caseinkinase

LY294002 (SF 1101) is a broad-spectrum inhibitor of PI3K, inhibiting PI3Kα, PI3Kδ, and PI3Kβ (IC50=0.5/0.57/0.97 μM). LY294002 is also an inhibitor of DNA-PK (IC50=1.4 μM) and an inhibitor of CK2 (IC50=98 nM). LY294002 activates apoptosis and autophagy.

IWP-2 is a Wnt pathway inhibitor (IC50=27 nM) and an ATP-competitive CK1δ inhibitor (IC50=40 nM for M82FCK1δ). IWP-2 inhibits self-renewal of embryonic stem cells and has been used in stem cell and organoid research.

Casein Kinase II Inhibitor IV is an inducer of epidermal keratinocyte differentiation.

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.

Emodin (Frangula emodin) is an 11β-HSD1 inhibitor with a selective IC50 of 186 and 86 nM against 11β-HSD1 in humans and mice, respectively. Emodin has antiviral, anti-inflammatory, and anti-cancer effects. Emodin can improve metabolic disorders in diet-induced obese mice.

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

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

Casein kinase 1δ-IN-8 is an inhibitor of casein kinase 1δ and is used to treat neurodegenerative diseases such as Alzheimer's disease type.

NCC007 is a novel CKIα and CKIδ dual inhibitors by structural modification of N9 and C2 position of longdaysin.

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).

(E/Z)-GO289, which strongly lengthened circadian period, is a potent and selective inhibitor of CK2. (E/Z)-GO289 exhibited cell type-dependent inhibition of cancer cell growth that correlated with cellular clock function. The discovery of (E/Z)-GO289 provides a direct link between the circadian clock and cancer regulation and reveals unique design principles underlying kinase selectivity.

BioE-1115 is a selective and potent inhibitor of serine-threonine protein kinase (PASK, IC50 = 4 nM). BioE-1115 is a potent inhibitor of CK2α (IC50 = 10 μM).

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.

NMS-P715 is a selective and ATP-competitive MPS1 inhibitor(IC50 of 182 nM).

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.

A-443654, a pan-Akt inhibitor, exhibits equal potency against Akt1, Akt2, and Akt3 within cells (Ki=160 pM).

Silmitasertib sodium salt (CX-4945 sodium salt) is a potent and orally bioavailable, highly selective inhibitor of CK2(IC50 of 1 nM, CK2α).

PF-5006739 is an effective and selective inhibitor of CK1δ/ε (IC50s: 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 selecti

PI-828 is a phosphatidylinositol 3-kinase (PI3K) inhibitor, which is widely used to study the physiological function of PI3K and also promotes stem cell differentiation into mesoderm.

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).

LY-364947 (HTS466284) is a potent ATP-competitive inhibitor of TGFβR-I.

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

IC261 (SU-5607) is a novel inhibitor of CK1, triggers the mitotic checkpoint control. The IC50 of IC261 for CK1 was 16 μM and for Cdk5 is 4.5 mM.