Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
1 mg
5 mg
10 mg
1 mM
2.2451 mL
11.2254 mL
22.4507 mL
5 mM
0.4490 mL
2.2451 mL
4.4901 mL
10 mM
0.2245 mL
1.1225 mL
2.2451 mL
50 mM
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Description
C646 is an inhibitor for , and inhibits with a of 400 nM in a cell-free assay. Preferentially selective for p300 versus other acetyltransferases. C646 induces cell cycle arrest, and .
Features
Extensively used as a pharmacologic probe in cancer cells. Potential use for prostate and lung cancers.
C646 is an inhibitor for histone acetyltransferase, inhibits p300 with a K of 400 nM and is selective versus other acetyltransferases. C646 produces 86% inhibition of p300 in vitro at 10 μM. C646 is a classical reversible p300 inhibitor. C646 treatment (25μM) reduces histone H3 and H4 acetylation levels and abrogates TSA-induced acetylation in cells. C646 (20μM) induces apoptosis in androgen-sensitive and castration-resistant prostate cancer cell lines by interfering with AR and NF-kB pathways. C646 blocks dynamic acetylation of H3K4me3 globally in mouse and fly cells, and locally across the promoter and start-site of inducible genes in the mouse, thereby disrupting RNA polymerase II association and the activation of these genes.
In vivo
C646 infused into the ILPFC immediately after weak extinction training enhances the consolidation of fear extinction memory. C646 attenuates mechanical allodynia and thermal hyperalgesia, accompanied by a suppressed COX-2 expression, in the spinal cord.