2. Epigenetics GPCR/G Protein
  3. Histone Methyltransferase GLP Receptor
  4. Antitumor agent-101

Antitumor agent-101 is a selective covalent inhibitor of lysine methyltransferases G9a/GLP, with IC50s of 8.5 nM and 5.5 nM for G9a and GLP, respectively. Antitumor agent-101 shows antitumor efficacy in the PANC-1 xenograft model.

For research use only. We do not sell to patients.

Antitumor agent-101 Chemical Structure

Antitumor agent-101 Chemical Structure

CAS No. : 2848632-52-8

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  
Synthetic products have potential research and development risk.

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Antitumor agent-101 Related Antibodies

Top Publications Citing Use of Products

View All Histone Methyltransferase Isoform Specific Products:

View All Isoforms

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Antitumor agent-101 is a selective covalent inhibitor of lysine methyltransferases G9a/GLP, with IC50s of 8.5 nM and 5.5 nM for G9a and GLP, respectively. Antitumor agent-101 shows antitumor efficacy in the PANC-1 xenograft model[1].

IC50 & Target[1]

G9a

8.5 nM (IC50)

GLP

5.5 nM (IC50)

In Vitro

Antitumor agent-101 (Compound 27) ( 0-5 μM; 48 hours) significantly exhibits proliferation and colony formation of PANC-1 and MDA-MB-231 cells with IC50s of 2.68 and 2.88 μM, respectively[1].
Antitumor agent-101 (0-10 μM; 0-96 hours) effectively reduces H3K9me2 in PANC-1 and MDA-MB-231 cells in a concentration- and time-dependent manner[1].

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

Antitumor agent-101 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: PANC-1 and MDA-MB-231 cells
Concentration: 0, 1.25, 2.5, 5 μM
Incubation Time: 48 hours
Result: Ihibited proliferation of PANC-1 and MDA-MB-231 cells with IC50s of 2.68 and 2.88 μM, respectively.
Significantly suppressed the colony formation in MDA-MB-231 and PANC-1 cell lines at 2.5 μM.

Western Blot Analysis[1]

Cell Line: PANC-1 and MDA-MB-231 cells
Concentration: 2.5, 5, 10 μM
Incubation Time: 4, 48, 72, or 96 hours
Result: Effectively reduced H3K9me2 in PANC-1 and MDA-MB-231 cells in a concentration- and time-dependent manner.
Still significantly inhibited the levels of H3K9me2 in the cells treated with compound 27 were still significantly inhibited within 24h after Antitumor agent-101 was washed out, and the levels of H3K9me2 were recovered after 48h.
In Vivo

Antitumor agent-101 (Compound 27) (2 mg/kg for i.p., 5 days a week) suppresses PANC-1 xenograft tumor growth by inhibiting the methyltransferase activity of G9a/GLP[1].
Antitumor agent-101 (2 mg/kg for p.o.) shows a Cmax of 316 ng/mL, and mean residence time (MRT) of 0.61 hour[1].

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

Animal Model: PANC-1 xenograft tumor models in male Balb/c nu/nu mice[1]
Dosage: 2 mg/kg
Administration: Intraperitoneal injection (i.p.), 5 days a week (5 days on and 2 days off).
Result: Exhibited potent antitumor activity with a tumor growth inhibition (TGI) rate of 52.2% with no obvious toxicity.
Showed lower levels of H3K9me2 than the vehicle group.
Animal Model: Male ICR Mice (Pharmacokinetic assay)[1]
Dosage: 2 mg/kg
Administration: Intraperitoneal injection (i.p.)
Result: Pharmacokinetic parameters for antitumor agent-101 (Compound 27) in rats [1]
Route Dose (mg/kg) Cmax (ng/mL) AUC0-t (h•ng/mL) AUC0-Ꝏ (h•ng/mL) MRT (h)
i.p. 2 316 208 214 0.61
Molecular Weight

482.62

Formula

C26H38N6O3
CAS No.
SMILES

COC1=CC2=C(N=C(N(C)C(C=C)=O)N=C2NC3CCN(C)CC3)C=C1OCCCN4CCCC4
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
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

Antitumor agent-101 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
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:

Antitumor agent-1012848632-52-8Antitumor agent101Antitumor agent 101Histone MethyltransferaseGLP ReceptorProtein lysine methyltransferasesG9aGLPPANC-1 xenograft modeMDA-MB-231 cellsInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Antitumor agent-101
Cat. No.:
HY-155020
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

Request for HNMR Report

We have received your request and will respond to you as soon as possible.