1. Cell Cycle/DNA Damage Stem Cell/Wnt
  2. Casein Kinase
  3. BAY-888

BAY-888 is a selective CK1α/CSNK1A1 (casein kinase) ATP-competitive inhibitor (IC50: 4 nM@10 μM ATP; 63 nM@1 mM ATP). BAY-888 blocks the negative regulation of p53 and other signaling pathways by CK1α, induces apoptosis and inhibits proliferation of tumor cells. BAY-888 has shown inhibitory efficacy against cancers such as acute myeloid leukemia (AML) in PRISM barcoded cell line screening and can mimic the effects of shRNA-mediated CK1α knockdown. BAY-888 is primarily used for the development of anticancer drugs for p53 wild-type tumors and for the study of the mechanisms of CK1α-related signaling pathways.

For research use only. We do not sell to patients.

BAY-888 Chemical Structure

BAY-888 Chemical Structure

CAS No. : 2468783-75-5

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Description

BAY-888 is a selective CK1α/CSNK1A1 (casein kinase) ATP-competitive inhibitor (IC50: 4 nM@10 μM ATP; 63 nM@1 mM ATP). BAY-888 blocks the negative regulation of p53 and other signaling pathways by CK1α, induces apoptosis and inhibits proliferation of tumor cells. BAY-888 has shown inhibitory efficacy against cancers such as acute myeloid leukemia (AML) in PRISM barcoded cell line screening and can mimic the effects of shRNA-mediated CK1α knockdown. BAY-888 is primarily used for the development of anticancer drugs for p53 wild-type tumors and for the study of the mechanisms of CK1α-related signaling pathways[1][2][3].

In Vitro

BAY-888 (example 5) inhibits WT EGFR with an IC50 of 11.5-15.5 μM (@2 mM ATP)[1].
BAY-888 inhibits CSNK1A1 and CSNK1D with IC50 of 3.62-6.34 μM and 1.21 μM, respectively[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

BAY-888 shows in vivo inhibitory efficacy in multiple mouse cell line xenograft models, including diffuse large B-cell lymphoma (TMD8) and multiple FAM83-overexpressing solid tumor models (colorectal cancer (HCT116 and HT29), gastric cancer (IM95), and urothelial carcinoma (KU19-19)). BAY-888 may act in vivo anti-cancer effect via RPS6 phosphorylation mechanism[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

483.54

Formula

C28H26FN5O2

CAS No.
Appearance

Solid

Color

Off-white to light brown

SMILES

O=C1C2=C(NC(C3=CC=NC(NC([C@@H](C)C4=CC=C(F)C=C4)=O)=C3)=C2NC5=CC=CC=C5)CCN1C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (103.40 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0681 mL 10.3404 mL 20.6808 mL
5 mM 0.4136 mL 2.0681 mL 4.1362 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0681 mL 10.3404 mL 20.6808 mL 51.7020 mL
5 mM 0.4136 mL 2.0681 mL 4.1362 mL 10.3404 mL
10 mM 0.2068 mL 1.0340 mL 2.0681 mL 5.1702 mL
15 mM 0.1379 mL 0.6894 mL 1.3787 mL 3.4468 mL
20 mM 0.1034 mL 0.5170 mL 1.0340 mL 2.5851 mL
25 mM 0.0827 mL 0.4136 mL 0.8272 mL 2.0681 mL
30 mM 0.0689 mL 0.3447 mL 0.6894 mL 1.7234 mL
40 mM 0.0517 mL 0.2585 mL 0.5170 mL 1.2926 mL
50 mM 0.0414 mL 0.2068 mL 0.4136 mL 1.0340 mL
60 mM 0.0345 mL 0.1723 mL 0.3447 mL 0.8617 mL
80 mM 0.0259 mL 0.1293 mL 0.2585 mL 0.6463 mL
100 mM 0.0207 mL 0.1034 mL 0.2068 mL 0.5170 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
BAY-888
Cat. No.:
HY-145939
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