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Atazanavir is a novel and potent azapeptide protease inhibitor that specifically inhibits the human immunodeficiency virus type 1 (HIV-1) protease enzyme with inhibition constant Ki of 66 nmol/L and also inhibits the viral replication of HIV-1 with 50% effective concentration EC50 ranging from 2.6 to 5.3 nmol/L. Atazanavir binds to HIV-1 protease preventing the cleavage of gag and gag-pol polyproteins, which results in the formation of immature virions in HIV-1-infected cells. Atazanavir has a different C-2 symmetric chemical structure and a generally greater antiretroviral potency in various HIV strains compared to other protease inhibitors, including indinavir, nelfinavir, ritonavir, saquinavir and amprenavir. Group: Pharmaceutical. CAS No. 198904-31-3. Pack Sizes: 1 g. Product ID: B0084-062263. Molecular formula: Custom synthesis is available. Send your inquiries for more information.
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Dimethyl-l-arginine
Dimethyl-l-arginine is naturally found in blood plasma. It is produced from the continual protein modification processes in the cytoplasm of all human cells. Uses: Enzyme inhibitors. Group: Pharmaceutical. CAS No. 30315-93-6. Pack Sizes: 250 mg. Product ID: B0350-054018. Molecular formula: Custom synthesis is available. Send your inquiries for more information.
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Humantenmine
Humantenmine, isolated from Gelsemium elegans Benth, may inhibit several CYP450 enzyme activities. Group: Pharmaceutical. CAS No. 82354-38-9. Pack Sizes: 10 mg. Product ID: NP0351. Molecular formula: Custom synthesis is available. Send your inquiries for more information.
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Ulinastatin
Ulinastatin is an acid-resistant protease inhibitor derived from human urine, acting as a potent anti-inflammatory agent. It was shown to inhibit the activities of a variety of enzymes, including trypsin, chymotrypsin, thrombin, kallikrein, plasmin, elastase, cathepsin, lipase, hyaluronidase, factors IXa, Xa, XIa, and XlIa, and polymorphonuclear leukocyte elastase. Group: Pharmaceutical. CAS No. 80449-31-6. Pack Sizes: 1 g. Product ID: B2693-135299. Molecular formula: Custom synthesis is available. Send your inquiries for more information.
1-[(5E)-3-O-[(Bis-diisopropylamino)(2-cyanoethoxy)phos-phino]-5,6-dideoxy-6-(diethoxyphosphinyl)-2-O-methyl-β-D-ribo-hex-5-enofuranosyl]uracil, a potent agent for the treatment of human immunodeficiency virus (HIV) infections, functions as a viral replication inhibitor by suppressing the reverse transcriptase enzyme. Its intricate molecular structure reflects the sophisticated nature of modern pharmaceuticals, which require cutting-edge research and development to ultimately undo the feats of viruses and other elusive adversaries. Group: Pharmaceutical. CAS No. 2361324-80-1. Pack Sizes: 100 mg. Product ID: B2706-341886. Molecular formula: Custom synthesis is available. Send your inquiries for more information.
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6-Methylchrysene
6-Methylchrysene, a polycyclic aromatic hydrocarbon, has been postulated as a potential carcinogen and may increase the likelihood of developing lung and skin cancer. Due to its carcinogenic properties, this compound is commonly employed in research to investigate the health risks posed by PAH and examine measures to mitigate such threats. Further studies indicate that catabolism of 6-Methylchrysene by enzymes CYP1A1 and CYP1B1 produces deleterious metabolites, implying that these enzymes could possibly contribute to the development of specific cancers. The intricate relationship between 6-Methylchrysene and cancer has encouraged extensive research to comprehend the mechanisms by which it adversely affects human health. Group: Pharmaceutical. CAS No. 1705-85-7. Pack Sizes: 10 mg. Product ID: B0001-085628. Molecular formula: Custom synthesis is available. Send your inquiries for more information.
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β-pseudoUridine
An isomer of the nucleoside uridine found in all species and in many classes of RNA except mRNA. It is formed by enzymes called synthases, which post-transcriptionally isomerize specific uridine residues in RNA in a process termed pseudouridylation. Studies suggest that Beta-Pseudouridine reduces radiation-induced chromosome aberrations in human lymphocytes. Group: Pharmaceutical. CAS No. 1445-07-4. Pack Sizes: 5 g. Product ID: BBF-04654. Molecular formula: Custom synthesis is available. Send your inquiries for more information.
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Cabazitaxel
Cabazitaxel increases CYP3A enzyme activities in rat hepatocytes. The mean ex-vivo human plasma protein binding of Cabazitaxel is 91.6%. Group: Pharmaceutical. CAS No. 183133-96-2. Pack Sizes: 500 mg. Product ID: B0084-461977. Molecular formula: Custom synthesis is available. Send your inquiries for more information.
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CAY10499
Monoglyceride lipase (MGL) plays an important role in the metabolism of the lipid transmitter 2-arachidonoylglycerol (2-AG). CAY10499 is a potent and selective monoglyceride lipase (MGL) inhibitor exhibiting an IC50 of 90 nM for the recombinant enzyme. It is also a non-selective lipase inhibitor (IC50s = 144, 90, and 14 nM for human recombinant MAGL, HSL, and FAAH, respectively). CAY10499 inhibits the growth of MCF-7, MDA-MB-231, COV318, and OVCAR-3 cancer cells (IC50s = 4.2, 46, 106.7, and 79.8 mM, respectively). Group: Pharmaceutical. CAS No. 359714-55-9. Pack Sizes: 100 mg. Product ID: B1370-292092. Molecular formula: Custom synthesis is available. Send your inquiries for more information.
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CGM097
CGM097 is an orally bioavailable HDM2 (human homolog of double minute 2) antagonist with potential antineoplastic activity. Upon oral administration, p53/HDM2 interaction inhibitor CGM097 inhibits the binding of the HDM2 protein to the transcriptional activation domain of the tumor suppressor protein p53. By preventing this HDM2-p53 interaction, the proteosome-mediated enzymatic degradation of p53 is inhibited, which may result in the restoration of p53 signaling and, thus, the p53-mediated induction of tumor cell apoptosis. HDM2, a zinc finger nuclear phosphoprotein, is a negative regulator of the p53 pathway, often overexpressed in cancer cells and has been implicated in cancer cell proliferation and survival. Group: Pharmaceutical. CAS No. 1313363-54-0. Pack Sizes: 5 mg. Product ID: B0084-462483. Molecular formula: Custom synthesis is available. Send your inquiries for more information.
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CUDA
CUDA is an inhibitor of soluble epoxide hydrolase (sEH) which catalyzes the conversion of EETs to the corresponding dihydroxy eicosatrienoic acids (DiHETrEs; DHETs) thereby diminishing their activity with IC50 values of 11.1 nM and 112 nM for the mouse and human enzymes, respectively. Group: Pharmaceutical. CAS No. 479413-68-8. Pack Sizes: 25 mg. Product ID: B2693-251168. Molecular formula: Custom synthesis is available. Send your inquiries for more information.
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Elacridar
Elacridar hydrochloride (GF120918A) is a P-glycoprotein inhibitor, and has been used both in vitro and in vivo as a tool inhibitor of P-glycoprotein (Pgp) to investigate the role of transporters in the disposition of various test molecules. In vitro, GF120918A demonstrated high plasma protein binding across species, although a definitive protein binding evaluation was precluded by poor recovery, particularly in buffer and in mouse, rat, and dog plasma. GF120918A did not demonstrate potent inhibition of several human cytochrome P450 enzymes evaluated in vitro, with IC(50) values well above concentrations anticipated to be achieved in vivo. Together, these data confirm the utility of GF120918A as a tool P-glycoprotein inhibitor in preclinical species and offer additional guidance on preclinical dose regimens likely to produce P-glycoprotein-mediated effects. Group: Pharmaceutical. CAS No. 143664-11-3. Pack Sizes: 100 mg. Product ID: B0084-311800. Molecular formula: Custom synthesis is available. Send your inquiries for more information.
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Encorafenib
Encorafenib, also known as LGX-818, is an orally available Raf kinase inhibitor with potential antineoplastic activity. LGX818 specifically inhibits Raf kinase, a serine/threonine enzyme in the RAF/mitogen-activated protein kinase kinase (MEK)/extracellular signal-related kinase (ERK) signaling pathway. By inhibiting the activation of the RAF/MEK/ERK signaling pathway, the administration of LGX818 may result in a decrease in proliferation of tumor cells. The Raf mutation BRAF V600E is frequently upregulated in a variety of human tumors and results in the constitutive activation of the RAF/MEK/ERK signaling pathway that regulates cellular proliferation and survival. Group: Pharmaceutical. CAS No. 1269440-17-6. Pack Sizes: 150 mg. Product ID: B0084-462563. Molecular formula: Custom synthesis is available. Send your inquiries for more information.
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Fulacimstat
Fulacimstat is a chymase inhibitor with IC50 of 4 nM and 3 nM for human and hamster chymase enzyme, respectively. Uses: Enzyme inhibitors. Group: Pharmaceutical. CAS No. 1488354-15-9. Pack Sizes: 10 mg. Product ID: B2693-302158. Molecular formula: Custom synthesis is available. Send your inquiries for more information.
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GSK2193874
GSK2193874 is a potent, orally active and specific antagonist of TRPV4 ion channels (IC50 values 2 and 40 nM for rat and human receptors, respectively). GSK2193874 is selective over a panel of ~200 human receptors, channels and enzymes. Group: Pharmaceutical. CAS No. 1336960-13-4. Pack Sizes: 20 mg. Product ID: B0084-007718. Molecular formula: Custom synthesis is available. Send your inquiries for more information.
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Lonafarnib
Lonafarnib is a farnesyl transferase inhibitor. Structurely, it is also a synthetic tricyclic derivative of carboxamide with antineoplastic properties. Lonarfanib binds to and inhibits farnesyl transferase, an enzyme involved in the post-translational modification and activation of Ras proteins. Ras proteins participate in numerous signalling pathways (proliferation, cytoskeletal organization), and play an important role in oncogenesis. Mutated ras proteins have been found in a wide range of human cancers. Uses: Enzyme inhibitors. Group: Pharmaceutical. CAS No. 193275-84-2. Pack Sizes: 25 mg. Product ID: B2693-086642. Molecular formula: Custom synthesis is available. Send your inquiries for more information.
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Loxiglumide
Loxiglumide is an orally active, potent and selective small-molecule antagonist of the cholecystokinin receptor CCKA. It stimulates calorie intake and hunger feelings in humans. It could antagonize the CCK-induced reduction of gastric emptying in rats, accelerate the intestinal transport and accelerate the gallbladder emptying in mice. It inhibits pancreatic secretion of digestive enzymes, and also blocks CCK-induced gastric secretions and emptying. Uses: Loxiglumide stimulates calorie intake and hunger feelings in humans. it inhibits pancreatic secretion of digestive enzymes. Group: Pharmaceutical. CAS No. 107097-80-3. Pack Sizes: 50 mg. Product ID: B0084-053945. Molecular formula: Custom synthesis is available. Send your inquiries for more information.
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Lycopene
Lycopene, in the concentration used, is not toxic and also its health benefits in adipose tissue may play a role against obesity-related complications. Lycopene in tomato puree has decreased indicating an indirect effect on lycopene stability caused by high concentration of hydrogen peroxide and the activation of peroxidase enzymes leading to the reduction of ascorbic acid and its regenerative action towards lycopene. Besides, Lycopene protected β-carotene against isomerization during reactions with singlet oxygen and radicals. These findings can explain the pattern of carotenoid isomers analyzed in fruits and vegetables, where lycopene containing samples showed higher (all-E)/(9Z)-β-carotene ratios, and also in in vivo samples such as human blood plasma. Lycopene can be used as pigment in food processing, and is also used as raw material of antioxidant health food. Uses: Ingredient of health care products. Group: Pharmaceutical. CAS No. 502-65-8. Pack Sizes: 1 g. Product ID: B0005-464994. Molecular formula: Custom synthesis is available. Send your inquiries for more information.
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Mevastatin
It is produced by the strain of Penicillum brevicompactum. It has weak anti-fungal activity and can inhibit the key enzyme (3-hydroxy-3-methyl glutaryl coenzyme A(HMGCoA) reductase) in the cholesterol biosynthesis pathway. It has been shown to lower cholesterol in animals and humans. It led the discovery of statins, lipid-lowering drugs. It is now used as a biochemical reagent. Uses: Hydroxymethylglutaryl-coa reductase inhibitors. Group: Pharmaceutical. CAS No. 73573-88-3. Pack Sizes: 25 g. Product ID: BBF-01732. Molecular formula: Custom synthesis is available. Send your inquiries for more information.
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Peficitinib
Peficitinib is a potent JAK inhibitor with IC50 values of 3.9, 5.0, 0.71 and 4.8 nM for JAK1, JAK2, JAK3 and TYK2 enzyme activities, respectively. It inhibits the IL-2-induced proliferation of human T cells with IC50 value of 18 nM. Moreover, peficitinib is 14-fold more potent against JAK1/3 than JAK2/2 on the basis of EPO-induced proliferation of human leukemia cells. Peficitinib has been used for the treatment of psoriasis and rheumatoid arthritis. Uses: Inhibited jak1, jak2, jak3 and tyk2 enzyme activities with ic50 values of 3.9, 5.0, 0.71 and 4.8 nm, respectively; inhibited the il-2-induced proliferation of human t cells with an ic50 value of 18 nm. Group: Pharmaceutical. CAS No. 944118-01-8. Pack Sizes: 25 mg. Product ID: B0084-462759. Molecular formula: Custom synthesis is available. Send your inquiries for more information.
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PF-1355
PF-1355 is a selective, mechanism-based inhibitor of myeloperoxidase (MPO) (IC50 = 1.5 μM in LPS-stimulated human whole blood) with excellent selectivity for MPO without disrupting a panel of 50 receptors, enzymes, ion channels and transporters, including thyroid peroxidase. PF-1355 was used to test the hypothesis that MPO activity is a critical mediator of disease activity in immune complex vasculitis mouse models, and to support the confidence in rationale for this mechanism as a therapeutic approach to treat related human condition such as alleviating tissue injury caused by Goodpasture syndrome and pulmonary vasculitis induced by immune complexes. Group: Pharmaceutical. CAS No. 1435467-38-1. Pack Sizes: 50 mg. Product ID: B0084-474818. Molecular formula: Custom synthesis is available. Send your inquiries for more information.
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Phenyl 2,3,4,6-tetra-O-acetyl-a-D-glucopyranoside
Phenyl 2,3,4,6-tetra-O-acetyl-a-D-glucopyranoside is an essential biochemical reagent involved in the synthesis of glycosides and glycosidase inhibitors with potential anti-cancer properties. Leveraging it as a substrate for enzyme assays makes it a valuable addition to research experiments. Caution must be exercised as it is not intended for human consumption and requires careful handling. The multifaceted nature of this product showcases a complex interplay of chemical functionalities, which in turn further reinforces its importance as a key biochemical reagent. Group: Pharmaceutical. CAS No. 3427-45-0. Pack Sizes: 1 g. Product ID: B2705-405005. Molecular formula: Custom synthesis is available. Send your inquiries for more information.
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Punicalagin
Punicalagin is an ellagitannin, a type of phenolic compounds. It had a greater antifungal activity against T. rubrum. It has the potential to be developed as an alternative or supplemental agent for prevention of Salmonella infection. After being absorbed by the human body, punicalagin can be decomposed into ellagic acid under the action of human enzymes. It has excellent antioxidant properties and has been used as a food antioxidant. It is now mostly used in cosmetics. Group: Pharmaceutical. CAS No. 65995-63-3. Pack Sizes: 100 mg. Product ID: B2703-464764. Molecular formula: Custom synthesis is available. Send your inquiries for more information.
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Rutin
Rutin is colored brown by tobacco enzymes under experimental conditions. In medicine, it has been used as an auxiliary drug and nutritional supplement for the treatment of cardiovascular system diseases. Because it is not toxic to the human body, it can also be used as an antioxidant and natural edible yellow pigment in the food industry. Rutin can reduce the generation of free radicals, promote the synthesis of antioxidant enzymes, and achieve the effect of anti-aging and wrinkling. By inhibiting tyrosinase and dopa autooxidation, it plays the role of whitening and lightening spots. At the same time, it also has the effect of antibacterial and anti-inflammatory, oil control and acne, and analgesic repair on the skin. Uses: Adcs cytotoxin. Group: Pharmaceutical. CAS No. 153-18-4. Pack Sizes: 1 kg. Product ID: NP1876. Molecular formula: Custom synthesis is available. Send your inquiries for more information.
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Talazoparib
Talazoparib, also known as BMN-673, is an orally bioavailable inhibitor of the nuclear enzyme poly(ADP-ribose) polymerase (PARP) with potential antineoplastic activity. BMN-673 selectively binds to PARP and prevents PARP-mediated DNA repair of single strand DNA breaks via the base-excision repair pathway. BMN-673 has been proven to be highly active in mouse models of human cancer and also appears to be more selectively cytotoxic with a longer half-life and better bioavailability as compared to other compounds in development. Uses: For research used only. Group: Pharmaceutical. CAS No. 1207456-01-6. Pack Sizes: 100 mg. Product ID: B0084-462689. Molecular formula: Custom synthesis is available. Send your inquiries for more information.
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TAS4464
TAS4464 is a potent and selective NEDD8 activating enzyme (NAE) inhibitor with IC50 of 0.955 nM. It selectively inhibits NAE relative to the other E1s UAE and SAE. TAS4464 treatment inhibits cullin neddylation and subsequently induces the accumulation of CRL substrates such as CDT1, p27, and phosphorylated IkBa in human cancer cell lines. Group: Pharmaceutical. CAS No. 1848959-10-3. Pack Sizes: 5 mg. Product ID: B2693-010141. Molecular formula: Custom synthesis is available. Send your inquiries for more information.
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Telaprevir-[d4]
Labelled Telaprevir. VX-950 is a potent, selective, peptidomimetic inhibitor of the hepatitis C virus (HCV) NS3-4A serine protease, and it demonstrated excellent antiviral activity both in genotype 1b HCV replicon cells (50% inhibitory concentration [IC50] = 354 nM) and in human fetal hepatocytes infected with genotype 1a HCV-positive patient sera (IC50 = 280 nM). VX-950 forms a covalent but reversible complex with the genotype 1a HCV NS3-4A protease in a slow-on, slow-off process with a steady-state inhibition constant (K(I)*) of 7 nM. Dissociation of the covalent enzyme-inhibitor complex of VX-950 and genotype 1a HCV protease has a half-life of almost an hour. A >4-log10 reduction in the HCV RNA levels was observed after a 2-week incubation of replicon cells with VX-950, with no rebound of viral RNA observed after withdrawal of the inhibitor. In several animal species, VX-950 exhibits a favorable pharmacokinetic profile with high exposure in the liver. In a recently developed HCV protease mouse model, VX-950 showed excellent inhibition of HCV NS3-4A protease activity in the liver. Group: Pharmaceutical. Pack Sizes: 50 mg. Product ID: BLP-006018. Molecular formula: Custom synthesis is available. Send your inquiries for more information.
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Tricirbine
Triciribine is a potent AKT inhibitor and a cell-permeable tricyclic nucleoside molecule with potential antineoplastic activity. Akt-1, -2, and -3 are serine/threonine protein kinases in the phosphatidylinositol (PI3)-kinase signalling pathway that play a critical role in the regulation of cell proliferation and survival. Following recruitment of Akt to the plasma membrane, phosphorylation at threonine 308 and serine 473 (Akt-1 numbering) by phosphoinositide-dependent kinases (PDK) 1 and 2 results in full activation of the enzyme. Triciribine is a cell-permeable tricyclic nucleoside that inhibits the phosphorylation, activation, and signalling of Akt-1, -2, and -3. It does not inhibit phosphatidylinositol 3 (PI3)-Kinase or PDK1, the direct upstream activators of Akt, nor does it inhibit PKC, PKA, ERK1/2, serum- and glucocorticoid-inducible kinase, p38, STAT3, or JNK signalling pathways. Triciribine effectively inhibits growth of Akt-overexpressing human cancer cell lines in vitro with 50% inhibition at ~5-10 μM. It also inhibit growth of tumor xenografts in mice by greater than 80% at a dose of 1 mg/kg/day. Group: Pharmaceutical. CAS No. 35943-35-2. Pack Sizes: 100 mg. Product ID: B1370-090988. Molecular formula: Custom synthesis is available. Send your inquiries for more information.
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TUG-770
TUG-770 displayed excellent physicochemical and in vitro ADME properties, with good aqueous solubility, good chemical stability, low lipophilicity, and decreased plasma protein binding (PPB). TUG-770 furthermore showed excellent stability toward human liver microsomes (HLM), no inhibition of selected CYP-enzymes implicated in drug-drug interactions, no P-glycoprotein (P-gp) inhibition, and good permeability in the Caco-2 cell assay. Examination of TUG-770 in an acute intraperitoneal glucose tolerance test (IPGTT) in normal mice revealed a good dose dependent response with maximal reduction in glucose level reached at 50 mg/kg. The effect of TUG-770 was fully sustained after 29 days of daily oral treatment. Additional evaluation of TUG-770 in rats confirmed a significant glucose lowering effect for the high doses already after 10 min and for all doses after 30 min. Group: Pharmaceutical. CAS No. 1402601-82-4. Pack Sizes: 25 mg. Product ID: B0084-463218. Molecular formula: Custom synthesis is available. Send your inquiries for more information.
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