Pramipexole-d7-1 (dihydrochloride) is the deuterium labeled Pramipexole dihydrochloride[1]. Pramipexole dihydrochloride is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole dihydrochloride can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS)[2][3][4].
BRD4-BD1/2-IN-2 is a potent BRD4 BD2 inhibitor with IC50s of <0.5 nM and <300 nM for BRD4 BD2 and BRD4 BD1, respectively (WO2021233371A1, compound 2)[1].
SB 243213 dihydrochloride is an orally active, selective and high-affinity 5-hydroxytryptamine (5-HT)2C receptor antagonist with a pKi of 9.37 and a pKb of 9.8 for human 5-HT2C receptor. SB 243213 dihydrochloride has improved anxiolytic profile and has the potential for schizophrenia and motor disorders[1].
Nrf2 activator-1 is a potent activator of NF-E2 related factor 2 (Nrf2). Nrf2 activator-1 has the potential for the treatment of COPD and other respiratory diseases, including asthma, Acute Lung Injury (ALI), Acute Respiratory Distress Syndrome (ARDS) and pulmonary fibrosis (extracted from patent WO2018109647A1)[1].
GS-9822 is a potent, non-catalytic site HIV integrase inhibitor with wild type EC50 of 3 nM.
BDP FL-PEG4-amine is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Dansyl-Glu-Gly-Arg-Chloromethylketone is a protease inhibitor, and inhibits serine/threonine proteases. Dansyl-Glu-Gly-Arg-Chloromethylketone inhibits activated porcine factor IX[1].
C18 Glucosyl(ß) ceramide-d5 is deuterium labeled C18 Glucosyl(ß) ceramide.
Vitamin D2 (Ergocalciferol) is a form of vitamin D, used as a vitamin D supplement. Target: Ergocalciferol is a secosteroid formed by a photochemical bond breaking of a steroid, specifically, by the action of ultraviolet light on ergosterol.
Ferbam (Iron(III) dimethyldithiocarbamate) is a potent fungicide[1].
TLR7 agonist 4 (Compound 1.2) is a TLR7 agonist with an EC50 of 4.3 nM[1].
6-(γ,γ-Dimethylallylamino)purine is a plant growth substance.
Bindarit(AF-2838), a CCL2, CCL7 and CCL8 inhibitor, is an anti-inflammatory agent.Target: OthersBindarit exhibits selective inhibition against monocyte chemotactic proteins MCP-1/CCL2, MCP-3/CCL7 and MCP-2/CCL8. Oral administration of Bindarit at 50 mg/kg in NZB/W mice delays the onset of proteinuria, significantly protects from renal function impairment, and prolongs survival of NZB/W mice or lupus mice. Bindarit treatment completely MCP-1 up-regulation during the progression of nephritis [1]. Inhibition of MCP-1 with Bindarit also reduces tumor growth and macrophage recruitment, rendering necrotic tumor masses in human melanoma xenografts [2]. Bindarit is effective in reducing neointima formation in both non-hyperlipidaemic and hyperlipidaemic animal models of vascular injury by a direct effect on VSMC proliferation and migration and by reducing neointimal macrophage content [3]. Administration of Bindarit results in impaired metastatic disease in prostate cancer PC-3M-Luc2 xenograft mice and impairment of local tumorigenesis in Balb/c mice with murine breast cancer 4T1-Luc cells. In addition, Bindarit treatment significantly decreases the infiltration of tumor-associated macrophages and myeloid-derived suppressor cells in 4T1-Luc primary tumors [4].
8-Epixanthatin is a potential colchicine binding site inhibitor isolated from Xanthium chinese Mill. 8-Epixanthatin can inhibit the activation of STAT3, induce apoptosis, and has anti-tumor activity[1].
SPDB-DM4 is a drug-linker conjugate for ADC by using the maytansinebased payload (DM4) via a SPDB linker, exhibiting potent anti-tumor activity.
Boc-L-Ala-OH-d3 is the deuterium labeled Boc-L-Ala-OH[1].
19:0 Lyso PG-d5 is deuterium labeled 19:0 Lyso PG.
cGAMP(Cyclic GMP-AMP) is an endogenous second messenger in metazoans and triggers interferon production in response to cytosolic DNA; STING ligand.Target:in vitro: cGAMP induced IFNβ RNA robustly even at concentrations as low as 10 nM. cGAMP was much more potent than c-di-GMP in inducing IFNβ based on ELISA assays. cGAMP was also more potent than c-di-GMP and c-di-AMP in activating IRF3. cGAMP binds to and activates STING to trigger the downstream signaling cascades [1]. On stimulation with cGAMP, fibroblasts from the patients showed increased transcription of IFNB1 but not of the genes encoding interleukin-1 (IL1), interleukin-6 (IL6), or tumor necrosis factor (TNF) [3]. cGAMP activates the endoplasmic reticulum (ER)-resident receptor STING, thereby inducing an antiviral state and the secretion of type I IFNs [4].in vivo: cGAMP can enhance the adaptive immune response to the model antigen ovalbumin in mice. cGAMP promotes antigen specific IgG and a balanced Th1/Th2 lymphocyte response in immunized mice [2].
Thymidine-13C5,15N is the 13C and 15N labeled Thymidine. Thymidine, a specific precursor of deoxyribonucleic acid, is used as a cell synchronizing agent. Thymidine is a DNA synthesis inhibitor that can arrest cell at G1/S boundary, prior to DNA replicatio
DNMDP is a potent and selective cancer cell cytotoxic agent that binds to PDE3A, promotes an interaction between PDE3A and Schlafen 12 (SLFN12); coexpression of SLFN12 with PDE3A correlates with DNMDP sensitivity, whereas depletion of SLFN12 results in decreased DNMDP sensitivity.
Halofantrine hydrochloride (SKF-102886) is a blocker of delayed rectifier potassium current via the inhibition of human-ether-a-go-go-related gene (HERG) channel and a potent antimalarial compound[1][2].
Azido-PEG4-NHS-ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Danicopan, a selective and orally active small-molecule factor D inhibitor, inhibits alternative pathway of complement (APC) activity. Danicopan has potential to block the alternative pathway of complement in paroxysmal nocturnal hemoglobinuria (PNH) and atypical hemolytic uremic syndrome (aHUS)[1].
Medetomidine(Domtor) is a potent, highly selective α2-adrenoceptor agonist (Ki values are 1.08 and 1750 nM for α2- and α1-adrenoceptors respectively). IC50 value:Target: α2-adrenoceptorMedetomidine displays greater selectivity over α1-adrenoceptors than clonidine and UK 14,304 (1620-, 220- and 300-fold respectively). Medetomidine inhibits twitch response in electrically stimulated mouse vas deferens (pD2 = 9.0). Active in vivo; displays hypotensive, bradycardic, sedative, anxiolytic, hypothermic and analgesic effects.
H-Glu-OtBu.HCl is a glutamic acid derivative[1].
1-Oleoyl-2-acetyl-sn glycerol is a synthetic, cell permeable diacylglycerol analog. 1-Oleoyl-2-acetyl-sn glycerol activates calcium-dependent protein kinase C (PKC) and induces the superoxide-production.
6′-Hydroxyjusticidin C is a lignan, that can be isolated from Justicia procumbens[1].
Mifamurtide sodium (MTP-PE sodium), an analog of the muramyl dipeptide (MDP), is a nonspecific immunomodulator by stimulating the immune response activating macrophages and monocytes. Mifamurtide sodium, an orphan drug, is a specific ligand of NOD2 used as an insulin sensitizer. Mifamurtide sodium has the potential for osteosarcoma research[1][2][3].
Ethoxysanguinarine is a benzophenanthridine alkaloid natural product that is mainly found in Macleaya cordata. Ethoxysanguinarine inhibits viability and induces apoptosis of colorectal cancer cells by inhibiting protein phosphatase 2A (CIP2A)[1].