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Art. -Nr.: HY-159570

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XD2-149

XD2-149 is a ZFP91 PROTAC degrader with DC₅₀ values of 0.08 μM and 0.06 μM, respectively. ZFP91 is a bifunctional nuclear protein with both transcription factor and E3 ubiquitin ligase activities, and is classified as an oncogenic non-canonical NF-κB pathway regulator in tumor and immune regulation. XD2-149 induces proteasome-dependent degradation of the E3 ubiquitin-protein ligase ZFP91. XD2-149 inhibits the STAT3 signaling pathway in pancreatic cancer cells and induces NQO1-dependent cell death independent of ZFP91 degradation. XD2-149 can be used for the research of pancreatic cancer.
(Pink: STAT3 ligand (HY-13919); Blue: Cereblon ligand (HY-14658); Black: linker (HY-159572)).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

CAS. Nr.: 2710221-08-0
Formel: C₃₈H₃₉N₅O₈
Molecular Weight:693.74

Speicherung:

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

Data Sheet (270 KB)

XD2-149 Chemical Structure

CAS. Nr.: 2710221-08-0

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Preis

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Use of MCE Products

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

XD2-149 is a ZFP91 PROTAC degrader with DC₅₀ values of 0.08 μM and 0.06 μM, respectively. ZFP91 is a bifunctional nuclear protein with both transcription factor and E3 ubiquitin ligase activities, and is classified as an oncogenic non-canonical NF-κB pathway regulator in tumor and immune regulation. XD2-149 induces proteasome-dependent degradation of the E3 ubiquitin-protein ligase ZFP91. XD2-149 inhibits the STAT3 signaling pathway in pancreatic cancer cells and induces NQO1-dependent cell death independent of ZFP91 degradation. XD2-149 can be used for the research of pancreatic cancer^[1]. (Pink: STAT3 ligand (HY-13919); Blue: Cereblon ligand (HY-14658); Black: linker (HY-159572)).

IC₅₀ & Target^[1]

ZFP91

0.06 μM (DC₅₀)

STAT3

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Alle STAT Isoform-spezifische Produkte anzeigen :

Alle NF-κB Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
BXPC-3	IC₅₀	0.8 μM Compound: 3-6d; XD2-149	Antiproliferative activity against human BxPC-3 cells assessed as reduction in cell viability incubated for 3 days by MTT assay Antiproliferative activity against human BxPC-3 cells assessed as reduction in cell viability incubated for 3 days by MTT assay	[PMID: 33506674]
BXPC-3	IC₅₀	1.2 μM Compound: 3-6d; XD2-149	Antiproliferative activity against human BxPC-3 cells harboring ZFP91siRNA assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human BxPC-3 cells harboring ZFP91siRNA assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 33506674]
BXPC-3	IC₅₀	2.1 μM Compound: 3-6d; XD2-149	Antiproliferative activity against ZFP91 knockdown human BxPC-3 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against ZFP91 knockdown human BxPC-3 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 33506674]
HEK293	IC₅₀	8.7 μM Compound: 3-6d; XD2-149	Antiproliferative activity against human HEK293 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay Antiproliferative activity against human HEK293 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay	[PMID: 33506674]
MIA PaCa-2	IC₅₀	1 μM Compound: 3-6d; XD2-149	Antiproliferative activity against human MIA PaCa-2 cells assessed as reduction in cell viability incubated for 3 days by MTT assay Antiproliferative activity against human MIA PaCa-2 cells assessed as reduction in cell viability incubated for 3 days by MTT assay	[PMID: 33506674]

In Vitro

XD2-149 (72 h) potently inhibits the proliferation of MIA PaCa-2 and BxPC-3 pancreatic cancer cells with an IC₅₀ of 0.9 μM for both, and its cytotoxicity is partially dependent on the expression of ZFP91^[1].
XD2-149 (0-0.5 μM; 7-10 days) inhibits colony formation of BxPC-3 pancreatic cancer cells^[1].
XD2-149 (24 h) potently inhibits STAT3-mediated transcription activated by IL-6 in HEK-293 cells, with an IC₅₀ of 0.9 μM^[1].
XD2-149 potentiates Cycloheximide (HY-12320)-mediated inhibition of STAT3 protein synthesis, and induces NQO1 downregulation in BxPC-3 pancreatic cancer cells in a de novo protein synthesis-dependent manner^[1].
XD2-149 (16 h) downregulates 84 proteins (including STAT3 and ZFP91) in BxPC-3 pancreatic cancer cells^[1].

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

Cell Proliferation Assay^[1]

Cell Line:

BxPC-3 cells
Concentration:

0, 0.06, 0.13, 0.25, 0.5 μM
Incubation Time:

7-10 days
Result:

Inhibited colony formation.

Chemical Information

CAS. Nr. 2710221-08-0
Molecular Weight 693.74
Formel C₃₈H₃₉N₅O₈
SMILES

O=C(C1=CC2=C(C(C3=C(C2=O)C=CC=C3)=O)O1)NCCN4CCC(CCCCCNC5=CC=CC(C(N6C7C(NC(CC7)=O)=O)=O)=C5C6=O)CC4
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (270 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]. Hanafi M, et al. Discovery of a Napabucasin PROTAC as an Effective Degrader of the E3 Ligase ZFP91. Journal of medicinal chemistry. 2021 Feb 11;64(3):1626-1648. [Content Brief]

Calculators

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)}

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

MOQ

Minimum order quantity

100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
Chemical Information
Reinheit & Dokumentation
Verweise

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XD2-149

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle STAT Isoform-spezifische Produkte anzeigen

Alle NF-κB Isoform-spezifische Produkte anzeigen