellulose/tween (MCT) suspension.
Dostarlimab (TSR-042) is a humanized anti-PD-1 monoclonal antibody. Dostarlimab binds with high affinity to human PD-1 and competitively inhibits its interaction with its ligands, PD-L1 and PD-L2, with IC50s of 1.8 and 1.5 nM, respectively[1].
Cyclopentenyl uracil, a non-cytotoxic inhibitor of uridine kinase, effectively blocks the salvage of circulating uridine by host and tumor tissues in the intact mouse[1].
UMI-77 is a selective Mcl-1 inhibitor, which shows high binding affinity to Mcl-1 (IC50=0.31 μM). UMI-77 binds to the BH3 binding groove of Mcl-1 with Ki of 490 nM, showing selectivity over other members of anti-apoptotic Bcl-2 members.
Irinotecan is a water soluble topoisomerase I inhibitor, preventing religation of the DNA strand by binding to topoisomerase I-DNA complex.
Nosiheptide (Multhiomycin), a thiopeptide antibiotic produced by Streptomyces actuosus, inhibits bacterial protein synthesis and bears a unique indole side ring system and regiospecific hydroxyl groups on the characteristic macrocyclic core. Nosiheptide has been widely used as a feed additive for animal growth[1][2].
Plevitrexed (ZD 9331; BGC 9331) is an orally active and potent thymidylate synthase (TS) inhibitor with a Ki of 0.44 nM. Plevitrexed is taken up via the α-folate receptor as well as the reduced folate carrier. Plevitrexed is used for gastric cancer in clinical[1][2][3].
Decursinol angelate, a cytotoxic and protein kinase C (PKC) activating agent from the root of Angelica gigas, possesses anti-tumor and anti-inflammatory activities[1][2].