PROTAC OSBP Degrader-1
PROTAC OSBP Degrader-1 is a CRBN-dependent oxysterol-binding protein (OSBP) PROTAC degrader with a DC50 of 322 nM. PROTAC OSBP Degrader-1 exhibits high specificity for OSBP over other ORP family proteins. PROTAC OSBP Degrader-1 directly interacts with OSBP, possesses rapid cell-penetrating ability, and shows cytotoxicity against cancer cells. PROTAC OSBP Degrader-1 can be used in the research of glioblastoma, lung cancer, triple-negative breast cancer and cervical cancer.
(Pink: Oxysterol-binding Protein-related Protein (ORP) ligand (HY-178035); Blue: Cereblon ligand (HY-10984); Black: linker).
For research use only. We do not sell to patients.
- Formula: C56H68N6O12
- Molecular Weight:1017.17
-
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
All PROTACs Isoforms
More
Biological Activity
Description
IC50 & Target
[1]|
OSBP 322 nM (DC50) |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| U-87MG ATCC | IC50 |
204 nM
|
Antiproliferative activity against human U-87 MG glioblastoma cells assessed as cell proliferation inhibition incubated for 72 hrs by cytotoxicity assay.
Antiproliferative activity against human U-87 MG glioblastoma cells assessed as cell proliferation inhibition incubated for 72 hrs by cytotoxicity assay.
|
40884917 |
| A549 | IC50 |
791 nM
|
Antiproliferative activity against human A549 lung cancer cells assessed as cell proliferation inhibition incubated for 72 hrs by cytotoxicity assay.
Antiproliferative activity against human A549 lung cancer cells assessed as cell proliferation inhibition incubated for 72 hrs by cytotoxicity assay.
|
40884917 |
| MCF7 | IC50 |
1097 nM
|
Antiproliferative activity against human MCF7 breast cancer cells assessed as cell proliferation inhibition incubated for 72 hrs by cytotoxicity assay.
Antiproliferative activity against human MCF7 breast cancer cells assessed as cell proliferation inhibition incubated for 72 hrs by cytotoxicity assay.
|
40884917 |
| HeLa | IC50 |
939 nM
|
Antiproliferative activity against human HeLa cervical cancer cells assessed as cell proliferation inhibition incubated for 72 hrs by cytotoxicity assay.
Antiproliferative activity against human HeLa cervical cancer cells assessed as cell proliferation inhibition incubated for 72 hrs by cytotoxicity assay.
|
40884917 |
| MDA-MB-231 | IC50 |
283 nM
|
Antiproliferative activity against human MDA-MB-231 triple-negative breast cancer cells assessed as cell proliferation inhibition incubated for 72 hrs by cytotoxicity assay.
Antiproliferative activity against human MDA-MB-231 triple-negative breast cancer cells assessed as cell proliferation inhibition incubated for 72 hrs by cytotoxicity assay.
|
40884917 |
In Vitro
PROTAC OSBP Degrader-1 (Compound 5) (72 h) inhibits the proliferation of U-87 MG, A549, MCF7, HeLa, MDA-MB-231 and RPE-1 cells, with IC50 values ranging from 204 nM to 1097 nM[1].
PROTAC OSBP Degrader-1 (1 μM; 10 min-24 h) rapidly penetrates MDA-MB-231 cells. It initially recruits OSBP to the TGN, but starts to translocate OSBP away from the TGN via a mechanism distinct from that of sterol trafficking inhibitor-1 at 3 h post-treatment[1].
PROTAC OSBP Degrader-1 (1-2000 nM; 6-48 h) induces CRBN-dependent, proteasome-mediated OSBP degradation in MDA-MB-231 cells, with a DC50 of 322 nM[1].
PROTAC OSBP Degrader-1 (500 nM; 24 h) specifically degrades OSBP in MDA-MB-231 cells, with no significant effect on the levels of other tested ORP family proteins[1].
PROTAC OSBP Degrader-1 (200 nM) directly binds to the ORD domain of purified OSBP[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:MDA-MB-231 cells (transfected with OSBP-mCherry, immunolabeled for endogenous OSBP)
-
Concentration:1 μM
-
Incubation Time:10, 20, 40 min (imaging); 0, 1, 3, 6, 12, 18, 24 h (fixed analysis)
-
Result:Rapidly penetrated cells within 10 min.
Colocalized with OSBP at the trans-Golgi network (TGN) with maximal recruitment observed slightly after 20 min.
Caused the TGN/cytosol ratio of OSBP to begin decreasing at 3 h post-treatment, with a pronounced drop by 6 h.
-
Cell Line:MDA-MB-231 cells
-
Concentration:1, 10, 25, 50, 100, 200, 500, 1000 and 2000 nM (24 h dose-response); 50, 500 nM (time-course); 50 nM (with 100 nM proteasome inhibitor MG-132 (HY-13259) or 10 μM Immunomodulator Pomalidomide (HY-10984)); 500 nM (with 50 μM protein synthesis inhibitor Cycloheximide (HY-12320) pre-treatment)
-
Incubation Time:24 h (dose-response); 6, 12, 18, 24, 36 and 48 h (time-course); null (MG-132/pomalidomide co-treatment); 1 h (Cycloheximide pre-treatment) followed by 6-24 h
-
Result:Induced dose-dependent OSBP degradation starting at 50 nM, with maximum efficiency at 500 nM, resulting in a DC50 of 322 nM and DCₘₐₓ < 55% after 24 h.
Caused OSBP levels to drop after 6 h, with significant reduction by 18 h and maximum degradation at 24 h.
Had OSBP levels rescued by co-treatment with MG-132 or pomalidomide.
Induced almost complete OSBP degradation by 24 h when protein synthesis was blocked with Cycloheximide.
Chemical Information
-
Molecular Weight 1017.17
-
Formula C56H68N6O12
-
SMILES
O=C(NC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O)COCCOCCCCCCN4N=NC(COC5=CC(/C=C/C6=CC7=C(C(OC)=C6)O[C@]8(C)CC[C@@H](O)C(C)(C)[C@@]8([H])C7)=CC(O)=C5C/C=C(C)\C)=C4
-
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 OSBP Degrader-1 Related Classifications
HY-178034 Related Classifications
Powered by Bioz
Keywords
- PROTAC OSBP Degrader-1
- PROTAC OSBP Degrader1
- PROTAC OSBP Degrader 1
- PROTACs
- Oxysterol-binding Protein-related Protein (ORP)
- PROTAC
- OSBP Degrader
- Oxysterol-binding protein
- Schweinfurthin
- CRBN
- Cereblon
- Protein Degradation
- Ubiquitin-Proteasome System
- Natural Product
- Anticancer
- Glioblastoma
- Triple-negative Breast Cancer
- Lung Cancer
- Cervical Cancer
- Cholesterol Homeostasis
- Lipid Transport
- Inhibitor
- inhibitor
- inhibit