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Results for "

CK1δ/ε

" in MedChemExpress (MCE) Product Catalog:

25

Inhibitors & Agonists

1

Fluorescent Dyes

1

Biochemical Assay Reagents

1

GMP Molecules

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-15490
    PF-670462 dihydrochloride
    5+ Cited Publications

    		 Casein Kinase Cancer
    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.
    PF-670462 dihydrochloride
  • HY-18340
    (R)​-​CR8
    1 Publications Verification

    CR8, (R)-Isomer

    		 Molecular Glues CDK Apoptosis Neurological Disease Cancer
    (R)-CR8, a second-generation analog of Roscovitine, is a potent CDK1/2/5/7/9 inhibitor. (R)-CR8 inhibits CDK1/cyclin B (IC50=0.09 μM), CDK2/cyclin A (0.072 μM), CDK2/cyclin E (0.041 μM), CDK5/p25 (0.11 μM), CDK7/cyclin H (1.1 μM), CDK9/cyclin T (0.18 μM) and CK1δ/ε (0.4 μM). (R)-CR8 induces apoptosis and has neuroprotective effect . (R)-CR8 acts as a molecular glue degrader that depletes cyclin K .
    (R)​-​CR8
  • HY-10456
    TAK-715
    Maximum Cited Publications
    12 Publications Verification

    		 p38 MAPK Casein Kinase Wnt Inflammation/Immunology
    TAK-715 is an orally active and potent p38 MAPK inhibitor with IC50s of 7.1 nM, 200 nM for p38α and p38β, respectively. TAK-715 inhibits casein kinase I (CK1δ/ε) to regulate activation of Wnt/β-catenin signaling. TAK-715 shows good significant efficacy in a rat arthritis model .
    TAK-715
  • HY-12879
    IWP-4
    2 Publications Verification

    		 Wnt Casein Kinase Cardiovascular Disease Neurological Disease Cancer
    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 .
    IWP-4
  • HY-12443
    PF-5006739

    		Casein Kinase Neurological Disease
    PF-5006739 is a potent and selective inhibitor of CK1δ/ε with IC50s of 3.9 nM and 17.0 nM, respectively. PF-5006739 is a potential therapeutic agent for a range of psychiatric disorders with low nanomolar in vitro potency for CK1δ/ε and high kinome selectivity. PF-5006739 attenuats opioid agent-seeking behavior in a rodent operant reinstatement model in animals in a dose-dependent manner . PF-5006739 improves glucose tolerance in both diet-induced obesity (DIO) and genetic (ob/ob) mice models of obesity .
    PF-5006739
  • HY-18285
    Longdaysin

    		Wnt Casein Kinase ERK CDK Cancer
    Longdaysin is a inhibitor of the Wnt/β-catenin signaling pathway, which exerts antitumor effect through blocking CK1δ/ε-dependent Wnt signaling. Longdaysin inhibits CK1α, CK1δ, CDK7, and ERK2 with IC50s of  5.6 µM, 8.8 µM, 29 µM, and 52 µM, respectively .
    Longdaysin
  • HY-111820
    CK1-IN-1

    		Casein Kinase p38 MAPK Cardiovascular Disease
    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 .
    CK1-IN-1
  • HY-100011
    SR-3029
    2 Publications Verification

    		 Casein Kinase Cancer
    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.
    SR-3029
  • HY-100114
    TA-01

    		Casein Kinase p38 MAPK Autophagy Cardiovascular Disease
    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.
    TA-01
  • HY-148251
    MU1742

    		Casein Kinase Cancer
    MU1742 is a probe for CK1δ and CK1ε protein kinases .
    MU1742
  • HY-158975
    VRK1/CK1-IN-1

    		Casein Kinase VRK Cancer
    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 .
    VRK1/CK1-IN-1
  • HY-18340A
    (R)-CR8 trihydrochloride
    1 Publications Verification

    CR8, (R)-Isomer trihydrochloride

    		 Molecular Glues CDK Apoptosis Neurological Disease Cancer
    (R)-CR8 (CR8) trihydrochloride, a second-generation analog of Roscovitine, is a potent CDK1/2/5/7/9 inhibitor. (R)-CR8 trihydrochloride inhibits CDK1/cyclin B (IC50=0.09 μM), CDK2/cyclin A (0.072 μM), CDK2/cyclin E (0.041 μM), CDK5/p25 (0.11 μM), CDK7/cyclin H (1.1 μM), CDK9/cyclin T (0.18 μM) and CK1δ/ε (0.4 μM). (R)-CR8 trihydrochloride induces apoptosis and has neuroprotective effect . (R)-CR8 trihydrochloride acts as a molecular glue degrader that depletes cyclin K .
    (R)-CR8 trihydrochloride
  • HY-170859
    AH078

    		PROTACs Casein Kinase Cancer
    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 .
    AH078
  • HY-108907
    SR-1277

    		Casein Kinase Cancer
    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 .
    SR-1277
  • HY-170860
    CK1δ/CK1ε liagnd-1

    		Ligands for Target Protein for PROTAC Casein Kinase Cancer
    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 .
    CK1δ/CK1ε liagnd-1
  • HY-170859A
    AH081

    		PROTACs Casein Kinase Cancer
    AH081 (Compound 38) is a CK1δ/ε PROTAC degrader. AH081 is the negative control compound of AH078 (HY-170859). AH081 has inhibitory but no degradation activity for CK1δ/ε by using an inactive stereoisomer of the VHL ligand . Pink: CK1δ/ε ligand (HY-148251); Blue: VHL ligase ligand (HY-125845B); Black: linker
    AH081
  • HY-100011R
    SR-3029 (Standard)

    		Casein Kinase Reference Standards Cancer
    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.
    SR-3029 (Standard)
  • HY-176825
    MU1742-amide-C6-acid

    		Casein Kinase Ligands for Target Protein for PROTAC Cancer
    MU1742-amide-C6-acid is a CK1δ/ε inhibitor. MU1742-amide-C6-acid can be used for synthesis of PROTAC AH081 (HY-170859A) .
    MU1742-amide-C6-acid
  • HY-170862
    E3 Ligase Ligand-linker Conjugate 163

    		E3 Ligase Ligand-Linker Conjugates Cancer
    E3 Ligase Ligand-linker Conjugate 163 is the E3 ligase ligand (E3 ligase Ligand 58, HY-170861)-linker conjugate part of AH078 (HY-170859). AH078 is a PROTAC that targets the degradation of CK1δ and CK1ε, and can be used for research related to circadian rhythm disorders .
    E3 Ligase Ligand-linker Conjugate 163
  • HY-171277
    Casein kinase 1δ-IN-27

    		Casein Kinase p38 MAPK Cancer
    Casein kinase 1δ-IN-27 (Compound 8) is the inhibitor for casein kinase 1 that inhibits CK1α, CK1δ, CK1ε, and p38α with IC50s of 22, 16.5, 9.41 and 14.8 nM, respectively. Casein kinase 1δ-IN-27 inhibits the DUX4 expression with an IC50 of 10 nM .
    Casein kinase 1δ-IN-27
  • HY-171279
    Casein kinase 1δ-IN-29

    		p38 MAPK Casein Kinase Apoptosis Inflammation/Immunology
    Casein kinase 1δ-IN-29 (Compound 18) is the inhibitor for p38α and casein kinase 1 that inhibits p38α, CK1δ and CK1ε with IC50 of 0.041 µM, 0.005 µM and 0.447 µM, respectively. Casein kinase 1δ-IN-29 arrests cell cycle at subG1 phase, induces apoptosis in cell AC1-M88 .
    Casein kinase 1δ-IN-29
  • HY-12879G
    IWP-4

    		Wnt Casein Kinase Cardiovascular Disease Neurological Disease Cancer
    IWP-4 (GMP) is the GMP-grade form of IWP-4 (HY-12879). 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 .
    IWP-4
  • HY-135629
    PF-5236216

    		Casein Kinase Neurological Disease
    PF-5236216 is a brain-penetrant CK1δ/CK1ε inhibitor with IC50 values of 8 and 36 nM. PF-5236216 inhibits CK1δ and CK1ε-mediated PER3 nuclear translocation. PF-5236216 forms an H-bond with the backbone NH of Leu85, hydrophobic stacking with Met82, and a water-mediated H-bond with Lys38 of CK1δ. PF-5236216 can be used as a tool ligand for CNS PET studies .
    PF-5236216
  • HY-123859
    SR-2890

    		Casein Kinase FLT3 CDK Neurological Disease Inflammation/Immunology Cancer
    SR-2890 is a highly selective, ATP-competitive inhibitor of casein kinase CK1δ and CK1ε, with IC50 values ​​of 4 nM and 44 nM, respectively, and a Ki of 14 nM for CK1δ. SR-2890 exhibits antiproliferative effects. SR-2890 blocks the serine/threonine kinase activity of CK1δ and weakly inhibits a few off-target kinases such as FLT3, CDK4. SR-2890 has an oral bioavailability of 10% and a blood-brain barrier penetration rate of <1%. SR-2890 demonstrates stable in vitro metabolism and favorable in vivo pharmacokinetic properties, effectively inhibiting the growth of human A375 melanoma cells. SR-2890 can be used in melanoma research and is also a useful compound for studying CK1δ/ε-related diseases such as Alzheimer's disease .
    SR-2890
  • HY-10456R
    TAK-715 (Standard)

    		Reference Standards p38 MAPK Casein Kinase Wnt Inflammation/Immunology
    TAK-715 (Standard) is the analytical standard of TAK-715 (HY-10456). This product is intended for research and analytical applications. TAK-715 is an orally active and potent p38 MAPK inhibitor with IC50s of 7.1 nM, 200 nM for p38α and p38β, respectively. TAK-715 inhibits casein kinase I (CK1δ/ε) to regulate activation of Wnt/β-catenin signaling. TAK-715 shows good significant efficacy in a rat arthritis model .
    TAK-715 (Standard)

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