SUMO1 Degrader-1
SUMO1 Degrader-1 is a blood-brain barrier-penetrant and selective SUMO1 degrader with antitumor activity. SUMO1 Degrader-1 induces ubiquitination and proteasomal degradation of SUMO1 and blocks the binding of SUMO1 to substrate proteins. SUMO1 Degrader-1 improves survival in mice with intracranial brain tumor xenografts and inhibits the progression of donor-derived xenograft tumors from human colon cancer, breast cancer, and non-small cell lung cancer. HB007 (HY-139662), a derivative of SUMO1 Degrader-1, is a molecular glue degrader. SUMO1 Degrader-1 can be used in cancer-related research, such as glioblastoma, breast cancer, etc.
For research use only. We do not sell to patients.
- CAS No.: 195066-24-1
- Formula: C14H9ClN4O3S
- Molecular Weight:348.76
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- Protocols
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
Description
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| LN-229 | IC50 |
2.3 μM
|
Inhibition of viability in human LN229 glioblastoma cells after 5 days exposure.
Inhibition of viability in human LN229 glioblastoma cells after 5 days exposure.
|
34644148 |
In Vitro
SUMO1 Degrader-1 (0.5-25 μM; 72 h) reduces conjugated and total SUMO1 protein levels in LN229 glioblastoma cells without affecting SUMO2/3 protein expression; it eliminates SUMO1-modified conjugation of SUMO1-UBC9 and SUMO1-CDK6 substrates in LN229 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:HCT116, LN229, H1299, and A549 human cancer cell lines
-
Concentration:10 μM
1 μM MG132 (HY-13259) -
Incubation Time:4 h
-
Result:Induced SUMO1 degradation in HeLa S100 fraction, which is blocked by the proteasome inhibitor MG132.
-
Cell Line:LN229 human cancer cell lines
-
Concentration:0.5, 1 ,2.5, 5, 7.5, 10, 25 μM
-
Incubation Time:72 h
-
Result:Reduced conjugated and total SUMO1 protein levels in LN229 glioblastoma cells without affecting SUMO2/3 protein expression; it eliminates SUMO1-modified conjugation of SUMO1-UBC9 and SUMO1-CDK6 substrates in LN229 cells.
In Vivo
SUMO1 Degrader-1 (100 mg/kg; intraperitoneal injection; once daily; 3 days) binds to SUMO1 and reduces SUMO1 protein and SUMOylation modifications in colon cancer PDX tissues[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:athymic BALB/c mice (female, 6- to 8-week-old, injected subcutaneously with LN229, HCT116, or A549 cells (5 × 106) in 100 μl of PBS)[1]
-
Dosage:100 mg/kg
-
Administration:intraperitoneal injection; once daily; 14 days
-
Result:Inhibited A549 non-small cell lung cancer and HCT116 colorectal cancer xenograft tumors, and prolongs the survival of mice with intracranial LN229 brain xenograft tumors.
Chemical Information
-
CAS No. 195066-24-1
-
Molecular Weight 348.76
-
Formula C14H9ClN4O3S
-
SMILES
O=C(NC1=CC=C(Cl)C([N+]([O-])=O)=C1)NC2=NC3=CC=CC=C3S2
-
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
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
SUMO1 Degrader-1 Related Classifications
HY-190188 Related Classifications
Powered by Bioz