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Catalog No.
Product Name
Application
Product Information
Citations
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CYP51 Inhibitor
CYP51-IN-21 is a potent inhibitor of cytochrome P450 51 (CYP51), demonstrating significant antifungal activity against various pathogenic fungi, including drug-resistant strains. By targeting CYP51, CYP51-IN-21 disrupts the biosynthesis of essential sterols, impairing fungal growth and viability. Additionally, CYP51-IN-21 effectively inhibits the formation of fungal biofilms, making it a valuable candidate for research in antifungal therapeutics and biofilm-related studies. -
CYP3A4 Inhibitor
Dihydrocubebin is a selective inhibitor of cytochrome P450 3A4 (CYP3A4), a key enzyme involved in drug metabolism. Isolated from Piper cubeba, it demonstrates potent inhibitory effects, making it a valuable tool for studying CYP3A4-related metabolic processes. Its role in research applications includes evaluating drug interactions and understanding the metabolic pathways of pharmaceutical compounds. -
Aromatase (CYP19) Inhibitor
2-Methoxy-5-acetoxyfuranogermacr-1(10)-en-6-one is a potent aromatase (CYP19) inhibitor, exhibiting an IC50 value of 0.21 μM against human targets. This compound is particularly relevant for research in breast cancer, providing insights into estrogen synthesis regulation and its implications in cancer progression. Its use in preclinical studies may advance the understanding of therapeutic strategies targeting estrogen-dependent tumors. -
CYP1B1 Inhibitor
CYP1B1-IN-9 is a highly selective competitive inhibitor of CYP1B1, demonstrating an IC50 of 1.48 nM. It effectively inhibits the migration and invasion of A549/T cells and has been shown to resensitize cells resistant to Paclitaxel. Notable for its favorable pharmacokinetic properties, metabolic stability, and safety profile, CYP1B1-IN-9 serves as a valuable tool for investigating tumor-drug resistance mechanisms in cancer research. -
CYP2A6/MAO Inhibitor
8α-(2-Methylacryloyloxy)-hirsutinolide-13-O-acetate functions as an irreversible inhibitor of CYP2A6, exhibiting IC50 values of 8.64 μM and 22.3 μM under pre-incubation and co-incubation conditions, respectively. Additionally, this compound demonstrates inhibitory activity against monoamine oxidase A (MAO-A) and monoamine oxidase B (MAO-B), with IC50 values of 60.2 μM and 38.6 μM, respectively. It serves as a valuable tool for research involving drug metabolism, neurochemistry, and the study of pharmacological responses influenced by these metabolic pathways. -
CYP2C9/CYP3A4 Inhibitor
GW694481 is a selective inhibitor of CYP2C9 and CYP3A4, exhibiting IC50 values of 2.1 μM and 17.0 μM, respectively. This compound functions as an ApoA1 upregulator, enhancing the expression of ApoA1 in human hepatic cells. GW694481 is valuable for research focused on atherosclerosis and related metabolic disorders, providing insights into lipid metabolism and cardiovascular health. -
11β-HSD1 Inhibitor
INCB13739 is a selective and potent inhibitor of 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1), exhibiting an IC50 of 3.2 nM in enzymatic assays and 1.1 nM in peripheral blood mononuclear cells (PBMC). This compound demonstrates significant potential for research in type 2 diabetes mellitus (T2DM) and obesity, targeting the regulation of glucocorticoid metabolism, which plays a critical role in metabolic conditions. Its tissue-specific action makes it a valuable tool for understanding 11β-HSD1-related pathways in metabolic disorders. -
Factor Xa Inhibitor
DPC423 free base is a selectively potent Factor Xa inhibitor, demonstrating inhibition constants (Kis) of 0.15 nM in humans and 0.3 nM in rabbits. It exhibits moderate selectivity with Kis of 60 nM against human trypsin, 61 nM against plasma kallikrein, and 6000 nM against thrombin. By inhibiting the formation of the prothrombinase complex, DPC423 reduces thrombin generation, thereby obstructing fibrin formation and platelet activation. This compound is valuable for research applications related to anticoagulation in arterial thrombosis. -
Heme Oxygenase Inhibitor
Zn(II) Deuteroporphyrin IX 2,4 bis ethylene glycol is a potent inhibitor of heme oxygenase (HO), a key enzyme involved in the degradation of heme to bilirubin. By inhibiting HO activity, this compound can effectively reduce the release of hypothalamic hormones such as arginine vasopressin (AVP), oxytocin (OT), and atrial natriuretic peptide (ANP) under hyperosmotic conditions. Its application extends to research involving hyperbilirubinemia and the physiological implications of HO modulation. -
AHR Inhibitor
IK-175 is a selective aryl hydrocarbon receptor (AHR) inhibitor that prevents the translocation of AHR from the cytoplasm to the nucleus. This compound exhibits high specificity for AHR, distinguishing itself from other receptors, transporters, and kinases. IK-175 is primarily used in research applications focused on studying AHR-related pathways and their implications in various diseases, including cancer and immune responses. -
AHR Inhibitor
KYN-101 is a selective AHR inhibitor that is potent and orally active. This compound effectively reduces CYP1A1 mRNA expression, contributing to its role in mediating anti-cancer activity. Researchers can utilize KYN-101 to investigate the therapeutic potential in cancer biology and the modulation of AHR-related signaling pathways. -
AhR activator/Thyroid hormone synthesis and Dopamine beta-hydroxylase inhibitor
2-Mercaptobenzothiazole is an activator of the aryl hydrocarbon receptor (AhR), functioning as an inhibitor of thyroid hormone synthesis and dopamine beta-hydroxylase activity. This compound promotes the invasion of bladder cancer cells by activating AhR transcription and upregulating the expression of CYP1A1 and CYP1B1, implicated in carcinogenesis. Additionally, 2-Mercaptobenzothiazole exhibits inhibition of thyroid peroxidase activity with an IC50 of 11.5 μM and induces significant histological changes in Xenopus laevis, including delayed metamorphosis. It also increases chromosomal aberrations in Chinese hamster ovary cells and inhibits norepinephrine synthesis in murine models, demonstrating its relevance in carcinogenic studies and neurobiological research. -
hCYP1B1 Inhibitor
hCYP1B1-IN-2 is a highly selective inhibitor of the human cytochrome P450 1B1 enzyme (hCYP1B1). It demonstrates remarkable potency in inhibiting hCYP1B1 activity, with an IC50 value of 0.040 nM, alongside a Ki value of 21.71 pM, indicating effective mixed inhibition. This compound also effectively disrupts aryl hydrocarbon receptor (AhR) transcription activities, making it a valuable tool for research applications focused on cancer and toxicology. -
AHR Inhibitor
AHR-IN-1 is a selective aryl hydrocarbon receptor (AHR) inhibitor, exhibiting an IC50 of less than 0.5 μM. This compound is useful for investigating the role of AHR in various biological processes, including immune response modulation and xenobiotic metabolism. AHR-IN-1 serves as a valuable tool for researchers studying the mechanisms by which AHR influences cellular signaling and gene expression. -
hCYP1B1 Inhibitor
CYP1B1-IN-10 is a potent and selective inhibitor of human cytochrome P450 1B1 (hCYP1B1), exhibiting an IC50 value of 0.11 μM. This compound plays a significant role in the investigation of hormone-dependent tumors, including breast and ovarian cancers. Its specificity makes it a valuable tool for studying the therapeutic potential in oncology research. -
COX/5-LOX Inhibitor
Phenethyl ferulate is a potent inhibitor of cyclooxygenase (COX) and 5-lipoxygenase (5-LOX), displaying IC50 values of 4.35 μM and 5.75 μM, respectively. This compound exhibits significant anti-inflammatory properties, making it a valuable tool for research into inflammation-related pathways. Its ability to modulate these key enzymes positions it as a promising candidate for studies focused on inflammatory diseases and therapeutic interventions. -
5-LOX/COX Inhibitor
FPL 62064 is a potent dual inhibitor of 5-lipoxygenase (5-LOX) and cyclooxygenase (COX), exhibiting IC50 values of 3.5 μM and 3.1 μM, respectively, in RBL-1 cells. This compound demonstrates significant anti-inflammatory activity, making it a valuable tool for research into inflammatory pathways and related diseases. Its dual inhibition of leukotriene and prostaglandin synthesis positions FPL 62064 as a pertinent reagent for studies focusing on inflammation and related therapeutic interventions. -
Carbonic anhydrase inhbitor
Indisulam (E7070) is a carbonic anhydrase inhbitor, is also a novel synthetic sulfon-amide that targets the G1 phase of the cell cycle. -
FTase inhibitor
FTI 276 is an inhibitor that inhibits farnesyltransferase (FTase) (IC50 = 0.5 nM). Inhibits H-Ras and K-Ras processing in whole cells (IC50 values are 0.1 and 10 μM respectively) and disrupts constitutive H-Ras-specific actvation of MAPK. Causes significant antiproliferative effects in human malignant glioma cells and many other tumor cell lines. -
GAPDH inhibitor
CGP 3466B maleate is an orally active glyceraldehyde-3-phosphate dehydrogenase (GAPDH) inhibitor. -
FAAH inhibitor
JNJ 1661010 is a selective and reversible inhibitor of fatty acid amide hydrolase (FAAH) (IC50 = 12nM). -
5-LPO inhibitor
ICI 211965 (ZM-211965) is a selective and orally potent 5-Lipoxygenase (5-LPO) inhibitor. -
DGAT1 inhibitor
Pradigastat (LCQ-908) is a diacylglycerol acyltransferase 1 (DGAT1) inhibitor. -
squalene synthetase inhibitor
YM-53601 free base is a squalene synthetase inhibitor which suppresses lipogenic biosynthesis and lipid secretion in rodents. -
NAMPT inhibitor
CHS-828 is a potent inhibitor of NAD+ biosynthesis enzyme NAMPT with IC50 <25 nM. -
FXa Inhibitor
Betrixaban is an anticoagulant drug which acts as a direct factor Xa inhibitor. It is potent, orally active and highly selective for factor Xa, being selected from a group of similar compounds for its low hERG affinity. -
CYP3A4 inhibitor
PF 4981517 is a potent and selective inhibitor of CYP3A4 (IC50 values are 0.03, 17 and 70 μM for CYP3A4, CYP3A5 and CYP3A7 respectively). -
PDE 3/4 inhibitor
Zardaverine is a phosphodiesterase inhibitor, selective for PDE3 and 4 (IC50 values are 0.5 and 0.8 uM respectively). -
platelet PDE inhibitor
Ro 15-2041 is a selective platelet phosphodiesterase inhibitor with antithrombotic properties. -
Mitochondrial respiratory chain inhibitor
Sulfosuccinimidyl oleate (Sulfo-N-succinimidyl oleate) is a long chain fatty acid that inhibits fatty acid transport into cells. Sulfosuccinimidyl oleate is a potent and irreversible inhibitor of mitochondrial respiratory chain. -
DGAT2 inhibitor
PF-06424439 is an oral, potent and selective imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an IC50 of 14 nM. -
CYP17 inhibitor
CYP17-IN-1 (compound 9c) is a potent and orally active CYP17 inhibitor against rat and human CYP17 with IC50s of 15.8 and 20.1 nM. -
HSF1 activation inhibitor
Rocaglamide (Rocaglamide A) is isolated from the genus Aglaia and can be used to treat coughs, injuries, asthma and inflammatory skin diseases. Rocaglamide is a potent inhibitor of NF-κB activation in T-cells. Rocaglamide is a potent and selective heat shock factor 1 (HSF1) activation inhibitor with an IC50 of ~50 nM. Rocaglamide inhibits the function of the translation initiation factor eIF4A. Rocaglamide also has anticancer properties in leukemia. -
PDE4 inhibitor?€?
AN2728 is a topically administered, boron-containing, anti-inflammatory compound that inhibits PDE4 activity and thereby suppresses the release of TNFalpha, IL-12, IL-23 and other cytokines -
factor Xa inhibitor
Letaxaban, also known as TAK-442, is a potent, selective, and orally active factor Xa inhibitor, which is a tetrahydropyrimidin-2(1H)-one derivative. TAK-442 inhibited endogenous FXa activity in platelet-poor human [half-maximal inhibitory concentration (IC(50)): 53 nM, TAK-442] and rat (IC(50): 32 nM, TAK-442) plasma. -
SCD1 inhibitor
stearoyl-CoA desaturase 1 (SCD1) inhibitor. Used to selectively eliminate undifferentiated human pluripotent stem cells (hPSCs) from culture; induces ER stress, attenuates protein synthesis and induces apoptosis in hPSCs. Prevents teratoma formation in immunocompromised mice. -
IDH1 inhibitor
AGI-5198, also know as IDH-C35, is the a very potent and selective mutant IDH1 inhibitor that was shown to potential anticancer activity.
