1. Epigenetics Cell Cycle/DNA Damage Apoptosis
  2. Small Interfering RNA (siRNA) HDAC Apoptosis
  3. HDAC/PSMD14-IN-1

HDAC/PSMD14-IN-1 is a thiolutin derivative. HDAC/PSMD14-IN-1 is a orally active dual-target inhibitor of PSMD14/HDAC1 (IC50 238.7 nM/141.2 nM, respectively). HDAC/PSMD14-IN-1 has good cytotoxicity against ESCC cell lines (IC50: 30-250 nM) and effectively reverses epithelial-mesenchymal transition (EMT). HDAC/PSMD14-IN-1 can induce apoptosis. HDAC/PSMD14-IN-1 has anti-tumor activity in a KYSE30 cell mouse xenograft model. HDAC/PSMD14-IN-1 can be used in anti-esophageal cancer research.

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

HDAC/PSMD14-IN-1 Chemical Structure

HDAC/PSMD14-IN-1 Chemical Structure

CAS No. : 3062141-62-9

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Description

HDAC/PSMD14-IN-1 is a thiolutin derivative. HDAC/PSMD14-IN-1 is a orally active dual-target inhibitor of PSMD14/HDAC1 (IC50 238.7 nM/141.2 nM, respectively). HDAC/PSMD14-IN-1 has good cytotoxicity against ESCC cell lines (IC50: 30-250 nM) and effectively reverses epithelial-mesenchymal transition (EMT). HDAC/PSMD14-IN-1 can induce apoptosis. HDAC/PSMD14-IN-1 has anti-tumor activity in a KYSE30 cell mouse xenograft model. HDAC/PSMD14-IN-1 can be used in anti-esophageal cancer research[1].

IC50 & Target[1]

HDAC1

141.2 nM (IC50)

Parmacokinetics[1]
Species Dose Route Indicator value
Mice 1.6 mg/kg i.v. CL 7.3417 mL/min/kg
Mice 3 mg/kg p.o. AUC0-∞ 5.199 μg·h/mL
Mice 1.6 mg/kg i.v. T1/2 6.65 hr
Mice 3 mg/kg p.o. AUC0-t 5.138 μg·h/mL
Mice 1.6 mg/kg i.v. Cmax 3486.7 ng/mL
Mice 3 mg/kg p.o. T1/2 3.63 hr
Mice 1.6 mg/kg i.v. AUC0-∞ 3.6375 μg·h/mL
Mice 3 mg/kg p.o. Cmax 1085.0 ng/mL
Mice 1.6 mg/kg i.v. AUC0-t 3.5712 μg·h/mL
Mice 3 mg/kg p.o. Tmax 0.670 hr
Mice 1.6 mg/kg i.v. Tmax 0.0833 hr
Molecular Weight

432.56

Formula

C20H24N4O3S2

CAS No.
SMILES

O=C(CCCCCCC(NC1=C2C(N(C)C1=O)=CSS2)=O)NC3=CC=CC=C3N

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Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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  • 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.

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HDAC/PSMD14-IN-1
Cat. No.:
HY-172878
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