2. Epigenetics Apoptosis
  3. Histone Methyltransferase Apoptosis
  4. F5446

F5446 (Compound 1) is a selective small molecule inhibitor of SUV39H1 methyltransferase. F5446 decreases H3K9me3 deposition at the FAS promoter, increases Fas expression and increases colorectal carcinoma cell sensitivity to FasL-induced apoptosis in vitro. F5446 suppresses human colon tumor xenograft growth in vivo.

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F5446 Chemical Structure

F5446 Chemical Structure

CAS No. : 2304465-89-0

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

F5446 Related Antibodies

Top Publications Citing Use of Products

View All Histone Methyltransferase Isoform Specific Products:

View All Isoforms
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

F5446 (Compound 1) is a selective small molecule inhibitor of SUV39H1 methyltransferase. F5446 decreases H3K9me3 deposition at the FAS promoter, increases Fas expression and increases colorectal carcinoma cell sensitivity to FasL-induced apoptosis in vitro. F5446 suppresses human colon tumor xenograft growth in vivo[1][2][3].

In Vitro

F5446 (0-1 μM, 2 days) has an EC50 of 4.96x10-7 M against recombinant human SUV39H1 and induces apoptotic cell death in the SW620 and LS411N cells[1].
F5446 (0-250 nM, 3 days) up-regulates tumor cell surface Fas expression and increases FasL- induced apoptosis in SW620 and LS411N cells[1][2].
F5446 (100 or 250 nM, 48 h) inhibits SUV39H1 expression and induces human colon tumor cell cycle arrest and apoptosis[2].

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

F5446 Related Antibodies

Apoptosis Analysis[1]

Cell Line: SW620 and LS411N cells
Concentration: 0-1 μM
Incubation Time: 2 days
Result: Showed the percentage of apoptotic cell death for the SW620 and LS411N cells at various concentrations.

Apoptosis Analysis[2]

Cell Line: SW620 and LS411N cells
Concentration: 100 or 250 nM
Incubation Time: 48 h
Result: Induced cell cycle arrest at the S phase in a concentration-dependent manner in both SW620 and LS411N cells.
In Vivo

IF5446 (10 mg/kg, s.c.,every two days for 14 days) inhibits SUV39H1 and colon tumor growth at least in part through inhibiting H3K9me3 to increase the expression part through inhibiting H3K9me3 to increase the expression level of granzyme B , perforin , Fasl and IFNy in tumor-infiltrating CTLs in the tumor microenvironment in mice bearing MC38 and CT26 tumor[1][2].
IF5446 (10 and 20 mg/kg, s.c.,every two days for 14 days) increases T-cell effector expression to suppress colon carcinoma growth[3].

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

Animal Model: Mice bearing MC38 and CT26 tumor[1][2][3]
Dosage: 10 mg/kg
Administration: s.c.,every two days for 14 days
Result: Suppressed the tumor growth in a time-dependent manner and significantly increased the expression levels of granzymeB, perforin, FasL and IFNγ.
Molecular Weight

552.94

Formula

C26H17ClN2O8S
CAS No.
Appearance

Solid

Color

Orange to reddish brown

SMILES

O=C(C1=CC(C2=C(C3=O)NC=C2C(OCC4=CC=CC=C4)=O)=C(N1S(=O)(C5=CC=C(C=C5)Cl)=O)C3=O)OC
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (180.85 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8085 mL 9.0426 mL 18.0851 mL
5 mM 0.3617 mL 1.8085 mL 3.6170 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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In Vivo:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  15% Cremophor EL    85% Saline

    Solubility: 2 mg/mL (3.62 mM); Suspended solution; Need ultrasonic

  • Protocol 2

    Add each solvent one by one:  10% Cremophor EL in PBS

    Solubility: 1.82 mg/mL (3.29 mM); Suspended solution; Need ultrasonic and warming and heat to 60°C

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8085 mL 9.0426 mL 18.0851 mL 45.2129 mL
5 mM 0.3617 mL 1.8085 mL 3.6170 mL 9.0426 mL
10 mM 0.1809 mL 0.9043 mL 1.8085 mL 4.5213 mL
15 mM 0.1206 mL 0.6028 mL 1.2057 mL 3.0142 mL
20 mM 0.0904 mL 0.4521 mL 0.9043 mL 2.2606 mL
25 mM 0.0723 mL 0.3617 mL 0.7234 mL 1.8085 mL
30 mM 0.0603 mL 0.3014 mL 0.6028 mL 1.5071 mL
40 mM 0.0452 mL 0.2261 mL 0.4521 mL 1.1303 mL
50 mM 0.0362 mL 0.1809 mL 0.3617 mL 0.9043 mL
60 mM 0.0301 mL 0.1507 mL 0.3014 mL 0.7535 mL
80 mM 0.0226 mL 0.1130 mL 0.2261 mL 0.5652 mL
100 mM 0.0181 mL 0.0904 mL 0.1809 mL 0.4521 mL
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F5446 Related Classifications

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:

F54462304465-89-0F 5446F-5446Histone MethyltransferaseApoptosisSUV39H1H3K9me3 depositionFascolorectal carcinoma cellapoptosiscolon tumorInhibitorinhibitorinhibit

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