1. Cell Cycle/DNA Damage
    Epigenetics
    Apoptosis
  2. HDAC
    Apoptosis
  3. GEM144

GEM144 

Cat. No.: HY-143411
Handling Instructions

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.

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

GEM144 Chemical Structure

GEM144 Chemical Structure

CAS No. : 2487526-28-1

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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].

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

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].

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.
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Storage

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GEM144
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