Bromosporine_product_DataBase

Bioactivity

Bromosporine is a potent BET inhibitor with an IC50 value of 2.1 μM for PCAF. Bromosporine can arrest cell cycle and induce apoptosis in cancer cells. Bromosporine exhibits excellent antitumor activity in xenograft mice model when combined with 5-FU (HY-90006). Bromosporine can increase CDK9 T-loop phosphorylation in HIV-1 latency models, resulting the protection of reactivate HIV-1 replication from latency. Bromosporine can be used to research colorectal cancer, acute myeloid leukemia (AML) and AIDS[1][2][3][4].

Target

IC50: 2.1 μM (PCAF)Apoptosis, BET, CDK9, HIV-1

Invitro

Bromosporine (0-1000 nM; 72 h) synergistically inhibits cell growth in CRC cells with 5-FU (HY-90006)[1].Bromosporine (various concentration; 48 h) causes a distinct increase in the cells arrested at G1 phase when combined with 5-FU[1].Bromosporine (various concentration; 48 h) decreases the expressions of PARP, caspase 3, and 9[1].Bromosporine (0.1, 0.5 and 1 μM; 6-10 days) inhibits AML cells in a dose-dependent manner[3].Bromosporine (2.5 μM; 72 h) activates HIV-1 replication in vitro in latent HIV-1 J-Lat clone C11 cells[4].Bromosporine (1-50 μM; 48 h) does not induce marked toxicity in primary CD4+ T cells[4]. Cell Proliferation Assay[1] Cell Line:

In Vivo

Bromosporine (100 mg/kg; i.p.; daily for 10 days) shows better antitumor activity than individual when co-treated with 5-FU (HY-90006)[1]. Animal Model:

Name

Bromosporine

CAS

1619994-69-2

Formula

C17H20N6O4S

Molar Mass

404.44

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

[1]. Cheng X, et al. BET inhibitor bromosporine enhances 5-FU effect in colorectal cancer cells. Biochem Biophys Res Commun. 2020 Jan 22;521(4):840-845. [2]. El-Shershaby MH, et al. From triazolophthalazines to triazoloquinazolines: A bioisosterism-guided approach toward the identification of novel PCAF inhibitors with potential anticancer activity. Bioorg Med Chem. 2021 Jul 15;42:116266. [3]. Picaud S, et al. Promiscuous targeting of bromodomains by bromosporine identifies BET proteins as master regulators of primary transcription response in leukemia. Sci Adv. 2016 Oct 12;2(10):e1600760. [4]. Pan H, et al. The bromodomain and extraterminal domain inhibitor bromosporine synergistically reactivates latent HIV-1 in latently infected cells. Oncotarget. 2017 Oct 6;8(55):94104-94116.

PeptideDB

Bromosporine

CAS: 1619994-69-2 F: C17H20N6O4S W: 404.44