SCH 529074

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SCH 529074

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Cat No: 21552

Biochemicals - Small Molecule Activators

SCH 529074 is a small molecule activator of p53, a tumor suppressor that is mutated or non-functional in 50% of human tumors.{41050} SCH 529074 restores DNA binding activity and increases DNA binding affinity of two recombinant GST fusion mutant p53 D...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

N3-[2-[[4-[bis(4-chlorophenyl)methyl]-1-piperazinyl]methyl]-4-quinazolinyl]-N1,N1-dimethyl-1,3-propanediamine

Correlated keywords:

p-53 oncogenic HDM2 anti-tumor antitumor SCH529074 DLD1

Product Overview:
SCH 529074 is a small molecule activator of p53, a tumor suppressor that is mutated or non-functional in 50% of human tumors.{41050} SCH 529074 restores DNA binding activity and increases DNA binding affinity of two recombinant GST fusion mutant p53 DNA binding domains (R273H and R249S) in an electrophoretic mobility shift assay with Kd values of 0.6740 and 0.4313, respectively. It also stimulates DNA binding activity and prevents human double minute-2 (Hdm-2) ubiquitination of wild-type p53 in vitro. SCH 29074 reduces proliferation of tumor cell lines with mutant and wild-type p53 (EC50s = 400-3,700 nM), with the p53 mutant cell lines being the most sensitive. In vivo, SCH 529074 reduces tumor growth in a DLD-1 human colorectal cancer xenograft model in mice in a dose-dependent manner.

Size	1 mg
Shipping	dry ice
CAS Number	922150-11-6
Molecular Formula	C₃₁H₃₆Cl₂N₆
SMILES	ClC1=CC=C(C(C2=CC=C(Cl)C=C2)N3CCN(CC4=NC(C=CC=C5)=C5C(NCCCN(C)C)=N4)CC3)C=C1
Molecular Weight	563,6
Formulation	A crystalline solid
Purity	≥98%
Custom Code	2933.59
UNSPSC code	12352100

Technical File

MSDS

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Cayman Chemical's mission is to help make research possible by supplying scientists worldwide with the basic research tools necessary for advancing human and animal health. Our utmost commitment to healthcare researchers is to offer the highest quality products with an affordable pricing policy.

Our scientists are experts in the synthesis, purification, and characterization of biochemicals ranging from small drug-like heterocycles to complex biolipids, fatty acids, and many others. We are also highly skilled in all aspects of assay and antibody development, protein expression, crystallization, and structure determination.

Over the past thirty years, Cayman developed a deep knowledge base in lipid biochemistry, including research involving the arachidonic acid cascade, inositol phosphates, and cannabinoids. This knowledge enabled the production of reagents of exceptional quality for cancer, oxidative injury, epigenetics, neuroscience, inflammation, metabolism, and many additional lines of research.

Our organic and analytical chemists specialize in the rapid development of manufacturing processes and analytical methods to carry out clinical and commercial GMP-API production. Pre-clinical drug discovery efforts are currently underway in the areas of bone restoration and repair, muscular dystrophy, oncology, and inflammation. A separate group of Ph.D.-level scientists are dedicated to offering Hit-to-Lead Discovery and Profiling Services for epigenetic targets. Our knowledgeable chemists can be contracted to perform complete sample analysis for analytes measured by the majority of our assays. We also offer a wide range of analytical services using LC-MS/MS, HPLC, GC, and many other techniques.

Accreditations
ISO/IEC 17025:2005
ISO Guide 34:2009

Cayman is a leader in the field of emerging drugs of abuse, providing high-purity Schedule I-V Controlled Substances to federally-licensed laboratories and qualified academic research institutions for forensic analyses. We are certified by ACLASS Accreditation Services with dual accreditation to ISO/IEC 17025:2005 and ISO Guide 34:2009.