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Chemical Structure| 17328-16-4 Chemical Structure| 17328-16-4

Structure of TC-E 5003
CAS No.: 17328-16-4

Chemical Structure| 17328-16-4

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TC-E 5003 is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor.

Synonyms: NSC 30176

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Product Details of TC-E 5003

CAS No. :17328-16-4
Formula : C16H14Cl2N2O4S
M.W : 401.26
SMILES Code : O=S(C1=CC=C(NC(CCl)=O)C=C1)(C2=CC=C(NC(CCl)=O)C=C2)=O
Synonyms :
NSC 30176
MDL No. :MFCD00028183
InChI Key :SHRCVZJKZJGIHQ-UHFFFAOYSA-N
Pubchem ID :87052

Safety of TC-E 5003

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P280-P301+P312-P302+P352-P305+P351+P338

Related Pathways of TC-E 5003

epigenetics

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
RAW264.7 cells 0-1 µM 15 min TC-E inhibited c-Jun transcription in RAW264.7 cells after LPS treatment Int J Mol Sci. 2020 Apr 26;21(9):3058.
RAW264.7 cells 0-1 µM 15-30 min TC-E decreased p-c-Jun levels but did not affect phosphorylated MAPKs Int J Mol Sci. 2020 Apr 26;21(9):3058.
RAW264.7 cells 0-1 µM 15-60 min TC-E suppressed the nuclear translocation of NF-κB subunits p65 and p50 and AP-1 transcriptional factor c-Jun Int J Mol Sci. 2020 Apr 26;21(9):3058.
HEK293T cells 0-1 µM 24 hours TC-E did not alter Src phosphorylation in Src-overexpressing HEK293T cells Int J Mol Sci. 2020 Apr 26;21(9):3058.
RAW264.7 cells 0-1 µM 24 hours TC-E significantly reduced LPS-induced NO production without cytotoxicity Int J Mol Sci. 2020 Apr 26;21(9):3058.
RAW264.7 cells 0-1 µM 2-5 min TC-E inhibited Src phosphorylation after 2 min of LPS treatment but not Syk Int J Mol Sci. 2020 Apr 26;21(9):3058.
MDA-MB-231 0.5965 µM (IC50) 48 hours Evaluate the anti-tumor effect of TC-E-5003 on MDA-MB-231 cells, IC50 was 0.5965 μM. Drug Deliv. 2020 Dec;27(1):491-501.
MCF-7 0.4128 µM (IC50) 48 hours Evaluate the anti-tumor effect of TC-E-5003 on MCF-7 cells, IC50 was 0.4128 μM. Drug Deliv. 2020 Dec;27(1):491-501.
NCL-H1299 0.6844 µM (IC50) 48 hours Evaluate the anti-tumor effect of TC-E-5003 on NCL-H1299 cells, IC50 was 0.6844 μM. Drug Deliv. 2020 Dec;27(1):491-501.
A549 0.7022 µM (IC50) 48 hours Evaluate the anti-tumor effect of TC-E-5003 on A549 cells, IC50 was 0.7022 μM. Drug Deliv. 2020 Dec;27(1):491-501.
RAW264.7 cells 0-1 µM 5 min TC-E significantly downregulated IκBα phosphorylation after 5 min of LPS treatment Int J Mol Sci. 2020 Apr 26;21(9):3058.
RAW264.7 cells 0-1 µM 6 hours TC-E downregulated the expression of inflammatory genes (iNOS, COX-2, TNF-α, IL-6) Int J Mol Sci. 2020 Apr 26;21(9):3058.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
ICR mice A549 cell xenograft model Subcutaneous injection 0.5 mg Single dose, lasting 28 days Evaluate the anti-tumor effect of TC-E-5003-INEI in A549 xenograft model, tumor inhibition efficiency was 68.23%. Drug Deliv. 2020 Dec;27(1):491-501.

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.49mL

0.50mL

0.25mL

12.46mL

2.49mL

1.25mL

24.92mL

4.98mL

2.49mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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