Transferases

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  1. HLGP Inhibitor

    CP-91149 is a selective glycogen phosphorylase inhibitor.

  2. NMPRTase Inhibitor

    FK866, a highly specific noncompetitive inhibitor of nicotinamide phosphoribosyltransferase, represents a novel mechanism for induction of tumor cell apoptosis.
  3. ACAT/SOAT inhibitor

    YM 750 is reported to act as a SOAT (acyl-CoA:cholesterol acyltransferase, ACAT) inhibitor.
  4. CPT-1 irreversible inhibitor

    Etomoxir is an inhibitor of carnitine palmitoyltransferase A (CPT1), which is required for the oxidation of long-chain acyl CoA esters. Also a strong inhibitor of mitochondrial CPT1 and a candidate as an anti-diabetic drug.
  5. Thymidine phosphorylase activator

    Doxifluridine is a thymidine phosphorylase activator for PC9-DPE2 cells with IC50 of 0.62 μM.
  6. GSTP1-1 inhibitor

    Ezatiostat is a liposomal small-molecule glutathione analog inhibitor of glutathione S-transferase (GST) P1-1 with hematopoiesis-stimulating activity.
  7. SPHK1 inhibitor

    SK1-IN-1 is a potent sphingosine kinase 1 (SPHK1) inhibitor with an IC50 of 58 nM.
  8. SphK2 inhibitor

    ABC294640 is an orally available, aryladamantane compound and selective inhibitor of sphingosine kinase-2 (SK2) with potential antineoplastic activity.
  9. MGAT3 inhibitor

    PF-06471553 is a potent, selective and orally available monoacylglycerol acyltransferase 3 (MGAT3) inhibitor, with an IC50 of 92 nM.
  10. SphK1 inhibitor

    PF-543 is a novel selective SK-1 inhibitor which inhibited SK-1 activity in a competitive manner with sphingosine.
  11. Thymidine phosphorylase inhibitor

    Tipiralacil hydrochloride, also known as TPI, is a thymidine phosphorylase inhibitor (TPI).

  12. CaMK/Phosphorylase inhibitor

    K252a is a highly potent cell permeable inhibitor of CaM kinase and phosphorylase kinase (IC50 = 1.8 and 1.7 nmol/L, respectively).
  13. ACAT1 Inhibitor

    ATR-101 is in clinical development for the treatment of adrenocortical carcinoma (ACC).
  14. SphK1 Inhibitor

    PF-543 Citrate is a novel cell-permeant inhibitor of SphK1 with a K(i) of 3.6 nM, PF-543 is sphingosine-competitive and is more than 100-fold selective for SphK1 over the SphK2 isoform.
  15. SphK Inhibitor

    SKI-II is a selective non-lipid inhibitor of sphingosine kinase (IC50 = 0.5 uM).
  16. SphK2 inhibitor

    K145 is a selective SphK2 inhibitor with an IC50 of 4.30?? 0.06 μM , while no inhibition of SphK1 at concentrations up to 10 uM.
  17. SphK2 inhibitor

    K145 is a selective sphingosine kinase-2 (SphK2) inhibitor and anticancer agent.
  18. ATP competitive SK inhibitor

    MP-A08 is a highly selective ATP competitive SK inhibitor that targets both SK1 and SK2 with Kivalues of 6.9 ±  0.8 uM and 27± 3 uM, respectively.

  19. ACAT/SOAT inhibitor

    VULM 1457 is an Acyl-CoA: cholesterol acyltransferase (ACAT) or SOAT inhibitor. VULM 1457 decreases cholesterol levels in the liver and plasma.
  20. ACAT/SOAT inhibitor

    CI 976 is a trimethoxy fatty acid anilide inhibitor of liver and intestinal acyl coenzyme A cholesterol acyltransferase (ACAT) and sterol O-acyltransferase (SOAT). Cl 976 lowers non-high density lipoprotein (non-HDL) cholesterol and increases HDL-cholesterol concentrations.
  21. ACAT inhibitor

    Cyclandelate is an effective inhibitor of rat hepatic acycloenzyme A: cholesterol acyltransferase (ACAT) with IC50 of 80 μM.
  22. Ghrelin O-acyltransferase (GOAT) inhibitor

    GOAT-IN-1 is an inhibitor of ghrelin O-acyltransferase (GOAT), which could be useful for the prophylaxis or treatment of obesity, diabetes, hyperlipidemia, metabolic, non-alcoholic fatty liver, steatohepatitis, sarcopenia, appetite control, alcohol/narcotic dependence, Alzheimer's disease, Parkinson's disease, cerebrovascular dementia, cerebral apoplexy, cerebral infarction, cardic disease, some kind of tumors.
  23. SPHK inhibitor

    Peretinoin, also known as NIK-333 , orally available, acyclic retinoid with potential antineoplastic and chemopreventive activities. Peretinoin binds to and activates nuclear retinoic acid receptors (RAR), which in turn recruit coactivator proteins and promote, with other transcriptional complexes, the transcription of target genes. As a result, this agent may modulate the expression of genes involved in the regulation of cell proliferation, cell differentiation, and apoptosis of both normal and tumor cells.
  24. ACAT inhibitor

    FR-190809 is a potent, nonadrenotoxic, orally efficacious ACAT inhibitor.
  25. OGT inhibitor

    OSMI-4 is a low nanomolar O-GlcNAc transferase (OGT) inhibitor, with an EC50 of 3 μM in cells.
  26. ACAT inhibitor

    RP 70676 is a potent inhibitor of ACAT, with IC50 of 25 and 44 nM for rat and rabbit ACAT.
  27. MHP

    SPHK1 activator

    MHP (Methyl caprooyl tyrosinate) is an activator of sphingosine kinase (SPHK1), and significantly stimulates CAMP mRNA and protein production. MHP (Methyl caprooyl tyrosinate) enhances antimicrobial defense and innate immunity.
  28. GSTO1 inhibitor

    GSTO1-IN-1 is a potent glutathione S-transferase omega 1 (GSTO1) inhibitor with an IC50 of 31 nM.
  29. MGAT2 inhibitor

    MGAT2-IN-1 is an orally active inhibitor of monoacylglycerol acyltransferase (MGAT2) with IC50 of 7.8 and 2.4 nM for human and mouse MGAT2, respectively.
  30. ACAT inhibitor

    ACAT-IN-1 cis isomer is a potent ACAT inhibitor with an IC50 of 100 nM.
  31. acyl CoA inhibitor

    YM17E is an inhibitor of acyl CoA:cholesterol acyltransferase (ACAT), with IC50 of 44 nM in rabbit liver microsomes in vitro.
  32. glutathione S-transferase inhibitor

    GSTO-IN-2 is a glutathione S-transferase inhibitor with IC50s of 3.6, 16.3, and 1.4 μM for GSTA2, GSTM1, and GSTP1-1.
  33. ACAT inhibitor

    RP 73163 Racemate is the racemate of RP 73163. RP 73163 is a potent ACAT inhibitor, with cholesterol lowering activity.
  34. ACAT inhibitor

    E-5324 is potent inhibitor of acyl-CoA:cholesterol acyltransferase (ACAT) with IC50s of 44 to 190 nM.
  35. PKC activator

    Phorbol 12,13-dibutyrate (Phorbol dibutyrate) is a PKC activator and a potent skin tumor promoter.
  36. RP-64477 is a potent inhibitor of the cholesterol esterifying enzyme Acyl-coenzyme A:cholesterol O-acyltransferase (ACAT).
  37. glutathione analog inhibitor

    Ezatiostat hydrochloride (TER199;TLK199 hydrochloride) is a glutathione analog inhibitor of glutathione S-transferase P1-1 (GSTP1-1).
  38. TLK117, the active metabolite of TLK199, selective inhibits Glutathione S-transferase P1?C1 (GSTP1-1) with a Ki of 0.4 μM for GSTP. TLK117 also competitively inhibits glyoxalase I with a Ki of 0.56 μM.
  39. ACAT1 inhibitor

    Nevanimibe hydrochloride (PD-132301 hydrochloride; ATR101 hydrochloride) is a selective and potent acyl-coenzyme A:cholesterol O-acyltransferase 1 (ACAT1) inhibitor with an EC50 of 9 nM.
  40. ACAT-1 inhibitor

    K-604 dihydrochloride is a potent and selective acyl-CoA:cholesterol acyltransferase 1 (ACAT-1) inhibitor with an IC50 of 0.45??0.06 μM.
  41. SphK1 inhibitor

    SKI-178 is a sphingosine kinase 1 (SphK1) inhibitor (IC50 = 0.1-1.8 μM). Induces CDK1-dependent apoptosis in human acute myeloid leukemia cell lines. Active in vivo.
  42. non-lipid sphingosine kinase inhibitor

    SKI V is a noncompetitive and potent non-lipid sphingosine kinase (SPHK; SK) inhibitor with an IC50 of 2 μM for GST-hSK.
  43. CerS1 inhibitor

    P053 is a potent, non-competitive, and selective inhibitor of ceramide synthase 1 (CerS1), exhibiting an IC₅₀ of 0.5 μM. It functions as an endogenous regulator of mitochondrial fatty acid oxidation in skeletal muscle, influencing cellular energy metabolism. By modulating ceramide synthesis, P053 also acts as a systemic regulator of whole-body adiposity, making it a valuable compound for studying lipid metabolism, energy homeostasis, and metabolic disorders.
  44. ACAT inhibitor

    Enniatin B1 is a mycotoxin produced by Fusarium species, known for its diverse bioactivities. It functions as a moderate inhibitor of acyl-CoA:cholesterol acyltransferase (ACAT), with an IC₅₀ of 73 μM in assays using rat liver microsomes, implicating a role in lipid metabolism modulation. Enniatin B1 is capable of crossing the blood-brain barrier, suggesting potential effects on central nervous system function. It also decreases the activation of ERK1/2 (p44/p42 MAPK) and moderately inhibits TNF-α-induced NF-κB activation, indicating anti-inflammatory and cell signaling modulatory properties.
  45. OGT inhibitor

    OSMI-1 is a potent cell-permeable inhibitor of O-GlcNAc transferase (OGT), with an IC50 value of 2.7 μM. This compound effectively decreases protein O-linked N-acetylglucosamine (O-GlcNAcylation) levels in various mammalian cell lines while maintaining the integrity of cell surface N- and O-linked glycans. OSMI-1 serves as a valuable tool for studying the regulatory roles of O-GlcNAcylation in cellular processes and diseases.
  46. Ionophore

    Enniatin complex is a mixture of cyclohexadepsipeptides isolated largely from Fusarium species of fungi, and has ionophoric, antibiotic, and in vitro hypolipidaemic properties. Enniatin complex inhibits enzymes like acyl-CoA: cholesterol acyl transferase and induces apoptosis in several cancer lines .
  47. SPHK1/2/MDA Inhibitor

    SKI-349 is a dual-target inhibitor of sphingosine kinase 1 and 2 (SPHK1/2) and modulates microtubule assembly (MDA). This compound exhibits significant anticancer activity, effectively reducing cell viability and invasion in liver cancer. SKI-349 also disrupts the AKT/mTOR signaling pathway, making it a valuable tool for investigating mechanisms of cancer progression and potential therapeutic strategies in oncology research.
  48. SPHK1 Inhibitor

    PF-543 hydrochloride is a potent and selective inhibitor of Sphingosine Kinase 1 (SPHK1), exhibiting an IC50 of 2 nM and a Ki of 3.6 nM. It demonstrates over 100-fold selectivity for SPHK1 compared to SPHK2, making it a valuable tool for studying sphingosine-mediated signaling pathways. PF-543 hydrochloride effectively inhibits the formation of sphingosine 1-phosphate (S1P) in whole blood with an IC50 of 26.7 nM, and it has been shown to induce apoptosis, necrosis, and autophagy in various cell types, highlighting its potential in cancer and therapeutic research applications.
  49. SphK1 Inhibitor

    SphK1-IN-2 is a selective inhibitor targeting sphingosine kinase 1 (SphK1), exhibiting an IC50 value of 19.81 nM for SphK1 while demonstrating minimal inhibition of SphK2 (IC50 > 10 μM). This compound demonstrates anti-proliferative properties, induces cell cycle arrest, and promotes apoptosis in various cancer cell lines. SphK1-IN-2 is applicable in cancer research, providing insights into the role of sphingolipid metabolism in tumor progression and potential therapeutic strategies.
  50. TPA Negative Control

    4α-TPA is an inactive analog of TPA, serving as a negative control in TPA-mediated experiments. This reagent is critical for distinguishing specific TPA-activated events from non-specific responses in biological assays. It aids researchers in validating experimental outcomes related to TPA signaling pathways and discerning the effects of TPA on various cellular processes.

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