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You are here:Home-Inhibitors & Agonists-Wnt/Notch/Hedgehog-Casein Kinase

Request The Product List ofCasein Kinase Casein Kinase

Casein Kinases (CKs) are serine/threonine-selective enzymes that function as regulators of signal transduction pathways in most eukaryotic cell types.

Cat. No. Product Name CAS No. Information
H8214

VU-WS211

A negative control of VU-WS113, which is a potent inhibitor of Wnt signaling with EC50 of 80 nM that selectively potentiates CK1α kinase activity.

H8213

VU-WS113

1415921-09-3

VU-WS113 is a potent inhibitor of Wnt signaling with EC50 of 80 nM that selectively potentiates CK1α kinase activity.

H8212

TBBz

577779-57-8

A potent, selective and ATP-competitive CK2 inhibitor with Ki of 0.5-1 uM; weakly inhibits CK1 (about 100-fold less potent), and has no activity for PKA and PKC; decreases the activity of GBM-initiating cell regulator β-catenin, reduces cell growth, decreases tumor size, and increases survival rates in GBM xenograft mouse models.

H8211

TA-01

1784751-18-3

A potent inhibitor of Casein Kinase CK1ε, CK1δ and p38α with IC50 of 6.4, 6.8 and 6.7 nM, respectively; inhibits the phosphorylation of proteins downstream of p38α MAPK such as MAPKAPK2 and HSP27 during cardiogenesis, and increases ATF-2 and MEF2C during cardiac differentiation.

H8210

SSTC3

1242422-09-8

SSTC3 is a novel small-molecule CK1α activator with EC50 of 30 nM (WNT-driven reporter gene assay), Kd of 32 nM; has better pharmacokinetic properties than pyrvinium, attenuates the growth of such Apc mutant organoids with EC50 of 2.9 uM; decreases the viability of the WNT-dependent cell lines (EC50 = 132, 63, and 123 nM for HT29, SW403, and HCT116 cells, respectively), inhibits the growth of CRC xenografts in mice; also attenuates the growth of patient-derived metastatic CRC xenograft, with minimal gastrointestinal toxicity compared to other classes of WNT inhibitors.

H8209

SR-653234

1446715-41-8

A purine scaffold casein kinase 1δ/1ε (CK1δ/ε) inhibitor with IC50 of 160/540 nM, respectively.

H8208

SR-3029

1454585-06-8

SR-3029 is a potent, highly selective, ATP-competitive and brain penetrating Casein Kinase 1δ/ε (CK1δ/ε) inhibitor with IC50 of 44/260 nM, respectively; inhibits melanoma A375 cell growth with IC50 of 86 nM; triggers apoptosis of CK1δ-expressing breast tumor cells ex vivo, tumor regression in orthotopic models of triple-negative breast cancer in mice model.

H8207

SR-2890

1454584-91-8

A potent, highly selective casein kinase 1δ/1ε (CK1δ/ε) inhibitor with IC50 of 4 nM for CK1δ; inhibits melanoma A375 cell growth with EC50 of 38 nM in MTT assays, has physical, in vitro and in vivo PK properties suitable for use in proof of principle animal xenograft studies against human cancer cell lines.

H8206

Quinalizarin

81-61-8

Quinalizarin is a potent, selective and cell-permeable inhibitor of CK2 with Ki of 58 nM; shows selectivity over DYRK1a, PIMs, HIPK2, MNK1, ERK8 and PKD1; inhibits endogenous CK2 and induces apoptosis more efficiently than Emodin in Jurkat cells; reduces cell viability with emphasis on adenocarcinoma cells harboring EGFR sensitive mutation, suppresses migration, and accelerates apoptosis in different human lung cancer cell lines.

H8205

Pyrvinium pamoate

3546-41-6

An anthelmintic effective agent for pinworms that shows to be a potent inhibitor of Wnt signaling with EC50 of 10 nM; binds to all CK1 family members in vitro at low nanomolar concentrations and selectively potentiates CK1α kinase activity; inhibits Wnt signaling downstream of β-catenin, and promotes Pygopus degradation; also is a potent inhibitor of HH signaling by reducing the stability of the Gli family of transcription factors.

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