1637394-01-4
Chemical Structure
GDC-0134
Synonym(s): RG6000
- CAS No.: 1637394-01-4
- Formula:C19H20F4N6O2
- Molecular Weight:440.39
IUPAC Name: 5-(6-((1S,4S)-2-oxa-5-azabicyclo[2.2.1]heptan-5-yl)-2-(3,3-difluoropyrrolidin-1-yl)pyrimidin-4-yl)-3-(difluoromethoxy)pyridin-2-amine
InChIKey: SKMKJBYBPYBDMN-RYUDHWBXSA-N
SMILES: NC1=C(C=C(C=N1)C2=NC(N3CC(F)(CC3)F)=NC(N4C[C@H]5OC[C@@H]4C5)=C2)OC(F)F
Biological Activity: GDC-0134 (RG6000) is a modulator targeting dual leucine zipper kinase (DLK/MAP3K12) that can cross the blood-brain barrier. By inhibiting the kinase activity of DLK, GDC-0134 blocks the activation of the downstream JNK signaling pathway, suppresses DLK-dependent retrograde signal transduction of axon-to-soma degeneration, and exerts neuroprotective activity. GDC-0134 reduces TDP-43 protein aggregation and decreases the degree of neuromuscular junction denervation in motor neurons. GDC-0134 can be used in the research of amyotrophic lateral sclerosis (ALS), Alzheimer's disease and other DLK-related neurodegenerative diseases[1][2][3].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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GDC-0134 | 99.18% | GDC-0134 (RG6000) is a modulator targeting dual leucine zipper kinase (DLK/MAP3K12) that can cross the blood-brain barrier. By inhibiting the kinase activity of DLK, GDC-0134 blocks the activation of the downstream JNK signaling pathway, suppresses DLK-dependent retrograde signal transduction of axon-to-soma degeneration, and exerts neuroprotective activity. GDC-0134 reduces TDP-43 protein aggregation and decreases the degree of neuromuscular junction denervation in motor neurons. GDC-0134 can be used in the research of amyotrophic lateral sclerosis (ALS), Alzheimer's disease and other DLK-related neurodegenerative diseases. | ||||||||||||||||||||
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References
- [1]. Hoffmann-Emery F, et al. Development of a Practical and Greener Process for the Dual Leucine Zipper Kinase Inhibitor GDC-0134 Comprising Two SNAr Reactions, Oxidation and Suzuki Coupling[J]. Organic Process Research & Development, 2022, 26(2): 313-322.
- [2]. Minaei A, et al. Novel neuroprotective strategy based on inhibition of acute axonal palmitoylation of dual leucine-zipper kinase[J]. Neural Regeneration Research, 10.4103.
- [3]. Palomo V, et al. Protein kinase inhibitors for amyotrophic lateral sclerosis therapy[J]. British Journal of Pharmacology, 2021, 178(6): 1316-1335.
