SR-4133

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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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SR-4133 Chemical Structure

CAS No. : 2999645-23-5

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CK1 CK2

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

CK1ε

58 nM (IC₅₀)

CK1γ2

10 μM (IC₅₀)

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.

Molecular Weight

512.51

Formula

C₂₇H₂₂F₂N₈O

CAS No.

2999645-23-5

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

References

[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]

SR-4133 Related Classifications

Molarity Calculator
Dilution Calculator

The molarity calculator equation

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

Mass		Concentration		Volume		Molecular Weight *
	=		×		×

The dilution calculator equation

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)	×	Volume _(start)	=	Concentration _(final)	×	Volume _(final)
	×		=		×
C1		V1		C2		V2

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.

Keywords:

SR-41332999645-23-5SR4133SR 4133Casein KinaseT245637UM-UC-3U2-OSbladder cancerInhibitorinhibitorinhibit

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