Bromosporine

Bromosporine, a chemical probe, 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-Fluorouracil (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].

Product Specifications

CAS Number

[1619994-69-2]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Apoptosis; CDK; Epigenetic Reader Domain; HIV

Type

Reference compound

Related Pathways

Anti-infection; Apoptosis; Cell Cycle/DNA Damage; Epigenetics

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/Bromosporine.html

Purity

99.89

Solubility

DMSO : 35 mg/mL (ultrasonic)

Smiles

O=C(OCC)NC1=CC(C2=CC=C(C)C(NS(=O)(C)=O)=C2)=NN3C1=NN=C3C

Molecular Formula

C17H20N6O4S

Molecular Weight

404.44

Precautions

H302, H315, H319, H335

References & Citations

[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.