1. TGF-beta/Smad
  2. TGF-β Receptor

A 83-01 

Cat. No.: HY-10432 Purity: >90.0%
Handling Instructions

A 83-01 is a potent inhibitor of TGF-β type I receptor ALK5 kinase, type I activin/nodal receptor ALK4 and type I nodal receptor ALK7, with IC50s of 12, 45 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 In-stock
50 mg USD 336 In-stock
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Other Forms of A 83-01:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

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

IC50 & Target

IC50: 12 nM (ALK5, cell-based), 45 nM (ALK4 cell-based), 7.5 nM (ALK7 cell-based)[1]

In Vitro

A 83-01 is a potent inhibitor of TGF-β type I receptor ALK5 kinase, type I activin/nodal receptor ALK4 and type I nodal receptor 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].

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].

References
Preparing Stock Solutions
Concentration Volume 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.
Cell Assay
[2]

A 83-01 is dissolved in DMSO[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]

A 83-01 is formulated in PBS with 0.5% DMSO[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
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

Storage

4°C, protect from light

Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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