- Shanghai Jizhi Biochemical Technology Co., Ltd
- China
- Product Name: ACY-738
- Price: ￥1066.0/10mg ￥3196.0/50mg ￥4796.0/100mg ￥706.0/5mg
- Purity: 98.0%
- Stocking Period: 2 Day
- Contact: Liu jia
- DC Chemicals Limited
- China
- Product Name: ACY-738
- Price: $550.0/100mg $1000.0/250mg $1900.0/1g
- Purity: 98.0%
- Stocking Period: 3 Day
- Contact: Tony Cao
1375465-91-0
1375465-91-0 structure
- Name: ACY-738
- Chemical Name: N-Hydroxy-2-[(1-phenylcyclopropyl)amino]-5-pyrimidinecarboxamide
- CAS Number: 1375465-91-0
- Molecular Formula: C14H14N4O2
- Molecular Weight: 270.287
- Catalog: Research Areas Cancer
- Create Date: 2018-12-17 17:43:05
- Modify Date: 2024-01-02 11:25:17
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ACY-738 is a potent, selective and orally-bioavailable HDAC6 inhibitor, with an IC50s of 1.7 nM; ACY-738 also inhibits HDAC1, HDAC2, and HDAC3, with IC50s of 94, 128, and 218 nM.
| Name | N-Hydroxy-2-[(1-phenylcyclopropyl)amino]-5-pyrimidinecarboxamide |
|---|---|
| Synonyms |
N-Hydroxy-2-[(1-phenylcyclopropyl)amino]-5-pyrimidinecarboxamide
5-Pyrimidinecarboxamide, N-hydroxy-2-[(1-phenylcyclopropyl)amino]- ACY-738 |
| Description | ACY-738 is a potent, selective and orally-bioavailable HDAC6 inhibitor, with an IC50s of 1.7 nM; ACY-738 also inhibits HDAC1, HDAC2, and HDAC3, with IC50s of 94, 128, and 218 nM. |
|---|---|
| Related Catalog | |
| Target |
HDAC6:1.7 nM (IC50) HDAC1:94 nM (IC50) HDAC2:128 nM (IC50) HDAC3:218 nM (IC50) |
| In Vitro | ACY-738 (2.5 μM) increases the acetylated (lysine 40) fraction of α-tubulin in RN46A-B14 cells[1]. ACY-738 (10 μM) induces cell death comparable to LBH589 and FK228[3]. |
| In Vivo | ACY-738 (5 mg/kg) leads to significant increase in α-tubulin acetylation in whole-brain lysates. ACY-738 (50 mg/kg) fails to produce an enhancement of locomotor activity in WT mice tested in a home cage environment[1]. ACY-738 (5 mg/kg) reaches a maximum plasma concentration of 1310 ng/mL at 0.0830 h following treatment. ACY-738 (5 mg/kg BW) alters BM B cell differentiation, but shows no significant effect on IgG and C3 deposition in NZB/W mice. ACY-738 (20 mg/kg) significantly attenuates the severity of proteinuria in NZB/W F1 mice. ACY-738 (5 mg/kg) shows a significant decrease in anti-dsDNA production in NZB/W mice as they aged. ACY-738 (5, 20 mg/kg) attenuates sera IL-1β production as the NZB/W mice aged. ACY-738 (5 mg/kg) significantly reduces glomerular IL-6 and IL-10 mRNA levels by more than 50% while treatment with 20 mg/kg ACY-738 reduced IL-6 and IL-10 mRNA to non-detectable levels[2]. |
| Animal Admin | Mice are injected i.p. 5 days/week with the vehicle control (DMSO), ACY-738 treatment at 5 mg/kg (low-dose), or ACY-738 treatment at 20 mg/kg (high-dose) beginning at 22-weeks-of-age until euthanasia at 38 weeks-of-age. The total volume injected is 80 μL. Proteinuria and weight are measured every 2 weeks and blood is collected every four weeks for sera analysis. Proteinuria is measured by a standard semi-quantitative test using Siemens Uristix dipsticks. Results are quantified and scored as follows: dipstick reading of 0 mg/dL = 0, trace = 1, 30-100 mg/dL = 2, 100-300 mg/dL = 3, 300-2000 mg/dL = 4, and 2000 + mg/dL = 5[2]. |
| References |
| Density | 1.4±0.1 g/cm3 |
|---|---|
| Molecular Formula | C14H14N4O2 |
| Molecular Weight | 270.287 |
| Exact Mass | 270.111664 |
| LogP | 0.24 |
| Index of Refraction | 1.715 |
| Storage condition | -20℃ |