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Cat. No.: HY-181084

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PROTAC BCL6/GSPT1 Degrader-1

PROTAC BCL6/GSPT1 Degrader-1 is a dual-target PROTAC degrader that targets BCL6 and GSPT1. PROTAC BCL6/GSPT1 Degrader-1 inhibits cell proliferation, promotes DNA damage, and induces cell cycle arrest and apoptosis in diffuse large B-cell lymphoma. PROTAC BCL6/GSPT1 Degrader-1 can be used for research on tumors such as lymphoma.
(Pink: BCL6 ligand (HY-111381); Blue: Cereblon ligand (HY-14658); Black: linker (HY-129637)).

For research use only. We do not sell to patients.

CAS No.: 3039500-55-2
Formula: C₄₇H₅₇ClN₁₀O₁₃
Molecular Weight:1005.47

Storage:

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

Data Sheet (268 KB)

PROTAC BCL6/GSPT1 Degrader-1 Chemical Structure

CAS No.: 3039500-55-2

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Use of MCE Products

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

Biological Activity
- Description
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

Description

PROTAC BCL6/GSPT1 Degrader-1 is a dual-target PROTAC degrader that targets BCL6 and GSPT1. PROTAC BCL6/GSPT1 Degrader-1 inhibits cell proliferation, promotes DNA damage, and induces cell cycle arrest and apoptosis in diffuse large B-cell lymphoma. PROTAC BCL6/GSPT1 Degrader-1 can be used for research on tumors such as lymphoma^[1]. (Pink: BCL6 ligand (HY-111381); Blue: Cereblon ligand (HY-14658); Black: linker (HY-129637)).

All PROTACs Isoforms :

All PARP Isoforms :

All Caspase Isoforms :

All CDK Isoforms :

In Vitro

PROTAC BCL6/GSPT1 Degrader-1 (Compound A5) (0-10000 nM; 0-72 h) degrades BCL6 (DC₅₀: 0.48 nM) and GSPT1 in a time- and concentration-dependent manner in Farage DLBCL cells^[1].
PROTAC BCL6/GSPT1 Degrader-1 (0.1-10 μM; 72 h) inhibits the proliferation (IC₅₀: 0.413) and induces DNA damage in Farage diffuse large B-cell lymphoma (DLBCL) cells^[1].
PROTAC BCL6/GSPT1 Degrader-1 (0.1-2.5 μM; 72 h) induces apoptosis and cell cycle arrest in Farage diffuse large B-cell lymphoma (DLBCL) cells^[1].

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

Cell Cycle Analysis^[1]

Cell Line:

Farage DLBCL cells
Concentration:

0.1, 0.5 and 2.5 μM
Incubation Time:

72 h
Result:

Caused substantial accumulation of cells in the G0/G1 phase and downregulated CDK4, CDK6, and CyclinD1.

Western Blot Analysis^[1]

Cell Line:

Farage DLBCL cells
Concentration:

0.1, 0.5 and 2.5 μM
Incubation Time:

72 h
Result:

Upregulated ATF4, ATF3, CHOP, cleaved Caspase 3, and cleaved PARP.

In Vivo

PROTAC BCL6/GSPT1 Degrader-1 (10 mg/kg; i.p.; daily; 3 days) effectively degrades BCL6 and GSPT1 in Farage xenograft tumors in NOD/SCID mice^[1].

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

Animal Model:

NOD/SCID (female, 6-week-old, 18-20 g, subcutaneous Farage cell inoculation)^[1]
Dosage:

10 mg/kg
Administration:

i.p.; daily; 3 days
Result:

Effectively degraded BCL6 and GSPT1 in tumor tissue as shown by immunohistochemical analysis and Western blotting.

Chemical Information

CAS No. 3039500-55-2
Molecular Weight 1005.47
Formula C₄₇H₅₇ClN₁₀O₁₃
SMILES

O=C(COC1=CC2=C(N(C)C1=O)C(OC)=CC(NC3=NC(N4CCC(CC4)C(NCCOCCOCCOCCOCCNC5=CC=CC(C(N6C7C(NC(CC7)=O)=O)=O)=C5C6=O)=O)=NC=C3Cl)=C2)NC
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (268 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]. Hu R, et al. Design synthesis and biological evaluation of novel BCL6/GSPT1 degrader as anti-DLBCL agent. Eur J Med Chem. 2026;305:118567. [Content Brief]

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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.

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Biological Activity
- Description
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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PROTAC BCL6/GSPT1 Degrader-1

All PROTACs Isoforms

All PARP Isoforms

All Caspase Isoforms

All CDK Isoforms