3-Deazaneplanocin A HCl

3-Deazaneplanocin A HCl is a synthetically derived inhibitor of the histone methyltransferase (EZH2) and S-adenosylhomocysteine hydrolase (SAHH). By regulating epigenetic methylation pathways, 3-deazaneplanocin A induces apoptosis and inhibits tumor cell proliferation, demonstrating significant antitumor activity in various tumor models. 3-deazaneplanocin A HCl can be used in research on epigenetic regulation, tumorigenesis and progression, and stem cell differentiation.

Methods: 3-Deazaneplanocin A HCl (0.25–2.0 μM) was added to OCI-AML3 and HL-60 cells and treated for 24, 48, or 72 hours. Annexin V/PI double staining flow cytometry and Western blot analysis for PARP cleavage were performed.
Results: 3-Deazaneplanocin A HCl induced apoptosis in a dose-dependent manner, with OCI-AML3 being more sensitive than HL-60. [1]
Methods: Tumor spheroids formed by PANC-1, MIA-PaCa-2, and LPC006 cells (cultured in serum-free stem cell medium for 10–14 days) were treated with 3-Deazaneplanocin A HCl (5 μM) for 72 hours. Tumor spheroid volume was measured microscopically; CD133 mRNA was detected by RT-qPCR.
Results: 3-Deazaneplanocin A HCl significantly reduced tumor spheroid volume. [2]
Methods: Rat primary HSCs; JS1 cells; LX-2 cells were treated with 3-Deazaneplanocin A HCl (1 μM) for 48–96 hours. Western Blot analyzed EZH2, H3K27me2/3, α-SMA, COL1A; CCK-8 assayed cell viability; flow cytometry assessed cell cycle and apoptosis; SA-β-Gal assay for senescence; TUNEL assay for apoptosis.
Results: 3-Deazaneplanocin A HCl treatment maintained HSCs in a more quiescent state, reduced EZH2, H3K27me2/3, α-SMA, and COL1A expression levels, leading to cell cycle arrest at S and G2 phases, decreased viability, increased senescence, and enhanced early apoptosis.[3]

Methods: NOD/SCID mice were injected with 5×10⁶ HL-60 cells via the tail vein to establish an AML model. Drug administration commenced on day 7 post-cell injection (control group: solvent; 3-Deazaneplanocin A HCl monotherapy group: 1 mg/kg, intraperitoneal injection, twice weekly for 2 weeks). Mouse survival times were recorded and Kaplan-Meier survival curves were plotted.
Results: The median survival time in the 3-Deazaneplanocin A HCl-treated group (43 days) was significantly longer than that in the control group (36 days). [1]
Methods: To investigate the therapeutic effect of 3-Deazaneplanocin A HCl in liver fibrosis, BALB/c mice were used. Hepatic fibrosis was induced by intraperitoneal injection of CCl₄ (for 4 weeks), concurrently with intraperitoneal injection of 3-Deazaneplanocin A HCl (1 mg/kg) twice weekly; The control group received DMSO injections for 4 weeks.
Results: 3-Deazaneplanocin A HCl significantly reduced hepatic levels of EZH2, H3K27me3, α-SMA, Col1a1, and Mmp2, markedly decreased collagen deposition and α-SMA-positive areas, and significantly lowered serum ALT and AST levels. [3]
Methods: Rats implanted with microdialysis probes in the nucleus accumbens (monoamine/adenosine) received intraperitoneal injections of 3-Deazaneplanocin A HCl (0.1, 1.0, 10 mg/kg) during the light phase. Dialysate was collected for 4 hours post-administration, and dopamine (DA), norepinephrine (NE), epinephrine (EP), serotonin (5-HT), adenosine (AD), and acetylcholine (ACh) were quantified by high-performance liquid chromatography (HPLC).
Results: 3-Deazaneplanocin A HCl significantly increased extracellular levels of all neurochemicals in a dose-dependent manner. [4]
Methods: Female SD rats were established with bone cancer pain by intraosseous injection of Walker 256 breast cancer cells (approximately 1×10⁵ cells/10 μL) into the tibial bone marrow cavity. 3-Deazaneplanocin A HCl (5 nM, 20 nM, 40 nM) was administered via intrathecal injection on days 3–5 post-injection, with observation of pain threshold (PWT) and spontaneous activity.
Results: 5 nM was ineffective; 40 nM increased spontaneous activity (potentially a side effect); 20 nM was both effective and safe.[5]

H2O: 50 mg/mL (167.38 mM), Sonication is recommended.

DMSO: 150 mg/mL (502.13 mM), Sonication is recommended.