SR-4133
Based on 1 Customer Validation
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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- Pureté : 99.85%
- CAS No.: 2999645-23-5
- Formule: C27H22F2N8O
- Masse moléculaire:512.51
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Stockage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Activité biologique
Description
IC50 & Target
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CK1ε 58 nM (IC50) |
CK1γ2 10 μM (IC50) |
Cellular Effect
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Cell Line
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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.
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Cell Line:T24, 5637, UM-UC-3, U2-OS
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Concentration:265 nM, 314 nM, 540 nM, 373 nM
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Incubation Time:72 h
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Result:Inhibited cell growth with EC50s of 265 nM (T24), 314 nM (5637), 540 nM (UM-UC-3 EC), 373 nM (U2-OS EC).
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Cell Line:T24
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Concentration:1 μM
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Incubation Time:24 h
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Result:Blocked the phosphorylation of T37/46, S65, and T70 of 4E-BP1.
Chemical Information
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CAS No. 2999645-23-5
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Appearance Solid
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Masse moléculaire 512.51
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Formule C27H22F2N8O
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Color Off-white to light yellow
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SMILES
FC1=C(F)C2=C(NC(CNC3=NC(N4CCOCC4)=NC5=C3N=CN5C6=CC(C=CC=C7)=C7C=C6)=N2)C=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Pureté et documentation
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Fiche technique (274 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)