Santacruzamate A (CAY10683) (Synonyms: Santacruzamate A) |
| Catalog No.GC14439 |
Santacruzamate A (CAY10683), a natural carbamate derivative, inhibits HDAC2 and HDAC6 with IC50 values of 0.119 and 434nM, respectively.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1477949-42-0
Sample solution is provided at 25 µL, 10mM.
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Santacruzamate A (CAY10683), a natural carbamate derivative, inhibits HDAC2 and HDAC6 with IC50 values of 0.119 and 434nM, respectively [1]. Santacruzamate A exhibits immunomodulatory and cell proliferation inhibitory activities and modulates the synaptic function in neurons by inhibiting microglial activation[2]. Santacruzamate A has been widely used in the development of a series of related derivatives aimed at inhibiting HDAC isoenzymes[3].
In vitro, Santacruzamate A treatment for 24 hours significantly inhibited the viability of NCM460 cells, with an IC50 value of 315.7nM[4]. Santacruzamate A treatment at 50µM for 6 hours inhibited the invasion and migration of NUCKS1-overexpressing colorectal cancer (CRC) cells, reduced the expression of HDAC2 protein without affecting the expression of NUCKS1 protein[5]. Treatment with 10µM Santacruzamate A for 24 hours significantly inhibited the cell viability of BV2 microglial cells, suppressed the expression of HDAC2 and increased the acetylation level of histone H3, accompanied by a decrease in the expression of IL-1β and TNF-α[6].
In vivo, Santacruzamate, administered via intraperitoneal injection (2mg/kg every other day) for 6 weeks, resulted in an increase in the expression of GLT-1, p-GluN2B and p-GluA1 in the hippocampal tissue of the mouse model of subarachnoid hemorrhage (SAH), alleviating the depressive symptoms of the SAH mice[7]. Intravenous injection of Santacruzamate A (3mg/kg) every three days for 35 days inhibited the distant metastasis of the tumor in the xenograft mouse model of SW620 cells[8].
References:
[1] Pavlik C M, Wong C Y B, Ononye S, et al. Santacruzamate A, a potent and selective histone deacetylase inhibitor from the Panamanian marine cyanobacterium cf. Symploca sp[J]. Journal of natural products, 2013, 76(11): 2026-2033.
[2] Zhou H, Cai Y, Liu D, et al. Pharmacological or transcriptional inhibition of both HDAC 1 and 2 leads to cell cycle blockage and apoptosis via p21Waf1/Cip1 and p19INK4d upregulation in hepatocellular carcinoma[J]. Cell proliferation, 2018, 51(3): e12447.
[3] Randino R, Gazzerro P, Mazitschek R, et al. Synthesis and biological evaluation of Santacruzamate-A based analogues[J]. Bioorganic & Medicinal Chemistry, 2017, 25(24): 6486-6491.
[4] Wang Y, Chen H, Chen Q, et al. The protective mechanism of CAY10683 on intestinal mucosal barrier in acute liver failure through LPS/TLR4/MyD88 pathway[J]. Mediators of Inflammation, 2018, 2018(1): 7859601.
[5]Zhu L, Zhao T, Su H, et al. NUCKS1 promotes invasion and metastasis of colorectal cancer by stabilizing HDAC2 and activating AKT[J]. Oncogenesis, 2025, 14(1): 19.
[6] Jiao F Z, Wang Y, Zhang H Y, et al. Histone deacetylase 2 inhibitor CAY10683 alleviates lipopolysaccharide induced neuroinflammation through attenuating TLR4/NF-κB signaling pathway[J]. Neurochemical research, 2018, 43(6): 1161-1170.
[7] Tao K, Cai Q, Zhang X, et al. Astrocytic histone deacetylase 2 facilitates delayed depression and memory impairment after subarachnoid hemorrhage by negatively regulating glutamate transporter-1[J]. Annals of Translational Medicine, 2020, 8(11): 691.
[8] Zheng Y, Dai M, Dong Y, et al. ZEB2/TWIST1/PRMT5/NuRD multicomplex contributes to the epigenetic regulation of EMT and metastasis in colorectal carcinoma[J]. Cancers, 2022, 14(14): 3426.
| Cell experiment [1]: | |
Cell lines | BV2 microglial cells |
Preparation Method | BV2 microglial cells were cultured in DMEM medium supplemented with heat-inactivated 10% fetal bovine serum and 100U penicillin/100g streptomycin. The cells were grown in a humidified incubator at 37°C with 95% air and 5% CO2. The cells (1×104 cells per well) were seeded in 96-well microtiter plates and treated with Santacruzamate A (0.01, 0.1, 1, 10 and 100µM) for 24 hours. Then, 10µL of CCK-8 dye was added to each well and the plates were incubated at 37°C for 2 hours. The absorbance of each well was measured at 450nm wavelength. |
Reaction Conditions | 0.01, 0.1, 1, 10 and 100µM; 24h |
Applications | Santacruzamate A treatment significantly inhibited viability of BV2 microglial cells ≥10µM. |
| Animal experiment [2]: | |
Animal models | C57BL/6 mice |
Preparation Method | Eighty-six adult C57BL/6 mice (body weight: 20.0-25.0g) were housed under a temperature of 25.0 ± 3.0°C and with a 12:12 light-dark cycle. Anesthesia with 2% isoflurane was administered to mice. A midline incision was made in the neck to expose the left carotid bifurcation. The external carotid artery was ligated and separated, and a 6-0 sharp-ended monofilament was inserted into the internal carotid artery. The monofilament was inserted 10-12mm to the bifurcation of the anterior cerebral artery and the middle cerebral artery, and then 3mm further inward for puncture. The line was left in place for 20 seconds to establish the intravascular perforation model of subarachnoid hemorrhage (SAH) in mice. Two weeks after the surgery, SAH mice were intraperitoneally injected with Santacruzamate A (2mg/kg) every other day for 6 weeks. The expressions of GLT-1, HDAC2, p-GluN2B and p-GluA1 in the hippocampal tissue of mice were detected. |
Dosage form | 2mg/kg every other day for 6 weeks; i.p. |
Applications | Santacruzamate A treatment led to an increase in the expression of GLT-1, p-GluN2B and p-GluA1 in the hippocampal tissue of mice, and the expression of HDAC2 decreased. |
References: | |
| Cas No. | 1477949-42-0 | SDF | |
| Synonyms | Santacruzamate A | ||
| Chemical Name | ethyl N-[4-oxo-4-(2-phenylethylamino)butyl]carbamate | ||
| Canonical SMILES | CCOC(=O)NCCCC(=O)NCCC1=CC=CC=C1 | ||
| Formula | C15H22N2O3 | M.Wt | 278.35 |
| Solubility | ≥ 8.8mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.5926 mL | 17.963 mL | 35.926 mL |
| 5 mM | 718.5 μL | 3.5926 mL | 7.1852 mL |
| 10 mM | 359.3 μL | 1.7963 mL | 3.5926 mL |
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- Purity: >99.00%
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Average Rating: 5 (Based on Reviews and 36 reference(s) in Google Scholar.)
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