2. Epigenetics Apoptosis Cell Cycle/DNA Damage Anti-infection
  3. Epigenetic Reader Domain Apoptosis CDK HIV
  4. Bromosporine

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.

For research use only. We do not sell to patients.

Bromosporine Chemical Structure

Bromosporine Chemical Structure

CAS No. : 1619994-69-2

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Based on 3 publication(s) in Google Scholar

Bromosporine Related Antibodies

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Description

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].

IC50 & Target

HIV-1

 

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.

Bromosporine Related Antibodies

Cell Proliferation Assay[1]

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[1]

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[1]

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[3]

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[4]

Cell Line: PBMCs
Concentration: 1 μM, 2.5 μM, 5 μM, 10 μM, 25 μM and 50 μM
Incubation Time: 48 h
Result: Did not induce marked toxicity in primary CD4+ T cells with CC50 over 10 μM.
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

404.44

Formula

C17H20N6O4S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4726 mL 12.3628 mL 24.7255 mL
5 mM 0.4945 mL 2.4726 mL 4.9451 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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C2

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Volume (final)

V2

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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (6.18 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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.

  • Protocol 1

    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:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation

Purity: 99.69%

SDS (393 KB)

COA (254 KB) HNMR (137 KB) LCMS (255 KB)

Handling Instructions (2659 KB)
References

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
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Bromosporine Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Bromosporine1619994-69-2Epigenetic Reader DomainApoptosisCDKHIVCyclin dependent kinaseHuman immunodeficiency virusanticancerantitumorcolorectal cancerAMLAIDSHCT116HT29MV4;11KASUMI-1T cellsInhibitorinhibitorinhibit

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