1. Metabolic Enzyme/Protease Apoptosis
  2. Phosphatase Apoptosis
  3. OA-Br-1

OA-Br-1  (Synonyms: 3-O-(6-Bromo-D-mannosyl)-28-acylamino-n-caproate methyl oleanolic acid)

Cat. No.: HY-173165
Handling Instructions Technical Support

OA-Br-1 is an orally active and selective inhibitor of PTP1B with an IC50 value of 7.08 μM. OA-Br-1 induces apoptosis. OA-Br-1 has broad spectrum anti-proliferative activity against cancer cells, and plays an anti-breast cancer role through the PTP1B/PI3K/AKT signaling pathway both in vitro and in vivo.

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

OA-Br-1 Chemical Structure

OA-Br-1 Chemical Structure

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Description

OA-Br-1 is an orally active and selective inhibitor of PTP1B with an IC50 value of 7.08 μM. OA-Br-1 induces apoptosis. OA-Br-1 has broad spectrum anti-proliferative activity against cancer cells, and plays an anti-breast cancer role through the PTP1B/PI3K/AKT signaling pathway both in vitro and in vivo[1].

IC50 & Target

IC50: PTP1B (7.08 μM)[1]

In Vitro

OA-Br-1 shows stronger inhibitory activity against PTP1B with an IC50 value of 7.08 μM, and weak inhibitory activity against TCPTP, with an IC50 value of 222.28μM[1].
OA-Br-1 (24-72 h) inhibits the proliferation of breast cancer cells in a concentration- and time-dependent manner, with IC50 values on MCF-7, MDA-MB-231 and MDA-MB-453 after 72 h were 8.76, 18.13, and 22.34 μM, respectively[1].
OA-Br-1 (5-30 μM; 48 h) induces apoptosis in MCF-7 and MDA-MB-231 cells[1].
OA-Br-1 increases the thermal stability of PTP1B[1].
OA-Br-1 (5-30 μM; 48 h) decreases the community formed by MCF-7 and MDA-MB-231 cell clones in dose-dependent manner[1].
OA-Br-1 (5-30 μM; 48 h) decreases the protein levels of p-PI3K and p-AKT, exerts its antitumor effects through the PTP1B/PI3K/AKT signaling pathway in breast cancer cells[1].

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

Cell Proliferation Assay[1]

Cell Line: MCF-7, MDA-MB-231
Concentration: 5, 10, 20 μM in MCF-7, 10, 20, 30 μM in MDA-MB-231
Incubation Time: 48 h
Result: The community formed by the two cell clones decreased significantly in dose-dependent manner.

Apoptosis Analysis[1]

Cell Line: MCF-7, MDA-MB-231
Concentration: 5, 10, 20, 30 μM
Incubation Time: 48 h
Result: Cells began to show chromatin aggregation, green fluorescence spots, and a few red fluorescence, indicating most cells to enter the early apoptosis stage.
With the continuous increase concentration, the nucleus and chromatin further contracted and aggregated, the proportion of cells with red fluorescence increased, and most cells entered the late apoptotic stage and died.
Induced apoptosis of most breast cancer cells at 20 μM.

Western Blot Analysis[1]

Cell Line: MCF-7 cells
Concentration: 5, 10, 20, 30 μM
Incubation Time: 48 h
Result: Inhibited PTP1B protein expression in a concentration-dependent manner in MCF-7 cells.
Decreased the protein levels of p-PI3K and p-AKT.
In Vivo

OA-Br-1 (30-60 mg/kg; i.g.; every day) exerts anti-tumor effects in MCF-7 subcutaneous xenograft BALB/c female nude mice model through inhibition of PTP1B/PI3K/AKT signaling pathway[1].

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

Animal Model: BALB/c female nude mice (4 weeks old and weighing around 18 g) (5 x 106 MCF-7 cells in 200 μL FBS-free medium were subcutaneously injected into the left axilla)[1]
Dosage: 30, 60 mg/kg
Administration: Intragastric gavage (i.g.); every day
Result: Tumor growth, volume, and weight were inhibited, with no observed toxicity on body weight or major organ weight indices.
Suppressed the expression of PTP1B, as well as the phosphorylation level of PI3K and AKT protein in the tumor.
Molecular Weight

808.92

Formula

C43H70BrNO8

SMILES

BrC[C@H]1O[C@H](O[C@@H]2C(C)(C)[C@@](CC[C@]3(C)[C@]4([H])CC=C5[C@@]3(C)CC[C@]6(C(NCCCCCC(OC)=O)=O)[C@@]5([H])CC(C)(C)CC6)([H])[C@]4(C)CC2)[C@@H](O)[C@@H](O)[C@@H]1O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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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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OA-Br-1
Cat. No.:
HY-173165
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