2. PROTAC Protein Tyrosine Kinase/RTK JAK/STAT Signaling Epigenetics Stem Cell/Wnt Apoptosis Immunology/Inflammation
  3. PROTACs JAK TNF Receptor Interleukin Related STAT
  4. PROTAC JAK1/2 degrader-1

PROTAC JAK1/2 degrader-1 (Compound A8) is a selective JAK1/2 PROTAC degrader, with DC50 values of 1.4 μM for JAK1 and 0.92 μM for JAK2. PROTAC JAK1/2 degrader-1 significantly inhibits the release of NO, IL-6 (IC50 = 12.89 μM) and TNF-α (IC50 = 17.17 μM). PROTAC JAK1/2 degrader-1 significantly alleviates inflammatory responses and colonic damage by inhibiting the JAK/STAT3 signaling pathway. PROTAC JAK1/2 degrader-1 can be used for research on colitis. (Pink: JAK1/2 ligand (HY-179716); Blue: CRBN ligand (HY-10984); Black: linker; CRBN ligand + linker (HY-131888A)).

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

PROTAC JAK1/2 degrader-1

PROTAC JAK1/2 degrader-1 Chemical Structure

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PROTAC JAK1/2 degrader-1 Related Antibodies

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STAT3 STAT5 STAT6 STAT1

  • Biological Activity

  • Purity & Documentation

  • References

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Description

PROTAC JAK1/2 degrader-1 (Compound A8) is a selective JAK1/2 PROTAC degrader, with DC50 values of 1.4 μM for JAK1 and 0.92 μM for JAK2. PROTAC JAK1/2 degrader-1 significantly inhibits the release of NO, IL-6 (IC50 = 12.89 μM) and TNF-α (IC50 = 17.17 μM). PROTAC JAK1/2 degrader-1 significantly alleviates inflammatory responses and colonic damage by inhibiting the JAK/STAT3 signaling pathway. PROTAC JAK1/2 degrader-1 can be used for research on colitis. (Pink: JAK1/2 ligand (HY-179716); Blue: CRBN ligand (HY-10984); Black: linker; CRBN ligand + linker (HY-131888A))[1].

IC50 & Target[1]

JAK1

1.4 μM (DC50)

JAK2

0.92 μM (DC50)

IL-6

 

STAT3

 

IL-10

 

Cereblon

 

Molecular Weight

603.63

Formula

C33H29N7O5
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(NCCCNC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O)C4=CC=C(C5=NC(NC6=CC=CC=C6)=NC=C5)C=C4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (165.66 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 1.6566 mL 8.2832 mL 16.5664 mL
5 mM 0.3313 mL 1.6566 mL 3.3133 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
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. 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 1.6566 mL 8.2832 mL 16.5664 mL 41.4161 mL
5 mM 0.3313 mL 1.6566 mL 3.3133 mL 8.2832 mL
10 mM 0.1657 mL 0.8283 mL 1.6566 mL 4.1416 mL
15 mM 0.1104 mL 0.5522 mL 1.1044 mL 2.7611 mL
20 mM 0.0828 mL 0.4142 mL 0.8283 mL 2.0708 mL
25 mM 0.0663 mL 0.3313 mL 0.6627 mL 1.6566 mL
30 mM 0.0552 mL 0.2761 mL 0.5522 mL 1.3805 mL
40 mM 0.0414 mL 0.2071 mL 0.4142 mL 1.0354 mL
50 mM 0.0331 mL 0.1657 mL 0.3313 mL 0.8283 mL
60 mM 0.0276 mL 0.1381 mL 0.2761 mL 0.6903 mL
80 mM 0.0207 mL 0.1035 mL 0.2071 mL 0.5177 mL
100 mM 0.0166 mL 0.0828 mL 0.1657 mL 0.4142 mL
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PROTAC JAK1/2 degrader-1 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:

PROTAC JAK1/2 degrader-1PROTACsJAKTNF ReceptorInterleukin RelatedSTATJanus kinaseTumor Necrosis Factor ReceptorTNFRILPROTACDegraderInflammatory bowel diseasesInhibitorinhibitorinhibit

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