2. Stem Cell/Wnt TGF-beta/Smad
  3. Organoid TGF-β Receptor
  4. A 83-01

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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1 mg USD 40 In-stock
5 mg USD 65 In-stock
10 mg USD 108 In-stock
50 mg USD 336 In-stock
100 mg USD 500 In-stock
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Customer Review

Based on 49 publication(s) in Google Scholar

Other Forms of A 83-01:

A 83-01 Related Antibodies

Top Publications Citing Use of Products

47 Publications Citing Use of MCE A 83-01

WB
IF

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

    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.

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

    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.

    View All TGF-β Receptor Isoform Specific Products:

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    ALK1 ALK2 ALK3 ALK4 ALK5 ALK6 ALK7 TGFβR2 ACVR2A ACVR2B

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    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[1]

    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].

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

    A 83-01 Related Antibodies
    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].

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

    421.52

    Formula

    C25H19N5S
    CAS No.
    Appearance

    Solid

    Color

    Off-white to light yellow

    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 : 100 mg/mL (237.24 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 2.3724 mL 11.8618 mL 23.7237 mL
    5 mM 0.4745 mL 2.3724 mL 4.7447 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    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    40% PEG300    5% Tween-80    45% Saline

      Solubility: 2.5 mg/mL (5.93 mM); Clear solution; Need ultrasonic

      This protocol yields a clear solution of 2.5 mg/mL.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

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

      Solubility: 2.5 mg/mL (5.93 mM); Clear solution; Need ultrasonic

      This protocol yields a clear solution of 2.5 mg/mL. 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.

    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 compound is unstable in solutions, freshly prepared is recommended.

    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: 99.41%

    COA (259 KB) HNMR (144 KB) RP-HPLC (248 KB)

    Handling Instructions (2659 KB)
    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

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.3724 mL 11.8618 mL 23.7237 mL 59.3092 mL
    5 mM 0.4745 mL 2.3724 mL 4.7447 mL 11.8618 mL
    10 mM 0.2372 mL 1.1862 mL 2.3724 mL 5.9309 mL
    15 mM 0.1582 mL 0.7908 mL 1.5816 mL 3.9539 mL
    20 mM 0.1186 mL 0.5931 mL 1.1862 mL 2.9655 mL
    25 mM 0.0949 mL 0.4745 mL 0.9489 mL 2.3724 mL
    30 mM 0.0791 mL 0.3954 mL 0.7908 mL 1.9770 mL
    40 mM 0.0593 mL 0.2965 mL 0.5931 mL 1.4827 mL
    50 mM 0.0474 mL 0.2372 mL 0.4745 mL 1.1862 mL
    60 mM 0.0395 mL 0.1977 mL 0.3954 mL 0.9885 mL
    80 mM 0.0297 mL 0.1483 mL 0.2965 mL 0.7414 mL
    100 mM 0.0237 mL 0.1186 mL 0.2372 mL 0.5931 mL
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    A 83-01 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:

    A 83-01909910-43-6OrganoidTGF-β ReceptorTransforming growth factor beta receptorsInhibitorinhibitorinhibit

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