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A selective inhibitor of calcineurin-mediated dephosphorylation of nuclear factor of activated T cells (NFAT). Synonyms: H-Met-Ala-Gly-Pro-His-Pro-Val-Ile-Val-Ile-Thr-Gly-Pro-His-Glu-Glu-OH; L-methionyl-L-alanyl-glycyl-L-prolyl-L-histidyl-L-prolyl-L-valyl-L-isoleucyl-L-valyl-L-isoleucyl-L-threonyl-glycyl-L-prolyl-L-histidyl-L-alpha-glutamyl-L-glutamic acid. Grades: >98%. CAS No. 249537-73-3. Molecular formula: C75H118N20O22S. Mole weight: 1683.93.
NFAT Inhibitor
Selective inhibitor of calcineurin-mediated dephosphorylation of nuclear factor of activated T cells (NFAT). Does not disrupt other calcineurin-dependent pathways. Inhibits NFAT activation and NFAT-dependent expression of endogenous cytokine genes in T cells. Group: Biochemicals. Grades: Purified. CAS No. 249537-73-3. Pack Sizes: 1mg. Molecular Formula: C75H118N20O22S, Sequence: MAGPHPVIVITGPHEE. US Biological Life Sciences.
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NFAT inhibitor, Cell Permeable
A cell-permeable NFAT inhibitor. It exhibits immunosuppressive effects and can enhance graft survival in mice. Synonyms: 11R-VIVIT; H-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Gly-Gly-Gly-Met-Ala-Gly-Pro-His-Pro-Val-Ile-Val-Ile-Thr-Gly-Pro-His-Glu-Glu-OH; L-arginyl-L-arginyl-L-arginyl-L-arginyl-L-arginyl-L-arginyl-L-arginyl-L-arginyl-L-arginyl-L-arginyl-L-arginyl-glycyl-glycyl-glycyl-L-methionyl-L-alanyl-glycyl-L-prolyl-L-histidyl-L-prolyl-L-valyl-L-isoleucyl-L-valyl-L-isoleucyl-L-threonyl-glycyl-L-prolyl-L-histidyl-L-alpha-glutamyl-L-glutamic acid. Grades: >95%. CAS No. 592517-80-1. Molecular formula: C147H259N67O36S. Mole weight: 3573.12.
NFAT Inhibitor, MCV1
The NFAT Inhibitor, MCV1 controls the biological activity of NFAT. Group: Fluorescence/luminescence spectroscopy.
A cell-permeable, synthetic maleimido-conjugated VIVIT motif peptide (HPVIVIT) that acts as a potent bipartite inhibitor of Nuclear factor of activated T-cells (NFAT) (IC50=62nM). Blocks NFAT-calcineurin interaction by targeting two separate calcineurin docking motifs. Completely blocks NFAT dephosphorylation at 1mM. Determined to be more potent that Cyclosporine A and VIVIT peptide (MAGPHPVIVITGPHEE) in blocking NFAT activity. Also shown to blocks NFAT-mediated T-cell activation and vascular smooth muscle cell proliferation, thereby reducing neoimtima (new thickening of arterial wall) formation in mouse models of restenosis (repeat blocking of blood vessels). The biological half life of MCV1 has been estimated to be about 36 hours in COS-1 cells. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 2mg. Molecular Formula: C??H??N??O??. US Biological Life Sciences.
9,10-Dihydro-9,10[1',2']-benzenoanthracene-1,4-dione. Uses: Designed for use in research and industrial production. Additional or Alternative Names: NFAT Activation Inhibitor III; triptycene quinone; Inhibitor of NFAT-Calcineurin Association-6; triptycene-1,4-quinone; triptycene-quinine; 9,10-dihydro-9,10-o-benzenoanthracene-1,4-dione. Product Category: Heterocyclic Organic Compound. CAS No. 3519-82-2. Molecular formula: C20H12O2. Mole weight: 284.313. Purity: >98 %. IUPACName: INCA-6. Canonical SMILES: C1=CC=C2C3C4=CC=CC=C4C(C2=C1)C5=C3C(=O)C=CC5=O. Density: 1.38g/cm³. Product ID: ACM3519822. Alfa Chemistry ISO 9001:2015 Certified.
Bavachalcone
Bavachalcone inhibited osteoclast formation from precursor cells with the IC(50) of approximately 1.5 microg ml(-1). The activation of MEK, ERK, and Akt by receptor activator of nuclear factor kappaB ligand (RANKL), the osteoclast differentiation factor, was prominently reduced in the presence of bavachalcone. The induction of c-Fos and NFATc1, key transcription factors for osteoclastogenesis, by RANKL was also suppressed by bavachalcone. Bavachalcone exhibited a significant inhibitory effect on baculovirus-expressed BACE-1 in vitro. Bavachalcone had stronger inhibition on UGT1A1 and UGT1A7 than corylin which did not inhibit UGT1A1, UGT1A3, UGT1A7, UGT1A8, UGT1A10, and UGT2B4. Data fitting using Dixon and Lineweaver-Burk plots demonstrated the noncompetitive inhibition of bavachalcone against UGT1A1 and UGT1A7-mediated 4-MU glucuronidation reaction. The values of inhibition kinetic parameters (Ki) were 5.41 μ M and 4.51μ M for UGT1A1 and UGT1A7, respectively. Synonyms: Broussochalcone B. Grades: >98%. CAS No. 28448-85-3. Molecular formula: C20H20O4. Mole weight: 324.37.
CRM1 Inhibitor III (Chromosome Region Maintenance 1 Protein Inhibitor III, (Z)-But-2-enedioic acid (4-bromophenyl)amide (3-chlorophenyl)amide, Exportin 1 Inhibitor III, XPO1 Inhibitor III)
A cell-permeable butenediamide compound that acts as a potent, active site cysteine reactive irreversible inhibitor of CRM1/exportin 1. Shown to selectively repress agonist-mediated nuclear export of HDAC4/5, Rev and NFAT proteins in neonatal rat ventricular myocytes (NRVMs; EC50=2.2 and 3.5nM for GFP-HDAC5 and GFP-HIV Rev) and suppress hypertrophic growth of NRVMs (EC50=52nM for ANF expression inhibition) with negligible effect either on the phosphorylation of HDAC5 or on the kinase activities of P and CaMKII at 1uM. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. Molecular Formula: C??H??BrClN?O?. US Biological Life Sciences.
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Cyclosporin A
Potent immunosuppressant (same as FK-506 and rapamycin). Forms a complex with cyclophilin. Inhibits the activity of the calcium/calmodulin-dependent protein phos- phatase 2B (PP2B; calcineurin). Prevents the dephosphorylation of nuclear factor of activated T cells (NFAT) transcription factor, leading to disruption of T cell activation. Suppresses proliferation of cytotoxic T cells and inhibits the production of T cell-derived mediators such as interleukin-2 (IL-2). Prevents rejection of transplanted organs. Anti-inflammatory compound in the treatment of several inflammatory skin diseases (e.g. atopic dermatitis) and with potential anti-rheumatic activity (rheumatoid arthritis). Antibacterial. Antifungal. Antiparasitic. Apoptosis inhibitor. Inhibits the mitochondrial permeability transition pore (MPTP) from opening, thus inhibiting cytochrome c release. NF-kappaB suppressor by induction of unfolded protein response (UPR). Anti-cancer compound. Apoptosis and autophagy inducer. Inhibits n Group: Biochemicals. Alternative Names: Antibiotic S 7481F1; Ciclosporin A; CsA; Cyclosporine; NSC 290193; Ramihyphin A; Sandimmun; Sandimmune; Neoral; Optimmune; Restasis; OL 27-400. Grades: Highly Purified. CAS No. 59865-13-3. Pack Sizes: 5g, 10g. US Biological Life Sciences.
Worldwide
Elagolix sodium
Elagolix sodium is a highly effective, selective, oral-active, short-term, non-peptide gonadotropin-releasing hormone receptor (GnRH receptor) antagonist (K D = 54 pM) and NFAT inhibitor, which can be used to study pain related to endometriosis. [1] [2] [3] [4] [5]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: NBI-56418 sodium. CAS No. 832720-36-2. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-14369.
INCA-6
INCA-6, a cell-permeable quinone compound, is a selective and potent inhibitor of Calcineurin Nuclear Factor of Activated T cells (NFAT) signaling. It binds to calcineurin with high affinity and does not affect calcineurin activity or its downstream signaling. It blocks its dephosphorylation and nuclear import, thus interferes with downstream targets of NFAT including induction of cytokine mRNAs. Synonyms: INCA-6; INCA 6; INCA6; 9,10-Dihydro-9,10-o-benzenoanthracene-1,4-dione; 9,10-Dihydro-9,10[1',2']-benzenoanthracene-1,4-dione; 1,4-Triptycenoquinone; 12,15-Dihydro-12,15-dioxotriptycene; NSC 25996; Triptycene-1,4-quinone. Grades: ≥98% by HPLC. CAS No. 3519-82-2. Molecular formula: C20H12O2. Mole weight: 284.31.
Kisspeptin-10, human
Kisspeptin-10, human is a potent vasoconstrictor and inhibitor of angiogenesis. Kisspeptin-10, human acts as a tumor metastasis suppressor via its receptor GPR54. Kisspeptin-10-GPR54 system plays an important role in embryonic kidney development. Kisspeptin-10/GPR54 signaling induces osteoblast differentiation via NFATc4-mediated BMP2 expression [1]. Uses: Scientific research. Group: Peptides. CAS No. 374675-21-5. Pack Sizes: 1 mg; 5 mg; 10 mg. Product ID: HY-P0254.
NDMC101
NDMC101 is a dipeptidyl peptidase-IV (DPPIV) inhibitor. It inhibits transcription factors as NF-κB and NFATc1, demonstrating that it has the potential as a therapeutic agent for inflammation-induced bone diseases. Synonyms: N-(4-chloro-2-fluorophenyl)-2-hydroxybenzamide. CAS No. 1308631-40-4. Molecular formula: C13H9ClFNO2. Mole weight: 265.7.
(R)-3-[1-(1-Acryloylpiperidin-3-yl)-4-amino-1H-pyrazolo[3,4-d]pyrimidin-3-yl]-N-(4-isopropyl-5-methylphenyl)benzamide is a potential covalent inhibitor of Interleukin-2 Inducible T Cell KInase (Itk). Itk is a member of the TEC-kinase family and is associated with the induction of T cell proliferation and drives cytokines through NFATc. Group: Biochemicals. Alternative Names: PF-06465469-00. Grades: Highly Purified. Pack Sizes: 5mg. US Biological Life Sciences.
A cell-permeable, selective inhibitor of cAMP-specific phosphodiesterase (PDE IV; IC50=800nM). A rolipram-insensitive PDE IV subtype is also known to exist. Also inhibits NF-kB and NFAT activation in Jurkat and primary T cells. Group: Biochemicals. Grades: Highly Purified. CAS No. 61413-54-5. Pack Sizes: 5mg. US Biological Life Sciences.
Worldwide
(+)-Syringaresinol
(+)-Syringaresinol, a lignan, is a NFAT transcription factor inhibitor, with an IC 50 of 329.4 μM. (+)-Syringaresinol also can be used for the research of lymphocytic leukemia [1] [2]. Uses: Scientific research. Group: Natural products. CAS No. 21453-69-0. Pack Sizes: 1 mg; 5 mg. Product ID: HY-126030.
Tamarixetin
Tamarixetin (4'-O-Methyl Quercetin) is an orally active natural flavonoid derivative of quercetin and caseinolytic protease p ( ClpP ) inhibitor with anti-inflammatory, antioxidant and antitumor effects. Tamarixetin inhibits the hydrolytic activity of ClpP to the fluorescent substrate Suc-LY-AMC with an IC 50 of 49.73 μM, which can be used for the study of Staphylococcus aureus infection. Tamarixetin inhibits tumor cell growth, induces apoptosis , and cell cycle arrest. Tamarixetin prevents cardiac hypertrophy by inhibiting the NFAT and AKT pathways [1] [2] [3] [4]. Uses: Scientific research. Group: Natural products. Alternative Names: 4'-O-Methyl Quercetin. CAS No. 603-61-2. Pack Sizes: 1 mg; 5 mg; 10 mg. Product ID: HY-N1181.
Usnic Acid
Usnic acid, a lichen-derived secondary metabolite, has a unique dibenzofuran skeleton. Usnic acid has excellent anticancer and antimicrobial properties. Usnic acid significantly inhibits RANKL-mediated osteoclast formation and function by reducing the transcriptional and translational expression of NFATc1. Uses: Designed for use in research and industrial production. Additional or Alternative Names: 1,3(2H,9bH)-Dibenzofurandione, 2,6-diacetyl-7,9-dihydroxy-8,9b-dimethyl-. Product Category: Inhibitors. Appearance: Solid. CAS No. 125-46-2. Molecular formula: C18H16O7. Mole weight: 344.32. Purity: 0.98. Canonical SMILES: O=C(C1(C)C(OC2=C(C(C)=O)C(O)=C(C)C(O)=C12)=C3)C(C(C)=O)C3=O. Density: 1.54 g/cm³. Product ID: ACM125462. Alfa Chemistry ISO 9001:2015 Certified.
A cell-permeable diaminoquinazoline compound that selectively blocks importin-b-mediated nuclear import of NLS- (nuclear localization signal) bearing cargos (IC50=15uM against Ca+2-induced NFAT nuclear import in HEK293 cells) in a reversible manner without affecting transportin-dependent nuclear import of M9 signal-containing cargos or CRM1-mediated nuclear export. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. US Biological Life Sciences.
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