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Quality Control of Fmoc-Gly-OH Purity: 98% SDS Specification

COA

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NMR

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CNMR

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HPLC

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LC-MS

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Product Citations Show More

Solid-phase DNA-encoded library synthesis: a master builder’s instructions

Dixit, Anjali ; Paegel, Brian M ;

DOI: 10.1038/s41596-025-01190-4 PubMed ID: 40404924 Nat. Protoc.,2025.

Abstract: Solid-phase DNA-encoded library (DEL) synthesis is a next-generation drug discovery technology with powerful activity-based and cellular lead identification capabilities. Solid-phase DELs combine the one-bead–one-compound approach with DNA encoding to furnish beads that display multiple copies of photocleavable library members and DNA encoding tags. Sequential chemical synthesis and enzymatic DNA ligation reactions yield an encoded library in which individual library members are physically isolable, enabling various high-throughput screening modalities. This advancement from on-DNA synthesis, in which small molecules are directly attached to their DNA-encoding tags, decouples the library member from the steric bulk of the DNA tag, which prevents biased binding to a target. Here we provide step-by-step instructions for solid-phase DEL synthesis, incorporating all of our most recent quality control innovations to ensure robust library production. The protocol begins with on-bead synthesis of a linker containing a spectroscopic handle for chromatographic analysis, an ionization enhancer for mass spectrometry and an alkyne for installation of DNA encoding sites via copper-catalyzed azide-alkyne cycloaddition click chemistry. Coupling of a photocleavable linker before library synthesis enables compound liberation from the bead for activity-based screening. Powerful combinatorial split-and-pool parallel synthesis tactics transform modest collections of small-molecule building blocks into large DELs of all possible building block combinations. Post synthesis, decoding and mass analysis of single DEL beads as well as whole-library deep sequencing provides rigorous chemical and bioinformatic quality control and establishes suitability for screening. The solid-phase chemistry is highly accessible: expertise in chemical synthesis is not necessary and solid-phase synthesis apparatus is routinely available in molecular biology laboratories. This procedure requires ~1 month to complete.

Purchased from AmBeed: 29022-11-5

Shorter Peptide Nucleic Acid Probes Improve Affibody-Mediated Peptide Nucleic Acid-Based Pretargeting

Kristina Westerlund ; Maryam Oroujeni ; Maxime Gestin ; Jacob Clinton ; Alia Hani Rosly ; Hanna Tano , et al.

DOI: 10.1021/acsptsci.4c00106 ACS Pharmacol. Transl. Sci.,2024,7(5):1595-1611.

Abstract: Affibody-mediated PNA-based pretargeting shows promise for HER2-expressing tumor radiotherapy. In our recent study, a 15-mer ZHER2:342-HP15 affibody-PNA conjugate, in combination with a shorter 9-mer [177Lu]Lu-HP16 effector probe, emerged as the most effective pretargeting strategy. It offered a superior tumor-to-kidney uptake ratio and more efficient tumor targeting compared to longer radiolabeled effector probes containing 12 or 15 complementary PNA bases. To enhance the production efficiency of our pretargeting system, we here introduce even shorter 6-, 7-, and 8-mer secondary probes, designated as HP19, HP21, and HP20, respectively. We also explore the replacement of the original 15-mer Z-HP15 primary probe with shorter 12-mer Z-HP12 and 9-mer Z-HP9 alternatives. This extended panel of shorter PNA-based probes was synthesized using automated microwave-assisted methods and biophysically screened in vitro to identify shorter probe combinations with the most effective binding properties. In a mouse xenograft model, we evaluated the biodistribution of these probes, comparing them to the Z-HP15:[177Lu]Lu-HP16 combination. Tumor-to-kidney ratios at 4 and 144 h postinjection of the secondary probe showed no significant differences among the Z-HP9:[177Lu]Lu-HP16, Z-HP9:[177Lu]Lu-HP20, and the Z-HP15:[177Lu]Lu-HP16 pairs. Importantly, tumor uptake significantly exceeded, by several hundred-fold, that of most normal tissues, with kidney uptake being the critical organ for radiation therapy. This suggests that using a shorter 9-mer primary probe, Z-HP9, in combination with 9-mer HP16 or 8-mer HP20 secondary probes effectively targets tumors while minimizing the dose-limiting kidney uptake of radionuclide. In conclusion, the Z-HP9:HP16 and Z-HP9:HP20 probe combinations offer good prospects for both cost-effective production and efficient in vivo pretargeting of HER2-expressing tumors.

Keywords: affibody ; pretargeting ; peptide nucleic acid ; radiotherapy

Purchased from AmBeed: 29022-11-5

Product Details of Fmoc-Gly-OH

CAS No. :	29022-11-5
Formula :	C₁₇H₁₅NO₄
M.W :	297.31
SMILES Code :	O=C(O)CNC(OCC1C2=C(C3=C1C=CC=C3)C=CC=C2)=O
Synonyms :	Fmoc glycine; N-(9-Fluorenylmethoxycarbonyl)glycine; [[[(9H-Fluoren-9-yl)methoxy]carbonyl]amino]acetic acid
MDL No. :	MFCD00037140
InChI Key :	NDKDFTQNXLHCGO-UHFFFAOYSA-N
Pubchem ID :	93124

Safety of Fmoc-Gly-OH

GHS Pictogram:
Signal Word:	Warning
Hazard Statements:	H315-H319-H335
Precautionary Statements:	P261-P305+P351+P338

Application In Synthesis of Fmoc-Gly-OH

* All experimental methods are cited from the reference, please refer to the original source for details. We do not guarantee the accuracy of the content in the reference.

Downstream synthetic route of [ 29022-11-5 ]

[ 29022-11-5 ] Synthesis Path-Downstream 1~35

1
[ 29022-11-5 ]
[ 71989-31-6 ]
[ 35661-40-6 ]
[ 108-24-7 ]
[ 198561-07-8 ]
Ac-Pro-Asp-Phe-Gly-OH [ No CAS ]