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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
138 Results for "
CK1
" in MedChemExpress (MCE) Product Catalog:
Products (138)
138 Results for "CK1" in MCE Product Catalog:
35
35 Publications Verification
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IWP-2 is an inhibitor of Wnt processing and secretion with an IC50 of 27 nM. IWP-2 targets the membrane-bound O-acyltransferase porcupine (Porcn) and thus preventing a crucial Wnt ligand palmitoylation. IWP-2 is also an ATP-competitive CK1δ inhibitor with an IC50 of 40 nM for the gatekeeper mutant M82FCK1δ [1] .
13
13 Cited Publications
Synonyms: NSC 113939; 5-ITu
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5-Iodotubercidin (NSC 113939), an ATP mimetic, is a potent adenosine kinase inhibitor with an IC50 of 26 nM. 5-Iodotubercidin (NSC 113939) initiates glycogen synthesis in isolated hepatocytes by causing inactivation of phosphorylase and activation of glycogen synthase. 5-Iodotubercidin (NSC 113939) also inhibits CK1, insulin receptor tyrosine kinase, phosphorylase kinase, PKA, CK2, PKC and Haspin [1] .
13
13 Cited Publications
Synonyms: Casein Kinase I Inhibitor
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D4476 is a potent, selective and cell-permeable inhibitor of casein kinase 1(CK1) with an IC50 value of 0.3 μM in vitro.
12
12 Cited Publications
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TAK-715 is an orally active and potent p38 MAPK inhibitor with IC50s of 7.1 nM, 200 nM for p38α and p38β, respectively. TAK-715 inhibits casein kinase I (CK1δ/ε) to regulate activation of Wnt/β-catenin signaling. TAK-715 shows good significant efficacy in a rat arthritis model [1] .
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8 Cited Publications
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PF-670462 dihydrochloride is a potent and selective inhibitor of casein kinase (CK1ε and CK1δ), with IC50s of 7.7 nM and 14 nM, respectively.
5
5 Cited Publications
Synonyms: TGR-1202; RP5264
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Umbralisib (TGR-1202) 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 exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib can be used for haematological malignancies reseach [1] .
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5 Cited Publications
Synonyms: TGR-1202 hydrochloride; RP5264 hydrochloride
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Umbralisib (TGR-1202) hydrochloride 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 hydrochloride exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib hydrochloride can be used for haematological malignancies reseach [1] .
4
4 Cited Publications
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IC261 is a selective, ATP-competitive CK1 inhibitor, with IC50s of 1 μM, 1 μM, 16 μM for Ckiδ, Ckiε and Ckiα1, respectively.
2
2 Cited Publications
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PF-4800567 is a potent and selective inhibitor of casein kinase 1? (CK1?), with an IC50 of 32 nM, which is greater than 20-fold selectivity over CK1δ (IC50, 711 nM).
2
2 Cited Publications
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IWP-4 is a Wnt inhibitor with an IC50 of 25 nM. IWP-4 specifically inhibits casein kinase 1δ/ε (CK1δ/ε), with an IC50 of 1.06 μM against wild-type CK1δ, 1.02 μM against the CK1δ kinase domain, and 7.07 μM against CK1ε; it shows enhanced inhibitory activity against the M82F CK1δ mutant (IC50 = 0.14 μM). IWP-4 is applicable to research related to cancer, Alzheimer's disease (AD), and heart failure [1] .
2
2 Cited Publications
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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.
2
2 Cited Publications
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SSTC3 is a casein kinase 1α (CK1α) activator (Kd = 32 nM) that inhibits WNT signaling (EC50 = 30 nM). SSTC3 exhibits minimal gastrointestinal toxicity compared to other classes of WNT inhibitors [1].
1
1 Cited Publications
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CK1-IN-1 (Compound 1c) is a casein kinase 1 (CK1) inhibitor with IC50 values of 15 nM and 16 nM for CK1δ and CK1ε, respectively. CK1-IN-1 inhibits p38α MAPK with an IC50 of 73 nM. CK1-IN-1 can be used to study cardiomyogenesis [1].
1
1 Cited Publications
Cat. No.: HY-W011109
CAS No.: 1177141-67-1
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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] .
1
1 Cited Publications
Cat. No.: HY-160444
CAS No.: 3026986-17-1
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SJ3149 is a selective and potent molecular glue degrader of CK1α protein with broad antiproliferative activity. SJ3149 can be used in cancer research [1] .
1
1 Cited Publications
Cat. No.: HY-133028
CAS No.: 120615-25-0
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CKI-7 free base 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 free base is a selective Cdc7 kinase inhibitor. CKI-7 free base also inhibits SGK, ribosomal S6 kinase-1 (S6K1) and mitogen- and stress-activated protein kinase-1 (MSK1). CKI-7 free base has a much weaker effect on casein kinase II and other protein kinases [1] .
1
1 Cited Publications
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Epiblastin A is an ATP competitive casein kinase 1 (CK1) inhibitor with IC50s of 8.9, 0.5, and 4.7 µM for CK1α, CK1δ, and CK1 ɛ, respectively. Epiblastin A induces reprogramming of epiblast stem cells into embryonic stem cells by inhibition of CK1 [1].
1
1 Cited Publications
JW67 inhibits the canonical Wnt signaling with an IC50 of 1.17μM [1]. JW67 affects the multiprotein complex consisting of β-catenin/GSK-3β/AXIN/APC/CK1 that rapidly reduces active β-catenin with a subsequent downregulation of Wnt target genes. JW67 also inhibits colorectal cancer cell growth [1].
1
1 Cited Publications
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TBCA is a highly selective CK2 (casein kinase II) inhibitor with an IC50 of 110 nM and a Ki of 77 nM. TBCA shows selectivity for CK2 over CK1, DYRK1A and a panel of 27 other kinases [1] .
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1 Cited Publications
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CK1-IN-2 (compound Nr.4) is a potent CK1 inhibitor with an IC50 values of 123, 19.8, 26.8, 74.3 nM for CK1a, CK1d, CK1e, p38a, respectively [1].
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
