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

Bromosporine 

Cat. No.: HY-15815 Purity: 99.69%
COA Handling Instructions

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

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 140 In-stock
Solution
10 mM * 1 mL in DMSO USD 140 In-stock
Solid
5 mg USD 127 In-stock
10 mg USD 231 In-stock
50 mg USD 726 In-stock
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Customer Review

Based on 3 publication(s) in Google Scholar

Bromosporine Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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

IC50: 2.1 μM (PCAF)[2]
Apoptosis, BET, CDK9, HIV-1[1][3][4]
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

Appearance

Solid

Formula

C17H20N6O4S
CAS No.
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 : ≥ 51.7 mg/mL (127.83 mM)

*"≥" means soluble, but saturation unknown.

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
10 mM 0.2473 mL 1.2363 mL 2.4726 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

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

*All of the co-solvents are available by MedChemExpress (MCE).
Purity & Documentation

Purity: 99.69%

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

Handling Instructions (2659 KB)
References
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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.

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Keywords:

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

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