BroMosporine
BroMosporine Basic information
- Product Name:
- BroMosporine
- Synonyms:
-
- BroMosporine
- ethyl 3-Methyl-6-(4-Methyl-3-(MethylsulfonaMido)phenyl)-[1,2,4]triazolo[4,3-b]pyridazin-8-ylcarbaMate
- N-[6-(3-Methanesulfonamido-4-methylphenyl)-3-methyl-[1,2,4]triazolo[4,3-b]pyridazin-8-yl]carbamate
- CS-921
- Carbamic acid, N-[3-methyl-6-[4-methyl-3-[(methylsulfonyl)amino]phenyl]-1,2,4-triazolo[4,3-b]pyridazin-8-yl]-, ethyl ester
- BroMosporine USP/EP/BP
- 11,Bromosporine,inhibit,AML,colorectal cancer,CDK,antitumor,T cells,HCT116,Apoptosis,HT29,anticancer,Epigenetic Reader Domain,Inhibitor,Cyclin dependent kinase
- KASUMI-1,HIV,AIDS,Human immunodeficiency virus,MV4
- CAS:
- 1619994-69-2
- MF:
- C17H20N6O4S
- MW:
- 404.44
- Product Categories:
-
- Inhibitors
- API
- Mol File:
- 1619994-69-2.mol
BroMosporine Chemical Properties
- Density
- 1.46±0.1 g/cm3(Predicted)
- storage temp.
- Sealed in dry,Store in freezer, under -20°C
- solubility
- Soluble in DMSO (up to 25 mg/ml)
- pka
- 6.21±0.46(Predicted)
- form
- solid
- color
- Off-white
- Stability:
- Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
- InChI
- 1S/C17H20N6O4S/c1-5-27-17(24)18-15-9-14(21-23-11(3)19-20-16(15)23)12-7-6-10(2)13(8-12)22-28(4,25)26/h6-9,22H,5H2,1-4H3,(H,18,24)
- InChIKey
- UYBRROMMFMPJAN-UHFFFAOYSA-N
- SMILES
- CC(C(NS(C)(=O)=O)=C1)=CC=C1C2=NN3C(C(NC(OCC)=O)=C2)=NN=C3C
BroMosporine Usage And Synthesis
Description
Bromosporine (1619994-69-2) is a potent pan-Bromodomain (BRD) inhibitor.1?Bromosporine was able to reactivate HIV-1 replication in different latency models.2
Uses
Bromosporine is a broad spectrum inhibitor for bromodomains.
in vivo
Bromosporine (100 mg/kg; i.p.; daily for 10 days) shows better antitumor activity than individual when co-treated with 5-Fluorouracil.html" class="link-product" target="_blank">5-FU (HY-90006)[1].
| Animal Model: | Female BALB/c nude mice (5-6 weeks; injected with 1?×?106?cells/100?μL of HT116?cells)[1] |
| 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. |
target
bromodomain
IC 50
HIV-1
storage
Store at +4°C
Background
Bromosporine is a potent broad-spectrum bromodomain inhibitor. Bromodomain and extra-terminal protein family members BRD2, BRD3, BRD4, and BRDT associate with acetylated lysines on histones and transcription factors to regulate their function, and have emerged as targets for cancer therapy. Treatment with Bromosporine induced the expression of latent HIV-1 in primary CD4+ T cells by inhibiting BET activity, leading to improved viral clearance in conjunction with antiretroviral therapy.
References
[1] SARAH PICAUD. Promiscuous targeting of bromodomains by bromosporine identifies BET proteins as master regulators of primary transcription response in leukemia[J]. Science Advances, 2016, 2 10. DOI:10.1126/sciadv.1600760
[2] HANYU PAN. The bromodomain and extraterminal domain inhibitor bromosporine synergistically reactivates latent HIV-1 in latently infected cells.[J]. Oncotarget, 2017: 94104-94116. DOI:10.18632/oncotarget.21585
BroMosporineSupplier
- Tel
- 1-631-485-4226; 16314854226
- info@bocsci.com
- Tel
- 021-58950125
- info@chemexpress.com
- Tel
- 027-87342388 18086026008
- sales@kaymke.com
- Tel
- +1 (866) 930-6790
- info@adooq.com
- Tel
- Mobile:13665161512