Art. -Nr.: HY-160528

IBG3

Name: IBG3
Brand: MedChemExpress
SKU: HY-160528
Price: 500.00 USD
Availability: InStock
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IBG3 is a bivalent molecular glue degrader that targets BRD2 and BRD4, with an EC₅₀ of 32 nM and a Kd of 0.6 µM against human BRD4. IBG3 exhibits selectivity for BRD2 and BRD4 over BRD3. By recruiting the DCAF16 E3 ligase, IBG3 cis-binds to the tandem bromodomains of BRD2 and BRD4, enhances BRD-DCAF16 binding affinity, promotes ubiquitination and proteasomal degradation, and does not degrade isolated bromodomains. IBG3 lacks degradation selectivity for PSMA-positive and PSMA-negative prostate cancer cells, but shows lower in vivo antitumor efficacy than the PSMA-targeting conjugate IBG-P3, and can be used in prostate cancer-related research.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 98.53%
Formel: C₅₄H₅₇N₉O₅S₂
Molecular Weight:976.22

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

IBG3 Chemical Structure

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

BRD2

8.6 pM (DC₅₀)

BRD4

6.7 pM (DC₅₀)

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Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	DC₅₀	8.6 pM	Degradation of BRD2 in HEK293 HiBiT knock-in cells expressing BRD2-HiBiT quantified via HiBiT lytic detection system after 5 h incubation. Degradation of BRD2 in HEK293 HiBiT knock-in cells expressing BRD2-HiBiT quantified via HiBiT lytic detection system after 5 h incubation.	38383787

In Vitro

IBG3 has enhanced stability in the BRD4-IBG3-DCAF16 ternary complex compared to the BRD4-IBG1-DCAF16 ternary complex and BRD4-DCAF16 binary complex, with a separation stage free energy contribution of −19.9 kcal/mol, consistent with biophysical assay trends^[1].
IBG3 (0.1 nM; 6 h) potently degrades BRD4Tandem in KBM7 reporter cells with a DC₅₀ of 6.7 pM, showing selectivity for BRD2 and BRD4 over BRD3 and requiring intact tandem bromodomains for activity^[2].
IBG3 (increasing concentrations; 5 h) potently degrades BRD2 in HEK293 HiBiT knock-in cells with a DC₅₀ of 8.6 pM, while also degrading BRD4 and sparing BRD3^[2].
IBG3 (increasing concentrations; 30 min) promotes formation of the BRD4_Tandem-DCAF16 ternary complex in vitro with an EC₅₀ of 32 nM^[2].
IBG3 (1:1.1 molar ratio of BRD4Tandem to IBG3; 30 min) enhances the affinity of DCAF16-DDB1(ΔBPB)-DDA1 for BRD4Tandem in vitro, with a measured K_d of 177 nM and endothermic binding thermodynamics^[2].
IBG3 (0.1 nM; 6 h)-mediated BRD4 degradation in KBM7 reporter cells is dependent on the CRL4-DCAF16 complex^[2].
IBG3 (0.001-10 nM; 24 h) potently induces BRD4 degradation in both PSMA-negative PC3 and PSMA-overexpressing PC3-PIP cells, with complete degradation achieved at 10 nM in PC3 cells and 0.01 nM in PC3-PIP cells, and no inherent cell-type selectivity^[4].

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

Western Blot Analysis^[4]

Cell Line:

human prostate adenocarcinoma PC3 (PSMA-negative), PC3-PIP (PSMA-overexpressing)
Concentration:

0.001, 0.01, 0.1, 1, 10 nM
Incubation Time:

24 h
Result:

Induced complete BRD4 degradation in PC3-PIP cells at concentrations as low as 0.01 nM.
Induced complete BRD4 degradation in PC3 cells at a concentration of 10 nM.
Showed no significant difference in BRD4 degradation activity between PC3 and PC3-PIP cells.

In Vivo

IBG3 (0.004 mg/kg; i.p.; daily; 5 days) induces 46.4% tumor growth inhibition in engineered PSMA-positive PC3-PIP prostate cancer xenografts^[4].
IBG3 (0.0004 mg/kg; i.p.; daily; 12 days) induces 29.7% tumor growth inhibition in endogenously PSMA-positive LNCaP prostate cancer xenografts^[4].
IBG3 (0.004 mg/kg; i.p.; daily; 5 days) shows detectable selectivity for PSMA-positive over PSMA-negative prostate cancer co-xenografts, inducing 46.4% tumor growth inhibition in PC3-PIP tumors and 16.7% inhibition in PC3 tumors^[4].

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

Animal Model:

NSG (male, 8-10 weeks old, subcutaneous xenograft of PC3-PIP cells)^[4]
Dosage:

0.004 mg/kg
Administration:

i.p.; daily; 5 days
Result:

Achieved 46.4% tumor growth inhibition in PC3-PIP xenografts.

Animal Model:

NSG (male, 8-10 weeks old, subcutaneous xenograft of LNCaP cells)^[4]
Dosage:

0.0004 mg/kg
Administration:

i.p.; daily; 12 days
Result:

Achieved 29.7% tumor growth inhibition in LNCaP xenografts.

Animal Model:

NSG (male, 8-10 weeks old, subcutaneous co-xenograft of PC3 cells and PC3-PIP cells)^[4]
Dosage:

0.004 mg/kg
Administration:

i.p.; daily; 5 days
Result:

Achieved 46.4% tumor growth inhibition in PSMA-positive PC3-PIP tumors.
Achieved 16.7% tumor growth inhibition in PSMA-negative PC3 tumors.

Chemical Information

Appearance Solid
Molecular Weight 976.22
Formel C₅₄H₅₇N₉O₅S₂
Color Off-white to light yellow
SMILES

O=C(NCC1=CC=C(C2=N[C@@H](CC(OC(C)(C)C)=O)C3=NN=C(C)N3C4=C2C(C)=C(C)S4)C=C1)C5=CC=C(C6=CC=C(C7=N[C@@H](CC(OC(C)(C)C)=O)C8=NN=C(C)N8C9=C7C(C)=C(C)S9)C=C6)C=C5
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (1)

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Structure

CAND1 and CAND2 drive CUL4 substrate receptor exchange with largely comparable biochemical efficiency, unlike their relative effects on CUL1. [Abstract]

2026 Mar 20:S0969-2126(26)00056-0. PMID: 41864201

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (102.44 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.0244 mL

5.1218 mL

10.2436 mL

5 mM

0.2049 mL

1.0244 mL

2.0487 mL

10 mM

0.1024 mL

0.5122 mL

1.0244 mL

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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (297 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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)

Verweise

[1]. Tan B, et al. Quantifying Ternary Complex Stability Through Binding Free Energy Calculations in the Geometric Route[J]. 2026.

[2]. Hsia O, et al. Targeted protein degradation via intramolecular bivalent glues. Nature. 2024 Mar;627(8002):204-211. [Content Brief]

[3]. Cai D, et al. Development of Prostate Cancer-Targeting BRD4 Intramolecular Bivalent Molecular Glue Degraders[J]. 2024.

[4]. Cai D, et al. In vivo validation of intramolecular bivalent glues targeting PSMA reveals potent and tissue-selective BRD4 degradation in prostate cancer[J]. Acta Pharmaceutica Sinica B, 2026.

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.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. 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	1.0244 mL	5.1218 mL	10.2436 mL	25.6090 mL
	5 mM	0.2049 mL	1.0244 mL	2.0487 mL	5.1218 mL
	10 mM	0.1024 mL	0.5122 mL	1.0244 mL	2.5609 mL
	15 mM	0.0683 mL	0.3415 mL	0.6829 mL	1.7073 mL
	20 mM	0.0512 mL	0.2561 mL	0.5122 mL	1.2804 mL
	25 mM	0.0410 mL	0.2049 mL	0.4097 mL	1.0244 mL
	30 mM	0.0341 mL	0.1707 mL	0.3415 mL	0.8536 mL
	40 mM	0.0256 mL	0.1280 mL	0.2561 mL	0.6402 mL
	50 mM	0.0205 mL	0.1024 mL	0.2049 mL	0.5122 mL
	60 mM	0.0171 mL	0.0854 mL	0.1707 mL	0.4268 mL
	80 mM	0.0128 mL	0.0640 mL	0.1280 mL	0.3201 mL
	100 mM	0.0102 mL	0.0512 mL	0.1024 mL	0.2561 mL

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IBG3

Publications Citing Use of MedChemExpress (MCE) IBG3

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