XF056-132 free base
XF056-132 free base (MS132N) is an inactive WDR5 PROTAC degrader with a Kd 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 free base binds to WDR5, does not induce WDR5 degradation in pancreatic cancer cells, and exerts no inhibitory effect on adenocarcinoma cells. XF056-132 free base 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).
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- CAS No.: 2407450-73-9
- 화학식: C51H57F4N9O7S
- 분자량:1016.11
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
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Biological Activity
제품 설명
IC50 & Target
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WDR5 106 nM nM (Kd) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BXPC-3 | GI50 |
4 μM
Compound: 11; MS132
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Growth inhibition of human BXPC-3 cells incubated for 6 days by MTS assay
Growth inhibition of human BXPC-3 cells incubated for 6 days by MTS assay
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[PMID: 38019706] |
| HPAF-II | GI50 |
9200 nM
Compound: 11; MS132
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Growth inhibition of human HPAF-II cells incubated for 6 days by MTS assay
Growth inhibition of human HPAF-II cells incubated for 6 days by MTS assay
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[PMID: 38019706] |
| MIA PaCa-2 | GI50 |
5700 nM
Compound: 11; MS132
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Growth inhibition of human MIA PaCa-2 cells incubated for 6 days by MTS assay
Growth inhibition of human MIA PaCa-2 cells incubated for 6 days by MTS assay
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[PMID: 38019706] |
| PANC-1 | GI50 |
32700 nM
Compound: 11; MS132
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Growth inhibition of human PANC-1 cells incubated for 6 days by MTS assay
Growth inhibition of human PANC-1 cells incubated for 6 days by MTS assay
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[PMID: 38019706] |
| Panc1005 | GI50 |
14300 nM
Compound: 11; MS132
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Growth inhibition of human Panc1005 cells incubated for 6 days by MTS assay
Growth inhibition of human Panc1005 cells incubated for 6 days by MTS assay
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[PMID: 38019706] |
In Vitro
XF056-132 free base binds to purified WDR5 protein with a Kd value of 106 nM, but does not bind to the VCB E3 ligase complex[1].
The free base form of 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) free base 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. .
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Cell Line:MIA PaCa-2, BxPC-3, HPAF-II, Panc10.05, PANC-1 (pancreatic ductal adenocarcinoma (PDAC) cell lines)
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Concentration:0.1, 0.5, 1.0, 5.0, 10.0 μM
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Incubation Time:18 h
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Result:Did not induce any significant reduction in WDR5 protein levels in any of the tested PDAC cell lines.
Chemical Information
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CAS No. 2407450-73-9
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분자량 1016.11
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화학식 C51H57F4N9O7S
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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
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Synonyms
MS132N
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
XF056-132 free base Related Classifications
HY-150400 Related Classifications
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