NICE 01

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Description: Heterobifunctional compound for nuclear import of FKBPF36V tagged proteins
Chemical Name: (R)-1-(3-((14-((S)-4-(4-Chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)-2,13-dioxo-6,9-dioxa-3,12-diazatetradecyl)oxy)phenyl)-3-(3,4-dimethoxyphenyl)propyl (S)-1-((S)-2-(3,4,5-trimethoxyphenyl)butanoyl)piperidine-2-carboxylate
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews

Biological Activity for NICE 01

NICE 01 is a bifunctional molecule consisting of (+)-JQ1 (Cat. No. 4499) and AP 1867 (Cat. No. 6207), with a PEG2-diamine linker. It has a high affinity (Kd = 94 pM) for FKBPF36V tagged proteins. It can induce nuclear localization of cytosolic proteins and target transcriptional regulation. It can be used to calculate the kinetic constant and passive diffusion across the nuclear pore.

Technical Data for NICE 01

M. Wt 1206.85
Formula C63H76ClN7O13S
Storage Store at -20°C
Purity ≥98% (HPLC)
PubChem ID 169183208
InChI Key USCBOLCYUGPYAF-YUZLDYPQSA-N
Smiles O=C(O[C@H](CCC1=CC=C(C(OC)=C1)OC)C2=CC=CC(OCC(NCCOCCOCCNC(C[C@H]3C4=NN=C(N4C5=C(C(C6=CC=C(C=C6)Cl)=N3)C(C)=C(S5)C)C)=O)=O)=C2)[C@H]7N(CCCC7)C([C@@H](CC)C8=CC(OC)=C(C(OC)=C8)OC)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for NICE 01

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 60.34 50

Preparing Stock Solutions for NICE 01

The following data is based on the product molecular weight 1206.85. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.5 mM 1.66 mL 8.29 mL 16.57 mL
2.5 mM 0.33 mL 1.66 mL 3.31 mL
5 mM 0.17 mL 0.83 mL 1.66 mL
25 mM 0.03 mL 0.17 mL 0.33 mL

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References for NICE 01

References are publications that support the biological activity of the product.

Lu et al (2022) Bioorthogonal chemical epigenetic modifiers enable dose-dependent CRISPR targeted gene activation in mammalian cells. A.C.S.Synth.Biol. 11 1397 PMID: 35302756

Gibson et al (2023) Bifunctional small molecules that induce nuclear localization and targeted transcriptional regulation. J.Am.Chem.Soc. 145 26028 PMID: 37461636


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Keywords: NICE 01, NICE 01 supplier, CEM207, FKBPF36V, tagged, proteins, BRD4, FKBP, NICE-01, NICE01, Protein, Dimerizers, 8088, Tocris Bioscience

Citations for NICE 01

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