K02288

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K02288

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Cat No: 16678

Biochemicals - Kinase Inhibitors

Activation of bone morphogenetic protein (BMP) type I receptors, also known as activin receptor-like kinases (ALK1-7), leads to the assembly of SMAD complexes, which translocate to the nucleus to induce transcriptional activation important for normal d...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

3-[6-amino-5-(3,4,5-trimethoxyphenyl)-3-pyridinyl]-phenol

Correlated keywords:

stem cells bone morphogenetic protein type I receptor BMP activin receptor-like kinase ALK SMAD complexes translocate nucleus induce transcriptional activation normal development tissue repair ALK1 ALK2 fibrodysplasia ossificans progressive cancer inhibitor intracellular signaling inhibit bone-related research biochemical biochemistry transcription factor K-02288 2-aminopyridine-based prevent BMP4-induced SMAD1/5/8 pathway in vitro dorsalization zebrafish embryo biology disease model musculoskeletal dysplasia ALK-1 ALK-2

Product Overview:
Activation of bone morphogenetic protein (BMP) type I receptors, also known as activin receptor-like kinases (ALK1-7), leads to the assembly of SMAD complexes, which translocate to the nucleus to induce transcriptional activation important for normal development and tissue repair.{9612} K02288 is a 2-aminopyridine-based inhibitor of ALK1 and ALK2 with IC50 values of 1.8 and 1.1 nM, respectively.{23387} It is less selective for ALK3, 4, 5, and 6 subtypes and the type II BMP receptor ActRIIA, demonstrating IC50 values of 34.4, 302, 321, 6.4, and 220 nM, respectively.{23387} K02288 can prevent BMP4-induced SMAD1/5/8 pathway activation in vitro (IC50 = 100 nM) without affecting TGF-β signaling. Furthermore, at 8-10 µM, K02288 has been used to induce the dorsalization of zebrafish embryos. Through specific inhibition of BMP signaling, this compound can be used to research stem cell biology and disease models of musculoskeletal dysplasia and cancer.{23387}

Size	1 mg
Shipping	dry ice
CAS Number	1431985-92-0
Molecular Formula	C₂₀H₂₀N₂O₄
SMILES	OC1=CC(C2=CN=C(N)C(C3=CC(OC)=C(OC)C(OC)=C3)=C2)=CC=C1
Molecular Weight	352,4
Formulation	A crystalline solid
Purity	≥98%
Custom Code	2933.39
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.