GBD-9

GBD-9 is a degrader based on the E3 ubiquitin ligase CRBN that targets BTK and the G1 to S phase transition protein GSPT1. GBD-9 has both PROTAC and molecular glue properties by inducing ubiquitination and proteasomal degradation of target proteins. GBD-9 can efficiently degrade wild-type and mutant BTK (such as C481S mutation) and GSPT1. GBD-9 significantly inhibits tumor cell proliferation by inducing G1 phase arrest in cancer cells, downregulating anti-apoptotic proteins (BCL-2, MCL-1) and activating Caspase-3 to induce apoptosis. GBD-9 is mainly used in the research of hematological tumors such as diffuse large B-cell lymphoma (DLBCL) and acute myeloid leukemia (AML) [1][2][3]. GBD-9 is composed of E3 ubiquitin ligase ligand (pink part) 5-Aminothalidomide (HY-W023573), target protein ligand (blue part) Btk Inhibitor: IBT6A (HY-13036A), and PROTAC linker (black part) Nonanoic acid (HY-N7057) .

Product Specifications

CAS Number

[2864408-92-2]

UNSPSC

12352005

Target

Btk; Molecular Glues; PROTACs

Type

Reference compound

Related Pathways

PROTAC; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/gbd-9.html

Purity

99.76

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C1N(C2CCC(NC2=O)=O)C(C(C1=C3)=CC=C3NCCCCCCCCC(N4CCC[C@@H](N5N=C(C6=CC=C(OC7=CC=CC=C7)C=C6)C8=C5N=CN=C8N)C4)=O)=O

Molecular Formula

C44H47N9O6

Molecular Weight

797.90

References & Citations

[1]Mann MK, et al. Structure-Activity Relationship of USP5 Inhibitors [published correction appears in J Med Chem. 2022 Jan 13;65 (1) :889]. J Med Chem. 2021;64 (20) :15017-15036.|[2]Yang Z, et al. Merging PROTAC and molecular glue for degrading BTK and GSPT1 proteins concurrently. Cell Res. 2021 Dec;31 (12) :1315-1318.|[3]Zhao L, et al. Targeted protein degradation: mechanisms, strategies and application. Signal Transduct Target Ther. 2022 Apr 4;7 (1) :113.