1. Metabolic Enzyme/Protease
    Stem Cell/Wnt
    JAK/STAT Signaling
    PI3K/Akt/mTOR
    Apoptosis
  2. PAI-1
    STAT
    PI3K
    Akt
    Apoptosis
  3. ACT001

ACT001 

Cat. No.: HY-128861A Purity: 98.85%
Handling Instructions

ACT001 is an orally active PAI-1 inhibitor by inhibiting the phosphorylation of PI3K and AKT. ACT001 inhibits the phosphorylation of STAT3 and PD-L1 expression by directly binding to STAT3. ACT001, a fumarate salt form of DMAMCL (a prodrug of Micheliolide), can cross the blood-brain barrier. ACT001 has potent anti-glioblastoma (GBM) activity and immunomodulatory effects.

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

ACT001 Chemical Structure

ACT001 Chemical Structure

CAS No. : 1582289-91-5

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 528 In-stock
Estimated Time of Arrival: December 31
Solid or liquid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 528 In-stock
Estimated Time of Arrival: December 31
Solid or liquid
5 mg USD 480 In-stock
Estimated Time of Arrival: December 31
10 mg USD 750 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1500 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2400 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

ACT001 is an orally active PAI-1 inhibitor by inhibiting the phosphorylation of PI3K and AKT. ACT001 inhibits the phosphorylation of STAT3 and PD-L1 expression by directly binding to STAT3. ACT001, a fumarate salt form of DMAMCL (a prodrug of Micheliolide), can cross the blood-brain barrier. ACT001 has potent anti-glioblastoma (GBM) activity and immunomodulatory effects[1][2].

IC50 & Target[1][2]

p-STAT3

 

PI3K

 

Akt

 

In Vitro

ACT001 (0-1000 μM; 24-96 hours) decreases cell viability when the concentration was higher than 10 μM in SNB19, U251MG cell lines[1].
ACT001 (10 μM; 48 h) can induce apoptosis in U118MG cells. ACT001 (3.75, 7.5 μM; 48 h) combined with Cisplatin (1-100 μM) increases the apoptosis of U118MG cells over either drug alone[2].
ACT001 (20-80 μM) decreases the expression of PD-L1 and phosphorylation of STAT3 in a dose-dependent manner[1].
ACT001 (10-40 μM) significantly decreases PD-L1 expression in a dose-dependent manner[1].
ACT001 (10 μM) inhibits the migration, invasion and vascular formation ability of U118MG cells[2].

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

Cell Viability Assay[1]

Cell Line: SNB19, U251MG and TJ179 cell lines
Concentration: 10, 100, 1000 μM
Incubation Time: 24, 48, 72, 96 hours
Result: Cell viability decreased when the concentration was higher than 10 μM, and the TJ179 cell line was most sensitive to high concentrations (40-80 μM).

Apoptosis Analysis[2]

Cell Line: U118MG cells
Concentration: 10 μM
Incubation Time: 48 hours
Result: Inducd apoptosis and that the inhibition effects cannot be enhanced by PAI-1 knockdown.

Western Blot Analysis[1]

Cell Line: SNB19, U251MG and TJ179 cell lines
Concentration: 20, 40, 80 μM
Incubation Time:
Result: Decreased the p-STAT3 level whereas the STAT3 level did not vary significantly from that of β-Actin.
Decreased PD-L1 expression relative to the expression of the loading control β-Actin.

RT-PCR[1]

Cell Line: SNB19, U251MG and TJ179 cell lines
Concentration: 10, 20, 40 μM
Incubation Time:
Result: Significantly decreased PD-L1 expression in a dose-dependent manner.
In Vivo

ACT001 (100 or 400 mg/kg/day; Orally; starting on day 7 for 42 days) significantly causes survived longer than control mice and decreases p-STAT3 and PD-L1 expression with 400 mg/kg[1].
ACT001 (200 mg/kg/day; oral administration) enhances the antitumour effect of Cisplatin (2.5 mg/kg, once every 3 days, IP) in U118 xenograft model[2].

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

Animal Model: C57BL/6 immuno-competent mice (6 weeks old)[1]
Dosage: 100 or 400 mg/kg
Administration: Orally; every day starting on day 7 for 42 days
Result: Significantly caused survived longer than control mice with 400 mg/kg, and has no significant survival benefit with 100 mg/kg.
Decreases p-STAT3 and PD-L1 expression and inhibits the progression of glioma with 400 mg/kg.
Decreased M2 macrophage numbers and increases antitumor immune response with 400 mg/kg.
Molecular Weight

409.47

Formula

C₂₁H₃₁NO₇

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 200 mg/mL (488.44 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4422 mL 12.2109 mL 24.4218 mL
5 mM 0.4884 mL 2.4422 mL 4.8844 mL
10 mM 0.2442 mL 1.2211 mL 2.4422 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 5 mg/mL (12.21 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 5 mg/mL (12.21 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 5 mg/mL (12.21 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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ACT001
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