Click Chemistry

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. 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.

SGC-CBP30 is a potent CBP/p300 bromodomain (BRD) inhibitor. SGC-CBP30 shows Kd values are 21 and 32 nM for CBP and p300 BRDs respectively. SGC-CBP30 also exhibits 40-fold and 250-fold selectivity for CBP over the first BRD of BRD4 (BRD4(1)) and BRD4(2) respectively. SGC-CBP30 accelerates FRAP recovery in cells at a concentration of 1 μM. Reagent grade, for research purpose. Please contact us for GMP-grade inquiries.