2. PROTAC Cell Cycle/DNA Damage
  3. PROTACs Telomerase
  4. NU-PRO-1

NU-PRO-1 is a covalent Telomerase reverse transcriptase (TERT) PROTAC degrader. NU-PRO-1 induces transient, VHL- and proteasome-dependent proteasomal degradation of TERT in cancer cells. NU-PRO-1 delays DNA repair in irradiated cancer cells without inducing DNA damage on its own. NU-PRO-1 can be used for the research of cancer.
(Pink: Telomerase ligand (HY-174352); Blue: VHL ligand (HY-125845); Black: linker (HY-125845)).

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NU-PRO-1

NU-PRO-1 Chemical Structure

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NU-PRO-1 Related Antibodies

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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Description

NU-PRO-1 is a covalent Telomerase reverse transcriptase (TERT) PROTAC degrader. NU-PRO-1 induces transient, VHL- and proteasome-dependent proteasomal degradation of TERT in cancer cells. NU-PRO-1 delays DNA repair in irradiated cancer cells without inducing DNA damage on its own. NU-PRO-1 can be used for the research of cancer[1]. (Pink: Telomerase ligand (HY-174352); Blue: VHL ligand (HY-125845); Black: linker (HY-125845)).

IC50 & Target[1]

VHL

 

In Vitro

NU-PRO-1 (0.1-0.4 μM; 3-36 h) induces transient, VHL- and proteasome-dependent degradation of TERT in MCF7 cells, with maximum degradation of 95% achieved at 0.1 μM after 3 h, and activity maintained in the 0.1-0.4 μM range over 8 h[1].
NU-PRO-1 (0.3 μM) enhances persistence of DNA double-strand break foci after ionizing radiation in MCF7 cells more effectively than TERT catalytic inhibition alone, indicating superior radiosensitization via TERT degradation[1].

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

NU-PRO-1 Related Antibodies

Western Blot Analysis[1]

Cell Line: human breast cancer MCF7 cells
Concentration: 0.1 μM; 0.2 μM; 0.3 μM; 0.4 μM
Incubation Time: 0, 2, 3, 4, 6, 8, 12, 36 h
Result: Induced transient TERT degradation, with a maximum degradation of 95% at 0.1 μM after 3 h.
Achieved effective degradation at 0.1-0.4 μM over 8 h, with the lowest relative TERT level observed at 0.2 μM (0.09 relative intensity).
Detected degradation as early as 2 h, reached a nadir around 10 h, and TERT levels rebounded to near baseline by 24 h.
Was prevented from inducing TERT degradation by pretreatment with MG132 (HY-13259), MLN4924 (HY-70062), AHPC-HCl, or VH-298 (HY-100947).
Molecular Weight

1021.14

Formula

C50H62F2N8O11S
SMILES

O=C([C@](C1=O)(C)[C@H](CCC2=CN(CC3=CC(C(NCCOCCOCC(N[C@@H](C(C)(C)C)C(N4[C@H](C(NCC5=CC=C(C6=C(C)N=CS6)C=C5)=O)C[C@@H](O)C4)=O)=O)=O)=C(F)C=C3F)N=N2)O[C@H](C)C1=C)OC
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Room temperature in continental US; may vary elsewhere.
Storage

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Purity & Documentation
References
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NU-PRO-1 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

NU-PRO-1PROTACsTelomeraseTelomerase Reverse TranscriptaseDNA double-strand break fociionizing radiationTERTVHLDNA repairDNA damageproteasomeMCF7 cellscancer cellsInhibitorinhibitorinhibit

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