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.

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Antitumor agent-101 Chemical Structure

Antitumor agent-101 Chemical Structure

CAS No. : 2848632-52-8

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Antitumor agent-101 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

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
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Antitumor agent-101 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:

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

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