2. Epigenetics Apoptosis
  3. Histone Methyltransferase Apoptosis
  4. CARM1-IN-4

CARM1-IN-4 (compound 11f) is a potent CARM1 inhibitor with IC50s of 9 nM and 56 nM for CARM1 and PRMT1, respectively. CARM1-IN-4 displays significant anti-proliferative effects on colorectal cancer cell lines. CARM1-IN-4 effectively inhibits the methyltransferase activity of CARM1 and prevents methylation of downstream proteins. CARM1-IN-4 induces apoptosis and shows antitumor activity.

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CARM1-IN-4 Chemical Structure

CARM1-IN-4 Chemical Structure

CAS No. : 2878481-07-1

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CARM1-IN-4 Related Antibodies

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

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Description

CARM1-IN-4 (compound 11f) is a potent CARM1 inhibitor with IC50s of 9 nM and 56 nM for CARM1 and PRMT1, respectively. CARM1-IN-4 displays significant anti-proliferative effects on colorectal cancer cell lines. CARM1-IN-4 effectively inhibits the methyltransferase activity of CARM1 and prevents methylation of downstream proteins. CARM1-IN-4 induces apoptosis and shows antitumor activity[1].

IC50 & Target[1]

CARM1

9 nM (IC50)

PRMT1

56 nM (IC50)

PRMT6

30 nM (IC50)

PRMT8

31 nM (IC50)

PRMT3

2637 nM (IC50)

PRMT5

>100,000 nM (IC50)

In Vitro

CARM1-IN-4 (compound 11f) exhibits significant anti-proliferative activity in the HCT116 cell lines (IC50=3.13 μM)[1].
CARM1-IN-4 (0.625-5 μM; 72 h) causes a dose-dependent induction of apoptosis in HCT116 cell[1].
CARM1-IN-4 (0.625-10 μM; 48 h) effectively inhibits the methyltransferase activity of CARM1, influencing the levels of asymmetric demethylation on CARM1 substrates within a cellular environment[1].
CARM1-IN-4 exhibits a relatively high mitochondrial stability, with an extended half-life in mouse mitochondria (T1/2=217 min)[1].

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

CARM1-IN-4 Related Antibodies

Apoptosis Analysis[1]

Cell Line: HCT116 cells
Concentration: 0.625, 1.25, 2.5, 5 μM
Incubation Time: 72 h
Result: Illustrated a noticeable increase in the overall percentages of both early and late apoptotic cells.

Western Blot Analysis[1]

Cell Line: HCT116 cells
Concentration: 0.625, 1.25, 2.5, 5, 10 μM
Incubation Time: 48 h
Result: Caused dose-dependent reductions in global asymmetric dimethylarginine (aDMA) and asymmetric dimethyl-PABP1 levels in HCT116 cells.
In Vivo

CARM1-IN-4 (compound 11f; 10, 25 mg/kg/day; ip; for 12 days) shows evident inhibitory effect in BALB/c nude mice bearing subcutaneous HCT116 xenograft[1].

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

Animal Model: 6 to 8-week-old female BALB/c nude mice bearing subcutaneous HCT116 xenograft[1]
Dosage: 10, 25 mg/kg
Administration: Intraperitoneal injection; daily; for 12 days
Result: Showed evident inhibitory effect.
Molecular Weight

422.60

Formula

C24H42N2O4
CAS No.
SMILES

CN(C[C@@H](O)CNC)CC1=CC=CC=C1OC2CCC(COCC)(COCC)CC2
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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CARM1-IN-4 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:

CARM1-IN-42878481-07-1Histone MethyltransferaseApoptosisCARM1PRMT1anti-proliferativecolorectal cancermethyltransferasemethylationantitumorInhibitorinhibitorinhibit

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