1. Protein Tyrosine Kinase/RTK
    TGF-beta/Smad
  2. ALK
    TGF-β Receptor
  3. A 83-01

A 83-01 

Cat. No.: HY-10432 Purity: ≥98.0%
Handling Instructions

Un 83-01 est un inhibiteur puissant du récepteur TGF-β de type I ALK5 kinase, du récepteur nodal de type I ALK4 et du récepteur nodal de type I ALK7, avec IC50s de 12 nM, 45 nM et 7,5 nM contre la transcription induite par ALK5, ALK4 et ALK7, respectivement.

A 83-01 is a potent inhibitor of TGF-β type I receptor ALK5 kinase, type I nodal receptor ALK4 and type I nodal receptor ALK7, with IC50s of 12 nM, 45 nM and 7.5 nM against the transcription induced by ALK5, ALK4 and ALK7, respectively.

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

A 83-01 Chemical Structure

A 83-01 Chemical Structure

CAS No. : 909910-43-6

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10 mg USD 108 Ask For Quote & Lead Time
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Top Publications Citing Use of Products

    A 83-01 purchased from MCE. Usage Cited in: Gynecol Oncol. 2019 Jun;153(3):639-650.

    Analysis of E-cadherin, N-cadherin,MMP-2 and pSmad2 in SK-OV-3 and OVCAR-3 cells treated with platelets, A83-01 or their combination at protein levels (n=3). GAPDH is used as loading control.

    A 83-01 purchased from MCE. Usage Cited in: FASEB J. 2020 Aug;34(8):11185-11199.

    Changes in the expression of E-Cadherin (green) and Vimentin (red) are detected by immunofluorescence. TGF-β1-induced changes in the expression of protein markers during EMT were blocked after A83-01 treatment.

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    Description

    A 83-01 is a potent inhibitor of TGF-β type I receptor ALK5 kinase, type I nodal receptor ALK4 and type I nodal receptor ALK7, with IC50s of 12 nM, 45 nM and 7.5 nM against the transcription induced by ALK5, ALK4 and ALK7, respectively[1].

    IC50 & Target

    ALK5

    12 nM (IC50)

    ALK4

    45 nM (IC50)

    ALK7

    7.5 nM (IC50)

    In Vitro

    A 83-01 is a potent inhibitor of TGF-β type I receptor ALK5 kinase, ALK4 and ALK7, reduces the level of ALK-5-induced transcription with an IC50 of 12 nM in Mv1Lu cells, also blocks the ALK4-TD and ALK7-TD induced transcription with IC50s of 45 nM and 7.5 nM in R4-2 cells, and weakly suppresses that induced by constitutively active ALK-6, ALK-2, ALK-3, and ALK-1. A 83-01 (0.03-10 µM) potently prevents the growth-inhibitory effects of TGF-β, and completely inhibits the effect at 3 µM. A 83-01 (1-10 µM) inhibits TGF-β-induced Smad activation in HaCaT cells[1]. A 83-01 (1 µM) decreases cell motility, adhesion and invasion increased by TGF-β1 in HM-1 cells, but does not change cell proliferation[2].

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

    In Vivo

    A 83-01 (50, 150 and 500 μg/mouse, i.p.) significantly improves survival of the mice without body weight or neurobehavioral appearances[2]. A 83-01 (0.5 mg/kg, i.p.) shows a significantly strong antitumor effect in mice bearing M109 cells[3].

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

    Molecular Weight

    421.52

    Formula

    C₂₅H₁₉N₅S

    CAS No.

    909910-43-6

    SMILES

    S=C(N1N=C(C2=NC(C)=CC=C2)C(C3=CC=NC4=CC=CC=C34)=C1)NC5=CC=CC=C5

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    -20°C, protect from light, stored under nitrogen

    *The compound is unstable in solutions, freshly prepared is recommended.

    Solvent & Solubility
    In Vitro: 

    DMSO : 30 mg/mL (71.17 mM; Need ultrasonic)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.3724 mL 11.8618 mL 23.7237 mL
    5 mM 0.4745 mL 2.3724 mL 4.7447 mL
    10 mM 0.2372 mL 1.1862 mL 2.3724 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: ≥ 0.83 mg/mL (1.97 mM); Clear solution

    • 2.

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

      Solubility: 0.83 mg/mL (1.97 mM); Suspended solution; Need ultrasonic

    • 3.

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

      Solubility: ≥ 0.83 mg/mL (1.97 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    Cell Assay
    [2]

    HM-1 cells are seeded into a 96-well plate and are incubated for 18 hr. A 83-01 (1 μM) or vehicle are then added for 12 hr followed by the addition of TGF-β1 (1 ng/mL) or vehicle for 60 hr. The number of viable cells in each well is examined using the WST-1 assay[2].

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

    Animal Administration
    [2]

    Mice[2]
    Female B6C3F1 mice used for the in vivo studies are maintained under specific pathogen-free conditions. To evaluate the effect of A 83-01 on the survival of mice bearing peritoneal dissemination, HM-1 cells (1×106) are injected into the abdominal cavity via the left flank of the mouse. Starting the next day, A 83-01 (150 μg/body) or vehicles (PBS with 0.5% DMSO) are injected into the abdominal cavity three times per week. Mice are euthanized before reaching the moribund state[2].

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

    References

    Purity: ≥98.0%

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    Keywords:

    A 83-01ALKTGF-β ReceptorAnaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246Transforming growth factor beta receptorsInhibitorinhibitorinhibit

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    Product Name:
    A 83-01
    Cat. No.:
    HY-10432
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