Skip to Content
Merck
All Photos(1)

Key Documents

More Documents

SML2496

Sigma-Aldrich

D-I03

≥98% (HPLC)

Synonym(s):

1-(2-(Diethylamino)ethyl)-3-(2-(4-ethylpiperazin-1-yl)-4-methylquinolin-6-yl)thiourea, N-[2-(Diethylamino)ethyl]-N′-[2-(4-ethyl-1-piperazinyl)-4-methyl-6-quinolinyl]-thiourea

Sign Into View Organizational & Contract Pricing
All Photos(1)

About This Item

Empirical Formula (Hill Notation):
C23H36N6S
CAS Number:
688342-78-1
Molecular Weight:
428.64
UNSPSC Code:
12352200

Assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

SMILES string

S=C(NCCN(CC)CC)NC1=CC2=C(C=C1)N=C(N3CCN(CC)CC3)C=C2C

Biochem/physiol Actions

D-I03 is a selective RAD52 inhibitor (IC50 = 5 and 8 μM, respectively, by SSA and DNA pairing (D-loop formation) assay; <5% RAD51 inhibition at 80 μM) that blocks single-strand DNA (ssDNA) annealing (SSA)-, but not homology dependent recombination (HDR)-, mediated double-strand break (DSB) repair (5-30 μM using respective U2OS reporter cells) and reduces nuclear RAD52, but not RAD51, foci formation (2.5 μM) upon DNA damage by cisplatin. D-I03 selectively suppresses BRCA1-deficient over BRCA1-proficient cancer cells and exerts synergistic activity with PARP1 inhibitors against BRCA1-deficient cancer both in cultures (1 & 2.5 μM) and in mice (50 mg/kg/day i.p.) in vivo.

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

Already Own This Product?

Find documentation for the products that you have recently purchased in the Document Library.

Visit the Document Library

Katherine Sullivan-Reed et al.
Cell reports, 23(11), 3127-3136 (2018-06-14)
PARP inhibitors (PARPis) have been used to induce synthetic lethality in BRCA-deficient tumors in clinical trials with limited success. We hypothesized that RAD52-mediated DNA repair remains active in PARPi-treated BRCA-deficient tumor cells and that targeting RAD52 should enhance the synthetic
Fei Huang et al.
Nucleic acids research, 44(9), 4189-4199 (2016-02-14)
RAD52 is a member of the homologous recombination (HR) pathway that is important for maintenance of genome integrity. While single RAD52 mutations show no significant phenotype in mammals, their combination with mutations in genes that cause hereditary breast cancer and

Our team of scientists has experience in all areas of research including Life Science, Material Science, Chemical Synthesis, Chromatography, Analytical and many others.

Contact Technical Service