Anticancer compound. Potent antiproliferative agent in vitro and in vivo. Combined inhibitor of pSTAT3 proteins such as JAK, SRC, ABL and class III/V receptor tyrosine kinases (RTK), including FLT3, c-KIT, CSF1-R, PDGFRs and VEGFRs, in nanomolar range.
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Human poly(ADP-ribose) glycohydrolase (PARG) inhibitor for in vitro studies. Inhibits human recombinant PARG enzymes (IC50=26nM) and PARG in cell assays (IC50=37nM). Inactive against related glycohydrolases ARH3 and PARP1s (IC50>30µM). Showed no cytotoxicity (IC50>30µM). Poly(ADP ribose) glycohydrolase (PARG) is a critical component in the repair of single strand DNA breaks and therefore a target in cancer […]
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NLRP3/NALP3 inflammasome activator. Specially crystallized and tested for biological activity. Stimulates the caspase-1 activating NLRP3/NALP3 inflammasome, resulting in the production of active IL-1beta and IL-18.
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Cell permeable, potent and selective class IIb HDAC6 inhibitor (IC50 =11nM). Displays high selectivity over HDAC1 (IC50=1.5µM). Neuroprotective. Effectively prevents neuronal cell death upon oxidative stress induction by HCA and selectively induces cellular alpha-tubulin hyperacetylation. HDAC6 deacetylates tubulin, HSP90 and the core histones (H2A, H2B, H3, H4). Histone deacetylases act via the formation of large […]
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Cell permeable, potent and selective class IIb HDAC6 inhibitor (IC50 =114nM). Displays selectivity over other HDACs (IC50=1-8µM). Neuroprotective and anti-neuroinflammatory agent. Reduced neuronal degeneration after traumatic brain injury (TBI). Shown to increase histone H3 acetylation. HDAC6 deacetylates tubulin, HSP90 and the core histones (H2A, H2B, H3, H4). Histone deacetylases act via the formation of large […]
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Cell permeable, potent and selective class IIb HDAC6 inhibitor (IC50 =114nM). Displays selectivity over other HDACs (IC50=1-8µM). Neuroprotective and anti-neuroinflammatory agent. Reduced neuronal degeneration after traumatic brain injury (TBI). Shown to increase histone H3 acetylation. HDAC6 deacetylates tubulin, HSP90 and the core histones (H2A, H2B, H3, H4). Histone deacetylases act via the formation of large […]
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Cell permeable, potent and selective class IIb HDAC6 inhibitor (IC50 =7.5nM). Displays high selectivity over HDAC1-9 (IC50=1-10µM). Shows improved brain bioavailability compared to tubastatin A (Prod. No. AG-CR1-3900). Induces hyperacetylation of alpha-tubulin in brain without concurrently altering the acetylation of histones. Shows antidepressant activity. HDAC6 deacetylates tubulin, HSP90 and the core histones (H2A, H2B, H3, […]
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Cell permeable, potent and selective class IIb HDAC6 inhibitor (IC50 =7.5nM). Displays high selectivity over HDAC1-9 (IC50=1-10µM). Shows improved brain bioavailability compared to tubastatin A (Prod. No. AG-CR1-3900). Induces hyperacetylation of alpha-tubulin in brain without concurrently altering the acetylation of histones. Shows antidepressant activity. HDAC6 deacetylates tubulin, HSP90 and the core histones (H2A, H2B, H3, […]
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Cell permeable, potent and selective class IIb HDAC6 inhibitor (IC50=3nM). Displays high selectivity over HDAC1 (300-fold). More soluble analog of nexturastat A (Prod. No. AG-CR1-3901). Suppresses cell proliferation of B16 cells (GI50=14.3µM) and human lymphoma cells HuT-78 at a slightly lower concentration than nexturastat A. Shown to be effective in a mouse melanoma tumor xenograft […]
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Cell permeable, potent and selective class IIb HDAC6 inhibitor (IC50=3nM). Displays high selectivity over HDAC1 (300-fold). More soluble analog of nexturastat A (Prod. No. AG-CR1-3901). Suppresses cell proliferation of B16 cells (GI50=14.3µM) and human lymphoma cells HuT-78 at a slightly lower concentration than nexturastat A. Shown to be effective in a mouse melanoma tumor xenograft […]
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