ACY-775 | CAS#1375466-18-4 | HDAC6 inhibitor

ACY-775
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 206493

CAS#: 1375466-18-4

Description: ACY-775 is a potent and selective HDAC6 inhbiitor. ACY-775 inhibits HDAC6 with low nanomolar potency and a selectivity of 60- to 1500-fold over class I HDACs. ACY-775 shares the antidepressant-like properties of other HDAC inhibitors, such as SAHA and MS-275, in the tail suspension test and social defeat paradigm.

Chemical Structure

ACY-775

CAS# 1375466-18-4

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 206493
Name: ACY-775
CAS#: 1375466-18-4
Chemical Formula: C17H19FN4O2
Exact Mass: 330.15
Molecular Weight: 330.360
Elemental Analysis: C, 61.81; H, 5.80; F, 5.75; N, 16.96; O, 9.69

Price and Availability

Size	Price	Availability
10mg	USD 75	Ready to ship
25mg	USD 150	Ready to ship
50mg	USD 250	Ready to ship
100mg	USD 450	Ready to ship
200mg	USD 750	Ready to ship
500mg	USD 1650	Ready to ship
1g	USD 2650	2 Weeks
2g	USD 4650	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Synonym: ACY-775; ACY 775; ACY775.

IUPAC/Chemical Name: 2-((1-(3-Fluorophenyl)cyclohexyl)amino)-N-hydroxypyrimidine-5-carboxamide

InChi Key: IYBURCQQEUNLDL-UHFFFAOYSA-N

InChi Code: InChI=1S/C17H19FN4O2/c18-14-6-4-5-13(9-14)17(7-2-1-3-8-17)21-16-19-10-12(11-20-16)15(23)22-24/h4-6,9-11,24H,1-3,7-8H2,(H,22,23)(H,19,20,21)

SMILES Code: O=C(C1=CN=C(NC2(C3=CC=CC(F)=C3)CCCCC2)N=C1)NO

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Product Data:

Product Data

Certificate of Analysis:

View CoA: current batch, Lot#S7S09C05

QC Data:

View QC data: current batch, Lot#S7S09C05

Safety Data Sheet (SDS):

View Safety Data Sheet (SDS)

Instruction:

View handling instruction

Biological target:	ACY-775 is an inhibitor of the of histone deacetylase 6 (HDAC6) with an IC50 of 7.5 nM.
In vitro activity:	The HDAC6 inhibitors, ACY-738 and ACY-775, hyperacetylated α-tubulin at a concentration of 1 μM. The histone acetylation was not affected (Fig. 1a–c). Immunocytochemistry was used to visualize the acetylation of α-tubulin, which is present in the cytoplasm, and of histone 3, visible in the nucleus. In vehicle-treated cells, α-tubulin was mainly present in the deacetylated form, while histone 3 was clearly acetylated (Fig. 1a, d). Upon treatment with ACY-738 and ACY-775, a clear enhancement of the acetylation of α-tubulin was visible, while histone acetylation remained unaltered (Fig. 1f–g). Reference: Neurotherapeutics. 2017 Apr; 14(2): 417–428. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5398982/
In vivo activity:	When ACY-775 (50 mg/kg) was administered repeatedly in wild-type mice at 24 h, 4 h, and 30 min before killing, significant increases in α-tubulin acetylation were observed in all tested brain regions (Figure 2c): cortex, F2, 7=582.5, P<0.0001; hippocampus, F2, 7=260.4, P<0.0001; DRN, F2, 7=54.00, P<0.0001; and cerebellum, F2, 7=136.2, P<0.0001. In contrast, an identical treatment regimen in KO mice did not produce increases in α-tubulin acetylation over baseline levels (Figure 2c). Reference: Neuropsychopharmacology. 2014 Jan; 39(2): 389–400. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3870780/

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	35.3	106.94
	DMF	20.0	60.54
	DMF:PBS (pH 7.2) (1:4)	0.2	0.61
	Ethanol	34.5	104.43

Preparing Stock Solutions

The following data is based on the product molecular weight 330.36 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:	1. Benoy V, Vanden Berghe P, Jarpe M, Van Damme P, Robberecht W, Van Den Bosch L. Development of Improved HDAC6 Inhibitors as Pharmacological Therapy for Axonal Charcot-Marie-Tooth Disease. Neurotherapeutics. 2017 Apr;14(2):417-428. doi: 10.1007/s13311-016-0501-z. PMID: 27957719; PMCID: PMC5398982. 2. Jochems J, Boulden J, Lee BG, Blendy JA, Jarpe M, Mazitschek R, Van Duzer JH, Jones S, Berton O. Antidepressant-like properties of novel HDAC6-selective inhibitors with improved brain bioavailability. Neuropsychopharmacology. 2014 Jan;39(2):389-400. doi: 10.1038/npp.2013.207. Epub 2013 Aug 19. PMID: 23954848; PMCID: PMC3870780.
In vitro protocol:	1. Benoy V, Vanden Berghe P, Jarpe M, Van Damme P, Robberecht W, Van Den Bosch L. Development of Improved HDAC6 Inhibitors as Pharmacological Therapy for Axonal Charcot-Marie-Tooth Disease. Neurotherapeutics. 2017 Apr;14(2):417-428. doi: 10.1007/s13311-016-0501-z. PMID: 27957719; PMCID: PMC5398982. 2. Jochems J, Boulden J, Lee BG, Blendy JA, Jarpe M, Mazitschek R, Van Duzer JH, Jones S, Berton O. Antidepressant-like properties of novel HDAC6-selective inhibitors with improved brain bioavailability. Neuropsychopharmacology. 2014 Jan;39(2):389-400. doi: 10.1038/npp.2013.207. Epub 2013 Aug 19. PMID: 23954848; PMCID: PMC3870780.
In vivo protocol:	1. Benoy V, Vanden Berghe P, Jarpe M, Van Damme P, Robberecht W, Van Den Bosch L. Development of Improved HDAC6 Inhibitors as Pharmacological Therapy for Axonal Charcot-Marie-Tooth Disease. Neurotherapeutics. 2017 Apr;14(2):417-428. doi: 10.1007/s13311-016-0501-z. PMID: 27957719; PMCID: PMC5398982. 2. Jochems J, Boulden J, Lee BG, Blendy JA, Jarpe M, Mazitschek R, Van Duzer JH, Jones S, Berton O. Antidepressant-like properties of novel HDAC6-selective inhibitors with improved brain bioavailability. Neuropsychopharmacology. 2014 Jan;39(2):389-400. doi: 10.1038/npp.2013.207. Epub 2013 Aug 19. PMID: 23954848; PMCID: PMC3870780.

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1: Jochems J, Boulden J, Lee BG, Blendy JA, Jarpe M, Mazitschek R, Van Duzer JH, Jones S, Berton O. Antidepressant-like properties of novel HDAC6-selective inhibitors with improved brain bioavailability. Neuropsychopharmacology. 2014 Jan;39(2):389-400. doi: 10.1038/npp.2013.207. Epub 2013 Aug 19. PMID: 23954848; PMCID: PMC3870780.

2: Benoy V, Vanden Berghe P, Jarpe M, Van Damme P, Robberecht W, Van Den Bosch L. Development of Improved HDAC6 Inhibitors as Pharmacological Therapy for Axonal Charcot-Marie-Tooth Disease. Neurotherapeutics. 2017 Apr;14(2):417-428. doi: 10.1007/s13311-016-0501-z. PMID: 27957719; PMCID: PMC5398982.

3: Tago T, Toyohara J, Ishii K. Preclinical Evaluation of an 18F-Labeled SW-100 Derivative for PET Imaging of Histone Deacetylase 6 in the Brain. ACS Chem Neurosci. 2021 Feb 17;12(4):746-755. doi: 10.1021/acschemneuro.0c00774. Epub 2021 Jan 27. PMID: 33502174.

4: Celen S, Rokka J, Gilbert TM, Koole M, Vermeulen I, Serdons K, Schroeder FA, Wagner FF, Bleeser T, Hightower BG, Hu J, Rahal D, Beyzavi H, Vanduffel W, Van Laere K, Kranz JE, Hooker JM, Bormans G, Cawthorne CJ. Translation of HDAC6 PET Imaging Using [18F]EKZ-001-cGMP Production and Measurement of HDAC6 Target Occupancy in Nonhuman Primates. ACS Chem Neurosci. 2020 Apr 1;11(7):1093-1101. doi: 10.1021/acschemneuro.0c00074. Epub 2020 Mar 19. PMID: 32159328; PMCID: PMC7205522.

5: Mithraprabhu S, Khong T, Jones SS, Spencer A. Histone deacetylase (HDAC) inhibitors as single agents induce multiple myeloma cell death principally through the inhibition of class I HDAC. Br J Haematol. 2013 Aug;162(4):559-62. doi: 10.1111/bjh.12388. Epub 2013 May 21. PMID: 23692150.

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