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[1][2][3][4].
CK2-IN-7 (compound 2) is an inhibitor of casein kinase 2 (CK2). CK2-IN-7 shows synergistic effect with structurally distinct CK2 chemical probe: SGC-CK2-1, against cancer[1].
IC261 is a selective, ATP-competitive CK1 inhibitor, with IC50s of 1 μM, 1 μM, 16 μM for Ckiδ, Ckiε and Ckiα1, respectively.
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 drug-seeking behavior in a rodent operant reinstatement model in animals in a dose-dependent manner[1]. PF-5006739 improves glucose tolerance in both diet-induced obesity (DIO) and genetic (ob/ob) mice models of obesity[2].
TTP 22 is a potent CK2 inhibitor, with an IC50 of 100 nM and a Ki of 40 nM.
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 II Substrate is a casein kinase II (CK2) peptide substrate that can be selectively phosphorylated by CK2[1].
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.
CK2-IN-1 is a CK2 inhibitor, with an IC50 of 150 nM[1].
Ac-VDVAD-CHO is a caspase-2/3 inhibitor (IC50: 46 and 15 nM)[1].
DMAT is a potent and specific CK2 inhibitor with an IC50 value of 130 nM.
GO289 (GO-289, GO 289) is a potent and selective inhibitor of casein kinase 2 (CK2) with IC50 of 7 nM in in vitro kinase assays, shows minor effects on CKIδ and CKIα activity in vitro; GO289 showed only a moderate or minor effect on the activity of 59 kinases from a variety of classes, the second most affected kinase was PIM2 with an IC50 of 13 nM; caused dose-dependent lengthening of circadian period not only in Bmal1-dLuc reporter cells but also in Per2-dLuc reporter cells with a phase opposite to that of Bmal1-dLuc, inhibits phosphorylation of clock protein PER2 S693 in cells; strongly inhibits Caki-2, A498, and 769-P cancer cells, significantly reduces growth of mouse MLL-AF9 leukemia cells without effect on hematopoietic progenitor cells; shows effectivity on circadian period and reporter signal intensity in spleen explants of MLL-AF9 mice.
Casein kinase 1δ-IN-8 (compound 494) is an inhibitor of Casein kinase 1δ, Casein kinase 1δ-IN-8 can be used in the treatment of neurodegenerative disorders such as Alzheimer's disease[1].
CX-4945 is a potent, selective and oral casein kinase 2 (CK2) inhibitor with a Ki of 0.38 nM.
Casein kinase 1δ-IN-10 is a casein kinase 1δ (CK1δ) inhibitor (WO2012080729A2; compound 685)[1].
TMCB is a selective, ATP-competitive CK2 (casein kinase II) inhibitor with distinct Ki values of 83 nM and 21 nM for the two different catalytic CK2 subunits α and α', respectively[1].
Casein Kinase 2 Substrate Peptide is a common CK2 substrate peptide. Casein Kinase 2 Substrate Peptide is synthesized with its C-terminus conjugated to 5-[(2-aminoethyl)amino]naphthalene-1-sulfonic acid (EDANS). Casein Kinase 2 Substrate Peptide can be used for protein kinase CK2 activity determination[1].
LH846 is a selective inhibitor of CKIδ, with an IC50 of 290 nM, and less potently inhibits CKIα and CKIε, with IC50s of 2.5 μM and 1.3 μM, respectively.
Quinalizarin is a potent, selective and cell-permeable protein kinase CK2 inhibitor with an Ki of ~50 nM and an IC50 of 110 nM. Quinalizarin can induce apoptosis of certain cancer cells[1].
Casein kinase 1δ-IN-14 (compound 481) is a casein kinase inhibitor that can be used to study neurodegenerative diseases such as Alzheimer's disease[1].
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[1].
CK2-IN-4 (compound 5) is a protein kinase (CK2) inhibitor (IC50=8.6 µM). CK2-IN-4 has good potential for research in the areas of cancer, viral infections and glomerulonephritis[1].
JNJ-6204 is a dual inhibitor for CSNK1D (Casein Kinase 1 Delta) and CSNK1E (Casein Kinase 1 Epsilon) (CSNK1D IC50=2.3 nM; CSNK1E IC50=137 nM). JNJ-6204 shows good brain exposure[1][2].
SGC-CK2-1 is a highly potent, ATP-competitive, and cell-active CK2 chemical probe with exclusive selectivity for both human CK2 isoforms, with IC50s of 36 and 16 nM for CK2α and CK2α′respectively in the nanoBRET assay. SGC-CK2-1 can be used for the research of neurodegenerative diseases[1][2].
CK2α-IN-1 (compound 2) is a selective CK2α inhibitor (IC50=7.0 µM; Ki=1.6 µM) that exhibits a non-ATP-competitive mode of action. CK2α-IN-1 exhibits good potential for anticancer studies[1].
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)[1][2].
Umbralisib (TGR-1202) tosylate 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 tosylate exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib tosylate can be used for haematological malignancies reseach[1][2][3][4].
ON 108600 is a inhibitor for CK2 (Casein Kinase2)/TNIK/DYRK1 , with the IC50s for DYRK1A/DYRKB, DYRK2, CK2α1/CK2α2, and TNIK of 0.016 μm/0.007 μM, 0.028 μM, 0.05 μM/0.005 μM, and 0.005 μM, respectively. ON 108600 has antitumor activity[1].
AMG-548 is a potent, oral and selective p38α inhibitor (Ki=0.5 nM), shows slightly selective over p38β (Ki=36 nM) and >1000 fold selective against p38γand p38δ. AMG 548 is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM) [1]. AMG-548 inhibits Wnt signaling by direcly inhibing Casein kinase 1 isoforms δ and ε[2].
Casein Kinase inhibitor A86 (CKIα inhibitor A86) is a novel pan-specific CKI (CSNK1) inhibitor (Kd=1-10 nM, CKIα Kd=9.8 nM) that co-targets the transcriptional kinases CDK7 and CDK9, with hardly inhibition of CDK8, CDK13, CDK11a, CDK11b, and CDK19; target both CDK7 and CDK9 with low nM Kd values; induces leukemia cell apoptosis at <160 nM, in correlation to the capacity to stabilize p53; shows high and selective sensitivity against leukemic CFUs in colony-forming unit (CFU) assay, without effect on normal hematopoietic CFUs; blocking CKIα together with CDK7 and/or CDK9 synergistically stabilize p53, deprive leukemia cells of survival and proliferation-maintaining SE-driven oncogenes, induce apoptosis, abolishes the expression of MYC, MDM2, and the anti-apoptotic oncogene MCL1; demonstrates therapeutic efficacy with preserved hematopoiesis and leukemia cure potential in AML mouse models.