MK-4101

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MK-4101

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Cat No: 29159

Biochemicals - Receptor Pharmacology

MK-4101 is a Smoothened (Smo) receptor antagonist.{48932} It binds to human recombinant Smo expressed in HEK293T cells (IC50 = 1.1 µM) and inhibits Gli1-mediated hedgehog signaling in a reporter assay (IC50 = 1.5 µM). It is also an inhibitor of 11β-hy...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

5-(3,3-difluorocyclobutyl)-3-[4-[4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazol-3-yl]bicyclo[2.2.2]oct-1-yl]-1,2,4-oxadiazole

Correlated keywords:

MK4101 HEK 293T 293 T Gli 1 11 ?

Product Overview:
MK-4101 is a Smoothened (Smo) receptor antagonist.{48932} It binds to human recombinant Smo expressed in HEK293T cells (IC50 = 1.1 µM) and inhibits Gli1-mediated hedgehog signaling in a reporter assay (IC50 = 1.5 µM). It is also an inhibitor of 11β-hydroxy steroid dehydrogenase-1. MK-4101 (40 and 80 mg/kg per day) reduces tumor growth in a murine medulloblastoma mouse allograft model, induces tumor regression when administered at a dose of 80 mg/kg twice per day, and reduces expression of the hedgehog pathway-associated transcription factor Gli1 in tumor tissue.

Size	1 mg
Shipping	dry ice
CAS Number	935273-79-3
Molecular Formula	C₂₄H₂₄F₅N₅O
SMILES	CN1C(C2=C(C(F)(F)F)C=CC=C2)=NN=C1C34CCC(CC4)(C5=NOC(C6CC(F)(F)C6)=N5)CC3
Molecular Weight	493,5
Formulation	A crystalline solid
Purity	≥98%
Custom Code	2933.99
UNSPSC code	12352100

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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.