5.30535

RPA Inhibitor, TDRL-505

• 동의어(들): RPA Inhibitor, TDRL-505, Replication Protein A Inhibitor, Pot1 Inhibitor, Protection of Telemeres Protein 1 Inhibitor, TDRL505
• 실험식(Hill 표기법): C₂₄H₂₁BrClN₃O₄
• CAS Number: 1785760-75-9
• Molecular Weight: 530.80
• UNSPSC 코드: 12352200
• PubChem Substance ID: 5212392
• NACRES: NA.77

속성

• 분석: ≥97% (HPLC)
• Quality Level: 100
• 형태: solid
• 제조업체/상표: Calbiochem^®
• 저장 조건: OK to freeze; protect from light
• 색상: off-white
• solubility: DMSO: 50 mg/mL
• 저장 온도: −20°C
• SMILES string: CCOC1=CC2=NC(=C(C=C2C=C1)C3CC(=NN3C(=O)CCC(=O)O)C4=CC=C(C=C4)Br)Cl

설명

일반 설명

A cell-permeable quinolinyl-dihydropyrazolyl-oxobutanoic acid compound that is shown to target human Replication Protein A (RPA) via primarily the oligosaccharide/oligonucleotide-binding (OB) folds of DNA-bonding domains A & B (DBD-A/B) in the p70 subunit, effectively inhibiting its DNA-binding activity as well as that of Schizosaccharomyces pombe telemere end-binding protein Pot1 (IC₅₀= 12.9 µM and 15.7 µM, respectively), but not Xeroderma pigmentosum group A protein (XPA) involved in the nucleotide excision repair (NER) pathway or E. coli SSB. Reported to induce cell cycle G1-arrest and decrease Annvex V^-/PI^- healthy cell population (by 50%; 30.8 µM for 48 h) in H460 non-small cell lung carcinoma (NSCLC) cultures with minimal cytotoxicity against freshly isolated human PBMC. Potentiates cisplatin (Cat. No. 232120) and etopside (Cat. No. 341205) cytotoxicity in H460 cultures in a synergistic manner.

A cell-permeable quinolinyl-dihydropyrazolyl-oxobutanoic acid compound that is shown to target human Replication Protein A via primarily the oligosaccharide/oligonucleotide-binding (OB) folds of DNA-bonding domains A & B (DBD-A/B) in the p70 subunit, effectively inhibiting its DNA-binding activity as well as that of Schizosaccharomyces pombe telemere end-binding protein Pot1 (IC₅₀= 12.9 µM/25 nM hRPA/25 nM 34-base AG-rich ssDNA and 15.7 µM/20 nM SpPot1 DBD/25 nM 15-base ssDNA), but not Xeroderma pigmentosum group A protein (XPA) involved in the nucleotide excision repair (NER) pathway or E. coli SSB (20% inhibition at 100 µM against 3.3 nM EcSSB & 25 nM 3Pc3 ssDNA binding). Reported to cause decreased nuclear RPA staining (50 µM for 3 h), cell cycle G1-arrest (75 to 100 µM), and a drop in Annvex V^-/PI^- healthy cell population (by 50%; 30.8 µM for 48 h) in H460 non-small cell lung carcinoma (NSCLC) cultures with minimal cytotoxicity against freshly isolated human PBMC. Potentiates cisplatin (Cat. No. 232120) and etopside (Cat. No. 341205) cytotoxicity in H460 cultures in a synergistic manner, consistent with blockage of RPA-mediated NER pathway.

생화학적/생리학적 작용

Cell permeable: yes

Primary Target
Replication Protein A

Reversible: yes

Target IC₅₀: 12.9, 15.7 and 30.8 &micro

포장

Packaged under inert gas

경고

Toxicity: Standard Handling (A)

재구성

Use only fresh DMSO for reconstitution.

기타 정보

Anciano Granadillo, V.J., et al. 2010. J. Nucleic Acids2010, 304035.

Shuck, S.C., and Turchi, J.J. 2010. Cancer Res.70, 3189.

법적 정보

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

안전성 정보

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point (°F): Not applicable
• Flash Point (°C): Not applicable