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Cat. No.: HY-189864

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PROTAC CK1δ degrader 1

PROTAC CK1δ degrader 1 is a potent and selective CK1δ PROTAC degrader with a DC₅₀ of 1.25 μM. PROTAC CK1δ degrader 1 degrades CK1δ via the ubiquitin-proteasome system by recruiting the CRBN E3 ubiquitin ligase, thereby promoting the ubiquitination and proteasomal degradation of mutant NRAS protein and blocking downstream signaling pathways to inhibit cell proliferation. PROTAC CK1δ degrader 1 can be used for research on NRAS-mutant melanoma.
(Pink: CK1δ ligand (HY-189865); Blue: Cereblon ligand (HY-41547); Black: linker).

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

Formula: C₃₇H₃₈FN₉O₄
Molecular Weight:691.75

Storage:

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

PROTAC CK1δ degrader 1 Chemical Structure

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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
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

PROTAC CK1δ degrader 1 is a potent and selective CK1δ PROTAC degrader with a DC₅₀ of 1.25 μM. PROTAC CK1δ degrader 1 degrades CK1δ via the ubiquitin-proteasome system by recruiting the CRBN E3 ubiquitin ligase, thereby promoting the ubiquitination and proteasomal degradation of mutant NRAS protein and blocking downstream signaling pathways to inhibit cell proliferation. PROTAC CK1δ degrader 1 can be used for research on NRAS-mutant melanoma^[1]. (Pink: CK1δ ligand (HY-189865); Blue: Cereblon ligand (HY-41547); Black: linker).

IC₅₀ & Target

^[1]

CK1δ

1.25 μM (DC₅₀)

Cereblon

NRAS

NRAS^Q61R

All PROTACs Isoforms :

All Casein Kinase Isoforms :

All Ras Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
SK-MEL-103	DC₅₀	1.25 μM	Half-maximal degradation of CK1δ in human SK-MEL-103 cells assessed by Western blotting after 24 hrs incubation. Half-maximal degradation of CK1δ in human SK-MEL-103 cells assessed by Western blotting after 24 hrs incubation.	acs.jmedchem.6c01152
SK-MEL-103	IC₅₀	1.48 μM	Antiproliferative activity against human SK-MEL-103 cells assessed as viability reduction after 72 hrs incubation by CCK-8 assay. Antiproliferative activity against human SK-MEL-103 cells assessed as viability reduction after 72 hrs incubation by CCK-8 assay.	acs.jmedchem.6c01152
SK-MEL-2	IC₅₀	1.14 μM	Antiproliferative activity against human SK-MEL-2 cells assessed as viability reduction after 72 hrs incubation by CCK-8 assay. Antiproliferative activity against human SK-MEL-2 cells assessed as viability reduction after 72 hrs incubation by CCK-8 assay.	acs.jmedchem.6c01152

In Vitro

Anti-cancer

PROTAC CK1δ degrader 1 (compound 8u) (0.3-10 μM; 24 h) dose-dependently degrades CK1δ and NRAS in SK-MEL-103 and SK-MEL-2 cells without significantly affecting the protein level of the homologous kinase CK1ε^[1].
PROTAC CK1δ degrader 1 (72 h) inhibits the proliferation of SK-MEL-103 and SK-MEL-2 cells with IC₅₀ values of 1.48 μM and 1.14 μM, respectively^[1].
PROTAC CK1δ degrader 1 (5 μM) downregulates NRAS protein levels and reduces the levels of downstream effectors p-AKT and p-ERK in SK-MEL-103 cells^[1].
PROTAC CK1δ degrader 1 (5 μM; 12 h) specifically downregulates CK1δ and NRAS in SK-MEL-103 cells without affecting CK1α, CK1ε, and p38 levels^[1].
PROTAC CK1δ degrader 1 (3 μM) promotes ubiquitination of NRAS^Q61R in SK-MEL-103 cells^[1].
PROTAC CK1δ degrader 1 (5 μM; 12-48 h) time-dependently degrades CK1δ in SK-MEL-103 cells and achieves maximum degradation at 36 h^[1].
PROTAC CK1δ degrader 1 (5 μM; 72 h) enhances cellular sensitivity to Dacarbazine (HY-B0078) in SK-MEL-103 cells^[1].

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

Western Blot Analysis^[1]

Cell Line:

SK-MEL-103 and SK-MEL-2 cells
Concentration:

0.3, 1, 3, 10 μM
Incubation Time:

24 h
Result:

Degraded CK1δ and NRAS proteins in a dose-dependent manner, but did not significantly degrade the highly homologous CK1ε protein.

Western Blot Analysis^[1]

Cell Line:

SK-MEL-103 cells
Concentration:

5 μM
Incubation Time:

12, 24, 36, 48 h
Result:

Time-dependently degraded CK1δ protein, achieving maximal degradation at 36 hours, and a modest recovery of target levels (hook effect) was observed at 48 hours.

Parmacokinetics

Species	Dose	Route	T_1/2	C_max	AUC_0-t	F	CL
Rat^[1]	2 mg/kg	i.v.	2.06 h	1390 ng/mL	804 ng·h/mL	/	41 mL/min/kg
Rat^[1]	10 mg/kg	p.o.	1.60 h	26 ng/mL	51 ng·h/mL	1.42 %	/

In Vivo

Anti-cancer

PROTAC CK1δ degrader 1 (30 mg/kg; i.p.; every other day; 18 days) significantly suppresses tumor growth (TGI 58.9%), induces CK1δ degradation, and reduces NRAS protein in tumor tissue without mortality related to the tested dose or significant body weight loss in BALB/c nude mice bearing SK-MEL-103 NRAS^Q61R xenografts^[1].

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

Animal Model:

BALB/c nude (female, 5-6 weeks old) weres ubcutaneously implanted with NRAS^Q61R-mutant SK-MEL-103 cells^[1]
Dosage:

30 mg/kg
Administration:

i.p.; every other day; for 18 days
Result:

Significantly suppressed tumor growth, achieving a tumor growth inhibition (TGI) rate of 58.9% at the 30 mg/kg dose.
Induced marked degradation of the target protein CK1δ and downstream NRAS protein in tumor tissues.
Caused no treatment-related animal mortality or significant body weight loss, indicating a favorable safety profile at the tested dose.

Related Protocols :

Chemical Information

Molecular Weight 691.75
Formula C₃₇H₃₈FN₉O₄
SMILES

O=C1N(C(CC2)C(NC2=O)=O)C(C3=C1C=CC=C3N4CCC(N5CCC(CN6C(C7=NC(N)=NC=C7)=C(C8=CC=C(F)C=C8)N=C6)CC5)CC4)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Zhang C, et al. Discovery and synthesis of selective casein kinase 1δ degraders for suppressing oncogenic NRAS-mutant melanoma. J Med Chem. 2026.

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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100 mg

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