Bromosporine

Research use only, not for human use.

Bromosporine is a broad spectrum inhibitor for bromodomains for BRD2/4/9 and CECR2 (IC50: 0.41/0.29/0.122/0.017 μM), respectively.

Bromosporine is a broad spectrum inhibitor for bromodomains and as such will be very useful in elucidating further biological roles of reader domains as well as a tool for the validation of functional assays. Proteins that contain BRDs have been implicated in the development of a large variety of diseases, including various cancers, inflammatory diseases and neurological diseases and the therapeutic potential of bromodomain inhibition has been shown in several of these diseases, such as HIV, cancer and inflammation.

Cell Proliferation Assay Cell Line:HCT116 and HT29 Concentration:0, 30, 60, 120, 240, 480 and 1000 nM Incubation Time:72 h Result:Synergistically inhibited cell growth in CRC cells with 5-FU (HY-90006) (0-16 μg/mL) and exhibited a dose-dependent manner.Cell Cycle Analysis Cell Line:HCT116 and HT29 Concentration:Various concentration Incubation Time:48 h Result:Caused a distinct increase in the cells arrested at G1 phase when combined with 5-FU (HY-90006). Western Blot Analysis Cell Line:HCT116 and HT29 Concentration:Various concentration Incubation Time:48 h Result:Elevated the level of apoptosis in both cell lines through cleavage of PARP, caspase 3, and 9.Cell Proliferation Assay Cell Line:MV4;11, KASUMI-1, OCI-AML3 and K562 Concentration:0.1, 0.5 and 1 μM Incubation Time:6-10 days Result:Inhibited these AML cells in a dose-dependent manner.Cell Cytotoxicity Assay Cell Line:PBMCs Concentration:1 μM, 2.5 μM, 5 μM, 10 μM, 25 μM and 50 μM Incubation Time:48 hResult:Did not induce marked toxicity in primary CD4+ T cells with CC50 over 10 μM.

Animal Model:Female BALB/c nude mice (5-6 weeks; injected with 1?×?106?cells/100?μL of HT116?cells) Dosage:100 mg/kg Administration:i.p.; daily for 10 days Result:Exhibited better antitumor activity than individual Bromosporine or 5-FU (HY-90006) when co-treated with the two agent.

Bromosporine

Others

Other Targets

BRD

Others-Field

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1619994-69-2

404.45

C17H20N6O4S

>98% (HPLC)

DMSO : ≥ 51.7 mg/mL; 127.83 mM

CCOC(=O)Nc1cc(nn2c(C)nnc12)c1cc(NS(=O)(=O)C)c(C)cc1

ethyl (3-methyl-6-(4-methyl-3-(methylsulfonamido)phenyl)-[1,2,4]triazolo[4,3-b]pyridazin-8-yl)carbamate

(-20℃)

With Ice Pack

≥ 2 years