MW 398.4 Da, Purity >99%. Selective cell-permeable inhibitor of casein kinase 1 (CK1) . (IC50 values are 0.3 (CK1), 0.5 (ALK5), 9.1 (PKd1) and 5.8 μM (p38αMAPK)). Displays selectivity over many other protein kinases.
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- Iranian journal of basic medical sciences 26:1212-12192023BAMLET (Bovine α-lactalbumin made lethal to tumor cells) inhibits autophagy flux and induces apoptosis via down-regulation of protein kinase CK1α and attenuation of the AKT/p-ß-catenin (S552) pathway in RAS-mutated human colorectal HCT 116 cells.Applications:Unspecified applicationReactive species:Unspecified reactive speciesHamid Behrouj,Pooneh MokarramPubMed 37736507
- Bio-protocol 12:2022Analysis of the Ubiquitination and Phosphorylation of Vangl Proteins.Applications:Unspecified applicationReactive species:Unspecified reactive speciesDi Feng,Ziwei He,Bo GaoPubMed 36353719
- Archivum immunologiae et therapiae experimentalis 69:262021Casein Kinase-1-Alpha Inhibitor (D4476) Sensitizes Microsatellite Instable Colorectal Cancer Cells to 5-Fluorouracil via Authophagy Flux Inhibition.Applications:Unspecified applicationReactive species:Unspecified reactive speciesMorvarid Siri,Hamid Behrouj,Sanaz Dastghaib,Mozhdeh Zamani,Wirginia Likus,Sedigheh Rezaie,Jacek Hudecki,Saeed Khazayel,Marek J Łos,Pooneh Mokarram,Saeid GhavamiPubMed 34536148
- Science advances 7:2021Regulation of Wnt/PCP signaling through p97/VCP-KBTBD7-mediated Vangl ubiquitination and endoplasmic reticulum-associated degradation.Applications:Unspecified applicationReactive species:Unspecified reactive speciesDi Feng,Jin Wang,Wei Yang,Jingyu Li,Xiaochen Lin,Fangzi Zha,Xiaolu Wang,Luyao Ma,Nga Ting Choi,Yusuke Mii,Shinji Takada,Michael S Y Huen,Yusong Guo,Liang Zhang,Bo GaoPubMed 33990333
- Scientific reports 6:344722016Casein kinase 1 is recruited to nuclear speckles by FAM83H and SON.Applications:Unspecified applicationReactive species:Unspecified reactive speciesTakahisa Kuga et. al.PubMed 27681590
- Nature communications 5:58272014Phosphorylation of LRRK2 by casein kinase 1α regulates trans-Golgi clustering via differential interaction with ARHGEF7.Applications:Unspecified applicationReactive species:Unspecified reactive speciesRuth Chia et. al.PubMed 25500533
Key facts
- CAS number
- 301836-43-1
- Purity
- > 99%
- Form
- Solid
- Molecular weight
- 398.4 Da
- Molecular formula
- C23H18N4O3
- PubChem identifier
- 6419753
- Nature
- Synthetic
Target data
Alternative names
AAT 5, ACVRLK 4, ALK-5, Activin A receptor type II like kinase, Activin A receptor type II like kinase 53kDa, Activin A receptor type II like kinase, 53kD, Activin receptor-like kinase 5, CDC-like kinase 1, CDC28/CDC2 like kinase, CLK/STY, CLK1_HUMAN, CSAID Binding Protein 1, CSAID-binding protein, CSBP, CSBP 1, CSBP 2, CSPB1, Csaids binding protein, Cytokine suppressive anti-inflammatory drug-binding protein, Dual specificity protein kinase CLK1, EXIP, KPCD1_HUMAN, LDS1A, LDS2A, MAP kinase 14, MAP kinase MXI2, MAP kinase p38 alpha, MAPK 14, MAX-interacting protein 2, MK14_HUMAN, MSSE, Mitogen-activated protein kinase 14, Mitogen-activated protein kinase p38 alpha, Mxi 2, P38, PKC, PKC MU, PKCM, PKD, PRKCM, PRKD 1, PRKM14, PRKM15, Protein kinase C mu, Protein kinase C mu type, Protein kinase D, Protein kinase D1, Protein tyrosine kinase STY, RK, SAPK2A, SKR 4, STY, Serine/threonine-protein kinase D1, Serine/threonine-protein kinase receptor R4, Stress-activated protein kinase 2a, TGF-beta receptor type I, TGF-beta receptor type-1, TGF-beta type I receptor, TGFBR 1, TGFBR1 protein, TGFR1_HUMAN, TbetaR-I, Transforming growth factor beta receptor 1, Transforming growth factor beta receptor I, Transforming growth factor beta receptor I (activin A receptor type II like kinase, 53kD), Transforming growth factor-beta receptor type I, activin A receptor type II-like protein kinase of 53kD, nPKC-D1, nPKC-mu, p38 ALPHA, p38 MAP kinase, p38 MAPK, p38 mitogen activated protein kinase, p38alpha Exip
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MW 398.4 Da, Purity >99%. Selective cell-permeable inhibitor of casein kinase 1 (CK1) . (IC50 values are 0.3 (CK1), 0.5 (ALK5), 9.1 (PKd1) and 5.8 μM (p38αMAPK)). Displays selectivity over many other protein kinases.
Key facts
- CAS number
- 301836-43-1
- Purity
- > 99%
- Form
- Solid
- Molecular weight
- 398.4 Da
- Molecular formula
- C23H18N4O3
- PubChem identifier
- 6419753
- Nature
- Synthetic
- Solubility
Soluble in DMSO to 100 mM.
- Biochemical name
- CK1 Inhibitor
- Biological description
Selective cell-permeable inhibitor of casein kinase 1 (CK1) . (IC50 values are 0.3 (CK1), 0.5 (ALK5), 9.1 (PKd1) and 5.8 μM (p38αMAPK)). Displays selectivity over many other protein kinases.
- Canonical SMILES
- C1COC2=C(O1)C=CC(=C2)C3=C(NC(=N3)C4=CC=C(C=C4)C(=O)N)C5=CC=CC=N5
- 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)
- InChIKey
- DPDZHVCKYBCJHW-UHFFFAOYSA-N
- IUPAC name
- 4-[4-(2,3-dihydro-1,4-benzodioxin-6-yl)-5-pyridin-2-yl-1H-imidazol-2-yl]benzamide
Storage
- Shipped at conditions
- Ambient - Can Ship with Ice
- Appropriate short-term storage conditions
- +4°C
- Appropriate long-term storage conditions
- +4°C
- Storage information
- The product can be stored for up to 12 months
Supplementary info
- This supplementary information is collated from multiple sources and compiled automatically.
- Activity summary
P38 also known as MAPK14 weighs approximately 43 kDa and is a member of the mitogen-activated protein kinase family. It is expressed in many tissues with high levels in the heart and skeletal muscle. p38 acts mechanically by phosphorylating various substrates involved in cellular responses to stress and inflammation. Protein Kinase C mu/PKD also referred to as PKD1 is part of the protein kinase D family. It has a mass of around 115 kDa and functions by relaying signaling pathways important for maintaining cellular activities. TGF beta Receptor I also known as activin receptor-like kinase 5 (ALK5) is a serine/threonine kinase of about 53 kDa found in various tissues. CLK1 or CDC-like kinase 1 has a mass of approximately 52 kDa and plays roles in pre-mRNA splicing and regulation.
- Biological function summary
All these proteins play key roles in cellular communication and response modulation. p38 adjusts the cellular response to external stress signals and inflammation and it often forms part of larger signaling complexes. PKC mu/PKD regulates signal transduction pathways involved in cell proliferation and migration. TGF beta Receptor I mediates signaling for TGF-beta regulating cell growth and differentiation. CLK1 influences aspect of RNA splicing affecting gene expression and cellular metabolism.
- Pathways
P38 MAPK signaling includes phosphorylation chains impacting cellular inflammatory response while closely interacting with proteins like MKK3 and MKK6. PKC mu/PKD signaling is integral to the DAG-activated pathway where it associates with proteins like Rac1. TGF beta Receptor I is critical for the TGF-beta signaling pathway interacting with SMAD proteins to transduce signals. CLK1 affects the CLK1 signaling pathway influencing RNA splicing through interactions with SR proteins.
- Associated diseases and disorders
P38 links to conditions such as inflammatory diseases and cancer. It connects with cytokine signaling proteins impacting disease progression. PKC mu/PKD associates with cancer and cardiovascular diseases through its role in cellular proliferation. TGF beta Receptor I's dysfunction correlates with fibrotic diseases through interactions with ECM-modifying proteins. CLK1 relates to neurological disorders influencing proteins involved in RNA processing such as ASF/SF2.
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2 product images
Chemical Structure - D4476, CK1 inhibitor (ab120220)
2D chemical structure image of ab120220, D4476, CK1 inhibitor
Functional Studies - D4476, CK1 inhibitor (ab120220)
ab38511 staining βcatenin (phospho Thr42 + Ser45) in SK-N-SH cells treated with D4476 (ab120220), by ICC/IF. Decrease in expression of βcatenin (phospho Thr42 + Ser45) correlates with increased concentration of D4476, as described in literature.
The cells were incubated at 37°C for 2h in media containing different concentrations of ab120220 (D4476) in DMSO, fixed with 4% formaldehyde for 10 minutes at room temperature and blocked with PBS containing 10% goat serum, 0.3 M glycine, 1% BSA and 0.1% tween for 2h at room temperature. Staining of the treated cells with ab38511 (5 μg/ml) was performed overnight at 4°C in PBS containing 1% BSA and 0.1% tween. A DyLight 488 goat anti-rabbit polyclonal antibody (Goat Anti-Rabbit IgG H&L (DyLight® 488) preadsorbed ab96899) at 1/250 dilution was used as the secondary antibody. Nuclei were counterstained with DAPI and are shown in blue.
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