1. Cell Cycle/DNA Damage
  2. LIM Kinase (LIMK)
  3. TH-257

TH-257 

Cat. No.: HY-122630 Purity: 98.91%
Handling Instructions

TH-257 is a potent inhibitor of LIMK1 and LIMK2 with IC50 values of 84 nM and 39 nM for LIMK1 and LIMK2, respectively, and it can be used as a chemical probe for LIMK1 and LIMK2. TH-257 is an allosteric inhibitor targeting a binding pocket induced by an αC and DFG-out conformation. TH257 is exquisitely selective and no significant activity against the wider kinome has been observed in the KINOMEscan assay at 1 μM.

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

TH-257 Chemical Structure

TH-257 Chemical Structure

CAS No. : 2244678-29-1

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 80 In-stock
Estimated Time of Arrival: December 31
5 mg USD 73 In-stock
Estimated Time of Arrival: December 31
10 mg USD 113 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

TH-257 is a potent inhibitor of LIMK1 and LIMK2 with IC50 values of 84 nM and 39 nM for LIMK1 and LIMK2, respectively, and it can be used as a chemical probe for LIMK1 and LIMK2. TH-257 is an allosteric inhibitor targeting a binding pocket induced by an αC and DFG-out conformation. TH257 is exquisitely selective and no significant activity against the wider kinome has been observed in the KINOMEscan assay at 1 μM[1].

IC50 & Target[1]

LIMK1

84 nM (IC50)

LIMK2

39 nM (IC50)

Molecular Weight

422.54

Formula

C₂₄H₂₆N₂O₃S

CAS No.

2244678-29-1

SMILES

O=C(N(CCCC)CC1=CC=CC=C1)C2=CC=C(S(=O)(NC3=CC=CC=C3)=O)C=C2

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 : 250 mg/mL (591.66 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3666 mL 11.8332 mL 23.6664 mL
5 mM 0.4733 mL 2.3666 mL 4.7333 mL
10 mM 0.2367 mL 1.1833 mL 2.3666 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 (4.92 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (4.92 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.08 mg/mL (4.92 mM); Clear solution

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

TH-257TH257TH 257LIM Kinase (LIMK)LIMKsInhibitorinhibitorinhibit

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Product name:
TH-257
Cat. No.:
HY-122630
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