2. PROTAC Stem Cell/Wnt Cell Cycle/DNA Damage
  3. PROTACs Casein Kinase
  4. AH078

AH078 is a PROTAC-based CK1δ/ε degrader (DC50=0.55 μM, Dmax=70%) that lacks subtype selectivity between CK1δ and CK1ε. AH078 induces target protein degradation either by recruiting the CUL4-CRBN E3 ligase complex and proteasome, or via the VHL- and ubiquitin-dependent pathway. AH078 also exhibits selectivity for CK1α, and is widely applicable to research related to colon cancer, pancreatic cancer, breast cancer, ovarian cancer, chronic lymphocytic leukemia, acute myeloid leukemia, glioma, and metastatic breast adenocarcinoma.
(Pink: CK1δ and CK1ε ligand (HY-170860); Blue: VHL ligand (HY-125845B); Black: linker (HY-W001958)).

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

AH078

AH078 Chemical Structure

CAS No. : 3110370-06-1

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of AH078:

AH078 Related Antibodies

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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CK1 CK2

  • Biological Activity

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  • Customer Review

Description

AH078 is a PROTAC-based CK1δ/ε degrader (DC50=0.55 μM, Dmax=70%) that lacks subtype selectivity between CK1δ and CK1ε. AH078 induces target protein degradation either by recruiting the CUL4-CRBN E3 ligase complex and proteasome, or via the VHL- and ubiquitin-dependent pathway. AH078 also exhibits selectivity for CK1α, and is widely applicable to research related to colon cancer, pancreatic cancer, breast cancer, ovarian cancer, chronic lymphocytic leukemia, acute myeloid leukemia, glioma, and metastatic breast adenocarcinoma[1][2][3]. (Pink: CK1δ and CK1ε ligand (HY-170860); Blue: VHL ligand (HY-125845B); Black: linker (HY-W001958)).

IC50 & Target

CK1δ

0.55 μM (DC50)

CK1ε

 

VHL

 

CRBN-DDB1

 

In Vitro

AH078 potently binds to CK1δ in permeabilized cells, with an EC50 of 3.2 nM[3].
AH078 degrades CK1δ in MV4-11 HiBiT-CK1δ cells, with a DC50 of 0.55 μM and a Dmax of 70.1% after 6 h of incubation[3].
AH078 (3-10 μM; 9 h) induces a dose-dependent slowdown of cell cycle progression in MEC-1 WT cells. At the concentration of 10 μM, it reduces the accumulation of cells at the G2/M phase boundary and increases the proportion of S-phase cells[2].
AH078 (3-10 μM; 9 h) induces a dose-dependent slowdown of cell cycle progression in HG-3 WT cells, reduces cell accumulation at the G2/M phase boundary, and increases the proportion of S-phase cells at a concentration of 10 μM[2].
AH078 (3-10 μM; 6 d) significantly inhibits microenvironment-induced proliferation of primary human chronic lymphocytic leukemia (CLL) cells in a dose-dependent manner, with the strongest effect observed under the incubation condition of 10 μM for 6 days[2].
AH078 (0.01-30 μM; 6 h) potently degrades endogenous CK1δ (DC50=200 nM) and CK1ε in HEK293 cells after a 6 h incubation, while only exerting weak degradation effects on CK1α at concentrations ≥10 μM[3].
AH078 (0.03-1.19 μM; 6 h)-mediated degradation of CK1δ depends on functional Cullin ring ligases, which is confirmed by experimental results showing that the degradation is reversed upon treatment with the neddylation inhibitor MLN4924[3].

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

AH078 Related Antibodies

Cell Cycle Analysis[2]

Cell Line: HG-3 WT and MEC-1 WT cells
Concentration: 3 μM; 10 μM
Incubation Time: 9 h
Result: Significantly reduced the accumulation of cells in the G2/M phase and increased the proportion of cells in the S phase at 10 μM compared to nocodazole-only treated cells.
Resulted in a non-significant reduction in in S-phase cells (MEC-1 WT) and G2/M-phase cells (MEC-1 WT) at 3 μM relative to nocodazole-only controls.

Western Blot Analysis[3]

Cell Line: HEK293 cells (endogenous CK1δ, CK1ε, CK1α)
Concentration: 0.01-30 μM
Incubation Time: 6 h
Result: Induced robust dose-dependent degradation of endogenous CK1δ and CK1ε, with near-complete degradation at 0.3-1 μM.
Weak degradation of CK1α was only detected at 10 μM and higher.
Quantified a DC50 of 200 nM for CK1δ, with slightly weaker potency for CK1ε.
Showed a hook effect (reduced degradation) at 30 μM for both CK1δ and CK1ε.
Molecular Weight

963.15

Formula

C51H60F2N10O5S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C([C@H]1N(C([C@@H](NC(CCCCCCC(N2CCC(CN3C(C4=C5C(NC=C5)=NC=C4)=C(C6=NC=C(F)C=C6)N=C3)(F)CC2)=O)=O)C(C)(C)C)=O)C[C@H](O)C1)NCC7=CC=C(C8=C(C)N=CS8)C=C7
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 (103.83 mM; Need ultrasonic; 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 1.0383 mL 5.1913 mL 10.3826 mL
5 mM 0.2077 mL 1.0383 mL 2.0765 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.

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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V2

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

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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 1.0383 mL 5.1913 mL 10.3826 mL 25.9565 mL
5 mM 0.2077 mL 1.0383 mL 2.0765 mL 5.1913 mL
10 mM 0.1038 mL 0.5191 mL 1.0383 mL 2.5956 mL
15 mM 0.0692 mL 0.3461 mL 0.6922 mL 1.7304 mL
20 mM 0.0519 mL 0.2596 mL 0.5191 mL 1.2978 mL
25 mM 0.0415 mL 0.2077 mL 0.4153 mL 1.0383 mL
30 mM 0.0346 mL 0.1730 mL 0.3461 mL 0.8652 mL
40 mM 0.0260 mL 0.1298 mL 0.2596 mL 0.6489 mL
50 mM 0.0208 mL 0.1038 mL 0.2077 mL 0.5191 mL
60 mM 0.0173 mL 0.0865 mL 0.1730 mL 0.4326 mL
80 mM 0.0130 mL 0.0649 mL 0.1298 mL 0.3245 mL
100 mM 0.0104 mL 0.0519 mL 0.1038 mL 0.2596 mL
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AH078 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:

AH0783110370-06-1AH 078AH-078PROTACsCasein Kinaseproteasomepancreatic cancerVHLCUL4CRBN E3 ligase complexCK1εchronic lymphocytic leukemiaCK1αcolon cancerbreast cancerCK1δInhibitorinhibitorinhibit

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