E3 ligase Ligand-Linker Conjugates 30 incorporates a cereblon (CRBN) ligand for the E3 ubiquitin ligase, and a PROTAC linker. E3 ligase Ligand-Linker Conjugates 30 can be used to design PROTAC MDM2 degrader[1].
CC260 is a selective PI5P4Kα and PI5P4Kβ inhibitor with Kis of 40 nM and 30 nM, respectively. CC260 does not inhibit or weakly inhibits other protein kinases, such as Plk1 and RSK2. CC260 can be used for cell energy metabolism, diabetes and cancer research[1].
Visilizumab (Anti-Human CD3E Recombinant Antibody) is a humanized low-Fc receptor binding anti-CD3 monoclonal IgG2 antibody. Visilizumab can be used for ulcerative colitis and Crohn's disease research[1].
Chloride Ionophore IV is a thiourea type hydrogen bonding-based receptor. Chloride Ionophore IV is a chloride ionophore[1][2].
1,3-Dimethoxybenzene-d4 is the deuterium labeled 1,3-Dimethoxybenzene[1]. 1,3-Dimethoxybenzene belongs to the class of organic compounds known as dimethoxybenzenes. 1,3-Dimethoxybenzene is an intermediate in synthesis of organic compounds[2].
22-(tert-Butoxy)-22-oxodocosanoic acid is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). 22-(tert-Butoxy)-22-oxodocosanoic acid is also a alkyl chain-based PROTAC linker that can be used in t
Argatroban monohydrate is a direct, selective thrombin inhibitor.Target: ThrombinArgatroban may have a complementary effect for preventing thrombus formation without aggravating bleeding tendency because of its monotarget specificity to thrombin. Administration (0.5 to 2 micrograms/kg/min) of argatroban is a safe anticoagulant for left heart bypass in repairs of traumatic aortic rupture associated with multiple organ injuries [1]. Argatroban, as compared with heparin, appears to enhance reperfusion with TPA in patients with AMI, particularly in those patients with delayed presentation. The incidences of major bleeding and adverse clinical outcome were lower in the patients receiving argatroban [2].
Baminercept (BG 9924) is a lymphotoxin β receptor IgG fusion protein (LTβR-Ig). Baminercept can be used for the research of many autoimmune diseases including primary Sjögren's syndrome (SS) and rheumatoid arthritis (RA) [1][2].
VS 8 (Compound VS 8) is a potent, orally active VEGFR-2 inhibitor with significant anti-angiogenic effects. VS 8 induces cancer cell apoptosis and migration. VS 8 is active against CSCs (Cancer stem cells)[1].
Koenimbine is an anticancer agent that can be obtained from the leaves and fruits of Murraya koenigii. Koenimbine can induce apoptosis and necrosis in HT-29 and SW48 cells. Koenimbine can be used in the research of cancer[1].
Pyridine-d5 is the deuterium labeled Pyridine[1].
GNE-900 is a an ATP-competitive, selective, and orally active ChK1 inhibitor with IC50s of 0.0011, 1.5 µM for ChKl, ChK2, respectively. GNE-900 abrogates the G2-M checkpoint, enhances DNA damage, and induces Apoptosis. gemcitabine (HY-17026) and GNE-900 administration shows anti-tumor activity[1].
Galanin Receptor Ligand M35 is a high-affinity galanin receptor ligand acting as a galanin receptor antagonist in the rat spinal cord, rat hippocampus and isolated mouse pancreatic islets. Galanin Receptor Ligand M35 exerts a Ki values of 0.11 and 2.0 nM for human GalR1 and GalR2, respectively[1][2].
m-3M3FBS is a potent phospholipase C (PLC) activator. m-3M3FBS stimulates superoxide generation in human neutrophils, upregulates intracellular calcium concentration, and stimulates inositol phosphate generation in various cell lines. m-3M3FBS induces monocytic leukemia cell apoptosis[1][2][3].
Zerlasiran is an apolipoprotein A (ApoA) synthesis reducer[1].
((2,3,5,6-Tetramethylphenyl)sulfonyl)glycine is a Glycine (HY-Y0966) derivative[1].
20(R)-Ginsenoside Rh2, a matrix metalloproteinase (MMP) inhibitor, acts as a cell antiproliferator. It has anticancer effects via blocking cell proliferation and causing G1 phase arrest. 20(R)-Ginsenoside Rh2 induces apoptosis, and has anti-inflammatory and antioxidative activity[1][2][3].
SMND-309 is a novel derivative of salvianolic acid B, and has shown protective effects against rat cortical neuron damage in vitro and in vivo. IC50 value:Target: SMND-309 mitigated the effects of ischemia and reperfusion injury on brain by decreasing the infract volume, improving neurological function, increasing the survival of neurons and promoting angiogenesis by increasing the levels of erythropoietin (EPO), erythropoietin receptor (EPOR), phosphorylated JAK2 (P-JAK2), phosphorylated STAT3 (P-STAT3), VEGF and VEGF receptor 2 (Flk-1) in the brain.
5,7,4'-Trihydroxy-8-Methylflavanone (Compound 2) is a flavanone isolated from Qualea grandiflora[1].
(RS)-AMPA ((±)-AMPA) monohydrate is a glutamate analogue and a potent and selective excitatory neurotransmitter L-glutamic acid agonist. (RS)-AMPA monohydrate does not interfere with binding sites for kainic acid or NMDA receptors[1][2].
Giredestrant (GDC-9545), a non-steroidal ER ligand, is an orally active and selective estrogen receptor (ER) antagonist. Giredestrant potently competes with estradiol for binding and induces a conformational change within the ER ligand binding domain. Giredestrant has anti-tumor activity[1].
(+)-Camphor is an ingredient in cooking, and as an embalming fluid for medicinal purposes,
PROTAC ER Degrader-3 is an intermediate for synthesis of PAC. PAC comprises an antibody conjugated via a linker to a PROTAC. PAC extracts from patent WO2017201449A1, compound LP2. PAC is a more marked estrogen receptor-alpha (ERα) degrader compared to PROTAC (without Ab).
Pranlukast-d5 (ONO-1078-d5) is the deuterium labeled Pranlukast. Pranlukast is a highly potent, selective and competitive antagonist of peptide leukotrienes. Pranlukast inhibits [3H]LTE4, [3H]LTD4, and [3H]LTC4 bindings to lung membranes with Kis of 0.63, 0.99, and 5640 nM, respectively.
Micafungin (Mycamine; FK463) is an echinocandin antifungal drug which can inhibit 1,3-beta-D-glucan synthase.
IQ 1 has many functions such as decreasing Wnt-stimulated phosphorylation, maintaining the pluripotency of murine ESCs, preventing PP2A/Nkd interaction and so on.IQ 1 maintains the pluripotency of murine ESCs in long-term culture in a Wnt-dependent manner. IQ 1 decreased Wnt-stimulated phosphorylation of p300 at Ser-89.IQ-1 binds to serine/threonine phosphatase PP2A and prevents PP2A/Nkd interaction.The binding of IQ 1 to PR72/130 leads to decreased phosphorylation of the coactivator protein p300 at Ser-89. IQ 1 thereby diminishes the β-catenin/p300 interaction and prevents β-catenin coactivator switching from CBP to p300.
RXP470.1 (RXP-470) is a potent, selective MMP-12 inhibitor with a Ki of 0.2 nM against human MMP-12. RXP470.1 is 2 to 4 orders of magnitude less potent against other MMPs. RXP470.1 significantly reduces atherosclerotic plaque cross-sectional area in mouse. RXP470.1 results in less complex plaques with increased smooth muscle cell:macrophage ratio, less macrophage apoptosis, increased cap thickness, smaller necrotic cores, and decreased incidence of calcification[1].
Nicaraven is a novel chemically synthesized hydroxyl radical-specific scavenger.
ML264 is an antitumor agent that potently and selectively inhibits Krüppel-like factor five (KLF5) expression.
BMS-470539 dihydrochloride is a highly potent and selective melanocortin-1 receptor (MC-1R) agonist with an IC50 of 120 nM, an EC50 of 28 nM. BMS-470539 dihydrochloride does not activate MC-3R and is a very weak partial agonist at MC-4R and MC-5R. BMS-470539 dihydrochloride has potently anti-inflammatory properties[1][2][3].