1. Cell Cycle/DNA Damage
    PI3K/Akt/mTOR
  2. DNA-PK
  3. LTURM34

LTURM34 

Cat. No.: HY-101667 Purity: 99.24%
Handling Instructions

LTURM34 is a specific DNA-PK inhibitor (IC50=34 nM). LTURM34 exhibits 170-fold selectivity for DNA-PK over PI3K. LTURM34 shows potent antiproliferative activity in a wide range of tumor cell lines.

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

LTURM34 Chemical Structure

LTURM34 Chemical Structure

CAS No. : 1879887-96-3

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 145 In-stock
Estimated Time of Arrival: December 31
5 mg USD 132 In-stock
Estimated Time of Arrival: December 31
10 mg USD 216 In-stock
Estimated Time of Arrival: December 31
50 mg USD 864 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1440 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

LTURM34 is a specific DNA-PK inhibitor (IC50=34 nM). LTURM34 exhibits 170-fold selectivity for DNA-PK over PI3K. LTURM34 shows potent antiproliferative activity in a wide range of tumor cell lines[1].

IC50 & Target[1]

DNA-PK

34 nM (IC50)

PI3Kβ

5.8 μM (IC50)

PI4Kδ

8.5 μM (IC50)

In Vitro

LTURM34 shows potent inhibition of DNA-PK with excellent selectivity over the Class I PI3K isoforms. The IC50s are 5.8 and 8.5 μM for PI3K β and δ, respectively. LTURM34 is more consistently active against the selected cell lines (11 of 16), but at best shows 54% inhibition against the HOP-92 non-small cell lung cancer line[1].

Molecular Weight

414.48

Formula

C₂₄H₁₈N₂O₃S

CAS No.

1879887-96-3

SMILES

O=C1C2=CC=CC(C3=CC=CC4=C3SC5=C4C=CC=C5)=C2OC(N6CCOCC6)=N1

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 : ≥ 37.5 mg/mL (90.47 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4127 mL 12.0633 mL 24.1266 mL
5 mM 0.4825 mL 2.4127 mL 4.8253 mL
10 mM 0.2413 mL 1.2063 mL 2.4127 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Kinase Assay
[1]

LTURM34 is dissolved at 10 mM in DMSO and stored at -20°C until use. PI3K enzyme activity is determined in 50 μL of 20 mM HEPES pH 7.5, 5 mM MgCl2 with 180 μM PI and 10 μM ATP. After a 60 min incubation at room temperature the reaction is stopped by the addition of 50 μl of Kinase-Glo followed by a further 15 min incubation. Luminescence is then read using a luostar plate reader. LTURM34 is diluted in 20% (v/v) DMSO at the ndicated concentrations in order to generate a concentration versus inhibition of enzyme activity curve which is then analysed using GraphPad Prism version 5.00 for Windows, in order to calculate the IC50[1].

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

References
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LTURM34
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