country

Change Language

EN - English
FR - Français
DE - Deutsch
ES - Español
JA - 日本語
KO - 한국어

Country or Region:

United States

Product Name	Size / Unit Price	Qty

Total: USD 0.00 Checkout

Cat. No.: HY-180177

Copy Link Print Information

PROTAC BLIMP-1 degrader-1

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: BLIMP-1 ligand (HY-180178); Blue: Ligands for E3 Ligase and Cereblon ligand (HY-W442918); Black: linker (HY-180180)).

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

Formula: C₄₁H₄₇BrN₈O₄
Molecular Weight:795.77

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (271 KB)

PROTAC BLIMP-1 degrader-1 Chemical Structure

Price

Stock

Quantity

Amount: USD 0.00

* Please select Quantity before adding items.

Use of MCE Products

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

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

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: BLIMP-1 ligand (HY-180178); Blue: Ligands for E3 Ligase and Cereblon ligand (HY-W442918); Black: linker (HY-180180)).

IC₅₀ & Target^[1]

BLIMP-1

13.1 nM (EC₅₀)

All PROTACs Isoforms :

All Histone Methyltransferase Isoforms :

In Vitro

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].
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].
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

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.

Chemical Information

Molecular Weight 795.77
Formula C₄₁H₄₇BrN₈O₄
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (271 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)

References

[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]

Calculators

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

Get Quote In-stock

Other size

Get Quote

Amount: USD 0.00

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent:

Product Name:
CAS No.:
Species:
Purity:
Quantity:

PROTAC BLIMP-1 degrader-1

All PROTACs Isoforms

All Histone Methyltransferase Isoforms