Bromosporine
Based on 5 publication(s) in Google Scholar
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.
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- Purity : 99.89%
- CAS No.: 1619994-69-2
- 화학식: C17H20N6O4S
- 분자량:404.44
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
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HY-16586
PFI-1BET Inhibitor -
HY-15826
SGC-CBP30CBP/p300 Inhibitor -
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(+)-JQ-1BET Inhibitor -
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MolibresibBET Inhibitor -
HY-13235
I-BET151BRD2/3/4 Inhibitor -
HY-18975
I-BRD9Chemical Probe -
HY-100352
BI-9564BRD9/BRD7 Bromodomains Inhibitor -
HY-14443
XMD8-92ERK5/BRD4 Inhibitor -
HY-15743
BirabresibBRD2/3/4 Inhibitor -
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WM-3835HBO1 Inhibitor -
HY-16652
ApabetaloneBET Inhibitor -
HY-B0627
MetforminAntihyperglycemic Agent
Publications Citing Use of MedChemExpress (MCE) Bromosporine
More
Biological Activity
제품 설명
IC50 & Target
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HIV-1 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| A549 | GI50 |
5.02 μM
Compound: 6; BSP
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Growth inhibition of human A549 cells
Growth inhibition of human A549 cells
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[PMID: 36736153] |
| HCT-116 | GI50 |
6.25 μM
Compound: 6; BSP
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Growth inhibition of human HCT-116 cells
Growth inhibition of human HCT-116 cells
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[PMID: 36736153] |
| HOP-62 | GI50 |
381 nM
Compound: 6; BSP
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Growth inhibition of human HOP-62 cells
Growth inhibition of human HOP-62 cells
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[PMID: 36736153] |
| NCI-H460 | GI50 |
5.35 μM
Compound: 6; BSP
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Growth inhibition of human NCI-H460 cells
Growth inhibition of human NCI-H460 cells
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[PMID: 36736153] |
| SF-268 | GI50 |
395 nM
Compound: 6; BSP
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Growth inhibition of human SF-268 cells
Growth inhibition of human SF-268 cells
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[PMID: 36736153] |
| UO-31 | GI50 |
334 nM
Compound: 6; BSP
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Growth inhibition of human UO-31 cells
Growth inhibition of human UO-31 cells
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[PMID: 36736153] |
In Vitro
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT116 and HT29
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Concentration:0, 30, 60, 120, 240, 480 and 1000 nM
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Incubation Time:72 h
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Result:Synergistically inhibited cell growth in CRC cells with 5-FU (HY-90006) (0-16 μg/mL) and exhibited a dose-dependent manner.
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Cell Line:HCT116 and HT29
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Concentration:Various concentration
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Incubation Time:48 h
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Result:Caused a distinct increase in the cells arrested at G1 phase when combined with 5-FU (HY-90006).
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Cell Line:HCT116 and HT29
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Concentration:Various concentration
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Incubation Time:48 h
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Result:Elevated the level of apoptosis in both cell lines through cleavage of PARP, caspase 3, and 9.
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Cell Line:MV4;11, KASUMI-1, OCI-AML3 and K562
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Concentration:0.1, 0.5 and 1 μM
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Incubation Time:6-10 days
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Result:Inhibited these AML cells in a dose-dependent manner.
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Cell Line:PBMCs
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Concentration:1 μM, 2.5 μM, 5 μM, 10 μM, 25 μM and 50 μM
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Incubation Time:48 h
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Result:Did not induce marked toxicity in primary CD4+ T cells with CC50 over 10 μM.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
- Western Blot
- Annexin V plus membrane-impermeant dye apoptosis staining
- BrdU Incorporation Assay
- Protocol for Cell Cycle
- Kinase activity and phosphorylation assays
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Flow cytometric DNA-content cell-cycle staining
- Patient-Derived Xenograft (PDX)
- Apoptosis Solutions
- Splenic/Portal-Vein Liver Metastasis Xenograft
- Protocol for Kinase activity and phosphorylation assays
- Subcutaneous Cell-Line-Derived Xenograft
- Orthotopic Cell-Line Xenograft
- Intraperitoneal/Peritoneal Dissemination Xenograft
Chemical Information
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CAS No. 1619994-69-2
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Appearance Solid
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분자량 404.44
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화학식 C17H20N6O4S
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Color White to off-white
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SMILES
O=C(OCC)NC1=CC(C2=CC=C(C)C(NS(=O)(C)=O)=C2)=NN3C1=NN=C3C
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (5)
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Journal Impact Factor
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Most Recent
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Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
Proc Natl Acad Sci U S A
2019 Feb 19;116(8):2961-2966. PMID: 30718431 -
Biochem Pharmacol
Metabolically stable diphenylamine derivatives suppress androgen receptor and BET protein in prostate cancer. [Abstract]2020 Jul:177:113946. PMID: 32247852 -
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용액&용해도
In Vitro:
DMSO : 35 mg/mL (86.54 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 10 mg/mL (24.73 mM); Suspended solution; Need ultrasonic
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (286 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4726 mL | 12.3628 mL | 24.7255 mL | 61.8139 mL |
| 5 mM | 0.4945 mL | 2.4726 mL | 4.9451 mL | 12.3628 mL | |
| 10 mM | 0.2473 mL | 1.2363 mL | 2.4726 mL | 6.1814 mL | |
| 15 mM | 0.1648 mL | 0.8242 mL | 1.6484 mL | 4.1209 mL | |
| 20 mM | 0.1236 mL | 0.6181 mL | 1.2363 mL | 3.0907 mL | |
| 25 mM | 0.0989 mL | 0.4945 mL | 0.9890 mL | 2.4726 mL | |
| 30 mM | 0.0824 mL | 0.4121 mL | 0.8242 mL | 2.0605 mL | |
| 40 mM | 0.0618 mL | 0.3091 mL | 0.6181 mL | 1.5453 mL | |
| 50 mM | 0.0495 mL | 0.2473 mL | 0.4945 mL | 1.2363 mL | |
| 60 mM | 0.0412 mL | 0.2060 mL | 0.4121 mL | 1.0302 mL | |
| 80 mM | 0.0309 mL | 0.1545 mL | 0.3091 mL | 0.7727 mL |
Bromosporine Related Classifications
HY-15815 Related Classifications
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