|S7152||C646||<1 mg/mL||13 mg/mL||<1 mg/mL|
|S1848||Curcumin||<1 mg/mL||73 mg/mL||<1 mg/mL|
|S8740||A-485||<1 mg/mL||100 mg/mL||100 mg/mL|
|S8776||WM-1119||<1 mg/mL||78 mg/mL||<1 mg/mL|
|S7582||Anacardic Acid||<1 mg/mL||69 mg/mL||69 mg/mL|
|S9432||Ginkgolic Acid||69 mg/mL|
|S7476||MG149||<1 mg/mL||68 mg/mL||68 mg/mL|
- Histone Acetyltransferase阻害剤(7)
- 新Histone Acetyltransferase製品
C646 is an inhibitor for histone acetyltransferase, and inhibits p300 with a Ki of 400 nM in a cell-free assay. Preferentially selective for p300 versus other acetyltransferases.
Phosphorylation of STAT6 in butyrate-treated M2-BMDMs. Western blotting was performed with anti-phospho-STAT6, STAT6, and β-actin. Data are representative of three independent experiments. M2:M2 macrophage; But:butyrate.
Curcumin is the principal curcuminoid of the popular Indian spice turmeric, which is a member of the ginger family (Zingiberaceae). It is an inhibitor of p300 histone acetylatransferase（IC50~25 μM） and Histone deacetylase; activates Nrf2 pathway and supresses the activation of transcription factor NF-κB.
Effect of NC1, NC1-CUR, NC2 and NC2-CUR on SH-SY5Y cell viability. The cells were treated for 24 h with different dilutions(1:1, 1:2 and 1:4) of empty nanocapsules (NC1 and NC2) and nanocapsules containing curcumin (NC1-CUR and NC2-CUR) followed by measurement of cell viability by MTT reduction assay (panel A) and cell toxicity by LDH release assay (panel B). Data after normalization to vehicle-treated cells (100%, MTT assay) or to total LDH release (TritonX100-treated cells, 100%) are presented as a mean±SEM from 3-8 independent experiments with five replicates. *p < 0.05, **p < 0.01 and ***p<0.001 versus vehicle-treated cells; &&&p<0.001 NC1 versus NC1-CUR.
A-485 is a potent, selective and drug-like p300/CBP catalytic inhibitor with an IC50 of 0.06 μM for p300 HAT. It is selective over BET bromodomain proteins and >150 non-epigenetic targets.
WM-1119 is a highly potent, selective inhibitor of lysine acetyltransferase KAT6A with IC50 of 0.25 μM. It is 1,100-fold and 250-fold more active against KAT6A than against KAT5 or KAT7, respectively.
Anacardic Acid is a potent inhibitor of p300 and p300/CBP-associated factor histone acetyltranferases, which also has antibacterial activity, antimicrobial activity, prostaglandin synthase inhibition, and tyrosinase and lipoxygenase inhibition.
Western blot analysis of α-SMA expression in whole-lung lysates. Data are expressed as means ± SEM, *P < 0.05 versus vehicle and #P < 0.05 versus PQ (n = 4-6).
Ginkgolic acid, toxic phenolic compounds present in the fruits and leaves of Ginkgo biloba L., is a potent sumoylation inhibitor also reported to inhibit histone acetylation transferase (HAT).
MG149 is a potent histone acetyltransferase inhibitor with IC50 of 74 μM and 47 μM for Tip60 and MOF,respectively.