PROTAC PRMT3 degrader 1
PROTAC PRMT3 degrader 1 is a selective PRMT3 PROTAC degrader with a DC50 of 2.566 μM. PROTAC PRMT3 degrader 1 forms a ternary complex with MDM2 E3 ubiquitin ligase to induce proteasomal and neddylation-dependent degradation of PRMT3. PROTAC PRMT3 degrader 1 activates intrinsic apoptosis, endoplasmic reticulum stress signaling pathways. PROTAC PRMT3 degrader 1 downregulates E2F, MYC, oxidative phosphorylation pathways. PROTAC PRMT3 degrader 1 reduces cellular asymmetric dimethylarginine (ADMA) levels. PROTAC PRMT3 degrader 1 inhibits acute leukemia cell growth. PROTAC PRMT3 degrader 1 acts with glycolysis inhibitor 2-DG to reduce ATP production, induce intrinsic apoptosis, drive synergistic antiproliferative effects. PROTAC PRMT3 degrader 1 can be used for the research of acute leukemia.
(Pink: PRMT3 ligand (HY-19715); Blue: MDM2 ligand (HY-130684); Black: linker (HY-42773)).
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- 화학식: C47H53Cl2FN8O5
- 분자량:899.88
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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
Biological Activity
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MDM2 |
PRMT3 2.566 μM (DC50) |
PROTAC PRMT3 degrader 1 (Compound 11) (0.1-20 μM; 6-48 h) induces dose- and time-dependent degradation of PRMT3 in RS4;11 acute leukemia cells with a DC50 of 2.566 μM and a Dmax of 90% and this effect depends on the proteasome and ubiquitin-like modification[1].
PROTAC PRMT3 degrader 1 (3 days) potently inhibits the growth of acute leukemia cell lines, with the highest activity in RS4;11 cells (IC50 = 1068 nM), and shows minimal activity against lymphoma and solid tumor cell lines[1].
PROTAC PRMT3 degrader 1 (compound 11) (1-10 μM) dose-dependently reduces global asymmetric dimethylarginine (ADMA) levels in RS4;11 acute leukemia cells[1].
PROTAC PRMT3 degrader 1 (5-20 μM; 24-48 h) induces intrinsic apoptosis and G2/M cell cycle arrest in RS4;11 acute leukemia cells via activation of endoplasmic reticulum stress and down-regulation of E2F, MYC, and oxidative phosphorylation pathways[1].
PROTAC PRMT3 degrader 1 (2.5-10 μM; 24 h) exhibits synergistic anti-proliferative and pro-apoptotic effects with glycolysis inhibitor 2-DG (HY-13966) in RS4;11 acute leukemia cells via further reduction of ATP production[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:RS4;11 acute leukemia cells
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Concentration:0.1, 1, 2.5, 5, 7.5, 10, 20 μM
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Incubation Time:6, 12, 24, 36, 48 h
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Result:Induced dose-dependent degradation of PRMT3, with a half-maximal degradation DC50 value of 2.566 μM and a maximum degradation Dₘₐₓ of 90%.
Showed significant PRMT3 degradation starting at 24 h of treatment with 10 μM of the reagent.
Induced PRMT3 degradation, which was effectively blocked by pre-treatment with Bortezomib (HY-10227), Carfilzomib (HY-10455), or MLN4924 (HY-70062).
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Cell Line:RS4;11 acute leukemia cells
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Concentration:5, 10, 20 μM
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Incubation Time:24, 48 h
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Result:Increased apoptoic cells.
Increased Bax, p-H2AX, cle-caspase-3 and cle-PARP levels.
Chemical Information
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분자량 899.88
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화학식 C47H53Cl2FN8O5
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SMILES
O=C([C@@H]1NC2([C@]3([C@H]1C4=CC=CC(Cl)=C4F)C(NC5=C3C=CC(Cl)=C5)=O)CCCCC2)NCCCCCCCCNC(C6CN(C(CNC(NC7=CC8=C(C=NC=C8)C=C7)=O)=O)C6)=O
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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)
PROTAC PRMT3 degrader 1 Related Classifications
HY-159728 Related Classifications
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- PROTAC PRMT3 degrader 1
- PROTACs
- Histone Methyltransferase
- Apoptosis
- Early 2 Factor (E2F)
- c-Myc
- Protein arginine methyltransferase 3
- endoplasmic reticulum stress
- oxidative phosphorylation
- MDM2 E3 ubiquitin ligase
- RS4;11 acute leukemia cells
- asymmetric dimethylarginine
- acute leukemia
- MYC
- intrinsic apoptosis
- E2F
- Inhibitor
- inhibitor
- inhibit