2. Apoptosis Immunology/Inflammation
  3. Apoptosis IRAK
  4. JNJ-1013

JNJ-1013 is a potent and selective IRAK1 degrader with an IC50s of 72, 443, 1071 nM for IRAK1, IRAK4, VHL FP respectively. JNJ-1013 induces Apoptosis and increases the expression of cleavaged PARP. JNJ-1013 decreases the expression IRAK1, p-IKBα, pSTAT3(Tyr705).

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JNJ-1013 Chemical Structure

JNJ-1013 Chemical Structure

CAS No. : 2597343-08-1

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Description

JNJ-1013 is a potent and selective IRAK1 degrader with an IC50s of 72, 443, 1071 nM for IRAK1, IRAK4, VHL FP respectively. JNJ-1013 induces Apoptosis and increases the expression of cleavaged PARP. JNJ-1013 decreases the expression IRAK1, p-IKBα, pSTAT3(Tyr705)[1].

IC50 & Target[1]

IRAK1

72 nM (IC50)

IRAK4

443 nM (IC50)

VHL FP

1071 nM (IC50)

In Vitro

JNJ-1013 (Degrader-3; 1.5-10000 nM; 24 h) dose-dependently degrades IRAK1 protein with an DC50 value of 3 nM.[1].
JNJ-1013 (1 µM) decreased the expression of MG-132 (HY-13259) stiyumed IRAK1 in a dose-dependent manner[1].
JNJ-1013 (0.01, 0.03, 0.1, 0.3, 1 µM; 24 h) decreases the expression IRAK1, p-IKBα, pSTAT3(Tyr705) and increases the expression of cleavaged PARP[1].

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

JNJ-1013 Related Antibodies

Western Blot Analysis[1]

Cell Line: HEK293T cells
Concentration: 1.5-10000 nM
Incubation Time: 24 h
Result: Decreased the expression of IRAK1 in a dose-dependent manner.
Molecular Weight

878.05

Formula

C46H55N9O7S
CAS No.
Appearance

Solid

Color

Light yellow to yellow

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

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (28.47 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.1389 mL 5.6944 mL 11.3889 mL
5 mM 0.2278 mL 1.1389 mL 2.2778 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.80%

COA (253 KB) HNMR (390 KB) RP-HPLC (101 KB) LCMS (98 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.1389 mL 5.6944 mL 11.3889 mL 28.4722 mL
5 mM 0.2278 mL 1.1389 mL 2.2778 mL 5.6944 mL
10 mM 0.1139 mL 0.5694 mL 1.1389 mL 2.8472 mL
15 mM 0.0759 mL 0.3796 mL 0.7593 mL 1.8981 mL
20 mM 0.0569 mL 0.2847 mL 0.5694 mL 1.4236 mL
25 mM 0.0456 mL 0.2278 mL 0.4556 mL 1.1389 mL
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JNJ-1013 Related Classifications

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:

JNJ-10132597343-08-1JNJ1013JNJ 1013ApoptosisIRAKInterleukin-1 receptor associated kinaseIL-1R associated kinaseHEK293T cellsapoptosisp-IKBαpSTAT3(Tyr705)Inhibitorinhibitorinhibit

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