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GBD-9

CAT: 0804-HY-153803-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-153803-01Size:5 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
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)[2][3]. GBD-9 is composed of E3 ubiquitin ligase ligand (pink part) 5-Aminothalidomide , target protein ligand (blue part) Btk Inhibitor: IBT6A (HY-13036A), and PROTAC linker (black part) Nonanoic acid (HY-N7057).
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.
Shipping Conditions
Blue Ice
Storage Conditions
-20°C (Powder, sealed storage, away from moisture and light)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
Cereblon

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