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CK1-IN-1

" in MedChemExpress (MCE) Product Catalog:

37

Inhibitors & Agonists

1

Fluorescent Dyes

1

Biochemical Assay Reagents

3

Peptides

1

GMP Molecules

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-10324
    D4476
    10+ Cited Publications

    CaseIN KINase I INhibitor

    		 Casein Kinase Autophagy Apoptosis Cancer
    D4476 is a potent, selective and cell-permeable inhibitor of casein kinase 1(CK1) with an IC50 value of 0.3 μM in vitro.
    D4476
  • 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-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-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-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-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-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-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-145939
    BAY-888

    BRD5846

    		 Casein Kinase Cancer
    BAY-888 is a selective CK1α/CSNK1A1 (casein kinase 1α) ATP-competitive inhibitor (IC50: 4 nM@10 μM ATP; 63 nM@1 mM ATP). BAY-888 blocks the negative regulation of p53 and other signaling pathways by CK1α, induces apoptosis and inhibits proliferation of tumor cells. BAY-888 has shown inhibitory efficacy against cancers such as acute myeloid leukemia (AML) in PRISM barcoded cell line screening and can mimic the effects of shRNA-mediated CK1α knockdown. BAY-888 is primarily used for the development of anticancer drugs for p53 wild-type tumors and for the study of the mechanisms of CK1α-related signaling pathways .
    BAY-888
  • HY-110052
    TBCA
    1 Publications Verification

    		 Casein Kinase Cancer
    TBCA is a highly selective CK2 (casein kinase II) inhibitor with an IC50 of 110 nM and a Ki of 77 nM. TBCA shows selectivity for CK2 over CK1, DYRK1A and a panel of 27 other kinases .
    TBCA
  • HY-100536
    IWP-3

    		Wnt Cancer
    IWP-3 is an potent inhibitor of Wnt production with an IC50 of 40 nM. IWP-3 inhibits Porcupine (Porcn) function thereby blocking palmitoylation of Wnt proteins. IWP-3 inhibits CK1γ3 and CK1ε only moderately and does not inhibit CK1α .
    IWP-3
  • 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-178335
    SGC-CK1γ-1

    		LDLR Wnt CMV Infection
    SGC-CK1γ-1 is a potent and selective probe for the CK1γ subfamily. SGC-CK1γ-1 can inhibit LRP6 phosphorylation levels. SGC-CK1γ-1 can selectively inhibit the CK1γ kinases in living cells and inhibit both WNT signaling and human cytomegalovirus (CMV) replication. SGC-CK1γ-1 can be used for the research of infection .
    SGC-CK1γ-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-103383
    (R)-DRF053 dihydrochloride

    		CDK Casein Kinase Neurological Disease Cancer
    (R)-DRF053 dihydrochloride is a potent casein kinases 1 (CK1), CDK1/cyclin B and CDK5/p25 inhibitor with IC50s of 14 nM, 220 nM and 80 nM, respectively. (R)-DRF053 dihydrochloride prevents the CK1-dependent production of amyloid-beta in a cell model .
    (R)-DRF053 dihydrochloride
  • HY-153904
    Casein kinase 1δ-IN-5

    		Casein Kinase Neurological Disease
    Casein kinase 1δ-IN-5 is a potent and selective protein kinase CK-1δ inhibitor with an IC50 of 47 nM. Casein kinase 1δ-IN-5 shows neuroprotective and anti-inflammatory properties both in vitro. Casein kinase 1δ-IN-5 has the potential for neurodegenerative diseases research.
    Casein kinase 1δ-IN-5
  • HY-153905
    Casein kinase 1δ-IN-6

    		Casein Kinase Neurological Disease
    Casein kinase 1δ-IN-6 is a potent and selective protein kinase CK-1δ inhibitor with an IC50 of 23 nM. Casein kinase 1δ-IN-6 shows neuroprotective and anti-inflammatory properties both in vitro and in vivo. Casein kinase 1δ-IN-6 is a promising drug candidate and can be used for neurodegenerative diseases research.
    Casein kinase 1δ-IN-6
  • HY-128433
    CK1-IN-3

    		Casein Kinase Neurological Disease
    CK1-IN-3 (compound 51) is a AC1 inhibitor with an IC50s 2.22 µM for CK-1δ .
    CK1-IN-3
  • 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-P11119
    CKS peptide

    		Casein Kinase Neurological Disease
    CKS peptide is a selective substrate peptide for CK1. CKS peptide can used to measure CK1 activity .
    CKS peptide
  • HY-169556
    CK1δ-IN-7

    		Casein Kinase Neurological Disease
    CK1δ-IN-7 (Compound 488) is the inhibitor for casein kinase 1δ (CK1δ) .
    CK1δ-IN-7
  • HY-173494
    GSK-3β/CK-1δ-IN-1

    		GSK-3 Casein Kinase Cancer
    GSK-3β/CK-1δ-IN-1 (8d) is a dual and blood-brain barrier penetrated GSK-3β / CK-1δ inhibitor, with IC50 values of 0.77 μM for GSK-3β and 0.57 μM for CK-1δ, respectively. GSK-3β/CK-1δ-IN-1 (8d) can be used in the research for neuroblastoma .
    GSK-3β/CK-1δ-IN-1
  • HY-P5526
    CCK1-specific peptide substrate

    		Casein Kinase Others
    CCK1-specific peptide substrate is a biological active peptide. (This peptide sequence is based on rabbit muscle glycogen synthase with Ser7 phosphorylated. It is a peptide substrate for Casein Kinase I (CK1). CK1 phosphorylates Ser10. Ser7 is phosphorylated by PKA in vivo.)
    CCK1-specific peptide substrate
  • 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-181586
    CK1γ-IN-1

    		Casein Kinase Others
    CK1γ-IN-1 is a non-selective CK1 kinase inhibitor with IC50 values of 780 nM, 570 nM and 990 nM against human CK1γ1, CK1γ2, CK1γ3, respectively. The non-specific binding of CK1γ-IN-1 to multiple kinases enables its application in biological studies of specific CK1γ .
    CK1γ-IN-1
  • HY-181048
    CK1α-IN-1

    		Casein Kinase MDM-2/p53 Cancer
    CK1α-IN-1 (Compound 7a) is a selective CK1α inhibitor with an IC50 of 10.96 nM. CK1α-IN-1 dose-dependently stabilizes p53 protein. CK1α-IN-1 has anticancer activity against acute monocytic leukemia .
    CK1α-IN-1
  • HY-164578
    CK1δ-IN-1

    		Casein Kinase Neurological Disease
    CK1δ-IN-1 (example 939) is a casein kinase 1 delta (CK1δ) inhibitor. CK1δ-IN-1 can be used for the study of Alzheimer's disease .
    CK1δ-IN-1
  • 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-P10606
    CK1tide

    		Biochemical Assay Reagents Others
    CK1tide is a substrate for casein kinase 1 (CK1) and can be used to assess CK1's in vitro catalytic activity by detecting whether CK1 can phosphorylate it .
    CK1tide
  • HY-181585
    FP1-24

    		Casein Kinase Others
    FP1-24 is a non-selective CK1 kinase inhibitor, with IC50 values of 40 nM, 10 nM, 10 nM, and 40 nM against human CK1γ1, CK1γ2, CK1γ3 and CK1δ, respectively. FP1-24 exerts its activity by reducing the phosphorylation level of LRP5/6 at the T1479 site during WNT signaling pathway activation. The non-specific binding of FP1-24 to multiple kinases can be used for biological studies of specific CK1γ .
    FP1-24
  • HY-51327
    CK1-IN-5

    		Casein Kinase Others
    CK1-IN-5 (compound B-AZ) is an inhibitor of CK1. CK1-IN-5 lengthened the circadian period by inhibits AtCKL3/AtCKL4 activity .
    CK1-IN-5
  • HY-10324R
    D4476 (Standard)

    CaseIN KINase I INhibitor (Standard)

    		 Reference Standards Casein Kinase Autophagy Apoptosis Cancer
    D4476 (Standard) is the analytical standard of D4476 (HY-10324). This product is intended for research and analytical applications. D4476 is a potent, selective and cell-permeable inhibitor of casein kinase 1(CK1) with an IC50 value of 0.3 μM in vitro.
    D4476 (Standard)
  • 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-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)
  • 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

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