2. Cell Cycle/DNA Damage Epigenetics Apoptosis
  3. HDAC Apoptosis DNA/RNA Synthesis
  4. GEM144

GEM144 is a potent and orally active DNA polymerase α (POLA1) and HDAC 11 dual inhibitor. GEM144 induces acetylation of p53, activation of p21, G1/S cell cycle arrest, and apoptosis. GEM144 has significant antitumor activity in human orthotopic malignant pleural mesothelioma xenografts.

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GEM144 Chemical Structure

GEM144 Chemical Structure

CAS No. : 2487526-28-1

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GEM144 Related Antibodies

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Description

GEM144 is a potent and orally active DNA polymerase α (POLA1) and HDAC 11 dual inhibitor. GEM144 induces acetylation of p53, activation of p21, G1/S cell cycle arrest, and apoptosis. GEM144 has significant antitumor activity in human orthotopic malignant pleural mesothelioma xenografts[1].

IC50 & Target

HDAC11

8.23 μM (IC50)

In Vitro

GEM144 (0-10 μM; 24 hours) exhibits antiproliferative activity in tested cancer cell lines with IC50s of 0.26 ~ 2.2 μM[1].
GEM144 (0.1 - 0.4 μM; 24 hours) strongly increases levels of H2AX phosphorylation on Ser 39 (γH2AX), and strongly upregulates p21 expression in a dose-dependent manner[1].
GEM144 (0.26 μM in NCI-H4609, 0.95 μM in A2780 and 1.4 μM in MM473; 72 hours) induced G1/S cell cycle arrest[1].

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

GEM144 Related Antibodies

Cell Proliferation Assay

Cell Line: NCI-H460, H460-R9A, A2780 and A2780-DX[1]
Concentration: 0-10 μM
Incubation Time: 24 hours (further 48 h growth in drug-free medium)
Result: Exhibited antiproliferative activity in tested cancer cell lines with IC50s of 0.26 ~ 2.2 μM.

Western Blot Analysis

Cell Line: NCI-H460[1]
Concentration: 0.1 μM, 0.25 μM and 0.4 μM
Incubation Time: 24 hours
Result: Strongly increased levels of H2AX phosphorylation on Ser 39 (γH2AX), and strongly upregulated p21 expression in a dose-dependent manner.

Cell Cycle Analysis

Cell Line: NCI-H4609, A2780 and MM473[1]
Concentration: 0.26 μM in NCI-H4609, 0.95 μM in A2780 and 1.4 μM in MM473
Incubation Time: 72 hours
Result: Induced G1/S cell cycle arrest.
In Vivo

GEM144 (50 mg/kg; p.o., bid, 5 days a week, for 3-4 weeks) significantly reduces tumor burden of MM487 with TGI of 72% in xenografts mice[1].

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

Animal Model: Female CD-1 nude mice (injected with MM473 and MM487)[1]
Dosage: 50 mg/kg
Administration: PO, bid, 5 days a week, for 3-4 weeks
Result: Significantly reduced tumor burden of MM487 with TGI of 72%.
Molecular Weight

461.55

Formula

C28H31NO5
CAS No.
SMILES

ONC(C(C)OC1=C(C=C(C2=CC=C(C=C2)/C=C/C(O)=O)C=C1)C34CC5CC(CC(C5)C4)C3)=O
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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GEM144 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:

GEM1442487526-28-1GEM 144GEM-144HDACApoptosisDNA/RNA SynthesisHistone deacetylasesPOLA1HDAC 11p53AntitumorMM473MM487CD-1 nude miceInhibitorinhibitorinhibit

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