(S)-JNJ-1013
(S)-JNJ-1013 is an isomer of IRAK1 PROTAC degrader JNJ-1013 (HY-153188). (S)-JNJ-1013 loses VHL binding affinity (IC50 >10 μM) and shows no significant IRAK1 degradation activity (DC50 > 10 μM). (S)-JNJ-1013 selectively inhibits IRAK1 with an IC50 of 79 nM. (S)-JNJ-1013 can be used to study cancers dependent on the scaffolding function of IRAK1.
(Pink: IRAK1 Target protein ligand; Blue: VHL ligand (HY-184855); Black: linker).
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- CAS. Nr.: 2755075-91-1
- Formel: C46H55N9O7S
- Molecular Weight:878.05
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
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IRAK1 79 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK-293T | DC50 |
3.3 nM
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IRAK1 protein degradation potency in HEK293T cells measured by immunoblotting after 24 h of treatment.
IRAK1 protein degradation potency in HEK293T cells measured by immunoblotting after 24 h of treatment.
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34279092 |
| HBL1 | DC50 |
3.0 nM
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IRAK1 protein degradation potency in HBL-1 ABC DLBCL cells measured by immunoblotting after 24 h of treatment.
IRAK1 protein degradation potency in HBL-1 ABC DLBCL cells measured by immunoblotting after 24 h of treatment.
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34279092 |
| OCI-Ly10 | DC50 |
20 nM
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IRAK1 protein degradation potency in OCI-LY10 ABC DLBCL cells measured by immunoblotting after 24 h of treatment.
IRAK1 protein degradation potency in OCI-LY10 ABC DLBCL cells measured by immunoblotting after 24 h of treatment.
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34279092 |
| HBL1 | IC50 |
60 nM
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Antiproliferative activity against HBL-1 ABC DLBCL cells assessed as reduction in cell viability incubated for 12 days by CTG assay.
Antiproliferative activity against HBL-1 ABC DLBCL cells assessed as reduction in cell viability incubated for 12 days by CTG assay.
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34279092 |
| OCI-Ly10 | IC50 |
170 nM
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Antiproliferative activity against OCI-LY10 ABC DLBCL cells assessed as reduction in cell viability incubated for 12 days by CTG assay.
Antiproliferative activity against OCI-LY10 ABC DLBCL cells assessed as reduction in cell viability incubated for 12 days by CTG assay.
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34279092 |
(S)-JNJ-1013 (Compound degrader-4) (1 μM) exhibits high kinome selectivity for IRAK1 in a cell-free KinomeScan competitive binding assay[1].
(S)-JNJ-1013 potently inhibits IRAK1 kinase activity in cell-free biochemical assays, with an IC50 of 79 nM[1].
(S)-JNJ-1013 (for 12 days) inhibits the proliferation of HBL-1 ABC DLBCL cells with an IC50 of >1.5 μM; it also inhibits the proliferation of OCI-LY10 ABC DLBCL cells, with an IC50 of >3 μM after 12 days of treatment[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 2755075-91-1
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Molecular Weight 878.05
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Formel C46H55N9O7S
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SMILES
COC(C=C1N(CC2)CCC2OCC(N[C@@H](C(C)(C)C)C(N3[C@@H](C[C@@H](C3)O)C(N[C@H](C4=CC=C(C5=C(C)N=CS5)C=C4)C)=O)=O)=O)=C(C=C1)NC(C6=CC=CC(C7=NNC=C7)=N6)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
(S)-JNJ-1013 Related Classifications
HY-153188A Related Classifications
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