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Cat. No.: HY-184913

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JHK-02-102-1

JHK-02-102-1 is a selective CDK5 degrader derived from the regorafenib kinase inhibitor scaffold. JHK-02-102-1 recruits CRL4_CRBN E3 ubiquitin ligase to induce ternary complex formation between CDK5 and CRBN, triggering ubiquitin-proteasome system-dependent degradation. JHK-02-102-1 achieves selectivity redirection from CDK6 to CDK5 via subtle PROTAC architecture modifications.
(Pink: CDK and CDK5 ligand (HY-184911); Blue: Cereblon ligand (HY-163169); Black: linker (HY-W017772)).

Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.

Formule: C₄₅H₅₀F₄N₈O₉
Masse moléculaire:922.92

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

JHK-02-102-1 Chemical Structure

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Fluorescent Dye

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

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- In Vitro
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Description

JHK-02-102-1 is a selective CDK5 degrader derived from the regorafenib kinase inhibitor scaffold. JHK-02-102-1 recruits CRL4_CRBN E3 ubiquitin ligase to induce ternary complex formation between CDK5 and CRBN, triggering ubiquitin-proteasome system-dependent degradation. JHK-02-102-1 achieves selectivity redirection from CDK6 to CDK5 via subtle PROTAC architecture modifications^[1]. (Pink: CDK and CDK5 ligand (HY-184911); Blue: Cereblon ligand (HY-163169); Black: linker (HY-W017772)).

IC₅₀ & Target^[1]

CDK5

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In Vitro

JHK-02-102-1 (1 μM; 5 h) selectively degrades CDK5 in MOLT-4 cells, with minimal off-target degradation^[1].
JHK-02-102-1 (0-50 μM; 6 h) potently and selectively degrades CDK5 (but not CDK2) in a dose-dependent manner in MOLT-4 cells, with activity dependent on CRBN binding^[1].
JHK-02-102-1 (0.001-100 μM) induces dose-dependent degradation of CDK5 in K562-Cas9 reporter cells, and this degradation is mediated by the ubiquitin-proteasome system via CRL4_CRBN activity^[1].
JHK-02-102-1 (0.001-100 μM) induces concentration-dependent ternary complex formation between recombinant CDK5 and CRBN proteins, as measured by NanoBRET assay^[1].

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

Western Blot Analysis^[1]

Cell Line:

MOLT-4 human leukemia cells
Concentration:

0, 0.01, 0.1, 1, 10 and 50 μM
Incubation Time:

6 h
Result:

Induced dose-dependent degradation of CDK5, with near-complete degradation observed at concentrations ≥0.1 μM.
Did not reduce CDK2 levels; instead caused a slight increase at higher concentrations.
Did not induce degradation of CDK5 when using the negative control JHK-02-138.

Chemical Information

Masse moléculaire 922.92
Formule C₄₅H₅₀F₄N₈O₉
SMILES

O=C(N1)CCC(C2=CC=C(OCC(NCCOCCOCCN3CCN(CC4=CC=C(NC(NC5=CC=C(OC6=CC=NC(C(NC)=O)=C6)C=C5F)=O)C=C4C(F)(F)F)CC3)=O)C=C2)C1=O
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

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

Pureté et documentation

Instruction de manipulation (2659 KB)

Références

[1]. Kim JH, et al. A Type II CDK6 Degrader Enables Cellular Targeting beyond the Limits of Type II Inhibition. Journal of the American Chemical Society. 2026 Jul 08;148(26):27951-27964. [Content Brief]

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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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- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Pureté et documentation
Références

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JHK-02-102-1

Voir tous les produits spécifiques à Isoform CDK

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Chemical Information

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JHK-02-102-1 Related Classifications

HY-184913 Related Classifications