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Cat. No.: HY-172769

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CM112

CM112 is a hydrophobic tag-based PRMT1 degrader (DC₅₀ = 0.83 μM) with pan-inhibitory activity against type I PRMTs. CM112 induces proteasome-dependent degradation of PRMT1, inhibits the methyltransferase activities of PRMT1, PRMT3, PRMT4 and PRMT6, downregulates the stability of orphan receptor TR3, thereby interfering with the non-enzymatic scaffolding function of PRMT1. CM112 suppresses clonogenicity and proliferation of tumor cells. CM112 is applicable to research related to breast cancer and non-small cell lung cancer.

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화학식: C₃₉H₆₁N₅O₇
분자량:711.93

보관:

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

Data Sheet (276 KB)

CM112 Chemical Structure

Amount: USD 0.00

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Use of MCE Products

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

Biological Activity
- 제품 설명
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target^[1]

PRMT1

9 nM (IC₅₀)

PRMT1

0.83 μM (DC₅₀)

PRMT3

224 nM (IC₅₀)

PRMT4

19 nM (IC₅₀)

PRMT6

108 nM (IC₅₀)

All Histone Methyltransferase Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
MCF7	DC₅₀	0.83 μM	Concentration causing 50% PRMT1 degradation in human breast cancer MCF-7 cells assessed via Western blot after 72 h incubation. Concentration causing 50% PRMT1 degradation in human breast cancer MCF-7 cells assessed via Western blot after 72 h incubation.	40245820

In Vitro

CM112 (compound 12) (5 μM; 48 h) induces PRMT1 degradation in human breast cancer MCF-7 cells, whereas analogs with shorter carbon chains or PEG linkers do not exert this effect^[1].
CM112 (0.04-10 μM; 72 h) induces concentration-dependent degradation of PRMT1 in MCF-7 human breast cancer cells, with a DC₅₀ of 0.83 μM^[1].
CM112 (0.04-10 μM; 12-96 h) induces time-dependent degradation of PRMT1 in human breast cancer MCF-7 cells, with complete elimination of PRMT1 observed at 10 μM after 96 h of treatment. Meanwhile, it inhibits the enzymatic activity of PRMT1 in a concentration-dependent manner, and reduces the levels of H₄R3me2a and global ADMA within 48 h^[1].
CM112 (10 μM; 12-48 h) induces proteasome-dependent degradation of PRMT1 in human MCF-7 breast cancer cells by binding to PRMT1. It acts at the post-translational level without affecting PRMT1 mRNA expression, and PRMT1 levels can recover after the compound is washed off^[1].
CM112 (0.02-10 μM; 48-72 h) induces concentration-dependent degradation of PRMT1 in the human triple-negative breast cancer cell line MDA-MB-231; it also induces PRMT1 degradation in human non-small cell lung cancer cell lines H3122 and H1299, and reduces the enzymatic activity of PRMT1 in MDA-MB-231 cells^[1].
CM112 (72 h) is a selective PRMT1 degrader in MCF-7 human breast cancer cells. It fails to degrade PRMT3, PRMT4 or PRMT6 at concentrations up to 10 μM, while retaining potent pan-inhibitory activity against type I PRMT enzyme activity, with IC₅₀ values ranging from 8.9 nM to 223.9 nM^[1].
CM112 (0.625-10 μM; 72 h) downregulates the stability of orphan receptor TR3 in a concentration-dependent manner in human breast cancer cell lines MCF-7 and MDA-MB-231, targeting the non-enzymatic scaffolding function of PRMT1, whereas the PRMT1 inhibitor MS023 (HY-19615) has no effect on TR3 stability^[1].
CM112 (10 μM; 0-10 days) inhibits the proliferation of MCF-7 and MDA-MB-231 human breast cancer cells, and reduces colony-forming ability and cell confluence in a time-dependent manner^[1].

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

Western Blot Analysis^[1]

Cell Line:

human breast cancer MCF-7 cells
Concentration:

5 μM
Incubation Time:

48 h
Result:

Induced obvious PRMT1 degradation.

Western Blot Analysis^[1]

Cell Line:

human breast cancer MCF-7 cells
Concentration:

0.04, 0.08, 0.16, 0.31, 0.62, 1.25, 2.5, 5.0, 10 μM
Incubation Time:

72 h
Result:

Reduced PRMT1 levels in a concentration-dependent manner, with a DC₅₀ of 0.83 μM.

Western Blot Analysis^[1]

Cell Line:

human breast cancer MCF-7 cells
Concentration:

10 μM (time-dependent assay)
0.04, 0.15, 0.62, 2.5, 10 μM (concentration-dependent enzymatic assay)
Incubation Time:

12, 24, 48, 72, 96 h (time-dependent assay)
48 h (concentration-dependent enzymatic assay)
Result:

Caused significant PRMT1 degradation after 24 h of treatment with 10 μM, with complete degradation by 96 h.
Completely eliminated H4R3me2a after 48 h at 10 μM.
Inhibited H4R3me2a and global ADMA in a concentration-dependent manner over 48 h.

Western Blot Analysis^[1]

Cell Line:

triple-negative breast cancer MDA-MB-231 cells, non-small cell lung cancer H3122 and H1299 cells
Concentration:

0.02, 0.04, 0.08, 0.16, 0.31, 0.62, 1.25, 2.5, 5.0, 10 μM (MDA-MB-231; 72 h)
1, 5, 10 μM (H3122, H1299)
0.04, 0.15, 0.62, 2.5, 10 μM (MDA-MB-231; 48 h)
Incubation Time:

72 h (MDA-MB-231, H3122, H1299)
48 h (MDA-MB-231)
Result:

Induced concentration-dependent PRMT1 degradation in MDA-MB-231 cells, with marked reduction at submicromolar concentrations.
Induced detectable PRMT1 degradation in H3122 and H1299 cells at 10 μM.
Caused concentration-dependent inhibition of H4R3me2a and global ADMA in MDA-MB-231 cells over 48 h.

Cell Proliferation Assay^[1]

Cell Line:

human breast cancer MCF-7 and MDA-MB-231 cells
Concentration:

10 μM
Incubation Time:

0, 2, 4, 6, 8, 10 days
Result:

Visually inhibited colony formation of both cell lines in a time-dependent manner.
Exhibited potent antiproliferative effects as measured by reduced cell confluence over time.

Western Blot Analysis^[1]

Cell Line:

human breast cancer MCF-7 and MDA-MB-231 cells
Concentration:

0.625, 1.25, 2.5, 5, 10 μM
Incubation Time:

72 h
Result:

Downregulated TR3 protein levels in a concentration-dependent manner in both cell lines, mirroring its effect on PRMT1 levels.

Parmacokinetics

Species	Dose	Route	AUC_0-last	C_max	T_max	T_1/2
Mice^[1]	60 mg/kg	i.p.	8732 ng·h/mL	6937 ng/mL	0.667 h	1.72 h

In Vivo

CM112 (compound 12) (60 mg/kg; i.p.; single dose) exhibits favorable in vivo pharmacokinetic properties in male BALB/c mice, with rapid absorption, high maximum exposure, and good tolerability following a single intraperitoneal dose of 60 mg/kg^[1].

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

Chemical Information

분자량 711.93
화학식 C₃₉H₆₁N₅O₇
SMILES

O=C(CCOCCOCCOCCOCCOCCNC(CC12C[C@@H](C[C@H]3C2)C[C@@H](C3)C1)=O)NC4=CC=C(C5=CNC=C5CN(CCN)C)C=C4
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 (276 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]. Ma C, et al. Discovery of a first-in-class protein arginine methyltransferase 1 (PRMT1) degrader for nonenzymatic functions studies. European journal of medicinal chemistry. 2025 Jul 05;291:117625. [Content Brief]

Calculators

몰농도 계산기

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

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Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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Other size

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Amount: USD 0.00

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
순도&문서
References

상품명:
Cat. No.:
수량:
MCE Japan Authorized Agent:

상품명:
CAS No.:
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Purity:
수량:

CM112

All Histone Methyltransferase Isoforms

Biological Activity

Chemical Information

순도&문서

References

Calculators

Help & FAQs

CM112 Related Classifications

HY-172769 Related Classifications

Bioz