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Cyclin-dependent Kinases [CDKs] & Cyclins / Related Products
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ALX-350-251 Revised 23-Oct-07
(R)-Roscovitine
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SYNONYMS 6-Benzylamino-2-(R)-[(1-ethyl)-2-hydroxyethylamino]-9-isopropylpurine
PRODUCT LINE Cell Cycle
PRODUCT CATEGORY CDK & Cyclin Inhibitors
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-350-251-M001   1 mg 30.00 USD Add To Cart
ALX-350-251-M005   5 mg 110.00 USD Add To Cart
ALX-350-251-M050   50 mg 450.00 USD Add To Cart
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Product Specification
FORMULA: C19H26N6O
MW: 354.5
CAS NUMBER: 186692-46-6
PURITY: ≥97%
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in chloroform, DMSO or methanol; moderately soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Potent and selective inhibitor of CDKs. Selective for CDK1/cyclin B kinase (IC50=450nM) [2], CDK2 (IC50=700nM) [4] and CDK5/p35 (IC50=160nM) [4,5]. More potent than olomoucine (Prod. No. ALX-350-013). Inhibits M phase promoting factor (MPF) kinase activity. Has effects on calcium channel gating.
Product Specific Literature References
[1] Activation of cyclin-dependent kinases by Myc mediates induction of cyclin A, but not apoptosis: B. Rudolph, et al.; EMBO J. 15, 3065 (1996) Abstract
[2] Inhibition of cyclin-dependent kinases by purine analogues: crystal structure of human cdk2 complexed with roscovitine: W.F. De Azvedo, et al.; Eur. J. Biochem. 243, 518 (1997) Abstract
[3] Cytokinin-derived cyclin-dependent kinase inhibitors: synthesis and cdc2 inhibitory activity of olomoucine and related compounds: L. Havlicek, et al.; J. Med. Chem. 40, 408 (1997) Abstract
[4] Chemical inhibitors of cyclin-dependent kinases: L. Meijer and S.H. Kim; Meth. Enzymol. 283, 113 (1997) Abstract
[5] Biochemical and cellular effects of roscovitine, a potent and selective inhibitor of the cyclin-dependent kinases cdc2, cdk2 and cdk5: L. Meijer, et al.; Eur. J. Biochem. 243, 527 (1997) Abstract
[6] Direct in vivo inhibition of the nuclear cell cycle cascade in experimental mesangial proliferative glomerulonephritis with Roscovitine, a novel cyclin-dependent kinase antagonist: J.W. Pippin, et al.; J. Clin. Invest. 100, 2512 (1997) Abstract
[7] Early inhibition of DNA synthesis in the developing rat cerebral cortex by the purine analogues olomoucine and roscovitine: J.S. Yakisich, et al.; BBRC 243, 674 (1998) Abstract
[8] The cyclin-dependent kinase inhibitors olomoucine and roscovitine arrest human fibroblasts in G1 phase by specific inhibition of CDK2 kinase activity: F. Alessi, et al.; Exp. Cell Res. 245, 8 (1998) Abstract
[9] Effects of cyclin-dependent kinase inhibitors on transcription and ocular circadian rhythm of Aplysia: N. Sankrithi & A. Eskin; J. Neurochem. 72, 605 (1999) Abstract
[10] Transcription of herpes simplex virus immediate-early and early genes is inhibited by roscovitine, an inhibitor specific for cellular cyclin- dependent kinases: L.M. Schang, et al.; J. Virol. 73, 2161 (1999) Abstract
[11] Roscovitine and other purines as kinase inhibitors. From starfish oocytes to clinical trials: L. Meijer & E. Raymond; Acc. Chem. Res. 36, 417 (2003), (Review) Abstract
[12] The specificities of protein kinase inhibitors: an update: J. Bain, et al.; Biochem. J. 371, 199 (2003) Abstract
[13] Roscovitine, olomoucine, purvalanol: inducers of apoptosis in maturing cerebellar granule neurons: E.A. Monaco, 3rd, et al.; Biochem. Pharmacol. 67, 1947 (2004) Abstract
[14] Roscovitine targets, protein kinases and pyridoxal kinase: S. Bach, et al.; J. Biol. Chem. 280, 31208 (2005) Abstract
[15] The effects of presynaptic calcium channel modulation by roscovitine on transmitter release at the adult frog neuromuscular junction: S. Cho & S.D. Meriney; Eur. J. Neurosci. 23, 3200 (2006) Abstract
[16] Roscovitine differentially affects CaV2 and Kv channels by binding to the open state: Z. Buraei, et al.; Neuropharmacology 52, 883 (2007) Abstract
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Ion Channels & Transporters Other Products
 
 
ALX-350-293 Revised 19-Oct-07
(S)-Roscovitine
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SYNONYMS 6-Benzylamino-2-(S)-[(1-Ethyl)-2-hydroxyethylamino]-9-isopropylpurine
PRODUCT LINE Cell Cycle
PRODUCT CATEGORY CDK & Cyclin Inhibitors
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ALX-350-293-M001   1 mg 40.00 USD Add To Cart
Product Specification
FORMULA: C19H26N6O
MW: 354.5
CAS NUMBER: 186692-46-6
PURITY: ≥98% (HPLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO, dimethyl formamide, 100% ethanol or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
(S)-Enantiomer of the CDK inhibitor roscovitine (Prod. No. ALX-350-251). Potent inhibitor of CDK1/cyclin B kinase (IC50=950nM) [1].
Product Specific Literature References
[1] Inhibition of cyclin-dependent kinases by purine analogues: crystal structure of human cdk2 complexed with roscovitine: W.F. De Azevedo, et al.; Eur. J. Biochem. 243, 518 (1997) Abstract
[2] Cytokinin-derived cyclin-dependent kinase inhibitors: synthesis and cdc2 inhibitory activity of olomoucine and related compounds: L. Havlicek, et al.; J. Med. Chem. 40, 408 (1997) Abstract
[3] The cyclin-dependent kinase inhibitors olomoucine and roscovitine arrest human fibroblasts in G1 phase by specific inhibition of CDK2 kinase activity: F. Alessi, et al.; Exp. Cell Res. 245, 8 (1998) Abstract
Maintenance of meiotic arrest in bovine oocytes using the S-enantiomer of roscovitine: effects on maturation, fertilization and subsequent embryo development in vitro: P. Coy, et al.; Reproduction 129, 19 (2005) Abstract
In vitro maturation and fertilization of porcine oocytes after a 48 h culture in roscovitine, an inhibitor of p34cdc2/cyclin B kinase: R. Romar & H. Funahashi; Anim. Reprod. Sci. 92, 321 (2006) Abstract
 
 
ALX-380-014 Revised 15-May-08
Staurosporine
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SYNONYMS Antibiotic AM-2282
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Apoptosis Inducers & Inhibitors
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ALX-380-014-C100   100 µg 47.00 USD Add To Cart
ALX-380-014-C250   250 µg 112.00 USD Add To Cart
ALX-380-014-M001   1 mg 270.00 USD Add To Cart
ALX-380-014-M005   5 mg 790.00 USD Add To Cart
Product Specification
FORMULA: C28H26N4O3
MW: 466.5
CAS NUMBER: 62996-74-1
MERCK INDEX: 14: 8802
RTECS: KC655000
SOURCE/HOST: Isolated from Streptomyces staurosporeus.
PURITY: ≥98%
APPEARANCE: Off-white to green powder.
SOLUBILITY: Soluble in ethyl acetate, DMSO or dimethyl formamide; only slightly soluble in chloroform and methanol. Insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
USE/STABILITY: Stable for at least 2 years after receipt when stored +4°C.
HANDLING: Protect from light and moisture.
HAZARD: HARMFUL. MAY BE CARCINOGENIC.

Product Description
Model apoptosis inducer. Potent cell-permeable inhibitor of a variety of protein kinases, e.g. protein kinase C (PKC), CDK1/cyclin B (IC50~5nM), CDK2/cyclin A (IC50=7nM), CDK4/cyclin D (IC50=3-10µM), CDK5/p25 (IC50=4nM) and GSK-3β (IC50=15nM).
Product Specific Literature References
A new alkaloid AM-2282 of Streptomyces origin. Taxonomy, fermentation, isolation and preliminary characterization: S. Omura, et al.; J. Antibiot. (Tokyo) 30, 275 (1977) Abstract
A. Furusaki, et al.; J. C. S. Chem. Commun. 800 (1978)
Staurosporine, a potent inhibitor of phospholipid/Ca++dependent protein kinase: T. Tamaoki, et al.; BBRC 135, 397 (1986) Abstract
Staurosporine, a potent platelet aggregation inhibitor from a Streptomyces species: S. Oka, et al.; Agric. Biol. Chem. 50, 2723 (1986)
Staurosporine inhibits tyrosine-specific protein kinase activity of Rous sarcoma virus transforming protein p60: N. Nakano, et al.; J. Antibiot. (Tokyo) 40, 706 (1987) Abstract
Contrasting actions of staurosporine, a protein kinase C inhibitor, on human neutrophils and primary mouse epidermal cells: T. Sako, et al.; Cancer Res. 48, 4646 (1988) Abstract
Staurosporine, a protein kinase C inhibitor interferes with proliferation of arterial smooth muscle cells: H. Matsumoto & Y. Sasaki; Biochem. Biophys. Res. Commun. 158, 105 (1989) Abstract
Staurosporine, K-252 and UCN-01: potent but nonspecific inhibitors of protein kinases: U.T. Ruegg & G.M. Burgess; TIPS 10, 218 (1989), (Review) Abstract
Staurosporine: an effective inhibitor for Ca2+/calmodulin-dependent protein kinase II: N. Yanagihara, et al.; J. Neurochem. 56, 294 (1991) Abstract
Is staurosporine a specific inhibitor of protein kinase C in intact porcine coronary arteries?: M. Kageyama, et al.; J. Pharmacol. Exp. Ther. 259, 1019 (1991) Abstract
Induction of a common pathway of apoptosis by staurosporine: R. Bertrand, et al.; Exp. Cell Res. 211, 314 (1994) Abstract
First total synthesis of Staurosporine and ent-Staurosporine: J.T. Link et al.; J. Am. Chem. Soc. 117, 552 (1995)
Staurosporine induces programmed cell death in embryonic neurons and activation of the ceramide pathway: D.A. Wiesner & G. Dawson; J. Neurochem 66, 1418 (1996) Abstract
Staurosporine and ent-staurosporine: the first total synthesis, prospects for a regioselective approach, and activity profile: J.T. Link et al.; J. Am. Chem. Soc. 118, 2825 (1996)
K252a and staurosporine microbial alkaloid toxins as prototype of neurotropic drugs: P. Lazarovici, et al.; Adv. Exp. Med. Biol. 391, 367 (1996), Review Abstract
Characterization of the cell death process induced by staurosporine in human neuroblastoma cell lines: J. Boix, et al.; Neuropharmacology 36, 811 (1997) Abstract
Caspase-3-dependent cleavage of Bcl-2 promotes release of cytochrome c: D.G. Kirsch, et al.; J. Biol. Chem. 274, 21155 (1999) Abstract; Full Text
Molecular mechanism of staurosporine-induced apoptosis in osteoblasts: H.J. Chae, et al.; Pharmacol. Res. 42, 373 (2000) Abstract
Glycogen synthase kinase-3beta facilitates staurosporine- and heat shock-induced apoptosis. Protection by lithium: G.N. Bijur, et al.; J. Biol. Chem. 275, 7583 (2000) Abstract; Full Text
Dissociation of staurosporine-induced apoptosis from G2-M arrest in SW620 human colonic carcinoma cells: initiation of the apoptotic cascade is associated with elevation of the mitochondrial membrane potential (deltapsim): B.G. Heerdt, et al.; Cancer Res. 60, 6704 (2000) Abstract
Changes in mitochondrial membrane potential during staurosporine- induced apoptosis in Jurkat cells: J.L. Scarlett, et al.; FEBS Lett. 475, 267 (2000) Abstract
Equivalent death of P-glycoprotein expressing and nonexpressing cells induced by the protein kinase C inhibitor staurosporine: K.M. Tainton, et al.; BBRC 276, 231 (2000) Abstract
Caspase-8 activation and bid cleavage contribute to MCF7 cellular execution in a caspase-3-dependent manner during staurosporine-mediated apoptosis: D. Tang, et al.; J. Biol. Chem. 275, 9303 (2000) Abstract; Full Text
Insulin-stimulated protein kinase B phosphorylation on Ser-473 is independent of its activity and occurs through a staurosporine-insensitive kinase: M.M. Hill, et al.; J. Biol. Chem. 276, 25643 (2001) Abstract; Full Text
Single-cell fluorescence resonance energy transfer analysis demonstrates that caspase activation during apoptosis is a rapid process. Role of caspase-3: M. Rehm, et al.; J. Biol. Chem. 277, 24506 (2002) Abstract; Full Text
Related Products
 
 
ALX-270-400 Revised 31-Mar-05
SU 9516
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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
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ALX-270-400-M005   5 mg 80.00 USD Add To Cart
ALX-270-400-M025   25 mg 320.00 USD Add To Cart
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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
 
 
ALX-270-168 Revised 18-May-06
Tyrphostin AG 490
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SYNONYMS Tyrphostin B42
N-Benzyl-3,4-dihydroxy-benzylidenecyanoacetamide
α-Cyano-(3,4-dihydroxy)-]N-benzylcinnamamide
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Tyrphostins
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ALX-270-168-M005   5 mg 45.00 USD Add To Cart
ALX-270-168-M025   25 mg 190.00 USD Add To Cart
Product Specification
FORMULA: C17H14N2O3
MW: 294.3
CAS NUMBER: 133550-30-8
PURITY: ≥98%
APPEARANCE: Yellow solid.
SOLUBILITY: Soluble in DMSO and acetone; slightly soluble in 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Selectively inhibits CDK2 activation leading to a potent cell cycle arrest at late G1 and S phase. Cell permeable inhibitor of JAK-2 tyrosine kinase. Does not significantly inhibit other kinases, such as Lck, Lyn, Btk, Syk or Src. Blocks IL-7 induced JAK kinase activity in T cells (JAK-1, JAK-3) and the consequent phosphorylation of PI-3 kinase. Valuable tool for studying the cellular role of JAK kinases in signal transduction.
Product Specific Literature References
Tyrphostins I: synthesis and biological activity of protein tyrosine kinase inhibitors: A. Gazit, et al.; J. Med. Chem. 32, 2344 (1989) Abstract
Tyrosine phosphorylation is an obligatory event in IL-2 secretion [published erratum appears in J Immunol 1991 May 1;146(9):3260]: A. Levitzki; Biochem. Pharmacol. 40, 913 (1990) Abstract
Activation of phosphatidylinositol-3 kinase by ligation of the interleukin-7 receptor is dependent on protein tyrosine kinase activity: H. Dadi, et al.; Blood 84, 1579 (1994) Abstract; Full Text
JAK3 protein tyrosine kinase mediates interleukin-7-induced activation of phosphatidylinositol-3’ kinase: N. Sharfe, et al.; Blood 86, 2077 (1995) Abstract; Full Text
Inhibition of acute lymphoblastic leukaemia by a Jak-2 inhibitor: N. Meydan, et al.; Nature 379, 645 (1996) Abstract
Tyrphostin AG-490 inhibits cytokine-mediated JAK3/STAT5a/b signal transduction and cellular proliferation of antigen-activated human T cells: R.A. Kirken, et al.; J. Leukoc. Biol. 65, 891 (1999) Abstract
JAK3, STAT, and MAPK signaling pathways as novel molecular targets for the tyrphostin AG-490 regulation of IL-2-mediated T cell response: L.H. Wang, et al.; J. Immunol. 162, 3897 (1999) Abstract
JAK2 tyrosine kinase inhibitor tyrphostin AG490 downregulates the mitogen-activated protein kinase (MAPK) and signal transducer and activator of transcription (STAT) pathways and induces apoptosis in myeloma cells: J. De Vos, et al.; Br. J. Haematol. 109, 823 (2000) Abstract
 
 
ALX-270-143 Revised 20-Feb-08
Tyrphostin AG 494
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SYNONYMS Tyrphostin B48
N-Phenyl-3,4-dihydroxybenzylidenecyanoacetamide
α-Cyano-(3,4-dihydroxy)-N-phenylcinnamamide
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Tyrphostins
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-270-143-M005   5 mg 25.00 USD Add To Cart
ALX-270-143-M025   25 mg 90.00 USD Add To Cart
Product Specification
FORMULA: C16H12N2O3
MW: 280.3
CAS NUMBER: 133550-35-3
PURITY: ≥98%
APPEARANCE: Yellow solid.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Blocks CDK2 activation and causes cells to arrest at late G1 and during S phase.
Product Specific Literature References
Tyrphostins. 2. Heterocyclic and alpha-substituted benzylidenemalononitrile tyrphostins as potent inhibitors of EGF receptor and ErbB2/neu tyrosine kinases: A. Gazit, et al.; J. Med. Chem. 34, 1896 (1991) Abstract
Tyrphostin AG 494 blocks Cdk2 activation: N. Osherov & A. Levitzki; FEBS Lett. 410, 187 (1997) Abstract
Inhibition of Cdk2 activation by selected tyrphostins causes cell cycle arrest at late G1 and S phase: N. Kleinberger-Doron, et al.; Exp. Cell Res. 241, 340 (1998) Abstract
 
 
ALX-380-222 Revised 19-Aug-08
UCN-01
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SYNONYMS 7-Hydroxystaurosporine
Staurosporine, 7-Hydroxy-
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Staurosporine / Related Products
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-380-222-MC25   0.25 mg 85.00 USD Add To Cart
ALX-380-222-M001   1 mg 265.00 USD Add To Cart
Product Specification
FORMULA: C28H26N4O4
MW: 482.5
CAS NUMBER: 112953-11-4
RTECS: KC6600010
SOURCE/HOST: Isolated from Streptomyces sp. MST-AS5345.
PURITY: ≥98% (HPLC)
APPEARANCE: Light tan to light yellow solid.
SOLUBILITY: Soluble in methanol, 100% ethanol, dimethyl formamide or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description

Inhibitor of protein kinase C (PKC) and cyclin-dependent kinases (CDKs) resulting in accumulation of cells in the G1 phase and induction of apoptosis. Enhances the cytotoxicity of other anticancer drugs, such as DNA-damaging agents and anti-metabolite drugs, through putative abrogation of G2 and/or S phase accumulation induced by these agents.

Product Specific Literature References
[1] UCN-01, a selective inhibitor of protein kinase C from Streptomyces: I. Takahashi, et al.; J. Antibiot. (Tokyo) 40, 1782 (1987) Abstract
[2] UCN-01 and UCN-02, new selective inhibitors of protein kinase C. II. Purification, physico-chemical properties, structural determination and biological activities: I. Takahashi, et al.; J. Antibiot. (Tokyo) 42, 571 (1989) Abstract
[3] UCN-01, 7-hydroxyl-staurosporine, inhibits kinase activity of cyclin-dependent kinases and reduces the phosphorylation of the retinoblastoma susceptibility gene product in A549 human lung cancer cell line: K. Kawakami, et al.; BBRC 219, 778 (1996) Abstract
[4] UCN-01 (7-hydroxystaurosporine) and other indolocarbazole compounds: a new generation of anti-cancer agents for the new century?: S. Akinaga, et al.; Anticancer Drug Des. 15, 43 (2000) Abstract
[5] UCN-01-induced cell cycle arrest requires the transcriptional induction of p21(waf1/cip1) by activation of mitogen-activated protein/extracellular signal-regulated kinase kinase/extracellular signal-regulated kinase pathway: M.M. Facchinetti, et al.; Cancer Res. 64, 3629 (2004) Abstract; Full Text
General Information
BACKGROUND/TECHNICAL INFORMATION Note: Some interconversion of UCN-01 to UCN-02 may occur under acidic HPLC conditions (see [2]).
 
 
ALX-380-206 Revised 19-Aug-08
UCN-02
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Staurosporine / Related Products
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ALX-380-206-MC25   0.25 mg 85.00 USD Add To Cart
ALX-380-206-M001   1 mg 265.00 USD Add To Cart
Product Specification
FORMULA: C28H26N4O4
MW: 482.5
CAS NUMBER: 121569-61-7
RTECS: KC6600000
SOURCE/HOST: Isolated from Streptomyces sp. MST-AS5345.
PURITY: ≥98% (HPLC)
APPEARANCE: White to pale yellow solid.
SOLUBILITY: Soluble in ethyl acetate, 100% ethanol, dimethyl formamide or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.