Determine the necessary mass, volume, or concentration for preparing a solution.
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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D125927-10mg | 10mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $135.90 | |
D125927-50mg | 50mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $369.90 | |
D125927-250mg | 250mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $1,665.90 |
CK1 inhibitor
Synonyms | D4476, >=98% (HPLC), solid | HMS3266B22 | 2-[bis(2-chloroethyl)amino]-1,3,2 | NSC-6253 | HMS3413F18 | SMR004701747 | 4-[4-(2,3-dihydro-1, 4-benzodioxin-6-yl)-5-(2-pyridinyl)1H-imidazol-2-yl]-benzamide | BD162789 | HMS3229C20 | NCGC00242498-01 | NCGC002424 |
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Specifications & Purity | Moligand™, ≥98% |
Biochemical and Physiological Mechanisms | D4476 is a cell-permeable triaryl substituted imidazolo compound that acts as a selective inhibitor of casein kinase 1 (CK1) and TGFβ RI (TGF-βtype-I receptor, ALK5). Weak inhibitor of Polycystin-1 (PKD1), p38? (p38α MAPK) and only weakly affects the acti |
Storage Temp | Store at 2-8°C |
Shipped In | Wet ice |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | Inhibitor of casein kinase 1 alpha 1;Inhibitor of casein kinase 1 delta |
Note | Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details. |
Product Description | D4476, a cell-permeant inhibitor of CK1δ (IC90 <10 uM), originally identified as inhibitors of activin receptor-like kinase ALK5. |
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IUPAC Name | 4-[4-(2,3-dihydro-1,4-benzodioxin-6-yl)-5-pyridin-2-yl-1H-imidazol-2-yl]benzamide |
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INCHI | InChI=1S/C23H18N4O3/c24-22(28)14-4-6-15(7-5-14)23-26-20(21(27-23)17-3-1-2-10-25-17)16-8-9-18-19(13-16)30-12-11-29-18/h1-10,13H,11-12H2,(H2,24,28)(H,26,27) |
InChi Key | DPDZHVCKYBCJHW-UHFFFAOYSA-N |
Canonical SMILES | C1COC2=C(O1)C=CC(=C2)C3=C(NC(=N3)C4=CC=C(C=C4)C(=O)N)C5=CC=CC=N5 |
Isomeric SMILES | C1COC2=C(O1)C=CC(=C2)C3=C(NC(=N3)C4=CC=C(C=C4)C(=O)N)C5=CC=CC=N5 |
WGK Germany | 3 |
PubChem CID | 6419753 |
Molecular Weight | 398.41 |
PubChem CID | 6419753 |
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ChEMBL Ligand | CHEMBL410456 |
CAS Registry No. | 301836-43-1 |
Enter Lot Number to search for COA:
Find and download the COA for your product by matching the lot number on the packaging.
Lot Number | Certificate Type | Date | Item |
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F1509053 | Certificate of Analysis | Jan 16, 2023 | D125927 |
Solubility | Soluble in DMSO (~20 mg/ml), ethanol (50 mM), and 1:10 DMSO:PBS (pH 7.2) (0.1 mg/ml). Insoluble in water |
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WGK Germany | 3 |
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1. Rena G, Bain J, Elliott M, Cohen P. (2004) D4476, a cell-permeant inhibitor of CK1, suppresses the site-specific phosphorylation and nuclear exclusion of FOXO1a.. EMBO Rep, 5 (1): (60-5). [PMID:14710188] [10.1021/op500134e] |
2. Kurihara T, Sakurai E, Toyomoto M, Kii I, Kawamoto D, Asada T, Tanabe T, Yoshimura M, Hagiwara M, Miyata A. (2014) Alleviation of behavioral hypersensitivity in mouse models of inflammatory pain with two structurally different casein kinase 1 (CK1) inhibitors.. Mol Pain, 10 (13): (17). [PMID:24612480] [10.1021/op500134e] |
3. Kuga T et al.. (2016) Casein kinase 1 is recruited to nuclear speckles by FAM83H and SON.. Sci Rep, 6 (34472). [PMID:27681590] |
4. Siri M et al.. (2021) Casein Kinase-1-Alpha Inhibitor (D4476) Sensitizes Microsatellite Instable Colorectal Cancer Cells to 5-Fluorouracil via Authophagy Flux Inhibition.. Arch Immunol Ther Exp (Warsz), 69 (26). [PMID:34536148] |
5. Chia R et al.. (2014) Phosphorylation of LRRK2 by casein kinase 1a regulates trans-Golgi clustering via differential interaction with ARHGEF7.. Nat Commun, 5 (5827). [PMID:25500533] |
6. Feng D et al.. (2021) Regulation of Wnt/PCP signaling through p97/VCP-KBTBD7-mediated Vangl ubiquitination and endoplasmic reticulum-associated degradation.. Sci Adv, 7 (20): [PMID:33990333] |