PROTAC PAPD5 degrader 1
PROTAC PAPD5 degrader 1 is a selective PAPD5 PROTAC degrader. PROTAC PAPD5 degrader 1 induces ubiquitination and degradation of PAPD5 without causing degradation of PAPD7. PROTAC PAPD5 degrader 1 reduces Hepatitis B virus mRNA and Hepatitis B surface antigen levels in vitro. PROTAC PAPD5 degrader 1 inhibits both Hepatitis A virus and Hepatitis B virus. PROTAC PAPD5 degrader 1 can be used for research on Hepatitis A virus infection and Hepatitis B virus infection.
(Pink: PAPD5 ligand (HY-175913); Blue: Cereblon ligand (HY-41547); Black: linker (HY-130486)).
For research use only. We do not sell to patients.
- Formula: C49H63N5O16
- Molecular Weight:978.05
-
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
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
|
Cereblon |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 2.2.15 | IC50 |
16.24 μM
Compound: 12b
|
Inhibition HBsAg secretion in human HepG2.2.15 cells treated for 3 days followed by medium replacement without compound measured after 2 days by CLIA
Inhibition HBsAg secretion in human HepG2.2.15 cells treated for 3 days followed by medium replacement without compound measured after 2 days by CLIA
|
[PMID: 38428537] |
| Huh-7 | CC50 |
>50 μM
Compound: 12b
|
Cytotoxicity against human Huh-7 cells assessed as cell viability by Cell Titer Glo assay
Cytotoxicity against human Huh-7 cells assessed as cell viability by Cell Titer Glo assay
|
[PMID: 38428537] |
| Huh-7 | IC50 |
10.59 μM
Compound: 12b
|
Inhibition HBsAg secretion in human Huh-7 cells harboring pHBV1.3 treated for 2 days followed by replacement of medium containing compound measured after 4 days by CLIA
Inhibition HBsAg secretion in human Huh-7 cells harboring pHBV1.3 treated for 2 days followed by replacement of medium containing compound measured after 4 days by CLIA
|
[PMID: 38428537] |
| Huh-7.5 | CC50 |
>50 μM
Compound: 12b
|
Cytotoxicity against human Huh7.5 cells
Cytotoxicity against human Huh7.5 cells
|
[PMID: 38428537] |
PROTAC PAPD5 degrader 1 (Compound 12b) (48 h) potently inhibits HAV replication in Huh7.5 cells, with an IC50 of 277 nM[1].
PROTAC PAPD5 degrader 1 (7.5-15 μM; 5 days) reduces HBV RNA levels in HepG2.2.15 cells, but its potency is lower than that of the parent compound RG7834 (HY-117650A)[1].
PROTAC PAPD5 degrader 1 inhibits HBsAg production in HepG2.2.15 cells, with an IC50 of 16.24 μM[1].
PROTAC PAPD5 degrader 1 inhibits the production of HBsAg in pHBV1.3-transfected Huh7 cells, with an IC50 of 10.59 μM[1].
PROTAC PAPD5 degrader 1 (10 μM; 24-48 h) induces proteasome-dependent degradation of PAPD5 (TENT4B) in Huh7.5 cells, but does not affect the expression level of PAPD7 (TENT4A)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:Huh7.5 cells
-
Concentration:10 μM
-
Incubation Time:24 h, 48 h
-
Result:Caused near-complete loss of detectable PAPD5 polypeptide by 24 hours, while actin levels remained unchanged.
Showed no observable change in PAPD7 levels.
Restored PAPD5 levels to amounts similar to DMSO-treated cells when co-incubated with epoxomicin, confirming proteasome-mediated degradation.
Chemical Information
-
Molecular Weight 978.05
-
Formula C49H63N5O16
-
SMILES
O=C(C1=CN([C@H](C(C)C)CC2=C3C=C(OC)C(OCCCNC(CCOCCOCCOCCOCCOCCOCCNC4=CC=CC(C(N5C(CC6)C(NC6=O)=O)=O)=C4C5=O)=O)=C2)C3=CC1=O)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
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PROTAC PAPD5 degrader 1 Related Classifications
HY-162327 Related Classifications
Powered by Bioz