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.

DNA-PK-IN-8 Chemical Structure

CAS No. : 2823369-81-7

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Description

IC₅₀ & Target

IC₅₀: 0.8 nM (DNA-PK)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
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]

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.

Molecular Weight

394.43

Formula

C₁₉H₂₂N₈O₂

CAS No.

2823369-81-7

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

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]

DNA-PK-IN-8 Related Classifications

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

DNA-PK-IN-82823369-81-7DNA-PKDNA-dependent protein kinaseAnticancerDNADamage responseDSBHCT-116HL-60AntiproliferativeInhibitorinhibitorinhibit

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