a-casein

Casein is a milk protein with multiple roles in a novel drug delivery system that affects postprandial amino acid delivery in different ways through its intragastric coagulation properties.

CK2/ERK8-IN-1 (TMCB) is a dual inhibitor of casein kinase 2 (CK2) (Ki: 0.25 µM) and ERK8 (IC50s: 0.50 μM) with pro-apoptotic efficacy. CK2/ERK8-IN-1 also binds to PIM1, DYRK1A, and HIPK2 (Kis: 8.65 µM, 11.9 µM, and 15.25 µM).

TBCA (Casein Kinase II Inhibitor III, TBCA) is a highly selective CK2 (casein kinase II) inhibitor, IC50 = 110 nM, Ki = 77 nM. TBCA shows selectivity for CK2 over CK1, DYRK1A and a panel of 27 other kinases.

H-89 is a selective inhibitor of cyclic AMP-dependent protein kinase (protein kinase A; IC50: 48 nM). H-89 has weak inhibition on PKG, Casein Kinase, PKC, and other kinases.

Silmitasertib (CX-4945) is a potent, orally bioavailable inhibitor of casein kinase 2 (CK2; Ki: 0.38 nM).

TBB (NSC-231634)(NSC-231634) is a highly selective, ATP GTP-competitive inhibitor of casein kinase-2 (CK2).

Casein kinase 1δ-IN-9 is a Quinone reductase 2 inhibitor with IC50 of 0.6μM.

CK1-IN-1 (PUN51207) is a casein kinase 1 (CK1) inhibitor. CK1-IN-1 has IC50s of 15 nM, 16 nM, 73 nM for CK1δ, and CK1ε, p38σ MAPK, respectively.

TTP 22 is a high affinity, ATP-competitive casein kinase 2 (CK2) inhibitor with IC50/Ki of 0.1 uM/40 nM, and shows selectivity >250-fold for CK2 over JNK3, ROCK1, and MET(IC50> 10 uM).

Epiblastin A is an inhibitor of Casein Kinase 1 (CK1). Epiblastin A engages CK1 isoenzymes in cell lysate and induces efficient conversion of epiblast stem cells (EpiSCs) into embryonic stem cells (cESCs).

A-3 hydrochloride is a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases. It inhibits PKC and casein kinase I with Ki values of 47 μM and 80 μM, respectively[1], and also inhibits PKA (Ki=4.3 μM), casein kinase II (Ki=5.1 μM), and myosin light chain kinase (MLCK) (Ki=7.4 μM).

Aureusimine B, also known as phevalin, is a natural pyrazinone produced by certain fungi and by Staphylococcus spp., including S. aureus. Its synthesis appears to be initiated by a conserved nonribosomal peptide synthetase that creates a dipeptide (phenylalanine-valine) aldehyde, which then undergoes cyclization and oxidation. Aureusimine B inhibits calpain in a casein hydrolysis assay (IC50 = 1.3 μM), contributes to S. aureus infection in mice, and alters human keratinocyte gene expression.

PF-4800567 is a selective inhibitor of casein kinase 1ε (CK1ε; IC50 = 32 nM) with greater than 20-fold selectivity over CK1δ.

PF-05236216 hydrochloride is a brain penetrant, potent and selective inhibitor of casein kinase 1 delta/epsilon (CK1δ/ε) that modulates circadian rhythms in mice.

Pyrvinium Iodide is a casein kinase 1α-dependent inhibitor of Wnt/β-Catenin.

Casein kinase 1δ-IN-4 (compound 567) is a potent inhibitor of casein kinase 1δ with potential application in Alzheimer's disease research [1].

WL47 is a high-affinity ligand for caveolin-1 (CAV1) with a dissociation constant (Kd) of 23 nM, demonstrating potent disruption of CAV1 oligomers. This compound exhibits selectivity for CAV1, with minimal interaction towards BSA, casein, and HEWL. Notably, WL47's molecular structure is 80% smaller than its T20 parent sequence, rendering it a useful tool for investigating caveolin-1 function [1].

Casein Kinase inhibitor A86 is a highly effective and orally bioavailable inhibitor of casein kinase 1α (CK1α) and also inhibits CDK7 (TFIIH) and CDK9 (P-TEFb). It induces apoptosis in leukemia cells, exhibiting substantial anti-leukemic effects.

ZK53 is a selective and potent activator of mitochondrial casein hydrolase protease P (HsClpP).ZK53 induces apoptosis and inhibits the hydrolysis of alpha-casein by HsClpP.ZK53 inhibits tumour growth in xenografts and native mouse models.

K-Casein (106-116), bovine, is a peptide that impedes platelet aggregation and fibrinogen binding, significantly contributing to the pathophysiology of atherosclerosis [1].

Benazoline oxalate salt is a pharmacological active compound that inhibits casein kinase Iε (CKIε) or CKIδ phosphorylation of the PER2 protein.

TMX-4113 has potential to be used in cancer that is a phosphodiesterase 6D(PDE6D) and casein kinase 1α(CK1α) degrader [1].

TMX-4116, a casein kinase 1α (CK1α) degrader, preferentially degrades CK1α in MOLT4, Jurkat, and MM.1S cells, exhibiting degradation concentration 50s (DC50s) below 200 nM. TMX-4116 is utilized in the research of multiple myeloma [1].

Casein Kinase II Substrate, a peptide substrate, is selectively phosphorylated by casein kinase II (CK2) [1].

Eflucimibe is an ACAT inhibitor. Eflucimibe regulates endogenous hypercholesterolemia in a synergistic manner in New Zealand rabbits fed a casein-enriched diet. In vivo, orally administered Eflucimibe displayed high potency and efficacy as an antihypercholesterolemic compound in different cholesterol-fed animals (guinea-pig, rat, rabbit).

CKI-7 free base is a potent, ATP-competitive inhibitor of casein kinase 1 (CK1; IC50: 6 μM; Ki: 8.5 μM) and a selective Cdc7 kinase inhibitor, also inhibiting SGK, ribosomal S6 kinase-1 (S6K1), and MSK1.

AMG-548 dihydrochloride is a selective, orally active p38α inhibitor with a Ki value of 0.5 nM, a slight selectivity for p38β (Ki=36 nM) and >1000-fold selectivity for p38γ and p38δ. AMG-548 dihydrochloride exhibits inhibition of whole blood LPS-stimulated TNFα with an IC50 value of 3 nM. AMG-548 dihydrochloride directly inhibited casein kinase 1 isoforms δ and ε, and inhibited Wnt signaling.

WL47 TFA, a high-affinity cavolin-1 (CAV1) ligand (Kd=23 nM), disrupts CAV1 oligomers with selectivity over BSA, casein, and HEWL. At 80% shorter than the original T20 parent sequence, WL47 TFA is utilized to investigate caveolin-1 function [1].

α-Casein (90-95) is a peptide fragment of α-Casein.

QLT0267 is an inhibitor targeting integrin-linked kinase (ILK; IC50= 26 nM), showing over 10-fold selectivity against cyclin-dependent kinases 1, 2, and 5 (Cdk1, Cdk2, and Cdk5), and over 1,000-fold selectivity against C-terminal Src kinase (CSK), DNA-PK, Pim-1, Akt, PKC, and casein kinase 2 (CK2) at a concentration of 10 mg/ml. This compound effectively inhibits the proliferation of NPA187 papillary thyroid cancer cells with an IC50 of approximately 3 µM and induces apoptosis in NPA187, DRO, and K4 cancer cell lines. In vivo studies reveal that QLT0267, administered at 100 mg/kg, significantly reduces tumor growth in a DRO mouse xenograft model and diminishes both tumor volume and intratumoral vascularization in a U87MG glioblastoma mouse xenograft model, showcasing its potential for therapeutic applications in cancer treatment.

Pepstatin Ammonium is a specific inhibitor of aspartic proteaseproduced by actinomycetes(hemoglobin-pepsin, hemoglobin-proctase, casein-pepsin, casein-proctase, casein-acid protease and hemoglobin-acid protease with IC50s of 4.5 nM, 6.2 nM, 150 nM, 290 nM

IN-1130 is a selective inhibitor of ALK5 with IC50 values of 5.3 nM, 36 nM, and 4.3 μM for phosphorylation of ALK5-mediated Smad3, ALK5 phosphorylation of casein and p38α mitogen-activated protein kinase.

Peptone from casein, obtained through the hydrolysis of casein by pancreatic enzymes, is refined to produce a peptone suitable for various applications.

Casein Kinase 2 Substrate Peptide, a widely recognized CK2 substrate, is synthesized with its C-terminus conjugated to 5-[(2-aminoethyl)amino]naphthalene-1-sulfonic acid (EDANS). This peptide serves as a tool for determining protein kinase CK2 activity [1].

AMG-548 hydrochloride is a selective, orally active p38α inhibitor with a Ki value of 0.5 nM, a slight selectivity for p38β (Ki=36 nM) and a 1000-fold selectivity for p38γ and p38δ. AMG 548 hydrochloride also effectively inhibits whole blood LPS-stimulated TNFα with an IC50 value of 3 nM. AMG-548 hydrochloride directly inhibited casein kinase 1 isoforms δ and ε, which in turn inhibited Wnt signaling.

ON 108600 is a chemical inhibitor targeting CK2 (Casein Kinase 2), TNIK, and DYRK1, demonstrating IC50 values of 0.016 μM and 0.007 μM for DYRK1A and DYRK1B, 0.028 μM for DYRK2, 0.05 μM and 0.005 μM for CK2α1 and CK2α2, and 0.005 μM for TNIK, respectively. This compound exhibits antitumor activity [1].

SSTC3 is a casein kinase 1α (CK1α) activator and a potent HIF1α inhibitor, each with a Kd of 32 nM. It has potential antitumor activity, inhibits WNT signaling, and suppresses SHH medulloblastoma tumor growth.

Rennin (Chymosin) is a proteolytic enzyme related to pepsin, produced in the stomachs of certain animals, that effectively coagulates liquid milk into a semi-solid form, prolonging its retention in the stomach. It specifically targets K-casein, cleaving the peptide bond between the amino acid residues phenylalanine and methionine (105 and 106), and plays a crucial role in cheese production [1].

ALV1 is a potent degradation agent of Ikaros and Helios, with similar degradation activity against IKZF1/2/3. ALV1 significantly reduced the protein abundance of IKZF1-4, CK1α (casein kinase 1α, CSNK1A1) and ribosomal protein RPL4, and induced Helios/CRBN dimerization, which promoted IL-2 secretion.

Casein kinase 1δ-IN-14 (WAY-637081) is a compound utilized in research to study atherosclerosis-related cardiovascular disease.

DRB is a nucleoside analog that inhibits several carboxyl-terminal domain (CTD) kinases including casein kinase II (IC50 range of 4-10 μM)

alpha-Casozepine is a fragment of alpha(s1)-casein with anxiolytic activity.

Knqdk peptide is a synthetic pentapeptide, located in residues 112-116 of bovine K-casein.

Casein kinase 1δ-IN-5 is a potent and selective CK-1δ inhibitor (IC50 = 47 nM) that exhibits neuroprotective and anti-inflammatory effects in vitro, with potential applications in neurodegenerative disease research.

D4476 (Casein Kinase I Inhibitor) is an effective, selective, and cell-permeant CK1 (casein kinase 1) inhibitor( IC50=300 nM in a cell-free assay).

Umbralisib (TGR-1202) sulfate, an orally active compound, serves as a potent, selective inhibitor targeting both PI3Kδ and casein kinase-1-ε (CK1ε), with EC50 values of 22.2 nM and 6.0 μM, respectively. It demonstrates unique immunomodulatory effects on T cells in chronic lymphocytic leukemia (CLL) and is applicable in the research of hematological malignancies.

DMAT (Casein kinase II Inhibitor) is a potent and specific inhibitor of CK2(IC50 value of 130 nM).

Ruboxistaurin hydrochloride (LY 333531 hydrochloride) is an Isozyme-selective inhibitor of protein kinase C (PKC); competitively and reversibly inhibits PKCβI and PKCβII (IC50 values are 4.7 and 5.9 nM respectively). Selective for PKCβ over other PKC isozymes (IC50values are 0.052, 0.25, 0.30, 0.36, 0.60 and >100 μM for PKCη, -δ, -γ, -α, -ε and -ζ respectively). Exhibits selectivity for PKC over other ATP-dependent kinases, including protein kinase A, casein kinase and src).

IQA is a casein kinase 2 (CK2) inhibitor.

Casein kinase 1δ-IN-7 is a Casein kinase 1δ inhibitor for neurodegenerative diseases such as Alzheimer's disease.