ALEXIS Biochemicals: Isobavachalcone

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ALX-105-011

Revised 18-Sep-06

S-Trityl-L-cysteine
SYNONYMS	NSC 83265
PRODUCT LINE	Cell Cycle
PRODUCT CATEGORY	Cell Cycle Blockers & Inhibitors / Related Products

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-105-011-M100		100 mg	20.00 USD
ALX-105-011-M500		500 mg	60.00 USD

Product Specification

FORMULA:	C₂₂H₂₁NO₂S
MW:	363.5
CAS NUMBER:	2799-07-7
RTECS:	AY7710000
APPEARANCE:	White to off-white solid.
SOLUBILITY:	Soluble in DMSO or acetic acid
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
HAZARD:	HARMFUL.

Product Description

Potent, cell permeable cysteine thioether displaying anti-mitotic and anti-tumor properties. Inhibits mitosis by blocking basal and microtubule-activated ATPase activities of the mitotic kinesin Eg5 (IC₅₀=1µM and 140nm). Induces mitotic arrest in HeLa cells (IC₅₀=700nM) and inhibits the growth of NCI tumor cell line panel (GI₅₀=1.31µM).

Product Specific Literature References

In vitro screening for inhibitors of the human mitotic kinesin Eg5 with antimitotic and antitumor activities: S. DeBonis, et al.; Mol. Cancer Ther. 3, 1079 (2004) Abstract; Full Text
S-trityl-l-cysteine is a reversible, tight-binding inhibitor of the human kinesin eg5 that specifically blocks mitotic progression: D.A. Skoufias, et al.; J. Biol. Chem. 281, 17559 (2006) Abstract; Full Text

Further Categories Containing This Product:

Kinesin & Kinesin-like Proteins / Related Products • Antitumor Agents (Anti-proliferative)

ALX-270-253

Revised 18-Mar-08

Rosmarinic acid
SYNONYMS	(R)-α-[[3-(3,4-Dihydroxyphenyl)-1-oxo-2E-propenyl]oxy]-3,4-dihydroxy-benzenepropanoic acid
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Natural Products - Antioxidants

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-253-M010		10 mg	20.00 USD
ALX-270-253-M050		50 mg	80.00 USD

Product Specification

FORMULA:	C₁₈H₁₆O₈
MW:	360.3
CAS NUMBER:	537-15-5, 20283-92-5
SOURCE/HOST:	Isolated from Rosmarinus officinalis.
PURITY:	≥98% (HPLC)
APPEARANCE:	White to brown solid.
SOLUBILITY:	Soluble in 100% ethanol, DMSO or dimethyl formamide; also soluble in PBS.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	+20°C

Product Description

Naturally occurring polyphenolic compound with antioxidant and anti-inflammatory properties. Anticarcinogenic. Inhibitor of lipid peroxidation, TCR-induced T cell activation and proliferation.

Product Specific Literature References

Modification of endotoxin-induced haemodynamic and haematological changes in the rabbit by methylprednisolone, F(ab')2 fragments and rosmarinic acid: H. Bult, et al.; Br. J. Pharmacol. 84, 317 (1985) Abstract
Complement-dependent stimulation of prostacyclin biosynthesis: inhibition by rosmarinic acid: M. Rampart, et al.; Biochem. Pharmacol. 35, 1397 (1986) Abstract
Studies on the activities of tannins and related compounds, X. Effects of caffeetannins and related compounds on arachidonate metabolism in human polymorphonuclear leukocytes: Y. Kimura, et al.; J. Nat. Prod. 50, 392 (1987) Abstract
Protective action of seven natural phenolic compounds against peroxidative damage to biomembranes: G.T. Liu, et al.; Biochem. Pharmacol. 43, 147 (1992) Abstract
Metabolism of rosmarinic acid in rats: T. Nakazawa & K. Ohsawa; J. Nat. Prod. 61, 993 (1998) Abstract
Rosmarinic acid inhibits TCR-induced T cell activation and proliferation in an Lck-dependent manner: J. Won, et al.; Eur. J. Immunol. 33, 870 (2003) Abstract
Rosmarinic acid inhibits Ca2+-dependent pathways of T-cell antigen receptor-mediated signaling by inhibiting the PLC-gamma 1 and Itk activity: M.A. Kang, et al.; Blood 101, 3534 (2003) Abstract
Rosmarinic acid inhibits epidermal inflammatory responses: anticarcinogenic effect of Perilla frutescens extract in the murine two-stage skin model: N. Osakabe, et al.; Carcinogenesis 25, 549 (2004) Abstract
Effects of rosmarinic acid against aflatoxin B1 and ochratoxin-A-induced cell damage in a human hepatoma cell line (Hep G2): C. Renzulli, et al.; J. Appl. Toxicol. 24, 289 (2004) Abstract
Rosmarinic acid inhibits angiogenesis and its mechanism of action in vitro: S.S. Huang & R.L. Zheng; Cancer Lett. 239, 271 (2006) Abstract

Further Categories Containing This Product:

T Cell Regulation Other Products • Lipid Peroxidation • Active Substances from Fruit and Vegetables • Natural Products - Anti-inflammatory Agents • Polyphenols Other Products • Antitumor Agents (Anti-proliferative) • Natural Products - Antitumor Reagents

ALX-270-303

Revised 13-Apr-06

Sodium 4-phenylbutyrate
SYNONYMS	SPB 4-Phenylbutyric acid 4PBA PBNa
PRODUCT LINE	DNA Regulation / Transcription
PRODUCT CATEGORY	HDAC Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-303-M100		100 mg	35.00 USD

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-270-346

Revised 28-May-08

Ratjadone A (synthetic)
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Antibiotics for Cell Cycle Research

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-346-C002		2 µg	150.00 USD

Product Specification

FORMULA:	C₂₈H₄₀O₅
MW:	456.6
CAS NUMBER:	163564-92-9
SOURCE/HOST:	Synthetic.
PURITY:	≥95%
FORMULATION:	Liquid. Solution in methanol.
SOLUBILITY:	Soluble in methanol (20mg/ml) or aqueous buffers (<100µM).
SHIPPING:	SHIPPED ON DRY ICE
LONG TERM STORAGE:	-20°C
USE/STABILITY:	Sensitive to acids and bases. Unstable in acidic buffer systems (pH<6). Stable in substance as oil and in solution in methanol at -20°C.
HANDLING:	Protect from light.
HAZARD:	TOXIC.

Product Description

Represents a new class of natural compounds, which inhibit proliferation in eukaryotes by blocking nuclear export. As potent as leptomycin B (Prod. No. ALX-380-100) and specific for G1/S checkpoint. Cytotoxic secondary metabolite (IC₅₀=50pg/ml in mouse cell line L929) that arrests tumor cells in the G1 phase at remarkably low concentrations (50pg/ml in HeLa cell line KB3.1). Inhibits the binding between the nuclear export signal (NES) of proteins and the chromosome maintenance region protein (CRM1). Anticancer compound. Belongs to the family of orphan ligands which include polyketides like leptomycin B, callystatin A and other related compounds.

Product Specific Literature References

Antibiotics from gliding bacteria, LXIII. Ratjadone: a new antifungal metabolite from Sorangium cellulosum: D. Schummer, et al.; Liebigs Ann. 685 (1995)
Ratjadon: a new antifungal compound from Sorangium cellulosum (myxobacteria) production, physio-chemical and biological properties: J. Gerth, et al.; J. Antibiot. 48, 973 (1995) Abstract
The chemistry and biology of ratjadone: M. Kalesse, et al.; ChemBioChem. 9, 709 (2001) Abstract
The chemistry and biology of the leptomycin family: M. Kalesse & M. Christmann; Synthesis 8, 981 (2002) Abstract
Ratjadone and leptomycin B block CRM1-dependent nuclear export by identical mechanisms: T. Meissner, et al.; FEBS Lett. 576, 27 (2004)
Nuclear targeting of adenovirus type 2 requires CRM1-mediated nuclear export: S. Strunze, et al.; Mol. Biol. Cell 16, 2999 (2005) Abstract

Further Categories Containing This Product:

Antitumor Antibiotics • Antibiotics - Antifungal • Cell Cycle Blockers & Inhibitors / Related Products • Nuclear Envelope & Nuclear Transport • Antitumor Agents (Anti-proliferative)

ALX-270-369

Revised 28-May-08

Ratjadone C (native)
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Antibiotics for Cell Cycle Research

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-369-C005		5 µg	180.00 USD

Product Specification

FORMULA:	C₂₈H₄₀O₅
MW:	456.6
SOURCE/HOST:	Isolated from Sorangium cellulosum.
PURITY:	≥95%
FORMULATION:	Liquid. Solution in methanol (5µg in 1ml).
SOLUBILITY:	Soluble in methanol (>50mg/ml). Sparingly soluble in aqueous buffers (up to 10µg/ml in PBS).
SHIPPING:	SHIPPED ON BLUE ICE
LONG TERM STORAGE:	-20°C
USE/STABILITY:	Acid and base sensitive. Unstable in acidic and alkaline buffer systems (pH <6 or >7). Stable in methanolic solution at -20°C.
HANDLING:	Protect from light.
HAZARD:	TOXIC.

Product Description

Cytotoxic secondary metabolite that inhibits cell growth of mammalian cell lines in the picomolar range (IC₅₀=0.2ng/ml with L929 mouse cells) including multidrug resistant (MDR) HeLa cells (IC₅₀=0.1ng/ml with KB-V1). Like leptomycin B (Prod. No. ALX-380-100), ratjadone C binds covalently to the nuclear export protein CRM1. It inhibits cargo protein binding to the leucine-rich nuclear export sequence and thereby blocks nuclear export.

Product Specific Literature References

Antibiotics from gliding bacteria, LXIII. Ratjadone: a new antifungal metabolite from Sorangium cellulosum: D. Schummer, et al.; Liebigs Ann. 685 (1995)
Ratjadon: a new antifungal compound from Sorangium cellulosum (myxobacteria) production, physico-chemical and biological properties: K. Gerth, et al.; J. Antibiot. (Tokyo) 48, 973 (1995) Abstract
The chemistry and biology of the leptomycin family: M. Kalesse & M. Christmann; Synthesis 8, 981 (2002) Abstract
Ratjadones inhibit nuclear export by blocking CRM1/exportin 1: M. Koster, et al.; Exp. Cell. Res. 286, 321 (2003) Abstract

Further Categories Containing This Product:

Antitumor Antibiotics • Antibiotics - Antifungal • Cell Cycle Blockers & Inhibitors / Related Products • Nuclear Envelope & Nuclear Transport • Antitumor Agents (Anti-proliferative)

ALX-270-392

Revised 08-Dec-04

3-(2-Chloro-3-indolylmethylene)-1,3-dihydroindol-2-one
PRODUCT LINE	Cell Cycle
PRODUCT CATEGORY	CDK & Cyclin Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-392-M001		1 mg	35.00 USD
ALX-270-392-M005		5 mg	130.00 USD

Product Specification

FORMULA:	C₁₇H₁₁ClN₂O
MW:	294.7
PURITY:	≥95% (HPLC)
APPEARANCE:	Yellow to orange solid.
SOLUBILITY:	Soluble in DMSO.
SHIPPING:	SHIPPED ON BLUE ICE
LONG TERM STORAGE:	+4°C
USE/STABILITY:	Stable for 3 years after receipt when stored at -20°C. Stock solutions are stable for up to 3 months when stored at -20°C.
HANDLING:	Packaged under inert gas. After reconstitution, prepare aliquots and store at -20°C. Protect from light.

Product Description

Selective, ATP-competitive inhibitor of CDK1/cyclin B (IC₅₀=5.8µM) and CDK5 (IC₅₀=25µM). Does not inhibit GSK-3β (IC₅₀>100µM). Exhibits potent antiproliferative properties (IC₅₀=2µM in HeLa cells).

Product Specific Literature References

Potential antitumor agents. 25 [1]. Synthesis and cytotoxic activity of 3-(2-chloro-3-indolylmethylene)1,3-dihydroindol-2-ones: A. Andreani, et al.; Anticancer Res. 16, 3585 (1996) Abstract
Imidazo[2,1 -b]thiazolylmethylene- and indolylmethylene-2-indolinones: a new class of cyclin-dependent kinase inhibitors. Design, synthesis, and CDK1/cyclin B inhibition: A. Andreani, et al.; Anticancer Drug Des. 15, 447 (2000) Abstract

Further Categories Containing This Product:

Antitumor Agents (Anti-proliferative) • Antitumor Agents (Enzyme Inhibitors)

ALX-270-400

Revised 31-Mar-05

SU 9516
SYNONYMS	3-[1-(3H-Imidazol-4-yl)-meth-(Z)-ylidene]-5-methoxy-1,3-dihydro-indol-2-one
PRODUCT LINE	Cell Cycle
PRODUCT CATEGORY	CDK & Cyclin Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-400-M005		5 mg	80.00 USD
ALX-270-400-M025		25 mg	320.00 USD

Product Specification

FORMULA:	C₁₃H₁₁N₃O₂
MW:	241.3
PURITY:	≥95%
APPEARANCE:	Yellow to orange solid.
SOLUBILITY:	Soluble in DMSO (10mg/ml).
SHIPPING:	SHIPPED ON BLUE ICE
LONG TERM STORAGE:	+4°C
HANDLING:	Protect from light. Packaged under inert gas.

Product Description

Cell permeable, potent, selective and ATP-competitive inhibitor of CDK2/cyclin A (IC₅₀=22nM), CDK1/cyclin B (IC₅₀=40nM) and CDK4/cyclin D1 (IC₅₀=200nM). Has no effect on the activity of PKC, p38, PDGFRβ and EGFR (IC₅₀>10µM). Displays anti-proliferative and pro-apoptotic properties in tumor cells. Inhibits proliferation of growth factor-stimulated colon carcinoma cells by binding to CDK2 and thus preventing the phosphorylation of pRb and its dissociation from E2F.

Product Specific Literature References

A novel cdk2-selective inhibitor, SU9516, induces apoptosis in colon carcinoma cells: M.E. Lane, et al.; Cancer Res. 61, 6170 (2001) Abstract
SU9516, a cyclin-dependent kinase 2 inhibitor, promotes accumulation of high molecular weight E2F complexes in human colon carcinoma cells: B. Yu, et al.; Biochem Pharmacol. 64, 1091 (2002) Abstract
SU9516: biochemical analysis of cdk inhibition and crystal structure in complex with cdk2: D.J. Moshinsky, et al.; BBRC 310, 1026 (2003) Abstract
Novel pyrrolyllactone and pyrrolyllactam indolinones as potent cyclin-dependent kinase 2 inhibitors: X. Li, et al.; Bioorg. Med. Chem. Lett. 13, 1939 (2003) Abstract

Further Categories Containing This Product:

Antitumor Agents (Anti-proliferative) • Antitumor Agents (Apoptosis Inducers) • Antitumor Agents (Enzyme Inhibitors)

ALX-270-442

Revised 21-Oct-08

CDK1/2 Inhibitor III
SYNONYMS	5-Amino-3-((4-(aminosulfonyl)phenyl)amino)-N-(2,6-difluorophenyl)-1H-1,2,4-triazole-1-carbothioamide
PRODUCT LINE	Cell Cycle
PRODUCT CATEGORY	CDK & Cyclin Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-442-M001		1 mg	118.00 USD

Product Specification

FORMULA:	C₁₅H₁₃F₂N₇O₂S₂
MW:	425.4
CAS NUMBER:	443798-55-8
PURITY:	≥95% (HPLC)
APPEARANCE:	White to off-white solid.
SOLUBILITY:	Soluble in DMSO (10mg/ml), tetrahydro-furan or acetone.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
USE/STABILITY:	Stock solutions are stable for up to 6 months when stored at -20°C.
HANDLING:	Protect from light.
HAZARD:	HARMFUL.
IDENTITY:	Identity determined by NMR.

Product Description

Cell permeable triazolo-diamine compound that displays anti-proliferative properties in various human cancer cells (IC₅₀=20nM, 35nM and 92nM in HCT-116, HeLa, and A375 cells). Acts as a highly potent, ATP-competitive inhibitor of CDK1/cyclin B and CDK2/cyclin A (IC₅₀=600pM and 500pM) with selectivity over VEGF-R2 and GSK-3β (IC₅₀=32nM and 140nM).

Product Specific Literature References

1-Acyl-1H-[1,2,4]triazole-3,5-diamine analogues as novel and potent anticancer cyclin-dependent kinase inhibitors: synthesis and evaluation of biological activities: R. Lin, et al.; J. Med. Chem. 48, 4208 (2005) Abstract

Further Categories Containing This Product:

Tyrosine Kinase Inhibitors • GSK-3 Inhibitors • VEGFs & VEGF-Rs Other Products • Antitumor Agents (Anti-proliferative)

ALX-270-454

Revised 26-Mar-07

ZSTK474
SYNONYMS	2-(2-Difluoromethylbenzimidazol-1-yl)-4,6-dimorpholino-1,3,5-triazine
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	Phosphoinositide 3-kinase [PI(3)K] / Related Products

Ordering Information

not sold in USA

Product Specification

FORMULA:	C₁₉H₂₁F₂N₇O₂
MW:	417.4
CAS NUMBER:	475110-96-4
PURITY:	≥98% (HPLC)
APPEARANCE:	White to off-white solid.
SOLUBILITY:	Soluble in DMSO.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
USE/STABILITY:	Stock solutions are stable for up to 6 months when stored at -20°C.
HANDLING:	Protect from light.
HAZARD:	IRRITANT.

Product Description

Cell permeable, reversible, potent and specific inhibitor of phosphoinositide 3-kinase (IC₅₀=17nM for PI(3)K p110β, IC₅₀=53nM for PI(3)K p110γ and IC₅₀=6nM for PI(3)K p110δ). Blocks cellular PI(3)K/Akt (PKB) signalling in vitro and inhibits Akt(PKB)-dependent tumor growth in mice in vivo without significant toxic effect. More effective than LY 294,002 (Prod. No. ALX-270-038) in vitro and as in vivo.

Product Specific Literature References

A novel phosphatidylinositol 3-kinase inhibitor, ZSTK474 exerted antitumor activity against human tumor xenografts by oral administration: S.Yaguchi et al.; Proc. Am. Assoc. Cancer Res. 46, 1691 (2005)
Antitumor activity of ZSTK474, a new phosphatidylinositol 3-kinase inhibitor: S. Yaguchi, et al.; J. Natl. Cancer Inst. 98, 545 (2006) Abstract