Potent, selective and orally available NLRP3 inflammasome inhibitor. Blocks the release of IL-1beta in macrophages primed with LPS and activated with ATP or nigericin, but it does not inhibit NLRP1, NLRC4, AIM2, TLR2 signaling or priming of NLRP3. Prevents oligomerization of ASC in cells stimulated with LPS and nigericin. Active in vivo, blocking the production […]
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Potent, selective and orally available NLRP3 inflammasome inhibitor. Blocks the release of IL-1beta in macrophages primed with LPS and activated with ATP or nigericin, but it does not inhibit NLRP1, NLRC4, AIM2, TLR2 signaling or priming of NLRP3. Prevents oligomerization of ASC in cells stimulated with LPS and nigericin. Active in vivo, blocking the production […]
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Antidiabetic agent. Potent and selective sodium glucose co-transporter 2 (SGLT-2) inhibitor. >300-fold selectivity over SGLT-1, 4, 5 and 6. SGLT-2 is found almost exclusively in the proximal tubules of nephronic components in kidneys. Inhibition of SGLT-2 reduces blood glucose by blocking renal glucose reabsorption and thereby increasing urinary glucose excretion (UGE). Shown to preserves beta […]
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Antidiabetic agent. Potent and selective sodium glucose co-transporter 2 (SGLT-2) inhibitor. >300-fold selectivity over SGLT-1, 4, 5 and 6. SGLT-2 is found almost exclusively in the proximal tubules of nephronic components in kidneys. Inhibition of SGLT-2 reduces blood glucose by blocking renal glucose reabsorption and thereby increasing urinary glucose excretion (UGE). Shown to preserves beta […]
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Antineoplastic, anti-inflammatory and immunomodulating agent. Orally bioavailable potent ATP mimetic that inhibits both JAK1 and JAK2 with IC50 values of 2.7 and 4.5nM, respectively and is less selective for JAK3 (IC50=322nM). Affects DC differentiation and function, leading to impaired T cell activation. Used in the treatment of myeloproliferative neoplasms and psoriasis. Anticancer agent. Shown to […]
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Antineoplastic, anti-inflammatory and immunomodulating agent. Orally bioavailable potent ATP mimetic that inhibits both JAK1 and JAK2 with IC50 values of 2.7 and 4.5nM, respectively and is less selective for JAK3 (IC50=322nM). Affects DC differentiation and function, leading to impaired T cell activation. Used in the treatment of myeloproliferative neoplasms and psoriasis. Anticancer agent. Shown to […]
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Orally bioavailable potent antitumor, antiangiogenic, antiproliferative and antineoplastic agent. Multi-target kinase inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRbeta, Kit, RET and Raf-1 with IC50 values of 13, 4.2, 46, 22, 7, 1.5 and 2.5nM, respectively.
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Orally bioavailable potent antitumor, antiangiogenic, antiproliferative and antineoplastic agent. Multi-target kinase inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRbeta, Kit, RET and Raf-1 with IC50 values of 13, 4.2, 46, 22, 7, 1.5 and 2.5nM, respectively.
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Immunostimulant. Potent stimulator of natural killer T (NKT) cells. Specific ligand of the lipid-binding MHC class I-like protein CD1d in human and mouse NKT cells. Potent antitumor compound. Stimulates the production of smaller amounts of IFN-gamma than alpha-GalCer, but induces equal or greater IL-4 secretion in mouse models.
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Potent stimulator of invariant natural killer T (iNKT) cells. Induces strong antitumor immunity through a nitric oxide (NO) and TNF-alpha dependent mechansim, different compared to the IFN-gamma dependent mechanism of alpha-GalCer (AG-CN2-0014). Does not induce anergy of iNKT cells.
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