2. Search Result
Search Result
Results for "

CK1 inhibitor

" in MedChemExpress (MCE) Product Catalog:

88

Inhibitors & Agonists

1

Fluorescent Dyes

1

Biochemical Assay Reagents

4

Natural
Products

1

GMP Molecules

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-13912
    IWP-2
    Maximum Cited Publications
    30 Publications Verification

    		 Wnt Porcupine Casein Kinase Cancer
    IWP-2 is an inhibitor of Wnt processing and secretion with an IC50 of 27 nM. IWP-2 targets the membrane-bound O-acyltransferase porcupine (Porcn) and thus preventing a crucial Wnt ligand palmitoylation. IWP-2 is also an ATP-competitive CK1δ inhibitor with an IC50 of 40 nM for the gatekeeper mutant M82FCK1δ .
    IWP-2
  • HY-15424
    5-Iodotubercidin
    10+ Cited Publications

    NSC 113939; 5-ITu

    		 Adenosine Kinase Cancer
    5-Iodotubercidin (NSC 113939), an ATP mimetic, is a potent adenosine kinase inhibitor with an IC50 of 26 nM. 5-Iodotubercidin (NSC 113939) initiates glycogen synthesis in isolated hepatocytes by causing inactivation of phosphorylase and activation of glycogen synthase. 5-Iodotubercidin (NSC 113939) also inhibits CK1, insulin receptor tyrosine kinase, phosphorylase kinase, PKA, CK2, PKC and Haspin .
    5-Iodotubercidin
  • 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-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-12279
    Umbralisib
    5 Publications Verification

    TGR-1202; RP5264

    		 PI3K Casein Kinase Cancer
    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 .
    Umbralisib
  • HY-10456
    TAK-715
    10+ Cited Publications

    		 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-123954
    BTX-A51
    1 Publications Verification

    Casein Kinase inhibitor A51

    		 Casein Kinase CDK Apoptosis Cancer
    BTX-A51 (Casein Kinase inhibitor A51) is a potent and orally active casein kinase 1α (CK1α) inhibitor. BTX-A51 induces leukemia cell apoptosis, and has potent anti-leukemic activities .
    BTX-A51
  • HY-12470
    PF-4800567
    2 Publications Verification

    		 Casein Kinase Others
    PF-4800567 is a potent and selective inhibitor of casein kinase 1? (CK1?), with an IC50 of 32 nM, which is greater than 20-fold selectivity over CK1δ (IC50, 711 nM).
    PF-4800567
  • HY-W011109
    CKI-7
    1 Publications Verification

    		 Casein Kinase CDK SGK Ribosomal S6 Kinase (RSK) Cancer
    CKI-7 is a potent and ATP-competitive casein kinase 1 (CK1) inhibitor with an IC50 of 6 μM and a Ki of 8.5 μM. CKI-7 is a selective Cdc7 kinase inhibitor. CKI-7 also inhibits SGK, ribosomal S6 kinase-1 (S6K1) and mitogen- and stress-activated protein kinase-1 (MSK1). CKI-7 has a much weaker effect on casein kinase II and other protein kinases .
    CKI-7
  • 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-12774
    IC261
    4 Publications Verification

    		 Casein Kinase Apoptosis Cancer
    IC261 is a selective, ATP-competitive CK1 inhibitor, with IC50s of 1 μM, 1 μM, 16 μM for Ckiδ, Ckiε and Ckiα1, respectively.
    IC261
  • 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-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-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-114858
    Epiblastin A
    1 Publications Verification

    		 Casein Kinase Cancer
    Epiblastin A is an ATP competitive casein kinase 1 (CK1) inhibitor with IC50s of 8.9, 0.5, and 4.7 µM for CK1α, CK1δ, and CK1 ɛ, respectively. Epiblastin A induces reprogramming of epiblast stem cells into embryonic stem cells by inhibition of CK1 .
    Epiblastin A
  • HY-133028
    CKI-7 free base
    1 Publications Verification

    		 Casein Kinase CDK SGK Ribosomal S6 Kinase (RSK) Cancer
    CKI-7 free base is a potent and ATP-competitive casein kinase 1 (CK1) inhibitor with an IC50 of 6 μM and a Ki of 8.5 μM. CKI-7 free base is a selective Cdc7 kinase inhibitor. CKI-7 free base also inhibits SGK, ribosomal S6 kinase-1 (S6K1) and mitogen- and stress-activated protein kinase-1 (MSK1). CKI-7 free base has a much weaker effect on casein kinase II and other protein kinases .
    CKI-7 free base
  • 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-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-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-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-120675
    SSTC3
    2 Publications Verification

    		 Casein Kinase Wnt Cancer
    SSTC3 is a casein kinase 1α (CK1α) activator (Kd = 32 nM) that inhibits WNT signaling (EC50 = 30 nM). SSTC3 exhibits minimal gastrointestinal toxicity compared to other classes of WNT inhibitors .
    SSTC3
  • HY-108442
    JW67
    1 Publications Verification

    		 Wnt Cancer
    JW67 inhibits the canonical Wnt signaling with an IC50 of 1.17μM . JW67 affects the multiprotein complex consisting of β-catenin/GSK-3β/AXIN/APC/CK1 that rapidly reduces active β-catenin with a subsequent downregulation of Wnt target genes. JW67 also inhibits colorectal cancer cell growth .
    JW67
  • HY-N3127
    Orobol

    		Casein Kinase PI3K VEGFR Metabolic Disease
    Orobol is one of the major soy isoflavones and has various pharmacological activities, including anti-skin-aging and anti-obesity effects. Orobol inhibits CK1ε, VEGFR2, MAP4K5, MNK1, MUSK, TOPK, and TNIK (IC50=1.24-4.45 μM). Orobol also inhibits PI3K isoforms (IC50=3.46-5.27 μM for PI3K α/β/γ/K/δ) .
    Orobol
  • HY-153866
    CK1-IN-2

    		Casein Kinase Cancer
    CK1-IN-2 (compound Nr.4) is a potent CK1 inhibitor with an IC50 values of 123, 19.8, 26.8, 74.3 nM for CK1a, CK1d, CK1e, p38a, respectively .
    CK1-IN-2
  • 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-121944
    Ricinine

    		Casein Kinase Wnt Others
    Ricinine exhibits hepatoprotection in CCl4-induced liver damage. Ricinine is also a CK1α inhibitor, and may activate Wnt pathway .
    Ricinine
  • HY-148455
    Casein kinase 1δ-IN-3

    		Casein Kinase Neurological Disease
    Casein kinase 1δ-IN-3 (Compound 23a) is a casein kinase 1 delta (CK1d) inhibitor with a pIC50 of 6.5376 M .
    Casein kinase 1δ-IN-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-12279C
    Umbralisib hydrochloride
    5 Publications Verification

    TGR-1202 hydrochloride; RP5264 hydrochloride

    		 PI3K Casein Kinase Cancer
    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 .
    Umbralisib hydrochloride
  • HY-123955
    Casein Kinase inhibitor A86

    		Casein Kinase CDK Apoptosis Cancer
    Casein Kinase inhibitor A86 is a potent and orally active casein kinase 1α (CK1α) inhibitor. Casein Kinase inhibitor A86 also inhibits of CDK7 (TFIIH) and CDK9 (P-TEFb). Casein Kinase inhibitor A861 induces leukemia cell apoptosis, and has potent anti-leukemic activities .
    Casein Kinase inhibitor A86
  • HY-174371
    INNO-220

    		Molecular Glues Casein Kinase MDM-2/p53 MALT1 Neurological Disease Cancer
    INNO-220 is an orally active, CRBN-dependent molecular glue degrader targeting CK1α. INNO-220 induces cell cycle arrest at G0/G1 phase and triggers apoptosis by degrading CK1α. INNO-220 disrupts the assembly and function of the CARD11/BCL10/MALT1 complex, thereby inhibiting NF-κB signaling in stimulated T cells and lymphoma cells that harbor an activating mutation in CARD11. INNO-220 provides a new direction for lymphoma research.
    INNO-220
  • HY-N6841
    Rhodiolin
    1 Publications Verification

    		 Glucose-6-Phosphate Isomerase (GPI) Casein Kinase Virus Protease Flavivirus PI3K Akt mTOR Apoptosis Infection Cancer
    Rhodiolin, a flavonoid, is an orally active glucose 6-phosphate isomerase (GPI) inhibitor. Rhodiolin inhibits papillary thyroid cancer (PTC) by targeting glycolysis enzyme glucose 6-phosphate isomerase GPI and suppressing PI3K/AKT/mTOR phosphorylation and induce apoptosis. Rhodiolin as a NS2B-NS3 protease inhibitor can disrupt dengue viral replication. Rhodiolin is also a potential candidate for developing anticancer strategies inhibiting CK1ε kinase. Rhodiolin can be used for the study of anti-tumor and anti-viral .
    Rhodiolin
  • HY-117857
    MRT00033659

    		Casein Kinase Checkpoint Kinase (Chk) MDM-2/p53 Early 2 Factor (E2F) Cancer
    MRT00033659 is a potent broad-spectrum kinase inhibitor of CK1 (IC50=0.9 μM for CK1δ) and CHK1 (IC50=0.23 μM). MRT00033659, a pyrazolo-pyridine analogue, induces p53 pathway activation and E2F-1 destabilisation .
    MRT00033659
  • HY-148112
    Casein kinase 1δ-IN-1

    		Casein Kinase Neurological Disease
    Casein kinase 1δ-IN-1 is an inhibitor of casein kinase 1δ (CK1δ). Casein kinase 1δ-IN-1 can be used for the research of neurodegenerative diseases such as tauopathies .
    Casein kinase 1δ-IN-1
  • HY-15424R
    5-Iodotubercidin (Standard)

    NSC 113939 (Standard); 5-ITu (Standard)

    		 Adenosine Kinase Reference Standards Cancer
    5-Iodotubercidin (Standard) is the analytical standard of 5-Iodotubercidin. This product is intended for research and analytical applications. 5-Iodotubercidin (NSC 113939), an ATP mimetic, is a potent adenosine kinase inhibitor with an IC50 of 26 nM. 5-Iodotubercidin (NSC 113939) initiates glycogen synthesis in isolated hepatocytes by causing inactivation of phosphorylase and activation of glycogen synthase. 5-Iodotubercidin (NSC 113939) also inhibits CK1, insulin receptor tyrosine kinase, phosphorylase kinase, PKA, CK2, PKC and Haspin .
    5-Iodotubercidin (Standard)
  • 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-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-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-12470A
    PF-4800567 hydrochloride

    		Casein Kinase Cancer
    PF-4800567 hydrochloride is a potent and selective inhibitor of?casein kinase?1? (CK1?), with an?IC50?of 32 nM, which is greater than 20-fold selectivity over CK1δ (IC50, 711 nM). PF-4800567 hydrochloride is useful in probing unique roles between these two kinases in multiple signaling pathways .
    PF-4800567 hydrochloride
  • HY-N7183
    9-Hydroxycanthin-6-one

    		NF-κB GSK-3 β-catenin Wnt Cancer
    9-Hydroxycanthin-6-one is a β-carboline alkaloid. 9-Hydroxycanthin-6-one can be isolated from the roots of E. longifolia. 9-Hydroxycanthin-6-one inhibits TNF-α-induced activation of the NF-κB pathway. 9-Hydroxycanthin-6-one activates GSK3β independently of CK1α, drives phosphorylation and degradation of β-catenin, and inhibits the Wnt signaling pathway. 9-Hydroxycanthin-6-one exerts selective cytotoxicity against Wnt-dependent colon cancer cells. 9-Hydroxycanthin-6-one can be used in studies related to colon cancer .
    9-Hydroxycanthin-6-one
  • HY-153866A
    CK1-IN-2 hydrochloride

    		Casein Kinase Cancer
    CK1-IN-2 (compound Nr.4) hydrochloride is a potent CK1 inhibitor with an IC50 values of 123, 19.8, 26.8, 74.3 nM for CK1a, CK1d, CK1e, p38a, respectively .
    CK1-IN-2 hydrochloride
  • HY-162756
    CK1-IN-4

    		Casein Kinase Neurological Disease
    CK1-IN-4 (Compound 59) is an inhibitor for casein kinase CK1δ with IC50 of 2.74 μM. CK1-IN-4 exhibits neuroprotective effect in Ethacrynic acid (HY-B1640)-treated SH-SY5Y cells .
    CK1-IN-4
  • 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-149292
    SR-4133

    		Casein Kinase Cancer
    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 .
    SR-4133
  • 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-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-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

Inquiry Online

Your information is safe with us. * Required Fields.

Salutation

  

Country or Region *

Applicant Name *

 

Organization Name *

Department *

     

Email Address *

 

Product Name *

Cat. No.

  

Requested quantity *

Phone Number *

     

Remarks

Inquiry Online

Inquiry Information

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent: