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HDAC Inhibitors
You are here: Product Lines > DNA Regulation / Transcription > Histones & Histone Modification > Histone Deacetylases [HDACs] / Related Products > HDAC Inhibitors
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ALX-350-095 Revised 03-Apr-08
Apicidin
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SYNONYMS cyclo-L-(2-Amino-8-oxodecanoyl)-L-(N-methoxy-tryptophan)-L-isoleucyl-D-pipecolinyl
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Other Natural Products - DNA Regulation / Transcription
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ALX-350-095-M001   1 mg 50.00 USD Add To Cart
ALX-350-095-M005   5 mg 200.00 USD Add To Cart
Product Specification
FORMULA: C34H49N5O6
MW: 623.8
CAS NUMBER: 183506-66-3
SOURCE/HOST: Isolated from Fusarium sp.
PURITY: ≥95% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: VERY TOXIC.

Product Description
Potent inhibitor of histone deacetylase (HDAC). Inhibits proliferation. Induces cell cycle arrest. Stimulates apoptosis of cancer cells. Antiprotozoal.
Product Specific Literature References
Apicidin: a novel antiprotozoal agent that inhibits parasite histone deacetylase: S.J. Darkin-Rattray, et al.; PNAS 93, 13143 (1996) Abstract
Apicidin, a histone deacetylase inhibitor, inhibits proliferation of tumor cells via induction of p21WAF1/Cip1 and gelsolin: J.W. Han, et al.; Cancer Res. 60, 6068 (2000) Abstract
Transcriptional activation of p21(WAF1/CIP1) by apicidin, a novel histone deacetylase inhibitor: J.S. Kim, et al.; BBRC 281, 866 (2001) Abstract
Broad spectrum antiprotozoal agents that inhibit histone deacetylase: structure-activity relationships of apicidin. Part 1: S.L. Colletti, et al.; Bioorg. Med. Chem. Lett. 11, 107 (2001) Abstract
Broad spectrum antiprotozoal agents that inhibit histone deacetylase: structure-activity relationships of apicidin. Part 2: S.L. Colletti, et al.; Bioorg. Med. Chem. Lett. 11, 113 (2001) Abstract
Structure and chemistry of apicidins, a class of novel cyclic tetrapeptides without a terminal alpha-keto epoxide as inhibitors of histone deacetylase with potent antiprotozoal activities: S.B. Singh, et al.; J. Org. Chem. 67, 815 (2002) Abstract
Apicidin, a histone deacetylase inhibitor, induces differentiation of HL-60 cells: J. Hong, et al.; Cancer Lett. 189, 197 (2003) Abstract
Activation of NF-kappaB by HDAC inhibitor apicidin through Sp1-dependent de novo protein synthesis: its implication for resistance to apoptosis: Y.K. Kim, et al.; Cell Death Differ. 13, 2033 (2006) Abstract
Apicidin, a novel histone deacetylase inhibitor, has profound anti-growth activity in human endometrial and ovarian cancer cells: T. Ueda, et al.; Int. J. Mol. Med. 19, 301 (2007) Abstract
Further Categories Containing This Product:
Cell Cycle Blockers & Inhibitors / Related Products • HDAC Inhibitors • Natural Products for Cell Cycle Research • Natural Products - Other Anti-infective Agents • Parasitic Diseases Other Products • Natural Products - Apoptosis Inducers & Inhibitors
 
 
ALX-630-102 Revised 05-Apr-08
HC Toxin
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SYNONYMS Cyclo-(D-Pro-L-Ala-D-Ala-L-2-amino-8-oxo-9,10-epoxydecanoic acid)
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Other Toxins
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ALX-630-102-M001   1 mg 195.00 USD Add To Cart
Product Specification
FORMULA: C21H32N4O6
MW: 436.5
CAS NUMBER: 83209-65-8
SOURCE/HOST: Isolated from Helminthosporium carbonium.
PURITY: ≥98%
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Stable as supplied for up to 1 year. Stock solutions are stable for up to 3 months when stored at -20°C
HAZARD: TOXIC.

Product Description
Potent, cell permeable, non-competitive and reversible inhibitor of histone deacetylase (HDAC) (IC50=30nM). Does not inhibit histone acetyltransferases. Induces expression of γ-globulin in erythroid cells. Shows anti-mitogenic activities. Induces cell cycle arrest and apoptosis in tumor cells.
Product Specific Literature References
The structure and conformation of HC-toxin: M. Kawai, et al.; Biochem. Biophys. Res. Commun. 111, 398 (1983) Abstract
Inhibition of maize histone deacetylases by HC toxin, the host-selective toxin of Cochliobolus carbonum: G. Brosch, et al.; Plant Cell 7, 1941 (1995) Abstract
Estrogen receptor enhances the antiproliferative effects of trichostatin A and HC-toxin in human breast cancer cells: K.N. Min, et al.; Arch. Pharm. Res. 27, 554 (2004) Abstract
Antiproliferative effect of trichostatin A and HC-toxin in T47D human breast cancer cells: K.E. Joung, et al.; Arch. Pharm. Res. 27, 640 (2004) Abstract
Further Categories Containing This Product:
HDAC Inhibitors • Natural Products - Apoptosis Inducers & Inhibitors • Cell Cycle Blockers & Inhibitors / Related Products • Natural Products for Cell Cycle Research
 
 
ALX-270-297 Revised 06-Dec-04
M344
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SYNONYMS 4-Dimethylamino-N-(6-hydroxycarbamoylhexyl)-benzamide
PRODUCT LINE DNA Regulation / Transcription
PRODUCT CATEGORY HDAC Inhibitors
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ALX-270-297-M001   1 mg 95.00 USD Add To Cart
ALX-270-297-M005   5 mg 390.00 USD Add To Cart
Product Specification
FORMULA: C16H25N3O3
MW: 307.4
CAS NUMBER: 251456-60-7
PURITY: ≥98%
APPEARANCE: White crystalline solid.
SOLUBILITY: Soluble in DMSO (1mg/ml)
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light.

Product Description
Potent inhibitor of histone deacetylase (HDAC) (IC50≤1µM).
Product Specific Literature References
Amide analogues of trichostatin A as inhibitors of histone deacetylase and inducers of terminal cell differentiation: M. Jung, et al.; J. Med. Chem. 42, 4669 (1999) Abstract
 
 
ALX-270-344 Revised 05-Feb-05
MC 1293
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SYNONYMS 3-(4-Toluoyl-1-methyl-1H-2-pyrrolyl)-N-hydroxy-2-propenamide
PRODUCT LINE DNA Regulation / Transcription
PRODUCT CATEGORY HDAC Inhibitors
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ALX-270-344-M005   5 mg 150.00 USD Add To Cart
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Product Specification
FORMULA: C16H16N2O3
MW: 284.3
APPEARANCE: Off-white powder.
SOLUBILITY: Soluble in DMSO.
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Inhibitor of histone deacetylase 1 (HDAC1) (IC50 = 4.5µM) [2] and maize histone deacetylase HD2 (IC50=1.9µM) [1].
Product Specific Literature References
[1] 3-(4-aroyl-1H-pyrrol-2-yl)-N-hydroxy-2-propenamides, a new class of synthetic histone deacetylase inhibitors: S. Massa, et al.; J. Med. Chem. 44, 2069 (2001) Abstract
[2] Binding mode analysis of 3-(4-benzoyl-1-methyl-1H-2-pyrrolyl)-N-hydroxy-2-propenamide: a new synthetic histone deacetylase inhibitor inducing histone hyperacetylation, growth inhibition, and terminal cell differentiation: A. Mai, et al.; J. Med. Chem. 45, 1778 (2002) Abstract
 
 
ALX-270-378 Revised 07-May-08
MS-275
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SYNONYMS N-(2-Aminophenyl)-4-[N-(pyridine-3-ylmethoxy-carbonyl)aminomethyl]benzamide
PRODUCT LINE DNA Regulation / Transcription
PRODUCT CATEGORY HDAC Inhibitors
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ALX-270-378-M001   1 mg Inquire
ALX-270-378-M005   5 mg Inquire
ALX-270-378-M025   25 mg Inquire
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Product Specification
FORMULA: C21H20N4O3
MW: 376.4
CAS NUMBER: 209783-80-2
PURITY: ≥95% (1H-NMR)
APPEARANCE: Off-white to tan solid.
SOLUBILITY: Soluble in DMSO or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light. Packaged under inert gas.
HAZARD: IRRITANT.

Product Description
Preferentially inhibits HDAC1 (IC50=300nM) over HDAC3 (IC50=8µM). Has no inhibitory activity towards HDAC8 (IC50>100µM).
Product Specific Literature References
A synthetic inhibitor of histone deacetylase, MS-27-275, with marked in vivo antitumor activity against human tumors: A. Saito, et al.; PNAS 96, 4592 (1999) Abstract; Full Text
MS-275, a histone deacetylase inhibitor, selectively induces transforming growth factor beta type II receptor expression in human breast cancer cells: B.I. Lee, et al.; Cancer Res. 61, 931 (2001) Abstract; Full Text
MS-27-275, an inhibitor of histone deacetylase, has marked in vitro and in vivo antitumor activity against pediatric solid tumors: J. Jaboin, et al.; Cancer Res. 62, 6108 (2002) Abstract; Full Text
Transcriptional regulation of the transforming growth factor beta type II receptor gene by histone acetyltransferase and deacetylase is mediated by NF-Y in human breast cancer cells: S.H. Park, et al.; J. Biol. Chem. 277, 5168 (2002) Abstract; Full Text
Identification of novel isoform-selective inhibitors within class I histone deacetylases: E. Hu, et al.; Pharmacol Exp. Ther. 307, 720 (2003) Abstract
The histone deacetylase inhibitor MS-275 promotes differentiation or apoptosis in human leukemia cells through a process regulated by generation of reactive oxygen species and induction of p21CIP1/WAF1 1: R.R. Rosato, et al.; Cancer Res. 63, 3637 (2003) Abstract
Gene expression profiling of multiple histone deacetylase (HDAC) inhibitors: defining a common gene set produced by HDAC inhibition in T24 and MDA carcinoma cell lines: K.B. Glaser, et al.; Mol. Cancer Ther. 2, 151 (2003) Abstract
Enhanced radiation-induced cell killing and prolongation of gammaH2AX foci expression by the histone deacetylase inhibitor MS-275: K. Camphausen, et al.; Cancer Res. 64, 316 (2004) Abstract
 
 
ALX-270-379 Revised 04-Mar-05
Oxamflatin
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SYNONYMS (2E)-5-[3-(Phenylsulfonylamino)phenyl]pent-2-en-4-ynohydroxamic acid
PRODUCT LINE Cancer
PRODUCT CATEGORY Antitumor Agents (Apoptosis Inducers)
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ALX-270-379-M001   1 mg 70.00 USD Add To Cart
ALX-270-379-M005   5 mg 275.00 USD Add To Cart
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Product Specification
FORMULA: C17H14N2O4S
MW: 342.4
PURITY: ≥95% (HPLC)
APPEARANCE: Solid.
SOLUBILITY: Soluble in DMSO, methanol or acetonitrile.
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: +4°C
HANDLING: After reconstitution, prepare aliquots and store at -20°C. Packaged under inert gas. Protect from light.

Product Description
Potent inhibitor of mammalian HDAC (IC50=15.7nM). Acts as a ligand for the enzyme active site metal ion. Upregulates plasminogen activator inhibitor type 2 (PAI-2) expression with concomitant inhibition of urokinase (u-PA) gene and protein expression in HT-1080 and U-937 cells. Elevates the expression of extracellular matrix proteins fibronectin and gelsolin. Induces apoptosis in P-glyoprotein (Pgp) positive and Pgp negative multidrug resistant cells.
Product Specific Literature References
Oxamflatin: a novel compound which reverses malignant phenotype to normal one via induction of JunD: H. Sonoda, et al.; Oncogene 13, 143 (1996) Abstract
Oxamflatin is a novel antitumor compound that inhibits mammalian histone deacetylase: Y.B. Kim, et al.; Oncogene 18, 2461 (1999) Abstract
The novel anti-tumour agent oxamflatin differentially regulates urokinase and plasminogen activator inhibitor type 2 expression and inhibits urokinase-mediated proteolytic activity: A.E. Dear & R.L. Medcalf; Biochim. Biophys. Acta 1492, 15 (2000) Abstract
Novel mechanisms of apoptosis induced by histone deacetylase inhibitors: M.J. Peart, et al.; Cancer Res. 63, 4460 (2003) Abstract
Further Categories Containing This Product:
HDAC Inhibitors • Antitumor Agents (DNA Interaction & Gene Regulation) • Antitumor Agents (Enzyme Inhibitors)
 
 
ALX-270-298 Revised 14-Nov-07
Scriptaid
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SYNONYMS 6-(1,3-Dioxo-1H,3H-benzo[de]isoquinolin-2-yl)-N-hydroxyhexanamide
PRODUCT LINE DNA Regulation / Transcription
PRODUCT CATEGORY HDAC Inhibitors
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ALX-270-298-M001   1 mg 33.00 USD Add To Cart
ALX-270-298-M005   5 mg 93.00 USD Add To Cart
Product Specification
FORMULA: C18H18N2O4
MW: 326.4
PURITY: ≥95%
APPEARANCE: Yellow solid.
SOLUBILITY: Soluble in DMSO (1mg/ml) or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light.

Product Description
Inhibitor of histone deacetylase (HDAC) (HDAC1 and 3: IC50~0.6µM; HDAC8: IC50~1µM) with lower toxicity than trichostatin A (Prod. No. ALX-380-068). Inhibits tumor growth in vitro and in vivo and, in conjunction with 5-aza-2’-deoxycytidine (Prod. No. ALX-480-096), enhances expression of estrogen receptor α.
Product Specific Literature References
A novel histone deacetylase inhibitor identified by high-throughput transcriptional screening of a compound library: G.H. Su, et al.; Cancer Res. 60, 3137 (2000) Abstract; Full Text
Identification of novel isoform-selective inhibitors within class I histone deacetylases: E. Hu, et al.; J. Pharmacol. Exp. Ther. 307, 720 (2003) Abstract
A novel histone deacetylase inhibitor, scriptaid, enhances expression of functional estrogen receptor alpha (ER) in ER negative human breast cancer cells in combination with 5-aza 2'-deoxycytidine: J.C. Keen, et al.; Breast Cancer Res. Treat. 81, 177 (2003) Abstract
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ALX-270-301 Revised 04-Apr-07
Sodium butyrate
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PRODUCT LINE DNA Regulation / Transcription
PRODUCT CATEGORY HDAC Inhibitors
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ALX-270-301-G001   1 g 105.00 USD Add To Cart
Product Specification
FORMULA: C4H7O2Na
MW: 110.1
CAS NUMBER: 156-54-7
RTECS: ET6400000
PURITY: ≥99%
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Hygroscopic.
HAZARD: IRRITANT. MAY BE MUTAGENIC.

Product Description
Short-chain fatty acid shown to be an inhibitor of histone deacetylase (HDAC). Induces apoptosis.
Product Specific Literature References
Sodium butyrate inhibits histone deacetylation in cultured cells: E.P. Candido, et al.; Cell 14, 105 (1978) Abstract
Induction of the differentiated phenotype in human colon cancer cell is associated with the attenuation of subcellular tyrosine phosphorylation: B. Schwartz, et al.; Oncol. Res. 7, 277 (1995) Abstract
Apoptosis induced by the histone deacetylase inhibitor sodium butyrate in human leukemic lymphoblasts: D. Bernhard, et al.; FASEB J. 13, 1991 (1999) Abstract
Sodium Butyrate Induces Transcription from the Galpha i2 Gene Promoter through Multiple Sp1 Sites in the Promoter and by Activating the MEK- ERK Signal Transduction Pathway: J. Yang, et al.; J. Biol. Chem. 276, 25742 (2001) Abstract; Full Text
Reduction of telomerase activity in human liver cancer cells by a histone deacetylase inhibitor: M. Nakamura, et al.; J. Cell Physiol. 187, 392 (2001) Abstract
Effects of retinoic acid and sodium butyrate on gene expression, histone acetylation and inhibition of proliferation of melanoma cells: K. Demary, et al.; Cancer Lett. 163, 103 (2001) Abstract
Further Categories Containing This Product:
Apoptosis Inducers & Inhibitors Other Products
 
 
ALX-270-303 Revised 13-Apr-06
Sodium 4-phenylbutyrate
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SYNONYMS SPB
4-Phenylbutyric acid
4PBA
PBNa
PRODUCT LINE DNA Regulation / Transcription
PRODUCT CATEGORY HDAC Inhibitors
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ALX-270-303-M100   100 mg 35.00 USD Add To Cart
Product Specification
FORMULA: C10H11O2Na
MW: 186.2
CAS NUMBER: 1716-12-7
PURITY: ≥98%
APPEARANCE: White to yellowish solid.
SOLUBILITY: Soluble in DMSO or water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Hygroscopic.
Product Description
Inhibitor of histone deacetylase (HDAC). Anti-neoplastic agent and transcriptional regulator. Also acts as an inducer of tumor cytostasis and differentiation. Shows chemical chaperone activity.
Product Specific Literature References
Discordant effects of butyrate analogues on erythroleukemia cell proliferation, differentiation and histone deacetylase: M.A. Lea & N. Tulsyan; Anticancer Res. 15, 879 (1995) Abstract
Therapeutic targeting of transcription in acute promyelocytic leukemia by use of an inhibitor of histone deacetylase: R.P. Warrell, Jr., et al.; J. Natl. Cancer Inst. 90, 1621 (1998) Abstract
Modifying histones to tame cancer: clinical development of sodium phenylbutyrate and other histone deacetylase inhibitors: S.D. Gore & M.A. Carducci; Expert Opin. Investig. Drugs 9, 2923 (2000), (Review) Abstract
Butyrate as a model for "gene-regulating chemoprevention and chemotherapy.": Y. Sowa & T. Sakai; Biofactors 12, 283 (2000) Abstract
Further Categories Containing This Product:
Antitumor Agents (Anti-proliferative)
 
 
ALX-270-380 Revised 09-Dec-04
Splitomicin
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SYNONYMS Splitomycin
1,2-Dihydro-3H-naphtho[2,1-b]pyran-3-one