BRPF2 Inhibitor
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BAY-299
0 ImagesBAY-299, a chemical probe, is a very potent, dual inhibitor with IC50s of 67 nM for BRPF2 bromodomains (BD), 8 nM for TAF1 BD2, and 106 nM for TAF1L BD2.
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GSK9311
0 ImagesGSK9311, a less active analogue of GSK6853, can be used as a negative control. GSK9311 inhibits BRPF bromodomain with pIC50 values of 6.0 and 4.3 for BRPF1 and BRPF2, respectively.
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NI-42
0 ImagesNI-42 (compound 13-d), a structurally orthogonal chemical probe for the BRPFs, is a biased, potent inhibitor of the BRD of the BRPFs (IC50s of BRPF1/2/3=7.9/48/260 nM; Kds of BRPF1/2/3=40/210/940 nM) with excellent selectivity over nonclass IV BRD proteins.
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GSK9311 hydrochloride
0 ImagesCat. No.: HY-100729ACAS No.: 2253733-09-2GSK9311 hydrochloride, a less active analogue of GSK6853, can be used as a negative control. GSK9311 hydrochloride inhibits BRPF bromodomain with pIC50 values of 6.0 and 4.3 for BRPF1 and BRPF2, respectively.
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BRPF1B/TRIM24-IN-1
0 ImagesCat. No.: HY-122626CAS No.: 1242907-48-7BRPF1B/TRIM24-IN-1 (compound 34) is a potent TRIM24/BRPF1/BRPF2 inhibitor, with IC50 values of 0.43, 0.34, 1.75 μM, respectively. BRPF1B/TRIM24-IN-1 binds the TRIM24 bromodomain with a KD of 222 nM and has a KD for the BRPF1 bromodomain of 137 nM and for BRD1 of 1130 nM.
