2. PROTAC Metabolic Enzyme/Protease MAPK/ERK Pathway PI3K/Akt/mTOR Apoptosis
  3. PROTACs HIF/HIF Prolyl-Hydroxylase p38 MAPK Akt PI3K MEK Apoptosis
  4. PROTAC HIF-1α degrader-2

PROTAC HIF-1α degrader-2 is a highly efficient and selective PROTAC degrader targeting HIF-1α. PROTAC HIF-1α degrader-2 promotes HIF-1α degradation via the ubiquitin-proteasome pathway by facilitating the formation of a HIF-1α/VHL ternary complex. PROTAC HIF-1α degrader-2 inhibits HeLa cell proliferation, migration, and colony formation, and induces apoptosis. PROTAC HIF-1α degrader-2 reduces p-MEK and p-AKT expression in the MAPK and PI3K/AKT pathways. PROTAC HIF-1α degrader-2 can be used for the study of cervical cancer.
(Pink: HIF-1α ligand (HY-179434); Blue: VHL ligand (HY-125845); Black: linker).

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

PROTAC HIF-1α degrader-2

PROTAC HIF-1α degrader-2 Chemical Structure

CAS No. : 3095636-64-6

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Based on 1 publication(s) in Google Scholar

PROTAC HIF-1α degrader-2 Related Antibodies

Top Publications Citing Use of Products

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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HIF-1α HIF

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p38 MAPK Akt1 p38α p38β MAPK13 p38δ p38γ

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Akt Akt1 Akt2 Akt3

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

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MEK1 MEK2 MEK5 MEK MAP2K4/MEK4 MAP2K7/MEK7

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Description

PROTAC HIF-1α degrader-2 is a highly efficient and selective PROTAC degrader targeting HIF-1α. PROTAC HIF-1α degrader-2 promotes HIF-1α degradation via the ubiquitin-proteasome pathway by facilitating the formation of a HIF-1α/VHL ternary complex. PROTAC HIF-1α degrader-2 inhibits HeLa cell proliferation, migration, and colony formation, and induces apoptosis. PROTAC HIF-1α degrader-2 reduces p-MEK and p-AKT expression in the MAPK and PI3K/AKT pathways. PROTAC HIF-1α degrader-2 can be used for the study of cervical cancer[1]. (Pink: HIF-1α ligand (HY-179434); Blue: VHL ligand (HY-125845); Black: linker).

IC50 & Target[1]

HIF-1α

22.4 μM (DC50)

VHL

 

In Vitro

PROTAC HIF-1α degrader-2 (Compound Z12) shows the strongest anti-proliferative activity against HeLa cells (IC50 = 10.10 μM)[1].
PROTAC HIF-1α degrader-2 (0-80 μM, 24 h) dose-dependently degrades HIF-1α protein in HeLa cells (DC50 = 22.40 μM), and high concentrations (> 40 μM) exhibit a "hook effect"[1].
PROTAC HIF-1α degrader-2 (20 μM, 0-36 h) degrades HIF-1α in HeLa cells in a time-dependent manner, with a degradation rate of 59.7% after 36 hours of incubation, and after removing the compound, the degradation effect could be maintained for 24 hours[1].
PROTAC HIF-1α degrader-2 (0-20 μM, 48 h) induces acute cytotoxicity in HeLa cells, dose-dependently reducing live cells (green fluorescence) and increasing dead cells (red fluorescence)[1].
PROTAC HIF-1α degrader-2 (0-10 μM, 15 days) dose-dependently inhibits HeLa cell colony formation[1].
PROTAC HIF-1α degrader-2 (0-20 μM, 0-24 h) inhibits the migration ability of HeLa cells[1].
PROTAC HIF-1α degrader-2 (0-20 μM, 24-48 h) induces apoptosis, morphological changes in HeLa cells, and increases the apoptosis rate of HeLa cells[1].
PROTAC HIF-1α degrader-2 (0-20 μM, 24 h) dose-dependently reduces the protein levels of p-MEK (44.6%-89.1%) and p-AKT (39.0%-63.0%) in HeLa cells[1].

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

PROTAC HIF-1α degrader-2 Related Antibodies

Western Blot Analysis[1]

Cell Line: HeLa cells
Concentration: 0 μM, 2.5 μM, 5 μM, 10 μM, 20 μM, 40 μM, 60 μM, 80 μM
Incubation Time: 24 h
Result: Dose-dependently degraded HIF-1α protein, with a DC50 of 22.40 μM and a maximum degradation rate (D%) of 73% (at 40 μM). A "hook effect" was observed at high concentrations (> 40 μM).

Cell Migration Assay [1]

Cell Line: HeLa cells
Concentration: 0 μM, 5 μM, 10 μM, 20 μM
Incubation Time: 0 h, 6 h, 24 h
Result: Dose-dependently degraded HIF-1α protein, with a DC50 of 22.40 μM and a maximum degradation rate (D%) of 73% (at 40 μM). A "hook effect" was observed at high concentrations (> 40 μM).
Molecular Weight

940.16

Formula

C50H65N7O9S
CAS No.
SMILES

COC(C1=CC(NC(COC2=CC=C(C=C2)N3CCN(CC3)CCCCCCCC(N[C@@H](C(C)(C)C)C(N4C[C@@H](C[C@H]4C(NCC5=CC=C(C=C5)C6=C(N=CS6)C)=O)O)=O)=O)=O)=C(C=C1)O)=O
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References
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PROTAC HIF-1α degrader-2 Related Classifications

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  • 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:

PROTAC HIF-1α degrader-23095636-64-6PROTACsHIF/HIF Prolyl-Hydroxylasep38 MAPKAktPI3KMEKApoptosisHypoxia-inducible factorsHIFsHIF-PHPKBProtein kinase BPhosphoinositide 3-kinaseMitogen-activated protein kinase kinaseMAPKKMAP2KHIF-1αLW-6PROTAC degraderHIF-1α degradation mechanismAnti-cervical cancerInhibitorinhibitorinhibit

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