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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
32 Results for "
CK1ε
" in MedChemExpress (MCE) Product Catalog:
Products (32)
32 Results for "CK1ε" in MCE Product Catalog:
8
8 Publications Verification
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PF-670462 dihydrochloride is a potent and selective inhibitor of casein kinase (CK1ε and CK1δ), with IC50s of 7.7 nM and 14 nM, respectively.
5
5 Cited Publications
Synonyms: TGR-1202; RP5264
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Umbralisib (TGR-1202) is an orally active, potent and selective dual PI3Kδ and casein kinase-1-ε (CK1ε) inhibitor, with EC50 of 22.2 nM and 6.0 μM, respectively. Umbralisib exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib can be used for haematological malignancies reseach [1] .
5
5 Cited Publications
Synonyms: TGR-1202 hydrochloride; RP5264 hydrochloride
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Umbralisib (TGR-1202) hydrochloride is an orally active, potent and selective dual PI3Kδ and casein kinase-1-ε (CK1ε) inhibitor, with EC50 of 22.2 nM and 6.0 μM, respectively. Umbralisib hydrochloride exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib hydrochloride can be used for haematological malignancies reseach [1] .
2
2 Cited Publications
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IWP-4 is a Wnt inhibitor with an IC50 of 25 nM. IWP-4 specifically inhibits casein kinase 1δ/ε (CK1δ/ε), with an IC50 of 1.06 μM against wild-type CK1δ, 1.02 μM against the CK1δ kinase domain, and 7.07 μM against CK1ε; it shows enhanced inhibitory activity against the M82F CK1δ mutant (IC50 = 0.14 μM). IWP-4 is applicable to research related to cancer, Alzheimer's disease (AD), and heart failure [1] .
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2 Cited Publications
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TA-02, an analog of SB 203580 (HY-10256), is a p38 MAPK inhibitor with an IC50 of 20 nM. TA-02 especially inhibits TGFBR-2. TA-02 exhibits similar cardiogenic properties as SB 203580 and SB 202190 (HY-10295) [1].
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2 Cited Publications
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SR-3029 is a potent and ATP competitive CK1δ and CK1ε inhibitor, with IC50s of 44 nM and 260 nM, respectively, and Kis of 97 nM for both kinases.
1
1 Cited Publications
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CK1-IN-1 (Compound 1c) is a casein kinase 1 (CK1) inhibitor with IC50 values of 15 nM and 16 nM for CK1δ and CK1ε, respectively. CK1-IN-1 inhibits p38α MAPK with an IC50 of 73 nM. CK1-IN-1 can be used to study cardiomyogenesis [1].
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Category:
Flavonoids Leguminosae Glycine max (L.) merr Metabolic Disease Phenols Polyphenols Plants Disease Research Fields Isoflavones
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1
1 Cited Publications
Cat. No.: HY-N6841
CAS No.: 86831-53-0
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TA-01 is a potent CK1 and p38 MAPK inhibitor, with IC50s of 6.4 nM, 6.8 nM, 6.7 nM for CK1ε, CK1δ and p38 MAPK, respectively. TA-01 acts as a cardiogenic inhibitor.
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MU1742 is a probe for CK1δ and CK1ε protein kinases [1].
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VRK1/CK1-IN-1 (compound 36) is a dual VRK1 and CK1 family inhibitor, with a Ki of 37.9 nM against human VRK1, 8.3 nM against human CK1δ, and 7.8 nM against human CK1ε. VRK1/CK1-IN-1 exhibits extremely low activity against VRK2. VRK1/CK1-IN-1 can be used in studies related to p53-deficient tumors [1].
Cat. No.: HY-170859
CAS No.: 3110370-06-1
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AH078 is a PROTAC-based CK1δ/ε degrader (DC50=0.55 μM, Dmax=70%) that lacks subtype selectivity between CK1δ and CK1ε. AH078 induces target protein degradation either by recruiting the CUL4-CRBN E3 ligase complex and proteasome, or via the VHL- and ubiquitin-dependent pathway. AH078 also exhibits selectivity for CK1α, and is widely applicable to research related to colon cancer, pancreatic cancer, breast cancer, ovarian cancer, chronic lymphocytic leukemia, acute myeloid leukemia, glioma, and metastatic breast adenocarcinoma [1] .
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IWP-3 is a Wnt production inhibitor with an IC50 of 40 nM. IWP-3 also acts as a CK1δ inhibitor, with an IC50 of 1.89 μM against rat full-length CK1δ. IWP-3 inhibits the function of Porcupine (Porcn), thereby blocking the palmitoylation of Wnt proteins, suppressing the canonical Wnt signaling pathway, reducing the proliferative capacity of cancer cells, promoting the differentiation of mesoderm into cardiomyocytes and increasing cardiomyocyte yield. IWP-3 reduces embryonic cell division, alters the cell movement along the anterior-posterior axis of embryos, and causes embryonic shortening. IWP-3 can be used in studies related to cancers such as pancreatic cancer [1] .
Cat. No.: HY-108907
CAS No.: 1446715-47-4
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SR-1277 is a potent, selective and ATP competitive CK1δ/ε inhibitor, with IC50s of 49 nM and 260 nM, respectively. SR-1277 also inhibits FLT3, CDK4/cyclin D1, CDK6/cyclin D3 and CDK9/cyclin K, with IC50s of 305 nM, 1340 nM, 311 nM and 109 nM, respectively. SR-1277 can be used for the research of cancer [1].
Cat. No.: HY-170405
CAS No.: 2940242-88-4
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YB-3-17 is a blood-brain barrier permeable mTOR inhibitor (IC50 = 0.22 nM) and GSPT1 PROTAC degrader. YB-3-17 inhibits mTORC1/2, CK1δ/ε, mutant ALK and HER2 kinases, induces CRBN-dependent selective GSPT1 degradation, ablates mTOR downstream phosphorylation, downregulates c-Myc/Cyclin D1 to impair tumor translation, triggers p53-mediated apoptosis, suppresses tumor proliferation and xenograft tumor growth, and can be used for the study of glioma, neuroblastoma, breast cancer, lymphoma, colorectal cancer and lung cancer [1].
Cat. No.: HY-149292
CAS No.: 2999645-23-5
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SR-4133 is a potent and highly CK1ε selective inhibitor with an IC50 of 58 nM. SR-4133 binds to the ATP-binding site of CK1ε. SR-4133 displays nanomolar growth inhibition of bladder cancer cells, and inhibits the phosphorylation of 4E-BP1 [1].
Cat. No.: HY-170860
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CK1δ/CK1ε liagnd-1 is the ligand for CK1δ/CK1ε that can be used for synthesis of CK1 PROTAC degrader AH078 (HY-170859) as the ligand for target protein [1].
Cat. No.: HY-100011R
CAS No.: 1454585-06-8
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SR-3029 (Standard) is the analytical standard of SR-3029 (HY-100011). This product is intended for research and analytical applications. SR-3029 is a potent and ATP competitive CK1δ and CK1ε inhibitor, with IC50s of 44 nM and 260 nM, respectively, and Kis of 97 nM for both kinases.
Cat. No.: HY-171278
CAS No.: 1095750-94-9
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Casein kinase 1δ-IN-28 (Compound 4) is the inhibitor for CK1ε with an IC50 of 0.0146 μM. Casein kinase 1δ-IN-28 exhibits a metabolite rate in human liver microsomes of 52% [1].
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
