2. PROTAC Protein Tyrosine Kinase/RTK
  3. Btk PROTACs Molecular Glues
  4. 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).
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).

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

GBD-9 Chemical Structure

GBD-9 Chemical Structure

CAS No. : 2864408-92-2

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Based on 1 publication(s) in Google Scholar

GBD-9 Related Antibodies

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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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)[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).

IC50 & Target[1]

Cereblon

 

In Vitro

GBD-9 (50 nM; 24 h) significantly degrades BTK and GSPT1 in DOHH2 cells, and the degradation could be blocked by 20 μM Ibrutinib (HY-10997) or Pomalidomide (HY-10984)[1].
GBD-9 (10-1000 nM; 72 h) inhibits the proliferation of DOHH2, WSU-NHL, HBL-1, THP-1, MV4-11 and other cells in a dose-dependent manner, with an IC50 of 133 nM for DOHH2 cells, which is significantly superior to Ibrutinib and single-target degraders[1].
GBD-9 (10-100 nM; 24 h) induces G1 arrest in DOHH2 cells[1].

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

GBD-9 Related Antibodies

Cell Viability Assay[2]

Cell Line: DOHH2 (DLBCL cell line)
Concentration: 50 nM, 100 nM
Incubation Time: 24 h (50 nM), 4 h (100 nM)
Result: Reduced BTK and GSPT1 protein levels to <20% of baseline at 50 μM, 4 h, with complete abrogation of BTK degradation when co-treated with Ibrutinib (20 μM), and loss of GSPT1 degradation when co-treated with pomalidomide (20 μM), confirming dependency on BTK binding and CRBN recruitment.
Molecular Weight

797.90

Formula

C44H47N9O6
CAS No.
Appearance

Solid

Color

Light yellow to green yellow

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (125.33 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.2533 mL 6.2664 mL 12.5329 mL
5 mM 0.2507 mL 1.2533 mL 2.5066 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.76%

SDS (252 KB)

COA (243 KB) HNMR (507 KB) LCMS (95 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.2533 mL 6.2664 mL 12.5329 mL 31.3322 mL
5 mM 0.2507 mL 1.2533 mL 2.5066 mL 6.2664 mL
10 mM 0.1253 mL 0.6266 mL 1.2533 mL 3.1332 mL
15 mM 0.0836 mL 0.4178 mL 0.8355 mL 2.0888 mL
20 mM 0.0627 mL 0.3133 mL 0.6266 mL 1.5666 mL
25 mM 0.0501 mL 0.2507 mL 0.5013 mL 1.2533 mL
30 mM 0.0418 mL 0.2089 mL 0.4178 mL 1.0444 mL
40 mM 0.0313 mL 0.1567 mL 0.3133 mL 0.7833 mL
50 mM 0.0251 mL 0.1253 mL 0.2507 mL 0.6266 mL
60 mM 0.0209 mL 0.1044 mL 0.2089 mL 0.5222 mL
80 mM 0.0157 mL 0.0783 mL 0.1567 mL 0.3917 mL
100 mM 0.0125 mL 0.0627 mL 0.1253 mL 0.3133 mL
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GBD-9 Related Classifications

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:

GBD-92864408-92-2GBD9GBD 9BtkPROTACsMolecular GluesBruton tyrosine kinaseBTKGSPT1CRBNPROTACmolecular glueInhibitorinhibitorinhibit

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