2. PROTAC Epigenetics Apoptosis Cell Cycle/DNA Damage
  3. PROTACs Histone Methyltransferase Apoptosis Early 2 Factor (E2F) c-Myc
  4. 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)).

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

PROTAC PRMT3 degrader 1

PROTAC PRMT3 degrader 1 Chemical Structure

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PROTAC PRMT3 degrader 1 Related Antibodies

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 NSD3/WHSC1L1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

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Description

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[1]. (Pink: PRMT3 ligand (HY-19715); Blue: MDM2 ligand (HY-130684); Black: linker (HY-42773)).

IC50 & Target[1]

MDM2

 

PRMT3

2.566 μM (DC50)

In Vitro

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.

PROTAC PRMT3 degrader 1 Related Antibodies

Western Blot Analysis[1]

Cell Line: RS4;11 acute leukemia cells
Concentration: 0.1, 1, 2.5, 5, 7.5, 10, 20 μM
Incubation Time: 6, 12, 24, 36, 48 h
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).

Apoptosis Analysis[1]

Cell Line: RS4;11 acute leukemia cells
Concentration: 5, 10, 20 μM
Incubation Time: 24, 48 h
Result: Increased apoptoic cells.
Increased Bax, p-H2AX, cle-caspase-3 and cle-PARP levels.
Molecular Weight

899.88

Formula

C47H53Cl2FN8O5
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PROTAC PRMT3 degrader 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:

PROTAC PRMT3 degrader 1PROTACsHistone MethyltransferaseApoptosisEarly 2 Factor (E2F)c-MycMycProtein arginine methyltransferase 3endoplasmic reticulum stressoxidative phosphorylationMDM2 E3 ubiquitin ligaseRS4;11 acute leukemia cellsasymmetric dimethylarginineacute leukemiaMYCintrinsic apoptosisE2FInhibitorinhibitorinhibit

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