Chemical Structure : GCJ-490A
CAS No.:
2194550-21-3
GCJ-490A
(GCJ490A)
Catalog No.: PC-25846Not For Human Use, Lab Use Only.
GCJ-490A is a pan-histone deacetylase (HDAC) inhibitor that exerts potent inhibitory activity against HDAC1, HDAC3, and HDAC6 with IC50 of 3.64, 3.02 and 4.96 nM respectively.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
GCJ-490A is a pan-histone deacetylase (HDAC) inhibitor that exerts potent inhibitory activity against HDAC1, HDAC3, and HDAC6 with IC50 of 3.64, 3.02 and 4.96 nM respectively.
GCJ-490A also inhibits HDAC2 (IC50=13.26 nM), HDAC8 (IC50=16.84 nM), HDAC10 (IC50=1.98 nM)and HDAC11 (IC50=77.82 nM), dos not inhibit HDAC4/5/7/9 and SIRT1/2/3.
GCJ-490A shows potent antiproliferative activity against NCI-N87 and T47D cells with IC50 values of 28 and 40 nM, respectively.
GCJ-490A (50 mg/kg) showsgood efficacy in solid tumors such as the HT-29 model, also directly decrease the incidence of colitis-associated cancer.
GCJ-490A effectively inhibits NSCLC cell proliferation, including gefitinib resistant A549, H460, HCC827/GR6, and H1975 (IC50=20-180 nM), induces apoptosis in vitro and in vivo.
GCJ-490A suppresses c-Met expression through IKKα and overcomes gefitinib resistance in NSCLC.
Physicochemical Properties
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M.Wt
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490.60
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Formula
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C25H22N4O3S2
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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(S)-5-Cyclopropyl-N-(1-(4-(hydroxycarbamoyl)phenyl)ethyl)-5'-phenyl-[2,2'-bithiazole]-4-carboxamide
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References
1. He T, et al. Cancer Biol Med. 2022 Feb 22;19(8):1172-92.
2. Zhang WX, et al. Acta Pharmacol Sin. 2025 Oct 1. doi: 10.1038/s41401-025-01646-z.
3. hang SW, et al. J Med Chem. 2020;63:804–15.
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