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Cat. No.: HY-150400A

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XF056-132

(Synonyms: MS132N TFA)

XF056-132 (MS132N TFA) is an inactive WDR5 PROTAC degrader with a K_d value of 106 nM against human targets, and exhibits no significant binding to the VHL complex, serves as a negative control for MS132. XF056-132 binds to WDR5, does not induce WDR5 degradation in pancreatic cancer cells, and exerts no inhibitory effect on adenocarcinoma cells. XF056-132 can be used in the research of pancreatic ductal adenocarcinoma.
(Pink: WDR5 ligand (HY-141799); Blue: Ligands for E3 Ligase ligand (HY-125845); Black: linker).

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

CAS No.: 2694057-55-9
Formula: C₅₃H₅₈F₇N₉O₉S
Molecular Weight:1130.14

Storage:

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

Data Sheet (275 KB)

XF056-132 Chemical Structure

CAS No.: 2694057-55-9

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Fluorescent Dye

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

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

Biological Activity

Description

XF056-132 (MS132N TFA) is an inactive WDR5 PROTAC degrader with a K_d value of 106 nM against human targets, and exhibits no significant binding to the VHL complex, serves as a negative control for MS132. XF056-132 binds to WDR5, does not induce WDR5 degradation in pancreatic cancer cells, and exerts no inhibitory effect on adenocarcinoma cells. XF056-132 can be used in the research of pancreatic ductal adenocarcinoma^[1]^[2]. (Pink: WDR5 ligand (HY-141799); Blue: Ligands for E3 Ligase ligand (HY-125845); Black: linker).

IC₅₀ & Target

WDR5

106 nM nM (Kd)

All PROTACs Isoforms :

In Vitro

XF056-132 binds to purified WDR5 protein with a K_d value of 106 nM, but does not bind to the VCB E3 ligase complex^[1].
XF056-132 (0.1-10.0 μM; 18 h) does not induce WDR5 degradation in the MIA PaCa-2, BxPC-3, HPAF-II, Panc10.05 or PANC-1 pancreatic ductal adenocarcinoma (PDAC) cell lines^[1].
XF056-132 (6 days) does not inhibit the proliferation of MIA PaCa-2, BxPC-3, HPAF-II, Panc10.05 or PANC-1 PDAC cell lines^[1]^[2].

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

Western Blot Analysis^[1]

Cell Line:

MIA PaCa-2, BxPC-3, HPAF-II, Panc10.05, PANC-1 (pancreatic ductal adenocarcinoma (PDAC) cell lines)
Concentration:

0.1, 0.5, 1.0, 5.0, 10.0 μM
Incubation Time:

18 h
Result:

Did not induce any significant reduction in WDR5 protein levels in any of the tested PDAC cell lines.

Chemical Information

CAS No. 2694057-55-9
Molecular Weight 1130.14
Formula C₅₃H₅₈F₇N₉O₉S
SMILES

O=C(C(C(C(F)(F)F)=C1)=CNC1=O)NC2=C(N3C[C@H](N([C@H](C3)C)C)C)C=CC(C4=CC(C(NCC(N[C@@H](C(C)(C)C)C(N5[C@@H](C[C@H](C5)O)C(NCC6=CC=C(C7=C(N=CS7)C)C=C6)=O)=O)=O)=O)=CC=C4F)=C2.O=C(O)C(F)(F)F
Synonyms

MS132N TFA
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 (275 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]. Yu X, et al. Discovery of Potent and Selective WDR5 Proteolysis Targeting Chimeras as Potential Therapeutics for Pancreatic Cancer. Journal of medicinal chemistry. 2023 Dec 14;66(23):16168-16186. [Content Brief]

[2]. Jian Jin, et al. Wd40 repeat domain protein 5 (wdr5) degradation / disruption compounds and methods of use. WO2019246570A1.

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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.

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100 mg

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

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XF056-132

All PROTACs Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

XF056-132 Related Classifications

HY-150400A Related Classifications