2. PROTAC Metabolic Enzyme/Protease
  3. Molecular Glues E1/E2/E3 Enzyme
  4. HGC652

HGC652 is a molecular glue degrader targeting TRIM21 with a TRIM21-dependent nuclear membrane disruption effect. HGC652 binds to the PRY-SPRY domain of TRIM21 with high affinity (Ka=0.061 μM), mediates the interaction between TRIM21 and NUP98, and redirects E3 ligase activity. By triggering the polyubiquitination and proteasomal degradation of nucleoporins (such as NUP155 and GLE1), HGC652 disrupts nuclear membrane integrity, alters nuclear morphology, induces genomic instability, and thereby induces cancer cell death.

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HGC652

HGC652 Chemical Structure

CAS No. : 3055558-98-7

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

HGC652 Related Antibodies

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Description

HGC652 is a molecular glue degrader targeting TRIM21 with a TRIM21-dependent nuclear membrane disruption effect. HGC652 binds to the PRY-SPRY domain of TRIM21 with high affinity (Ka=0.061 μM), mediates the interaction between TRIM21 and NUP98, and redirects E3 ligase activity. By triggering the polyubiquitination and proteasomal degradation of nucleoporins (such as NUP155 and GLE1), HGC652 disrupts nuclear membrane integrity, alters nuclear morphology, induces genomic instability, and thereby induces cancer cell death[1][2].

In Vitro

The IC50 of HGC652 for inhibiting the proliferation of PANC-1 pancreatic cancer cells is 0.094 μM (72 h)[1].
HGC652 (0.5-5 μM; 24 h) induces dose-dependent degradation of GLE1 and NUP155 in PANC-1 cells via a proteasome-dependent pathway[1].
HGC652 (0.05-5 μM; 24 h incubation) induces NUP155 degradation in PANC-1 cells, and this process is independent of GLE1; whereas the degradation of GLE1 depends on NUP155, indicating that NUP155 is its primary target[1].
HGC652 (0.01-25 μM; room temperature; 40 min) induces the formation of a concentration-dependent ternary complex between TRIM21PRY-SPRY and NUP98APD proteins[1].
HGC652 (0.5-15 μM; incubated on ice; 30 min; incubated with streptavidin agarose beads for 2 h) induces direct interaction between TRIM21 (124-475) and NUP98APD in cell-free Strep-tag pull-down assays[2].

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

HGC652 Related Antibodies

Western Blot Analysis[1]

Cell Line: PANC-1 pancreatic cancer cells
Concentration: 0.5 μM; 5 μM
Incubation Time: 24 h
Result: Induced dose-dependent degradation of GLE1 and NUP155 proteins in PANC-1 cells.
Prevented degradation of GLE1 and NUP155 when cells were pre-treated with 5 μM proteasome inhibitor MG132, but not by autophagy-lysosome inhibitors 100 μM chloroquine or 0.1 μM bafilomycin A1.

Western Blot Analysis[1]

Cell Line: PANC-1 pancreatic cancer cells (TRIM21 siRNA-transfected)
Concentration: 0.020, 0.078, 0.313, 1.25, 5 μM
Incubation Time: 48 h (siRNA transfection); 24 h (compound incubation)
Result: Completely abrogated degradation of GLE1 and NUP155 in TRIM21-knockdown PANC-1 cells, compared to control siRNA-transfected cells.

Western Blot Analysis[1]

Cell Line: PANC-1 pancreatic cancer cells (GLE1 or NUP155 siRNA-transfected)
Concentration: 0.05, 0.5, 5 μM
Incubation Time: 24 h (compound incubation, following siRNA transfection)
Result: Allowed NUP155 degradation to persist in GLE1-knockdown PANC-1 cells. Completely abolished GLE1 degradation in NUP155-knockdown PANC-1 cells.
Molecular Weight

449.60

Formula

C23H28FNO3S2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CN(C(C1=CC=C(C2=C(SC)C=C(F)C=C2)C=C1S(=O)(C)=O)=O)CC3CCCCC3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 62.5 mg/mL (139.01 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 2.2242 mL 11.1210 mL 22.2420 mL
5 mM 0.4448 mL 2.2242 mL 4.4484 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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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 2.2242 mL 11.1210 mL 22.2420 mL 55.6050 mL
5 mM 0.4448 mL 2.2242 mL 4.4484 mL 11.1210 mL
10 mM 0.2224 mL 1.1121 mL 2.2242 mL 5.5605 mL
15 mM 0.1483 mL 0.7414 mL 1.4828 mL 3.7070 mL
20 mM 0.1112 mL 0.5560 mL 1.1121 mL 2.7802 mL
25 mM 0.0890 mL 0.4448 mL 0.8897 mL 2.2242 mL
30 mM 0.0741 mL 0.3707 mL 0.7414 mL 1.8535 mL
40 mM 0.0556 mL 0.2780 mL 0.5560 mL 1.3901 mL
50 mM 0.0445 mL 0.2224 mL 0.4448 mL 1.1121 mL
60 mM 0.0371 mL 0.1853 mL 0.3707 mL 0.9267 mL
80 mM 0.0278 mL 0.1390 mL 0.2780 mL 0.6951 mL
100 mM 0.0222 mL 0.1112 mL 0.2224 mL 0.5560 mL
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HGC652 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:

HGC6523055558-98-7HGC 652HGC-652Molecular GluesE1/E2/E3 EnzymeE1 activating enzymeE2 conjugating enzymeE3 ligating enzymeUbiquitin activating enzymeUbiquitin conjugating enzymeUbiquitin ligaseGLE1NUP98PRY-SPRY domainnuclear pore proteinsPANC-1HEK-293E3 ligaseubiquitin-proteasome systemTRIM21NUP155Inhibitorinhibitorinhibit

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