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  3. A-3 hydrochloride

A-3 hydrochloride 

Cat. No.: HY-125957
Handling Instructions

A-3 hydrochloride is a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases. It against PKA (Ki=4.3 µM), casein kinase II (Ki=5.1 µM) and myosin light chain kinase (MLCK) (Ki=7.4 µM). A-3 hydrochloride also inhibits PKC and casein kinase I with Ki values of 47 µM and 80 µM, respectively.

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

A-3 hydrochloride Chemical Structure

A-3 hydrochloride Chemical Structure

CAS No. : 78957-85-4

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10 mM * 1  mL in DMSO USD 132 In-stock
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10 mg USD 120 In-stock
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100 mg USD 560 In-stock
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Description

A-3 hydrochloride is a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases. It against PKA (Ki=4.3 µM), casein kinase II (Ki=5.1 µM) and myosin light chain kinase (MLCK) (Ki=7.4 µM). A-3 hydrochloride also inhibits PKC and casein kinase I with Ki values of 47 µM and 80 µM, respectively[1].

IC50 & Target[1]

CK1

80 μM (Ki)

CK2

5.1 μM (Ki)

PKC

47 μM (Ki)

PKA

4.3 μM (Ki)

In Vitro

A-3 hydrochloride inhibits MLC-kinase competitively with respect to ATP and that the Ki value is 7.4 μM. A-3 is also a competitive inhibitor of cAMP-dependent protein kinase, cGMP-dependent protein kinase, protein kinase C, casein kinase I, and casein kinase II, with respect to ATP, exhibits Ki values of 4.3 μM, 3.8 μM, 47 μM, 80 μM, and 5.1 μM, respectively[1].

Molecular Weight

321.22

Formula

C₁₂H₁₄Cl₂N₂O₂S

CAS No.

78957-85-4

SMILES

O=S(C1=C2C=CC=C(Cl)C2=CC=C1)(NCCN)=O.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (389.14 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1131 mL 15.5657 mL 31.1313 mL
5 mM 0.6226 mL 3.1131 mL 6.2263 mL
10 mM 0.3113 mL 1.5566 mL 3.1131 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: ≥ 2.08 mg/mL (6.48 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (6.48 mM); Clear solution

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

A-3A3A 3PKACasein KinaseCaMKPKCProtein kinase ACalmodulin-dependent protein kinasesCalmodulin-dependent kinasesProtein kinase CcaseinkinasecAMPMLC-kinasecalmodulininhibitorInhibitorinhibit

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Product Name:
A-3 hydrochloride
Cat. No.:
HY-125957
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