2. PROTAC Stem Cell/Wnt Cell Cycle/DNA Damage Immunology/Inflammation Apoptosis
  3. Molecular Glues Casein Kinase IKZF Family Bcl-2 Family CDK Apoptosis
  4. DEG-77

DEG-77 is a molecular glue targeting IKZF2 and CK1α, with DC50 values of 15.3 nM and 10 nM, respectively. DEG-77 exhibits significant anti-tumor activity, inducing increased transcriptional levels of the pro-apoptotic protein Bax and the cell cycle arrest protein p21. DEG-77 is applicable to the research of acute myeloid leukemia (AmL), diffuse large B-cell lymphoma and ovarian cancer.

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

DEG-77

DEG-77 Chemical Structure

CAS No. : 3032265-06-5

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Based on 1 publication(s) in Google Scholar

DEG-77 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE DEG-77

View All Casein Kinase Isoform Specific Products:

View All Isoforms
CK1 CK2

View All IKZF Family Isoform Specific Products:

View All Isoforms
IKZF1 IKZF2 IKZF3 IKZF4

View All Bcl-2 Family Isoform Specific Products:

View All Isoforms
Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3 Bad

View All CDK Isoform Specific Products:

View All Isoforms
CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

DEG-77 is a molecular glue targeting IKZF2 and CK1α, with DC50 values of 15.3 nM and 10 nM, respectively. DEG-77 exhibits significant anti-tumor activity, inducing increased transcriptional levels of the pro-apoptotic protein Bax and the cell cycle arrest protein p21. DEG-77 is applicable to the research of acute myeloid leukemia (AmL), diffuse large B-cell lymphoma and ovarian cancer.

IC50 & Target[1][2]

CK1α

10 nM (DC50)

IZKF2

15.3 nM (DC50)

Bax

 

Cellular Effect
Cell Line Type Value Description References
A2780 EC50
27 nM
Compound: 77; DEG-77
Cytotoxicity against human A2780 cells incubated for 5 days by MTT assay
Cytotoxicity against human A2780 cells incubated for 5 days by MTT assay
[PMID: 38085607]
OCI-Ly3 EC50
14 nM
Compound: 77; DEG-77
Cytotoxicity against human OCILY3 cells incubated for 5 days by MTT assay
Cytotoxicity against human OCILY3 cells incubated for 5 days by MTT assay
[PMID: 38085607]
In Vitro

DEG-77 (1-1000 nM; 0.5-24 h) induces dose- and time-dependent co-degradation of CK1α, SACK1B, hyperphosphorylated SACK1D, SACK1F and SACK1G in wild-type DLD1, U2OS, A549 and TOV-21G cells, whereas SACK1H remains unaffected. Significant protein depletion is observed following treatment with 100 nM DEG-77 for 24 h[1].
DEG-77 (100 nM; 6 h)-mediated co-degradation of CK1α, SACK1B, SACK1F and SACK1G is completely abrogated in CRBN-/- and CSNK1A1-/- DLD1 human colorectal cancer cells, indicating that this process is dependent on the expression of CRBN and CK1α[1].
The co-degradation of CK1α, SACK1B, SACK1F and SACK1G mediated by DEG-77 (100 nM; 6 h) in wild-type DLD1 human colorectal cancer cells depends on proteasomal activity but not on autophagy[1].
DEG-77 (100 nM; 24 h) potently and selectively degrades IKZF2 and CK1α in stably engineered HEK293T cells, with minimal degradative effects on IKZF1 and GSPT1[2].
DEG-77 (50 nM; 2 h) selectively induces the degradation of CK1α in MOLM-13 acute myeloid leukemia cells and activates p53[2].
DEG-77 (100 pM-10 μM; 5 d) inhibits the viability of A2780 ovarian cancer cells and OCI-LY3 diffuse large B-cell lymphoma cells within 5 days, with EC50 values of 27 nM and 14 nM, respectively[2].
DEG-77 (1 nM-10 μM; 24 h) degrades CK1α and IKZF2 in A2780 ovarian cancer cells, and degrades CK1α but exerts no degrading effect on GSPT1 in OCI-LY3 diffuse large B-cell lymphoma cells[2].
DEG-77 (1 μM; 24 h) upregulates the transcription levels of Bax and p21 in A2780 ovarian cancer cells and OCI-LY3 diffuse large B-cell lymphoma cells, which indicates that p53 is activated[2].

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

DEG-77 Related Antibodies

Western Blot Analysis[1]

Cell Line: wild-type human DLD1 colorectal cancer cells
Concentration: 1, 10, 100, 500 and 1000 nM
Incubation Time: 0.5-24 h
Result: Robustly depleted CK1α, SACK1F, and SACK1G protein levels, caused a substantial reduction in the 100 kDa hyperphosphorylated (CK1α-bound) form of SACK1D without affecting unphosphorylated SACK1D, and caused a modest reduction in SACK1B levels at 100 nM for 24 h.
Induced a dose-dependent co-depletion of CK1α, SACK1B, hyperphosphorylated SACK1D, SACK1F, and SACK1G, with robust reduction observed at 100 nM and above across 1-1000 nM for 24 h.
Induced a time-dependent reduction in CK1α, SACK1B, hyperphosphorylated SACK1D, SACK1F, and SACK1G levels at 100 nM over 0.5-24 h, with CK1α reduction observed as early as 30 min, robust depletion after 1 h, peak degradation at 3 h, and depletion sustained for 24 h.
Left SACK1H levels unchanged across all conditions.

Western Blot Analysis[1]

Cell Line: wild-type human U2OS osteosarcoma cells, wild-type human A549 lung adenocarcinoma cells, wild-type human TOV-21G ovarian cancer cells
Concentration: 1, 10, 100, 500 and 1000 nM
Incubation Time: 0.5-24 h
Result: Induced a dose-dependent co-depletion of CK1α, hyperphosphorylated SACK1D, and SACK1G in all three cell lines, with robust reduction observed at 100 nM and above across 1-1000 nM for 24 h.
Reduced SACK1B levels in a dose-dependent manner in U2OS and A549 cells across 1-1000 nM for 24 h.
Induced a time-dependent reduction in CK1α, hyperphosphorylated SACK1D, and SACK1G levels in all three cell lines at 100 nM over 0.5-24 h, with depletion kinetics mirroring that seen in DLD1 cells.
Reduced SACK1B levels in a time-dependent manner in U2OS and A549 cells at 100 nM over 0.5-24 h.
Left SACK1H levels unchanged across all cell lines and conditions.

Western Blot Analysis[1]

Cell Line: wild-type human DLD1 colorectal cancer cells, CRBN-/- human DLD1 colorectal cancer cells, CSNK1A1-/- (CK1α knockout) human DLD1 colorectal cancer cells
Concentration: 100 nM
Incubation Time: 6 h
Result: Depleted CK1α, SACK1B, SACK1F, and SACK1G levels in wild-type DLD1 cells.
Did not deplete CK1α, SACK1B, SACK1F, or SACK1G levels in CRBN-/- DLD1 cells.
Did not deplete SACK1B, SACK1F, or SACK1G levels (CK1α was not detectable) in CSNK1A1-/- DLD1 cells.

Western Blot Analysis[1]

Cell Line: wild-type human DLD1 colorectal cancer cells
Concentration: 100 nM
Incubation Time: 4 h (following 2 h pre-incubation with inhibitor)
Result: Had its mediated depletion of CK1α, SACK1B, SACK1F, and SACK1G levels completely rescued by pre-treatment with 20 μM MG132.
Had its mediated depletion of CK1α, SACK1B, SACK1F, and SACK1G levels not rescued by pre-treatment with 50 nM bafilomycin A1.

Western Blot Analysis[1]

Cell Line: human control skin fibroblasts (FIB03), palmoplantar keratoderma patient-derived skin fibroblasts (FIB04, homozygous SACK1G^R265P mutation with disrupted CK1α binding)
Concentration: 100 nM
Incubation Time: 24 h
Result: Robustly depleted CK1α and SACK1G levels, and reduced hyperphosphorylated SACK1D levels in control FIB03 fibroblasts.
Robustly depleted CK1α levels and reduced hyperphosphorylated SACK1D levels, but did not deplete SACK1G^R265P levels in patient-derived FIB04 fibroblasts.

Western Blot Analysis[1]

Cell Line: SACK1G-/- human DLD1 colorectal cancer cells stably transduced with SACK1G-GFP, SACK1G-/- human DLD1 colorectal cancer cells stably transduced with SACK1G^R265P-GFP
Concentration: 100 nM
Incubation Time: 6 h
Result: Robustly depleted CK1α and SACK1F levels in all transduced cells.
Robustly depleted SACK1G-GFP levels in cells expressing SACK1G-GFP.
Did not deplete SACK1G^R265P-GFP levels in cells expressing SACK1G^R265P-GFP.

Western Blot Analysis[2]

Cell Line: A2780 ovarian cancer cells and OCI-LY3 diffuse large B cell lymphoma cells
Concentration: 1, 10, 100 nM, 1, 10 μM
Incubation Time: 24 h
Result: Induced degradation of CK1α, with relative ratio reduced to 0.17 at all concentrations ≥ 1 nM.
Induced degradation of IKZF2, with relative ratio reduced to 0.06 at 10 μM.
Did not induce degradation of GSPT1 at any tested concentration.

Real Time qPCR[2]

Cell Line: A2780 ovarian cancer cells and OCI-LY3 diffuse large B cell lymphoma cells
Concentration: 1 μM
Incubation Time: 24 h
Result: Increased transcript levels of pro-apoptotic protein Bax.
Increased transcript levels of cell cycle arrest protein p21.
Left CK1α transcript levels unchanged.
Molecular Weight

447.44

Formula

C24H21N3O6
CAS No.
Appearance

Solid

Color

Light yellow to green yellow

SMILES

O=C1C2=CC=C(C=C2CN1C3CCC(NC3=O)=O)NC(C4=CC5=C(OC4)C(OC)=CC=C5)=O
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 : 50 mg/mL (111.75 mM; ultrasonic and warming and heat to 80°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 2.2349 mL 11.1747 mL 22.3494 mL
5 mM 0.4470 mL 2.2349 mL 4.4699 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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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: 2.5 mg/mL (5.59 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL. If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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.
Please enter your animal formula composition:
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
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 2.2349 mL 11.1747 mL 22.3494 mL 55.8734 mL
5 mM 0.4470 mL 2.2349 mL 4.4699 mL 11.1747 mL
10 mM 0.2235 mL 1.1175 mL 2.2349 mL 5.5873 mL
15 mM 0.1490 mL 0.7450 mL 1.4900 mL 3.7249 mL
20 mM 0.1117 mL 0.5587 mL 1.1175 mL 2.7937 mL
25 mM 0.0894 mL 0.4470 mL 0.8940 mL 2.2349 mL
30 mM 0.0745 mL 0.3725 mL 0.7450 mL 1.8624 mL
40 mM 0.0559 mL 0.2794 mL 0.5587 mL 1.3968 mL
50 mM 0.0447 mL 0.2235 mL 0.4470 mL 1.1175 mL
60 mM 0.0372 mL 0.1862 mL 0.3725 mL 0.9312 mL
80 mM 0.0279 mL 0.1397 mL 0.2794 mL 0.6984 mL
100 mM 0.0223 mL 0.1117 mL 0.2235 mL 0.5587 mL
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DEG-77 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:

DEG-773032265-06-5DEG77DEG 77Molecular GluesCasein KinaseIKZF FamilyBcl-2 FamilyCDKApoptosisIkaros zinc finger protein familyCyclin dependent kinaseSer/Thr kinaseacute myeloid leukaemiaDLD1 human colorectal cancer cellsovarian cancerMOLM-13 acute myeloid leukemia cellsdiffuse large B cell lymphomaSACK1(A-H) proteinsCUL4ACRBN E3 ligase complexCK1αIKZF2Inhibitorinhibitorinhibit

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