2. PROTAC Immunology/Inflammation Membrane Transporter/Ion Channel Cell Cycle/DNA Damage Epigenetics Apoptosis
  3. PROTACs BCL6 Aquaporin PARP Caspase CDK
  4. 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.

PROTAC BCL6/GSPT1 Degrader-1

PROTAC BCL6/GSPT1 Degrader-1 Chemical Structure

CAS No. : 3039500-55-2

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PROTAC BCL6/GSPT1 Degrader-1 Related Antibodies

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PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

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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)).

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.

PROTAC BCL6/GSPT1 Degrader-1 Related Antibodies

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.
Molecular Weight

1005.47

Formula

C47H57ClN10O13
CAS No.
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
References
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PROTAC BCL6/GSPT1 Degrader-1 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PROTAC BCL6/GSPT1 Degrader-13039500-55-2PROTACsBCL6AquaporinPARPCaspaseCDKB-cell lymphoma 6 proteinB-cell lymphoma 5 protein (BCL-5)Zinc finger and BTB domain-containing protein 27Zinc finger protein 51AQPpoly ADP ribose polymerase Cyclin dependent kinaseFarage xenograft tumorsDNA damageFarage DLBCL cellsGSPT1apoptosisNOD/SCID micecell cycle arrestInhibitorinhibitorinhibit

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