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Cat. No.: HY-149292

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SR-4133

SR-4133 is a potent and highly CK1ε selective inhibitor with an IC₅₀ of 58 nM. SR-4133 binds to the ATP-binding site of CK1ε. SR-4133 displays nanomolar growth inhibition of bladder cancer cells, and inhibits the phosphorylation of 4E-BP1.

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CAS No.: 2999645-23-5
Formule: C₂₇H₂₂F₂N₈O
Masse moléculaire:512.51

Stockage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (272 KB)

SR-4133 Chemical Structure

CAS No.: 2999645-23-5

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

CK1ε

58 nM (IC₅₀)

CK1γ2

10 μM (IC₅₀)

Voir tous les produits spécifiques à Isoform Casein Kinase :

Cellular Effect

Cell Line	Type	Value	Description	References
5637	EC₅₀	314 nM Compound: SR-4133	Antiproliferative activity against human 5637 cells assessed as reduction in cell proliferation incubated for 72 hrs by Cell Titer Glo assay Antiproliferative activity against human 5637 cells assessed as reduction in cell proliferation incubated for 72 hrs by Cell Titer Glo assay	[PMID: 37204207]
T-24	EC₅₀	265 nM Compound: SR-4133	Antiproliferative activity against human T24 cells assessed as reduction in cell proliferation incubated for 72 hrs by Cell Titer Glo assay Antiproliferative activity against human T24 cells assessed as reduction in cell proliferation incubated for 72 hrs by Cell Titer Glo assay	[PMID: 37204207]
U2OS	EC₅₀	373 nM Compound: SR-4133	Antiproliferative activity against human U2OS cells assessed as reduction in cell proliferation incubated for 72 hrs by Cell Titer Glo assay Antiproliferative activity against human U2OS cells assessed as reduction in cell proliferation incubated for 72 hrs by Cell Titer Glo assay	[PMID: 37204207]
UMUC3	EC₅₀	540 nM Compound: SR-4133	Antiproliferative activity against human UMUC3 cells assessed as reduction in cell proliferation incubated for 72 hrs by Cell Titer Glo assay Antiproliferative activity against human UMUC3 cells assessed as reduction in cell proliferation incubated for 72 hrs by Cell Titer Glo assay	[PMID: 37204207]

In Vitro

SR-4133 (200-600 nM, 72 h) inhibits cancer cells growth significantly with EC₅₀s of 265 nM (T24), 314 nM (5637), 540 nM (UM-UC-3 EC), 373 nM (U2-OS EC)^[1].
SR-4133 (1 μM, 24 h) inhibits the phosphorylation of 4E-BP1 in T24 cells^[1].

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

Cell Viability Assay^[1]

Cell Line:

T24, 5637, UM-UC-3, U2-OS
Concentration:

265 nM, 314 nM, 540 nM, 373 nM
Incubation Time:

72 h
Result:

Inhibited cell growth with EC₅₀s of 265 nM (T24), 314 nM (5637), 540 nM (UM-UC-3 EC), 373 nM (U2-OS EC).

Western Blot Analysis^[1]

Cell Line:

T24
Concentration:

1 μM
Incubation Time:

24 h
Result:

Blocked the phosphorylation of T37/46, S65, and T70 of 4E-BP1.

Chemical Information

CAS No. 2999645-23-5
Masse moléculaire 512.51
Formule C₂₇H₂₂F₂N₈O
SMILES

FC1=C(F)C2=C(NC(CNC3=NC(N4CCOCC4)=NC5=C3N=CN5C6=CC(C=CC=C7)=C7C=C6)=N2)C=C1
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (272 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Choi JY, et al. Structure-Based Development of Isoform-Selective Inhibitors of Casein Kinase 1ε vs Casein Kinase 1δ. J Med Chem. 2023 Jun 8;66(11):7162-7178. [Content Brief]

Calculators

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Keywords

MOQ

Minimum order quantity

100 mg

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Pureté et documentation
Références

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SR-4133

Voir tous les produits spécifiques à Isoform Casein Kinase