Referencia número: HY-180177

PROTAC BLIMP-1 degrader-1

Name: PROTAC BLIMP-1 degrader-1
Brand: MedChemExpress
SKU: HY-180177
Price: 1340.00 USD
Availability: InStock
Rating: 5 (1 reviews)

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PROTAC BLIMP-1 degrader-1 is an orally active BLIMP-1 PROTAC degrader with an EC₅₀ of 13.1 nM. PROTAC BLIMP-1 degrader-1 recruits the neprilysin (CRBN) E3 ligase to mediate ubiquitination and subsequent degradation of BLIMP-1α via the 26S proteasome, without affecting the BLIMP-1β isoform. PROTAC BLIMP-1 degrader-1 inhibits cancer cell proliferation and tumor growth. It can be used in research related to multiple myeloma.
(Pink: ligand (HY-180178); Blue: ligand (HY-W442918); Black: linker (HY-180180)).

Para uso exclusivo en investigación. No vendemos a pacientes.

Pureza : 98.49%
Fòrmula: C₄₁H₄₇BrN₈O₄
Peso molecular:795.77

Almacenamiento:

4°C, sealed storage, away from moisture

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

PROTAC BLIMP-1 degrader-1 Chemical Structure

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Solvente y solubilidad
- In Vitro
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

PROTAC BLIMP-1 degrader-1 is an orally active BLIMP-1 PROTAC degrader with an EC₅₀ of 13.1 nM. PROTAC BLIMP-1 degrader-1 recruits the neprilysin (CRBN) E3 ligase to mediate ubiquitination and subsequent degradation of BLIMP-1α via the 26S proteasome, without affecting the BLIMP-1β isoform. PROTAC BLIMP-1 degrader-1 inhibits cancer cell proliferation and tumor growth. It can be used in research related to multiple myeloma^[1]. (Pink: ligand (HY-180178); Blue: ligand (HY-W442918); Black: linker (HY-180180)).

IC₅₀ & Target

^[1]

BLIMP-1

13.1 nM (EC₅₀)

Ver todos los productos específicos de isoformas PROTACs :

Ver todos los productos específicos de isoformas Histone Methyltransferase :

In Vitro

OthersAnti-cancerCell Cycle Regulation

Others

PROTAC BLIMP-1 degrader-1 (Compound 49) (2 h) potently induces BLIMP-1 degradation in BLIMP-1-overexpressing HEK293 cells with an EC₅₀ of 13.1 nM, while exhibiting high human liver microsomal stability, moderate permeability, and low efflux potential^[1].

Anti-cancer

PROTAC BLIMP-1 degrader-1 (0.01-10.0 μM; 24 h) induces dose-dependent depletion of endogenous BLIMP-1α (but not BLIMP-1β) in OPM2 and MM1.s multiple myeloma cell lines^[1].

Anti-cancer

Cell Cycle Regulation

PROTAC BLIMP-1 degrader-1 (log₁₀ μM from -4 to 1; 5 days) drives CRBN-dependent cytostatic antiproliferative activity in OPM2 multiple myeloma cells^[1].

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

Western Blot Analysis^[1]

Cell Line:

OPM2, MM1.s multiple myeloma cell lines
Concentration:

0.01, 0.02, 0.04, 0.08, 0.16, 0.32, 0.63, 1.26, 2.5, 5 and 10.0 μM
Incubation Time:

24 h
Result:

Dose-dependently depleted endogenous BLIMP-1α protein in both OPM2 and MM1.s cell lines.
Spares the shorter BLIMP-1β isoform.

Parmacokinetics

Species	Dose	Route	AUC_last	AUC_all	CL	V_ss	T_1/2	MRT	C_max	T_max	Bioavailability
Mice^[1]	1 mg/kg	i.v.	19452 nM·h	21330 nM·h	1.040 mL/min/kg	0.551 L/kg	6.070 h	9.420 h	/	/	/
Mice^[1]	10 mg/kg	p.o.	35489 nM·h	37133 nM·h	/	/	/	/	3577 nM	5.00 h	18.800 %

In Vivo

Anti-cancer

PROTAC BLIMP-1 degrader-1 (Compound 49) (200 mg/kg; p.o.; twice daily; 3 days) achieves sustained BLIMP-1 degradation (54-60%) in MM1.s CDX tumors in NSG mice^[1].

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

Animal Model:

NSG mice^[1]
Dosage:

200 mg/kg
Administration:

p.o.; twice daily; 3 days
Result:

Achieved 54% BLIMP-1 degradation at 6 hours post last dose.
Sustained 60% BLIMP-1 degradation at 14 hours post last dose.

Related Protocols :

Chemical Information

Appearance Solid
Peso molecular 795.77
Fòrmula C₄₁H₄₇BrN₈O₄
Color White to off-white
SMILES

CC1=CC(Br)=CC=C1[C@@H](C(N)=O)N2CCN3N=C(C=C3C2)CNC(C4=NC(C)=C([C@H]5CC[C@@H](CC5)CNC6=CC=C(C7CCC(NC7=O)=O)C=C6)C=C4)=O
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

4°C, sealed storage, away from moisture

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

Solvente y solubilidad

In Vitro:

DMSO : 50 mg/mL (62.83 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

1.2566 mL

6.2832 mL

12.5664 mL

5 mM

0.2513 mL

1.2566 mL

2.5133 mL

10 mM

0.1257 mL

0.6283 mL

1.2566 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Working solution concentration: 0.22 mg/mL

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (272 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)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Simmons BJ, et al. Discovery and Characterization of Novel BLIMP-1 Heterobifunctional Ligand-Directed Degraders. Journal of medicinal chemistry. 2025 Dec 11;68(23):25385-25402. [Content Brief]

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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.2566 mL	6.2832 mL	12.5664 mL	31.4161 mL
	5 mM	0.2513 mL	1.2566 mL	2.5133 mL	6.2832 mL
	10 mM	0.1257 mL	0.6283 mL	1.2566 mL	3.1416 mL
	15 mM	0.0838 mL	0.4189 mL	0.8378 mL	2.0944 mL
	20 mM	0.0628 mL	0.3142 mL	0.6283 mL	1.5708 mL
	25 mM	0.0503 mL	0.2513 mL	0.5027 mL	1.2566 mL
	30 mM	0.0419 mL	0.2094 mL	0.4189 mL	1.0472 mL
	40 mM	0.0314 mL	0.1571 mL	0.3142 mL	0.7854 mL
	50 mM	0.0251 mL	0.1257 mL	0.2513 mL	0.6283 mL
	60 mM	0.0209 mL	0.1047 mL	0.2094 mL	0.5236 mL

Bioz

Keywords

PROTAC BLIMP-1 degrader-1

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PROTAC BLIMP-1 degrader-1

Ver todos los productos específicos de isoformas PROTACs

Ver todos los productos específicos de isoformas Histone Methyltransferase

Actividad biológica

Descripciòn

IC50 & Target

In Vitro

Parmacokinetics

In Vivo

Chemical Information

Solvente y solubilidad

In Vitro:

In Vivo Dissolution Calculator

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table