1. Cell Cycle/DNA Damage
    PI3K/Akt/mTOR
  2. DNA-PK
    CRISPR/Cas9

KU-57788 (Synonyms: NU7441)

Cat. No.: HY-11006 Purity: 98.74%
Handling Instructions

KU-57788 is a potent and selective inhibitor of DNA-PK, with an IC50 of 13 nM, and also increases CRISPR/Cas9-mediated editing frequencies.

For research use only. We do not sell to patients.
KU-57788 Chemical Structure

KU-57788 Chemical Structure

CAS No. : 503468-95-9

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 73 In-stock
5 mg USD 66 In-stock
10 mg USD 108 In-stock
50 mg USD 346 In-stock
100 mg USD 484 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

KU-57788 is a potent and selective inhibitor of DNA-PK, with an IC50 of 13 nM, and also increases CRISPR/Cas9-mediated editing frequencies.

IC50 & Target[1]

DNA-PK

13 nM (IC50)

CRISPR/Cas9

 

In Vitro

NU7441 at non-toxic concentration of 0.3 μM induces radio-sensitization in non-small cell lung cancer cells irradiated with low-LET and high-LET radiation, and does not show double strand break-repair inhibition in irradiated cells. NU7441 (3 μM) shows significantly increased persistent γ-H2AX signals. NU7441 (0.3 μM) causes significant G2/M arrest and a remarkable increase of DNA fragmentation and enhances cellular senescence in irradiated H1299 cells[1]. NU7441 (0.5 to 10 µM) inhibits the growth of liver cancer HepG2 cells dose- and time-dependently. NU7441 reduces pDNA-PKcs (S2056) protein expression in liver cancer cells. Furthermore, double treatment of NU7441 and 60Coγ IR affects DNA damage repair[2]. NU7441 is solvent-exposed in BRD4, this inhibitor can be classified as a Type I BRD inhibitor[4]. NU7441 reduces the frequency of NHEJ while increasing the rate of HDR following Cas9-mediated DNA cleavage[5].

In Vivo

lung cancer cells irradiated with low-LET and high-LET radiation, and does not show double strand break-repair inhibition in irradiated cells. KU-57788 (3 μM) shows significantly increased persistent γ-H2AX signals. KU-57788 (0.3 μM) causes significant G2/M arrest and a remarkable increase of DNA fragmentation and enhances cellular senescence in irradiated H1299 cells[1]. KU-57788 (0.5 to 10 µM) inhibits the growth of liver cancer HepG2 cells dose- and time-dependently. KU-57788 reduces pDNA-PKcs (S2056) protein expression in liver cancer cells. Furthermore, double treatment of KU-57788 and 60Coγ IR affects DNA damage repair[2]. KU-57788 weakly inhibits BRD4 and BRDT with IC50s of 1 μM and 3.5 μM, respectively. KU-57788 is solvent-exposed in BRD4, this inhibitor can be classified as a Type I BRD inhibitor[4]. KU-57788 reduces the frequency of NHEJ while increasing the rate of HDR following Cas9-mediated DNA cleavage[5].

References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 2.4184 mL 12.0922 mL 24.1844 mL
5 mM 0.4837 mL 2.4184 mL 4.8369 mL
10 mM 0.2418 mL 1.2092 mL 2.4184 mL
Please refer to the solubility information to select the appropriate solvent.
Kinase Assay
[4]

The inhibitory activities of compounds against BRD4-1 and BRDT-1 are assessed by DSF using a StepOnePlus Real-Time PCR system. Purified BRD4-1 (4 μM final concentration; 10 mM HEPES (pH7.5), 100 mM NaCl, and 1 mM DTT), and BRDT-1 (4 μM final concentration; 50 mM phosphate (pH7.4), 100 mM NaCl, and 1 mM DTT) are assayed, in quadruplicates, in a 96-well plate. Inhibitors are added to a final concentration of 100 μM and 2% DMSO. Protein Thermal Shift Dye (1:8000) is used as the fluorescent probe, and fluorescence is measured using the ROX Reporter channel (620 nm). Protein stability is investigated by programing the thermocycler to increase the temperature from 25 to 99°C using 0.2°C increments and 10 s incubations per increment. The inflection point of the transition curve/melting temperature (Tm) is calculated using the Boltzmann equation within the Protein Thermal Shift Software (v.1.1). JQ1(+) and dinaciclib are used as controls for strong and weak binders of BRD4-1, respectively. The ΔTm is calculated by using DMSO control wells as a reference. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[2]

HepG2 cells (4000 per well) are cultured in a 96-well plate for 24 h. Once the cells complete the attachment, 0.1 µM, 1 µM, 5 µM, and 10 µM of KU-57788 are added to the culture media. After 12 h of KU-57788 treatment, 10% CCK-8 solution is added into the culture media, and the incubation continued for two h. OD450 values are determined by a spectrometer, and the results are analyzed to measure the cell growth. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

413.49

Formula

C₂₅H₁₉NO₃S

CAS No.

503468-95-9

SMILES

O=C1C=C(N2CCOCC2)OC3=C1C=CC=C3C4=CC=CC5=C4SC6=C5C=CC=C6

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
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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Product Name:
KU-57788
Cat. No.:
HY-11006
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