Casein Kinase Inhibitor

Casein Kinase Inhibitors (194):

Art. -Nr.	Produktname	Wirkung	Reinheit

HY-12470

PF-4800567	Inhibitor	99.69%
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).

HY-15535

DMAT	Inhibitor	98.13%
DMAT is a potent and specific CK2 inhibitor with an IC₅₀ value of 130 nM.

HY-108642B

AMG-548 dihydrochloride	Inhibitor	99.86%
AMG-548 dihydrochloride, an orally active and selective p38α inhibitor (K_i=0.5 nM), shows slightly selective over p38β (K_i=36 nM) and >1000 fold selective against p38γ and p38δ. AMG-548 dihydrochloride is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC₅₀=3 nM). AMG-548 dihydrochloride inhibits Wnt signaling by directly inhibiting Casein kinase 1 isoforms δ and ε.

HY-100011

SR-3029	Inhibitor	99.73%
SR-3029 is a potent and ATP competitive CK1δ and CK1ε inhibitor, with IC₅₀s of 44 nM and 260 nM, respectively, and K_is of 97 nM for both kinases.

HY-158975

VRK1/CK1-IN-1	Inhibitor	98.69%
VRK1/CK1-IN-1 (compound 36) is a dual VRK1 and CK1 family inhibitor, with a K_i 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.

HY-12774

IC261	Inhibitor	99.63%
IC261 is a selective, ATP-competitive CK1 inhibitor, with IC₅₀s of 1 μM, 1 μM, 16 μM for Ckiδ, Ckiε and Ckiα1, respectively.

HY-N0559

Kirenol	Inhibitor	99.82%
Kirenol is a diterpenoid compound, an orally active apoptosis inducer and signaling pathway regulator, with a K_d value of 5.47 μM against the target CK2. Kirenol promotes the cleavage of Bid into tBid, regulates the protein levels/phosphorylation of Bax, Bcl-2, p53 and p21, and induces caspase-independent apoptosis, S-phase cell cycle arrest, ROS accumulation and cytotoxicity in cancer cells. Kirenol activates the CK2/AKT and AMPK-mTOR-ULK1 pathways, inhibits the signaling of NF-κB, TGF-β/Smads and NLRP3 inflammasome, and regulates the GSK3β, BMP and Wnt/β-catenin pathways. Kirenol induces autophagy, mitophagy and osteoblast differentiation, promotes mitochondrial fusion, and exerts antioxidant, anti-inflammatory, antifibrotic, renoprotective, cardioprotective, neuroprotective and analgesic effects. Kirenol is applicable to research related to chronic myeloid leukemia, ischemic stroke, diabetic nephropathy, heart failure, acute lung injury and osteoporosis.

HY-12443

PF-5006739	Inhibitor	99.70%
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.

HY-145322

TMX-4116	Inhibitor	99.76%
TMX-4116 is a casein kinase 1α (CK1α) degrader. TMX-4116 shows the degradation preference for CK1α with DC₅₀s less than 200 nM in MOLT4, Jurkat, and MM.1S cells. TMX-4116 can be used for the research of multiple myeloma.

HY-129571

BioE-1115	Inhibitor	98.17%
BioE-1115 is a highly selective and potent PAS kinase (PASK) inhibitor with an IC₅₀ of ~4 nM. BioE-1115 is also a potent casein kinase 2α inhibitor with an IC₅₀ of ~10 μM.

HY-119751

Hematein	Inhibitor
Hematein is a oxidation product of hematoxylin acted as a dye. Hematein is an allosteric casein kinase II inhibitor with an IC₅₀ of 0.74 μM. Hematein inhibits Akt/PKB Ser129 phosphorylation, the Wnt/TCF pathway and increases apoptosis in lung cancer cells.

HY-145939

BAY-888	Inhibitor	98.27%
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.

HY-145940

BAY-204	Inhibitor	99.94%
BAY-204 (BRD3727) is a potent, ATP-competitive, and selective CSNK1α inhibitor (IC₅₀ = 2 nM at 10 μM ATP; 12 nM at 1 mM ATP). BAY-204 can be used for the study of acute myeloid leukemia (AML).

HY-115519

(E/Z)-GO289	Inhibitor	98.98%
(E/Z)-GO289 is a potent and selective casein kinase 2 (CK2) inhibitor (IC₅₀=7 nM). (E/Z)-GO289 strongly lengthens circadian period. (E/Z)-GO289 exhibits cell type–dependent inhibition of cancer cell growth that correlated with cellular clock function.

HY-133028

CKI-7 free base	Inhibitor	99.31%
CKI-7 free base is a potent and ATP-competitive casein kinase 1 (CK1) inhibitor with an IC₅₀ of 6 μM and a K_i 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.

HY-153866

CK1-IN-2	Inhibitor	99.20%
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.

HY-108642

AMG-548	Inhibitor	≥99.0%
AMG-548, an orally active and selective p38α inhibitor (K_i=0.5 nM), shows slightly selective over p38β (K_i=36 nM) and >1000 fold selective against p38γ and p38δ. AMG 548 is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC₅₀=3 nM). AMG-548 inhibits Wnt signaling by directly inhibiting Casein kinase 1 isoforms δ and ε.

HY-18285

Longdaysin	Inhibitor	99.83%
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.

HY-148491

CSNK1-IN-2	Inhibitor	99.22%
CSNK1-IN-2 is a CSNK1A1 inhibitor. CSNK1-IN-1 has inhibitory activity for CSNK1A1 kinase with IC₅₀ values of 44 nM. CSNK1-IN-2 can be used for the research of proliferative disorders.

HY-135906

CK2/ERK8-IN-1	Inhibitor	99.0%
CK2/ERK8-IN-1 is a dual casein kinase 2 (CK2) (K_i of 0.25 µM) and ERK8 (MAPK15, ERK7) inhibitor with IC₅₀s of 0.50 μM. CK2/ERK8-IN-1 also binds to PIM1, HIPK2 (homeodomain-interacting protein kinase 2), and DYRK1A with K_is of 8.65 µM, 15.25 µM, and 11.9 µM, respectively. CK2/ERK8-IN-1 has pro-apoptotic efficacy.

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