2. PROTAC Epigenetics
  3. PROTACs Histone Methyltransferase
  4. PROTAC PRMT1 degrader-1

PROTAC PRMT1 degrader-1 (compound 4) is a PRMT1 PROTAC degrader, with a DC50 of 0.77 μM (MCF-7 cells). PROTAC PRMT1 degrader-1 recruits the CRBN E3 ubiquitin ligase to induce proteasome-dependent degradation of PRMT1; it also forms a ternary complex with PRMT1 and CRBN, promoting ubiquitination and subsequent proteasomal degradation of PRMT1. PROTAC PRMT1 degrader-1 reduces the level of asymmetric dimethylarginine in cancer cells, as well as the level of asymmetric dimethylation of arginine 3 on histone H4, while inhibiting the growth of various cancer cells. PROTAC PRMT1 degrader-1 can be used in the research of breast cancer and melanoma.
(Pink: PRMT1 ligand (HY-182297); Blue: Cereblon ligand (HY-14658); Black: linker (HY-133388)).

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PROTAC PRMT1 degrader-1

PROTAC PRMT1 degrader-1 Chemical Structure

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PROTAC PRMT1 degrader-1 Related Antibodies

Top Publications Citing Use of Products

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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 PRMT1 degrader-1 (compound 4) is a PRMT1 PROTAC degrader, with a DC50 of 0.77 μM (MCF-7 cells). PROTAC PRMT1 degrader-1 recruits the CRBN E3 ubiquitin ligase to induce proteasome-dependent degradation of PRMT1; it also forms a ternary complex with PRMT1 and CRBN, promoting ubiquitination and subsequent proteasomal degradation of PRMT1. PROTAC PRMT1 degrader-1 reduces the level of asymmetric dimethylarginine in cancer cells, as well as the level of asymmetric dimethylation of arginine 3 on histone H4, while inhibiting the growth of various cancer cells. PROTAC PRMT1 degrader-1 can be used in the research of breast cancer and melanoma[1]. (Pink: PRMT1 ligand (HY-182297); Blue: Cereblon ligand (HY-14658); Black: linker (HY-133388)).

In Vitro

PROTAC PRMT1 degrader-1 (1 μM) inhibits purified PRMT1 methyltransferase activity with an 86.2% inhibition rate at 1 μM and an IC50 of 185.7 nM in AlphaLISA biochemical assays, while also inhibiting other type I PRMT enzymes in the same assay format[1].
PROTAC PRMT1 degrader-1 (0.1-5 μM; 3-96 h) induces concentration- and time-dependent degradation of PRMT1 in MCF-7 human breast cancer cells, with a DC50 of 0.77 μM, Dmax of 84.83%, and detectable degradation starting at 6 h post-treatment[1].
PROTAC PRMT1 degrader-1 (0.1-5 μM; 48 h) induces concentration-dependent degradation of PRMT1 in A2058 human melanoma cells, with a DC50 of 0.65 μM and a Dmax of 93.03%[1].
PROTAC PRMT1 degrader-1 (0.1-5 μM; 48 h) induces concentration-dependent degradation of PRMT1 in MDA-MB-231, MDA-MB-468, and A375 human cancer cells, with a DC50 of 0.52 μM and Dmax of 88.36% in A375 cells[1].
PROTAC PRMT1 degrader-1 (2 μM; 12-96 h) selectively degrades PRMT1 over PRMT3, PRMT4, PRMT6, and PRMT8 in MCF-7 human breast cancer cells, and does not degrade common CRBN neosubstrates GSPT1, IKZF1, or IKZF3[1].
PROTAC PRMT1 degrader-1 (2 μM; 12-96 h) reduces global asymmetric dimethylarginine levels and histone H4R3me2a levels in a time-dependent manner in MCF-7 human breast cancer cells[1].
PROTAC PRMT1 degrader-1 (1.25-5 μM; 5 days) exhibits dose-dependent growth inhibition of MCF-7 human breast cancer cells and A2058 human melanoma cells over 5 days, with stronger activity than the parental inhibitor DCPT2145, and greater sensitivity observed in A2058 cells[1].
PROTAC PRMT1 degrader-1 (0.63-10 μM; 14 days) inhibits colony formation of MCF-7 human breast cancer cells at 2.5 μM and above, and of A2058 human melanoma cells at 1.25 μM and above, with A2058 cells showing greater sensitivity[1].
PROTAC PRMT1 degrader-1 (1 μM; 0-60 min) has moderate metabolic stability in mouse liver microsomes, with a half-life of 26.0 min and an intrinsic clearance rate of 211 mL/min/kg[1].

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

PROTAC PRMT1 degrader-1 Related Antibodies

Western Blot Analysis[1]

Cell Line: MCF-7 human breast cancer cells
Concentration: 0.1-5 μM (48 h concentration-dependent); 5 μM (time-course); 2 μM (time-course)
Incubation Time: 3-96 h (time-course); 48 h (concentration-dependent)
Result: Reduced PRMT1 protein levels by 40%, 60%, and 86.5% respectively at 0.2, 1, 5 μM for 48 h.
Induced concentration-dependent PRMT1 degradation with a DC50 of 0.77 μM and a maximum degradation (Dₘₐₓ) of 84.83% at 0.1, 0.3, 0.5, 1, 3, 5 μM for 48 h.
Induced detectable PRMT1 degradation as early as 6 h, with near-maximal degradation observed at 48 h at 5 μM.
Caused significant PRMT1 degradation at 48 h, with maximum degradation achieved between 72-96 h at 2 μM.

Western Blot Analysis[1]

Cell Line: A2058 human melanoma cells
Concentration: 0.1-5 μM
Incubation Time: 48 h
Result: Induced concentration-dependent PRMT1 degradation with a DC50 of 0.65 μM and a Dₘₐₓ of 93.03%.

Western Blot Analysis[1]

Cell Line: MDA-MB-231, MDA-MB-468, A375 human cancer cells
Concentration: 0.1-5 μM (A375 cells only)
Incubation Time: 48 h (A375 cells only)
Result: Reduced PRMT1 protein levels in a concentration-dependent manner in MDA-MB-231 and MDA-MB-468 cells.
Induced concentration-dependent PRMT1 degradation with a DC50 of 0.52 μM and a Dₘₐₓ of 88.36% in A375 cells.

Western Blot Analysis[1]

Cell Line: MCF-7 human breast cancer cells
Concentration: 2 μM
Incubation Time: 12-96 h
Result: Reduced PRMT1 protein levels in a time-dependent manner, but had no significant effect on PRMT3, PRMT4, or PRMT6 protein levels over 12-96 h, and only slightly reduced PRMT8 protein levels at 96 h.
Did not degrade CRBN neosubstrates GSPT1, IKZF1, or IKZF3 at these concentrations and time points.\nInduced a time-dependent reduction in global aDMA levels and asymmetric dimethylation of histone H4 arginine 3 (H4R3me2a) levels, consistent with PRMT1 degradation kinetics.

Cell Viability Assay[1]

Cell Line: MCF-7 human breast cancer cells, A2058 human melanoma cells
Concentration: 1.25-5 μM
Incubation Time: 5 days
Result: Showed stronger dose-dependent growth inhibition than the parental inhibitor DCPT2145 at all tested concentrations over 5 days in MCF-7 cells.
Showed stronger dose-dependent growth inhibition than DCPT2145 at all tested concentrations over 5 days in A2058 cells, with greater sensitivity observed in A2058 cells compared to MCF-7 cells.
Molecular Weight

752.94

Formula

C43H56N6O6
SMILES

O=C1N(C(C2=C1C=CC=C2NCCCCCCCCCCCCNC(C3=CC=C(OC4=CC=CC=C4CN(C)CCNC)C=C3)=O)=O)C(C(N5)=O)CCC5=O
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Room temperature in continental US; may vary elsewhere.
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Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PROTAC PRMT1 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 PRMT1 degrader-1PROTACsHistone MethyltransferaseCRBNmelanomaPRMT1breast cancerA2058 human melanoma cellshistone H4proteasomeMCF-7 human breast cancer cellsasymmetric dimethylarginineE3 ubiquitin ligaseInhibitorinhibitorinhibit

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