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Cat. No.: HY-145762

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YM281

YM281 is a potent EZH2 inhibitor. YM281 induces cell apoptosis and cell cycle arrest at the G0/G1 phase. YM281 shows antitumor effects in vivo. YM281 has the potential for the research of lymphoma.

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CAS No.: 2230914-84-6
화학식: C₅₆H₇₁N₇O₉S
분자량:1018.27

보관:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (275 KB)

YM281 Chemical Structure

CAS No.: 2230914-84-6

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

All Histone Methyltransferase Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
EOL1	IC₅₀	5.4 μM Compound: YM281	Anti-proliferative activity against human EOL1 cells assessed as cell viability measured after 5 days incubation by CCK-8 assay Anti-proliferative activity against human EOL1 cells assessed as cell viability measured after 5 days incubation by CCK-8 assay	[PMID: 38295690]
MV4-11	IC₅₀	>10 μM Compound: YM281	Anti-proliferative activity against human MV4-11 cells assessed as cell viability measured after 5 days incubation by CCK-8 assay Anti-proliferative activity against human MV4-11 cells assessed as cell viability measured after 5 days incubation by CCK-8 assay	[PMID: 38295690]
RS4-11	IC₅₀	4.07 μM Compound: YM281	Anti-proliferative activity against human RS4-11 cells assessed as cell viability measured after 5 days incubation by CCK-8 assay Anti-proliferative activity against human RS4-11 cells assessed as cell viability measured after 5 days incubation by CCK-8 assay	[PMID: 38295690]

In Vitro

YM281 (compound V2) (0-6 µM; 0-48 h) decreases the EZH2 protein level and the PRC2 (polycomb repressive complex 2) complex through the VHL (vonHippel−Lindau)-dependent ubiquitin-proteasome system^[1].
YM281 (0-10 µM; 24 h) shows anticancer effects in lymphoma cells^[1].
YM281 (0-5 µM) induces cell apoptosis and cell cycle arrest at the G0/G1 phase^[1].
YM281 (0-5 µM; 24 h) increases the activity of caspase-3 and -7 and meanwhile reduces the cell viability in primary lymphoma cells^[1].

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

Western Blot Analysis^[1]

Cell Line:

SU-DHL-2, 22Rv1 cells
Concentration:

0-6 µM
Incubation Time:

0-48 h
Result:

Abrogated both the EZH2 protein level and the H3K27me3 degree in a concentration-dependent manner in 24 h, had no significant effect on the protein level of EZH1,and significantly increased the expression of EZH2 ubiquitination.

Cell Viability Assay^[1]

Cell Line:

SU-DHL-2, SU-DHL-4, SU-DHL-6 cells
Concentration:

0-10 µM
Incubation Time:

24 h
Result:

Induced nearly complete cell viability inhibition.

Cell Cycle Analysis^[1]

Cell Line:

SU-DHL-6 cells
Concentration:

1, 3, 5 µM
Incubation Time:

24 h
Result:

Induced cell cycle arrest at the G0/G1 phase and a profound sub-G1 population increasein a concentration-dependent manner.

Apoptosis Analysis^[1]

Cell Line:

SU-DHL-6 cells
Concentration:

0-5 µM
Incubation Time:

48 h
Result:

Significantly increased the expression of cleaved caspase-3 and PARP.

In Vivo

YM281 (80, 100 mg/kg; i.v.; 6 times for 3 weeks) shows antitumor effects and significantly reduces the expression of EZH2 protein and H3K27me3 levels^[1].

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

Animal Model:

Balb/c nude mice (SU-DHL-6 xenograft model)^[1]
Dosage:

80 mg/kg
Administration:

I.v.; 6 times for 3 weeks
Result:

Remarkably suppressed the tumor volume and significantly reduced the EZH2 protein and H3K27me3 levels.

Animal Model:

Balb/c nude mice (Jeko-1 xenograft model)^[1]
Dosage:

100 mg/kg
Administration:

I.v.; 6 times for 3 weeks
Result:

Shows anti-tumor effects with the significantly reduced the expression of EZH2 protein and H3K27me3 levels.

Chemical Information

CAS No. 2230914-84-6
분자량 1018.27
화학식 C₅₆H₇₁N₇O₉S
SMILES

CCN(C1CCOCC1)C2=CC(C3=CC=C(C=C3)OCCCOCC(N[C@@H](C(C)(C)C)C(N4[C@@H](C[C@H](C4)O)C(NCC5=CC=C(C6=C(N=CS6)C)C=C5)=O)=O)=O)=CC(C(NCC7=C(C=C(NC7=O)C)C)=O)=C2C
선적

Room temperature in continental US; may vary elsewhere.
보관

Please store the product under the recommended conditions in the Certificate of Analysis.

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Tu Y,et al. Design, Synthesis, and Evaluation of VHL-Based EZH2 Degraders to Enhance Therapeutic Activity against Lymphoma. J Med Chem. 2021 Jul 22;64(14):10167-10184. [Content Brief]

Calculators

몰농도 계산기

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

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Molecular Weight Molecular Weight

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Concentration _(final) Concentration _(final)

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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MOQ

Minimum order quantity

100 mg

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Biological Activity
- 제품 설명
- In Vitro
- In Vivo
Chemical Information
순도&문서
References

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YM281

All Histone Methyltransferase Isoforms

Biological Activity

Chemical Information

순도&문서

References

Calculators

Help & FAQs

YM281 Related Classifications

HY-145762 Related Classifications