Click Chemistry

GSK2801 is a selective, cell-permeable inhibitor of the BAZ2 family of bromodomain-containing proteins. GSK 2801 is selective for BAZ2A and BAZ2B inhibitors, with Kd values of 0.26 and 0.14 µM (IC50 values are 0.40 and 0.43 μM), respectively. GSK2801 does not interact with the bromodomains of BRD4(BD1), CREBBP, TRIM24/TIF1α, PB1(BD5), PCAF, or ATAD2. Reagent grade, for research purpose. Please contact us for GMP-grade inquiries.

GSK 5959 exhibits >100-fold selectivity for BRPF1 (IC50 = 80 nM) over a panel of 35 other bromodomains, including BRPF2/3 and BET family bromodomains. Inhibits BRPF1 interaction with histone H3.3, which is involved in the epigenetic regulation of gene expression and have been implicated in human cancer. Reagent grade, for research purpose. Please contact us for GMP-grade inquiries.

GSK 6853 is a potent and selective BRPF1 inhibitor. GSK 6853 exhibits >1600-fold selectivity for BRPF1 over other bromodomains (pIC50 values by TR-FRET are 8.1, 5.1/4.8 and 4.7/<4.3 for BRPF1, BRPF2/3 and BRD4 BD1/2, respectively). The structural analog of GSK 6853, GSK9311, serves as a good inactive control (125- and 185-fold reduced potency in cell-free and cell-based assays, respectively). Reagent grade, for research purpose. Please contact us for GMP-grade inquiries.

I-BRD9 is a selective cellular chemical probe for bromodomain-containing protein 9 (BRD9). I-BRD9 has a pIC50 value of 7.3 for BRD9 inhibitor, with greater than 700-fold selectivity over the BET family and 200-fold over the highly homologous bromodomain-containing protein 7 (BRD7). I-BRD9 is also shows a greater than 70-fold selectivity against a panel of 34 bromodomains. I-BRD9 downregulates CLEC1, DUSP6, FES and SAMSN1 genes in Kasumi-1 cells. Reagent grade, for research purpose. Please contact us for GMP-grade inquiries.

NI-57 is a selective and potent inhibitor of BRPF (Bromodomain and PHD Finger) family of proteins (BRPF1/2/3). NI 57 shows Kd values of 31, 108 and 408 nM, for BRPF1B, 2 and 3, respectively. NI 57 also exhibits >32-fold selectivity for BRPFs over BRD9 and other non-Class IV bromodomains. Inhibits RANKL-induced differentiation of primary murine bone marrow cells and human primary monocytes into osteoclasts. Reagent grade, for research purpose. Please contact us for GMP-grade inquiries.

OTX-015 is a selective BRD2, BRD3, and BRD4 inhibitor and inhibits the binding of BRD2, BRD3, and BRD4 to AcH4. OTX-015 has shown inhibition of BRD2, BRD3, and BRD4 with IC50 values are in the range 92 - 112 nM. OTX 015 displays antiproliferative effects at a sub-micromolar range in vitro in a wide range of solid tumor types and leukemias, downregulating c-Myc expression and inducing cell cycle arrest and apoptosis. Reagent grade, for research purpose. Please contact us for GMP-grade inquiries.

PFI 1 is a BET bromodomain inhibitor that exhibits inhibitory activity at BRD2 and BRD4. PFI-1 is a selective BET bromodomain inhibitor with activity at BRD2 (IC50 = 98 nM) and BRD4 (IC50 = 220 nM). PFI 1 induces apoptosis and G1 cell cycle arrest in BET inhibitor-sensitive cell lines (MV4;11). PFI 1 also downregulates Aurora B expression in MV4;11 cells. Reagent grade, for research purpose. Please contact us for GMP-grade inquiries.

PFI-3 is a selective chemical probe for SMARCA bromodomains that inhibits SMARCA2, SMARCA4 and PB1(5) bromodomains. PFI-3 is a probe that binds avidly to the structurally-similar SMARCA4 bromodomain and PB1(bromodomain 5) with Kd values of 89 and 48 nM, respectively. PFI-3 displays 30-fold selectivity over other sub-family branches and accelerates FRAP recovery in cells at a concentration of 1 μM. Reagent grade, for research purpose. Please contact us for GMP-grade inquiries.

PFI 4 is an SGC chemical probe for the bromodomains of the BRPF (BRomodomain and PHD Finger containing) scaffolding protein BRPF1B. PFI 4 specifically binds to BRPF1B with an IC50 = 172 nM and Kd =13 nM as determined by ITC. PFI 4 reduces recovery time in triple BRD cell construct in FRAP and is potent in cells with IC50 250nM, while showing no effect on BRPF1A. PFI 4 exhibits >100-fold selectivity for BRPF1 over a panel of other bromodomains including BRPF2 (BRD1), BRPF3 and BRD4. Reagent grade, for research purpose. Please contact us for GMP-grade inquiries.