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Cat. No.: HY-146565

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DNA-PK-IN-8

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DNA-PK-IN-8 is a highly potent, selective and orally active DNA-dependent protein kinase (DNA-PK) inhibitor with an IC₅₀ value of 0.8 nM. DNA-PK-IN-8 exhibits synergistic antiproliferative activity against a series of cancer cell lines and significantly suppresses HL-60 tumor growth, when using in combination with Doxorubicin.

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

Purity: 99.74%
CAS No.: 2823369-81-7
Formula: C₁₉H₂₂N₈O₂
Molecular Weight:394.43

Storage:

4°C, stored under nitrogen, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)

DNA-PK-IN-8 Chemical Structure

CAS No.: 2823369-81-7

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

IC₅₀: 0.8 nM (DNA-PK)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
B16-F10	IC₅₀	20.6 μM Compound: DKI	Synergistic antiproliferative activity against mouse B16-F10 cells assessed as reduction in cell viability incubated for 48 hrs in presence of doxorubicin by CCK-8 assay Synergistic antiproliferative activity against mouse B16-F10 cells assessed as reduction in cell viability incubated for 48 hrs in presence of doxorubicin by CCK-8 assay	[PMID: 38587857]
B16-F10	IC₅₀	46.8 μM Compound: DKI	Antiproliferative activity against mouse B16-F10 cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay Antiproliferative activity against mouse B16-F10 cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay	[PMID: 38587857]
CT26	IC₅₀	32.9 μM Compound: DKI	Antiproliferative activity against mouse CT26 cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay Antiproliferative activity against mouse CT26 cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay	[PMID: 38587857]
CT26	IC₅₀	9.35 μM Compound: DKI	Synergistic antiproliferative activity against mouse CT26 cells assessed as reduction in cell viability incubated for 48 hrs in presence of doxorubicin by CCK-8 assay Synergistic antiproliferative activity against mouse CT26 cells assessed as reduction in cell viability incubated for 48 hrs in presence of doxorubicin by CCK-8 assay	[PMID: 38587857]
HCT-116	IC₅₀	17.1 μM Compound: DK1	Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 48 hrs in presence of 100 nM doxorubicin by MTT assay Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 48 hrs in presence of 100 nM doxorubicin by MTT assay	[PMID: 35468512]
HCT-116	IC₅₀	24.1 μM Compound: DK1	Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 35468512]
HL-60	IC₅₀	<100 nM Compound: DK1	Synergistic antiproliferative activity against human HL-60 cells assessed as inhibition of cell growth in presence of 100 nM doxorubicin by MTT assay Synergistic antiproliferative activity against human HL-60 cells assessed as inhibition of cell growth in presence of 100 nM doxorubicin by MTT assay	[PMID: 35468512]
Jurkat	IC₅₀	0.11 μM Compound: DKI	Synergistic antiproliferative activity against human Jurkat cells assessed as reduction in cell viability incubated for 48 hrs in presence of doxorubicin by CCK-8 assay Synergistic antiproliferative activity against human Jurkat cells assessed as reduction in cell viability incubated for 48 hrs in presence of doxorubicin by CCK-8 assay	[PMID: 38587857]
Jurkat	IC₅₀	11.4 μM Compound: DKI	Antiproliferative activity against human Jurkat cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay Antiproliferative activity against human Jurkat cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay	[PMID: 38587857]

In Vitro

DNA-PK-IN-8 (compound DK1) decreases the expression levels of γH2A.X in a concentration-dependent manner in HCT-116 cells^[1].

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

Immunofluorescence

Cell Line:

HCT-116 (treated with Bleomycin for 6 hours)^[1]
Concentration:

1, 5, and 10 μM
Incubation Time:

6 hours
Result:

Decreased the expression levels of γH2A.X in a concentration-dependent manner.

In Vivo

DNA-PK-IN-8 (100 mg/kg; PO; QD for 16 days) significantly suppresses HL-60 tumor growth when co-administrating with Doxorubicin^[1].
DNA-PK-IN-8 (5 mg/kg; PO; single dosage) exhibits reasonable pharmacokinetic properties in vitro and in vivo as an oral drug candidate^[1].
Pharmacokinetic Parameters of DNA-PK-IN-8 in Sprague-Dawley rats^[1].

	PO (5 mg/kg)
T_max (h)	0.42 ± 0.11
t_1/2 (h)	1.59 ± 0.26
C_max (ng/mL)	810 ± 122.32
AUC_0-∞ (ng/mL·h)	3598.7 ± 769.81
MRT_0-∞ (h)	2.29 ± 0.18

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

Animal Model:

HL-60 tumor-bearing nude mice model^[1]
Dosage:

100 mg/kg
Administration:

PO; QD for 16 days
Result:

Led to significant tumor-suppressing effects with TGI values of 52.4% and 62.4% for tumor weight and tumor volume, respectively, when co-administrated with Doxorubicin.

Animal Model:

Sprague-Dawley rats^[1]
Dosage:

5 mg/kg
Administration:

PO; single dosage (Pharmacokinetic Analysis)
Result:

Exhibited reasonable pharmacokinetic properties in vitro and in vivo as an oral drug candidate.

Chemical Information

CAS No. 2823369-81-7
Appearance Solid
Molecular Weight 394.43
Formula C₁₉H₂₂N₈O₂
Color White to light yellow
SMILES

CC1=CC2=NC=NN2C=C1NC3=NC=C4C(N(CC(N4C)=O)C5CCOCC5)=N3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, stored under nitrogen, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Ding Z, et al. Discovery of novel 7,8-dihydropteridine-6(5H)-one-based DNA-PK inhibitors as potential anticancer agents via scaffold hopping strategy. Eur J Med Chem. 2022;237:114401. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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DNA-PK-IN-8

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Biological Activity

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DNA-PK-IN-8 Related Classifications

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