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Art. -Nr.: HY-175271

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JWJ-01-378

JWJ-01-378 is a TPM3-TRKA fusion protein inhibitor and a wild-type TRK PROTAC degrader. JWJ-01-378 induces degradation via the ubiquitin-proteasome system, and does not degrade TRK inhibitor-resistant mutants or ALK fusion proteins. JWJ-01-378 inhibits downstream signaling pathways activated by TPM3-TRKA fusion, and reduces the viability of cancer cells harboring TPM3-TRKA fusion. JWJ-01-378 can be used to evaluate targeted degradation of TRK fusion proteins in cancer.
(Pink: Trk Receptor ligand (HY-160520); Blue: Cereblon ligand (HY-103596); Black: linker).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Formel: C₅₅H₆₂F₂N₁₀O₉
Molecular Weight:1045.14

Speicherung:

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

Data Sheet (276 KB)

JWJ-01-378 Chemical Structure

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Preis

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Menge

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Use of MCE Products

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

Biologische Aktivität
- Beschreibung
- In Vitro
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

JWJ-01-378 is a TPM3-TRKA fusion protein inhibitor and a wild-type TRK PROTAC degrader. JWJ-01-378 induces degradation via the ubiquitin-proteasome system, and does not degrade TRK inhibitor-resistant mutants or ALK fusion proteins. JWJ-01-378 inhibits downstream signaling pathways activated by TPM3-TRKA fusion, and reduces the viability of cancer cells harboring TPM3-TRKA fusion. JWJ-01-378 can be used to evaluate targeted degradation of TRK fusion proteins in cancer^[1]. (Pink: Trk Receptor ligand (HY-160520); Blue: Cereblon ligand (HY-103596); Black: linker).

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Alle Trk Receptor Isoform-spezifische Produkte anzeigen :

In Vitro

JWJ-01-378 (10-1000 nM; 2 h) efficiently and selectively degrades endogenous TPM3-TRKA in KM12 cells via the ubiquitin-proteasome system, thereby inhibiting the downstream pERK signaling pathway^[1].
JWJ-01-378 (10-1000 nM; 6 h) degrades wild-type TRKA in HEL and NIH/3T3 cells, but fails to degrade TRK inhibitor-resistant TPM3-TRKA^G595R, EML4-ALK or EML4-ALK^G1202R in NIH/3T3 cells^[1].
JWJ-01-378 (0.1 nM-1 μM; 120 h) reduces the viability of TPM3-TRKA fusion-positive KM12 cells in both 2D and 3D culture systems, but does not reduce the viability of HEL cells expressing wild-type TRKA^[1].
JWJ-01-378 (100 nM; 2 h) is a rapid-acting and selective TPM3-TRKA degrader in KM12 cells, with minimal altering effects on off-target proteins^[1].

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

Western Blot Analysis^[1]

Cell Line:

KM12 colorectal cancer cells (endogenous TPM3-TRKA fusion)
Concentration:

10, 100, 1000 nM
Incubation Time:

2 h
Result:

Induced rapid and pronounced degradation of TPM3-TRKA at doses as low as 10 nM.
Suppressed phosphorylated ERK (pERK) levels.

Western Blot Analysis^[1]

Cell Line:

HEL and NIH/3T3 cells
Concentration:

10, 100, 1000 nM
Incubation Time:

6 h
Result:

Degraded wild-type TRKA in HEL and NIH/3T3 cells, but failed to degrade TRK inhibitor-resistant TPM3-TRKAG595R, EML4-ALK or EML4-ALKG1202R in NIH/3T3 cells.

Chemical Information

Molecular Weight 1045.14
Formel C₅₅H₆₂F₂N₁₀O₉
SMILES

O=C(NCCCCCCCCNC(CN1CCN(CC1)C2=CC(NC3CCOCC3)=C(C=C2)C(NC4=NNC5=C4C=C(C=C5)CC6=CC(F)=CC(F)=C6)=O)=O)COC7=C8C(N(C(C8=CC=C7)=O)C9CCC(NC9=O)=O)=O
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Kumar S, et al. Development of PROTACs for targeted degradation of oncogenic TRK fusions. RSC Chem Biol. 2026 Mar 18;7(4):596-614.

Calculators

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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Biologische Aktivität
- Beschreibung
- In Vitro
Chemical Information
Reinheit & Dokumentation
Verweise

Produktname:
Art. -Nr.:
Menge:
MCE Japan Authorized Agent:

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JWJ-01-378

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle Trk Receptor Isoform-spezifische Produkte anzeigen