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Casein Kinase Inhibitors

Cat.No. Product Name Information Product Use Citations Product Validations
S6578 Longdaysin Longdaysin is a Casein Kinase inhibitor with IC50 values of 8.8 μM, 5.6 μM, 52 μM and 29 μM for CKIδ, CKIα, ERK2 and CDK7.
Nat Commun, 2021, 12(1):7003
S2249 PF 4800567 PF 4800567 is a novel and potent inhibitor of casein kinase 1 epsilon (IC50=32 nM) with greater than 20-fold selectivity over casein kinase 1 delta(IC50=711 nM).
Blood Adv, 2020, 4(13):3072-3084
E2914 5,6-Dichlorobenzimidazole 1-beta-D-ribofuranoside 5,6-Dichlorobenzimidazole riboside(DRB) is a nucleoside analog that inhibits several carboxyl-terminal domain (CTD) kinases including casein kinase II and CDKs. It trigger p53-dependent apoptosis of human colon adenocarcinoma cells without inducing genotoxic stress to healthy cells.
Cancer Sci, 2025, 10.1111/cas.70081
S5516 Ellagic Acid hydrate Ellagic acid is a potent inhibitor of protein kinase CK2 with IC50s of 0.04, 2.9 and 3.5 μM for CK2, Lyn and PKA respectively. It shows potent antioxidant, anti-mutagenic and antidepressant properties.
J Cell Biol, 2022, 221-11e202202100
S9331 7-Hydroxy-4-methyl-8-nitrocoumarin 7-Hydroxy-4-methyl-8-nitrocoumarin is a chemical.
E1455New BTX-A51 BTX-A51 (Casein Kinase inhibitor A51) is a first-in-class oral and potent inhibitor of casein kinase 1α (CK1α) and cyclin dependent kinase (CDK7/9) with an IC50 of 17 nM for CK1α and Kd of 1.3 nM and 4 nM for CDK7 and CDK9, respectively. It induces apoptosis of leukemic cells by activating p53 and inhibiting expression of Mcl1 and can be used in Acute myeloid leukemia (AML) cancer research.
S6544 SR-3029 SR-3029 is a potent and selective casein kinase 1δ/1ε (CK1δ/ε) inhibitor with IC50 values of 44 and 260 nM for CK1δ and CK1ε, respectively.
E1413 DEG-77 DEG-77 is a cereblon-dependent degrader of IKZF2 and casein kinase 1α (CK1α). It blocks cell growth and delays leukemia progression in murine and human acute myeloid leukemia (AML) mouse models.
E1412 DEG-35 DEG-35 is a cereblon-dependent degrader of IKZF2 and casein kinase 1α (CK1α). It blocks cell growth and delays leukemia progression in murine and human acute myeloid leukemia (AML) mouse models.
E7852 CKI-7 CKI-7 (CKI-7 2HCl) is an inhibitor of casein kinase 1 (CK1) with ki of 8.5 μM and IC50 of 6 μM. It is selective for CK1 over CK2, PKC, CaM kinase II (CaMKII), and cyclic AMP-dependent protein kinase (PKA) with IC50 of 90, >1000, 195, and 550 μM, respectively. This compound also inhibits SGK, ribosomal S6 kinase-1 (S6K1) and mitogen- and stress-activated protein kinase-1 (MSK1).
E6444New SSTC3 SSTC3 is a potent activator of casein kinase 1α (CK1α) with a Kd of 32 nM that inhibits WNTsignaling with an EC50 of 30 nM. It attenuates CRC cell growth through CK1α-dependent WNT pathway inhibition, offering an improved therapeutic index for targeting WNT-driven tumors.
E4725New BMS-986397 BMS-986397 (CC-91633) is a potent and selective thalidomide-derived molecular glue degrader of CK1α and a modulator of CRBN E3 ubiquitin ligase. As a first-in-class CELMoD agent, it exhibits strong anti-leukemic activity in AML (Acute Myeloid Leukemia) and HR-MDS (High-Risk Myelodysplastic Syndrome) models, with enhanced efficacy and potency for hematologic malignancies and immunomodulation.
E1927 PF-05251749（CK1-IN-2） PF-05251749 (CK1-IN-2, Compound Nr.4) is a potent, selective, brain-penetrant inhibitor of Casein Kinase 1 (CK1) in a concentration-dependent manner, with IC50 values of 33.1 nM for CK1d and 51.6 nM for CK1e. It also functions as an inducer of CYP3A, with the potential to treat circadian rhythm disruptions in Alzheimer's and Parkinson's diseases.
S0350 CK1-IN-1 CK1-IN-1 (PUN51207, Compound 1C) is an inhibitor of casein kinase 1 (CK1) with IC50 of 15 nM, 16 nM and 73 nM for CK1δ, CK1ε and p38α MAPK, respectively.
E2659 DMAT DMAT is a high affinity and selective casein kinase-2 (CK2) inhibitor with IC50 of ~0.14 μM and Ki of ~40 nM.
E2826 Hematein Hematein inhibits casein kinase II activity in a selective, dose-dependent and ATP non-competitive manner in vitro, with IC50 of 0.55 μM in the presence of 10 μM ATP.
S0186 TA-01 TA-01 is a potent inhibitor of CK1δ/ε and p38 MAPK with IC50 of 6.4 nM, 6.8 nM and 6.7 nM for CK1ε, CK1δ and p38 MAPK, respectively.
S2805 LY364947 LY364947 (HTS 466284) is a potent ATP-competitive inhibitor of TGFβR-I with IC50 of 59 nM in a cell-free assay, shows 7-fold selectivity over TGFβR-II.
Adv Sci (Weinh), 2024, 11(4):e2304987
Cell Rep Med, 2024, 5(2):101416
Cell Commun Signal, 2024, 22(1):242
Verified customer review of LY364947
S3143 Pyruvic acid

Pyruvic acid (Acetylformic acid) is an important organic chemical intermediate that plays a role in cardiomyocyte pathophysiology and therapy. This compound markedly increases the level of lactate dehydrogenase (LDH) and creatine kinase (CK) and reduces the level of Ca2+Mg2+-ATPase and Na+K+-ATPase.
S0995 BioE-1115 BioE-1115 is a highly selective and potent dual inhibitor of PAS kinase (PASK) and casein kinase 2α (CK2α) with IC50 of ~4 nM and ~10 μM, respectively.
E2506 A-3 hydrochloride A-3 hydrochloride, a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases, againsts cAMP-dependent protein kinase (PKA) (Ki=4.3 µM), casein kinase II (CK2) (Ki=5.1 µM) and myosin light chain kinase (MLCK) (Ki=7.4 µM), also inhibits Protein Kinase C (PKC) and casein kinase I (CK1) with Ki values of 47 µM and 80 µM, respectively.