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Cat. No.: HY-178034

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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).

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

화학식: C₅₆H₆₈N₆O₁₂
분자량:1017.17

보관:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (275 KB)

PROTAC OSBP Degrader-1 Chemical Structure

Amount: USD 0.00

* 장바구니에 담기 전 물품의 수량을 선택해 주십시오.

Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

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^[1]. (Pink: Oxysterol-binding Protein-related Protein (ORP) ligand (HY-178035); Blue: Cereblon ligand (HY-10984); Black: linker).

IC₅₀ & Target

^[1]

OSBP

322 nM (DC₅₀)

All PROTACs Isoforms :

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

Anti-cancerOthers

Anti-cancer

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].

Others

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.

Immunofluorescence^[1]

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.

Western Blot Analysis^[1]

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.

Related Protocols :

Chemical Information

분자량 1017.17
화학식 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
선적

Room temperature in continental US; may vary elsewhere.
보관

Please store the product under the recommended conditions in the Certificate of Analysis.

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Guimard C, et al. Elaboration and profiling of the first OSBP degrader issued from natural Schweinfurthins. Bioorganic chemistry. 2025 Sep;164:108909. [Content Brief]

Calculators

몰농도 계산기

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

MOQ

Minimum order quantity

100 mg

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Other size

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Amount: USD 0.00

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
Chemical Information
순도&문서
References

상품명:
Cat. No.:
수량:
MCE Japan Authorized Agent:

상품명:
CAS No.:
Species:
Purity:
수량:

PROTAC OSBP Degrader-1

All PROTACs Isoforms