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Cat. No.: HY-153188A

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(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 ligand (HY-138834); Blue: VHL ligand (HY-184855); Black: linker).

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

CAS No.: 2755075-91-1
Formula: C₄₆H₅₅N₉O₇S
Molecular Weight:878.05

Storage:

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

(S)-JNJ-1013 Chemical Structure

CAS No.: 2755075-91-1

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Use of MCE Products

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Protocols (1)
Purity & Documentation
References
Calculators
Help & FAQs
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Biological Activity

Description

(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^[1]. (Pink: IRAK1 ligand (HY-138834); Blue: VHL ligand (HY-184855); Black: linker).

IC₅₀ & Target

^[1]

IRAK1

79 nM (IC₅₀)

All IRAK Isoforms :

All PROTACs Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
HEK-293T	DC₅₀	3.3 nM	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.	34279092
HBL1	DC₅₀	3.0 nM	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.	34279092
OCI-Ly10	DC₅₀	20 nM	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.	34279092
HBL1	IC50	60 nM	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.	34279092
OCI-Ly10	IC50	170 nM	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.	34279092

In Vitro

(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. Further protocols information, click here.

Chemical Information

CAS No. 2755075-91-1
Molecular Weight 878.05
Formula C₄₆H₅₅N₉O₇S
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Protocols

All Cell Biology

Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Fu L, et al. Discovery of Highly Potent and Selective IRAK1 Degraders to Probe Scaffolding Functions of IRAK1 in ABC DLBCL. Journal of medicinal chemistry. 2021 Aug 12;64(15):10878-10889. [Content Brief]

Calculators

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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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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Protocols
Purity & Documentation
References

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(S)-JNJ-1013

All IRAK Isoforms

All PROTACs Isoforms