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CDK & Cyclin Inhibitors
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 Items 40-59 of 59 Page 3 of 3 Select Page: << 1 2 3   
ALX-350-090 Revised 10-Mar-08
Olomoucine, Iso-
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SYNONYMS 6-Benzylamino-2-(2-hydroxyethylamino)-7-methylpurine
PRODUCT LINE Cell Cycle
PRODUCT CATEGORY CDK & Cyclin Inhibitors
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ALX-350-090-M005   5 mg 70.00 USD Add To Cart
ALX-350-090-M025   25 mg 280.00 USD Add To Cart
Product Specification
FORMULA: C15H18N6O
MW: 298.4
CAS NUMBER: 101622-50-8
PURITY: ≥98%
APPEARANCE: Off-white solid.
SOLUBILITY: Soluble in DMSO or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Inactive negative control for use in studies involving olomoucine (Prod. No. ALX-350-013).
Product Specific Literature References
Inhibition of cyclin-dependent kinases by purine analogues: J. Vesely, et al.; Eur. J. Biochem. 224, 771 (1994) Abstract
The cyclin-dependent kinase (cdk) inhibitors, olomoucine and roscovitine, alter the expression of a molluscan circadian pacemaker: N.A. Krucher, et al.; Cell. Mol. Neurobiol. 17, 495 (1997) Abstract
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
Inhibition of Cdk5 in the nucleus accumbens enhances the locomotor-activating and incentive-motivational effects of cocaine: J.R. Taylor, et al.; PNAS 104, 4147 (2007) Abstract
Further Categories Containing This Product:
CDKs & Cyclins Other Products
 
 
ALX-350-250 Revised 22-Jul-08 New product
Butyrolactone I
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PRODUCT LINE Cell Cycle
PRODUCT CATEGORY CDK & Cyclin Inhibitors
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ALX-350-250-C200   200 µg 135.00 USD Add To Cart
Product Specification
FORMULA: C24H24O7
MW: 424.5
CAS NUMBER: 87414-49-1
PURITY: ≥99% (TLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: 25mg/ml soluble in 100% ethanol or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Cell permeable and selective inhibitor of the cyclin-dependent kinases CDK1/cyclin B, CDK2 and CDK5. Inhibits cell cycle progression at the G1/S and G2/M transitions. Blocks Fas-induced apoptosis. Displays antitumor activity.
Product Specific Literature References
Butyrolactone I, a selective inhibitor of cdk2 and cdc2 kinase: M. Kitagawa, et al.; Oncogene 8, 2425 (1993) Abstract
Inhibition of cell cycle oscillation of DNA replication by a selective inhibitor of the cdc2 kinase family, butyrolactone I, in Xenopus egg extracts: A. Someya, et al.; BBRC 198, 536 (1994) Abstract
A cyclin-dependent kinase inhibitor, butyrolactone I, inhibits phosphorylation of RB protein and cell cycle progression: M. Kitagawa, et al.; Oncogene 9, 2549 (1994) Abstract
Evidence for cdk5 as a major activity phosphorylating tau protein in porcine brain extract: T. Hosoi, et al.; J. Biochem. 117, 741 (1995) Abstract
Transcriptional activation of the cdc2 gene is associated with Fas- induced apoptosis of human hematopoietic cells: Y. Furukawa, et al.; J. Biol. Chem. 271, 28469 (1996) Abstract; Full Text
Antitumor effects of butyrolactone I, a selective cdc2 kinase inhibitor, on human lung cancer cell lines: K. Nishio, et al.; Anticancer Res. 16, 3387 (1996) Abstract
An exogenous cdk inhibitor, butyrolactone-I, induces apoptosis with increased Bax/Bcl-2 ratio in p53-mutated pancreatic cancer cells: M. Wada, et al.; Anticancer Res. 18, 2559 (1998) Abstract
Effects of cyclin-dependent kinase inhibitors on transcription and ocular circadian rhythm of Aplysia: N. Sankrithi and A. Eskin; J. Neurochem. 72, 605 (1999) Abstract
Butyrolactone I induces cyclin B1 and causes G2/M arrest and skipping of mitosis in human prostate cell lines: M. Suzuki, et al.; Cancer Lett. 138, 121 (1999) Abstract
Butyrolactone I reversibly inhibits meiotic maturation of bovine oocytes, without influencing chromosome condensation activity: M. Kubelka, et al.; Biol. Reprod. 62, 292 (2000) Abstract; Full Text
Involvement of Cdk5/p25 in digoxin-triggered prostate cancer cell apoptosis: H. Lin, et al.; J. Biol. Chem. 279, 29302 (2004) Abstract; Full Text
Regulation of mitotic function of Chk1 through phosphorylation at novel sites by cyclin-dependent kinase 1 (Cdk1): T. Shiromizu, et al.; Genes Cells 11, 477 (2006) Abstract
 
 
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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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
Further Categories Containing This Product:
Ion Channels & Transporters Other Products
 
 
ALX-350-273 Revised 03-Apr-08
3-ATA
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SYNONYMS 3-Amino-9-thio(10H)-acridone
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products for Cell Cycle Research
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ALX-350-273-M001   1 mg 60.00 USD Add To Cart
ALX-350-273-M005   5 mg 240.00 USD Add To Cart
Product Specification
FORMULA: C13H10N2S
MW: 226.3
CAS NUMBER: 12982-10-85
PURITY: ≥95%
APPEARANCE: White solid powder.
SOLUBILITY: Soluble in DMSO or dimethyl formamide.
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C

Product Description
Specific CDK4 inhibitor (IC50=3.1µM) inducing growth inhibition of p16-altered tumors.
Product Specific Literature References
The p16 status of tumor cell lines identifies small molecule inhibitors specific for cyclin-dependent kinase 4: A. Kubo, et al.; Clin. Cancer Res. 5, 4279 (1999) Abstract
3-Amino thioacridone, a selective cyclin-dependent kinase 4 inhibitor, attenuates kainic acid-induced apoptosis in neurons: E. Verdaguer, et al.; Neuroscience 120, 599 (2003) Abstract
Further Categories Containing This Product:
CDK & Cyclin Inhibitors
 
 
ALX-350-289 Revised 18-Nov-08
10Z-Hymenialdisine
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SYNONYMS 4-(2-Amino-4-oxo-2-imidazolin-5-ylidene)-2-bromo-4,5,6,7-tetrahydropyrrolo[2,3-c]azepin-8-one
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Protein Kinase Inhibitors
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ALX-350-289-C500   500 µg 190.00 USD Add To Cart
ALX-350-289-M001   1 mg 340.00 USD Add To Cart
Product Specification
FORMULA: C11H10BrN5O2
MW: 324.1
CAS NUMBER: 82005-12-7
SOURCE/HOST: Isolated from sponge Axinella carteri.
PURITY: ≥97% (HPLC)
APPEARANCE: Yellow needles.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
HAZARD: TOXIC.
IDENTITY: Identity determined by 1H- NMR and MS.

Product Description
Originally isolated from the sponges Axinella verrucosa and Acantella aurantiaca. Potent inhibitor of mitogen-activated protein kinase kinase-1 (MEK-1) (IC50=6nM). Blocks the in vivo phosphorylation of the microtubule-binding protein tau at sites that are hyperphosphorylated by glycogen synthase kinase-β (GSK-3β) and CDK5/p35 in Alzheimer’s disease. Inhibitor of DNA damage checkpoint at G2 phase (IC50=6µM), cyclin-dependent kinases CDK1/cyclin B (IC50=22nM), CDK2/cyclin A (IC50=70nM), CDK2/cyclin E (IC50=40nM), CDK4/cyclin D1 (IC50=600nM), CDK5/p25 (IC50=28nM), GSK-3β (IC50=10nM), and casein kinase 1 (CK1) (IC50=35nM). Inhibitor of NF-κB activation and of various pro-inflammatory cytokines such as IL-1, IL-2 (IC50=2.4µM), IL-6, IL-8, TNF-α (IC50=1.4µM) and nitric oxide (NO) (IC50=0.8µM) in a variety of cell lines.
Product Specific Literature References
Isolation and x-ray crystal structure of a novel bromo-compound from two marine sponges: G. Cimino, et al.; Tetrahedron Lett. 23, 767 (1982)
Bioactive alkaloids from the tropical marine sponge Axinella carteri: A. Supriyono, et al.; Z. Naturforsch. [C] 50, 669 (1995) Abstract
The natural product hymenialdisine inhibits interleukin-8 production in U937 cells by inhibition of nuclear factor-kappaB: J.J. Breton & M.C. Chabot-Fletcher; J. Pharmacol. Exp. Ther. 282, 459 (1997) Abstract; Full Text
Inhibition of NFkappaB-mediated interleukin-1beta-stimulated prostaglandin E2 formation by the marine natural product hymenialdisine: A. Roshak, et al.; J. Pharmacol. Exp. Ther. 283, 955 (1997) Abstract; Full Text
Inhibition of interleukin-1-induced proteoglycan degradation and nitric oxide production in bovine articular cartilage/chondrocyte cultures by the natural product, hymenialdisine: A.M. Badger, et al.; J. Pharmacol. Exp. Ther. 290, 587 (1999) Abstract; Full Text
Inhibition of cyclin-dependent kinases, GSK-3beta and CK1 by hymenialdisine, a marine sponge constituent: L. Meijer, et al.; Chem. Biol. 7, 51 (2000) Abstract
Inhibition of the G2 DNA damage checkpoint and of protein kinases Chk1 and Chk2 by the marine sponge alkaloid debromohymenialdisine: D. Curman, et al.; J. Biol. Chem. 276, 17914 (2001) Abstract; Full Text
An investigation of cell proliferation and soluble mediators induced by interleukin 1beta in human synovial fibroblasts: comparative response in osteoarthritis and rheumatoid arthritis: H. Inoue, et al.; Inflamm. Res. 50, 65 (2001) Abstract
Aldisine alkaloids from the Philippine sponge Stylissa massa are potent inhibitors of mitogen-activated protein kinase kinase-1 (MEK-1): D. Tasdemir, et al.; J. Med. Chem. 45, 529 (2002) Abstract
Inhibition of cytokine production by hymenialdisine derivatives: V. Sharma, et al.; J. Med. Chem. 47, 3700 (2004) Abstract
 
 
ALX-350-291 Revised 19-Oct-07
Hymenidin
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SYNONYMS 2-Debromooroidin
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products for Cell Cycle Research
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ALX-350-291-M001   1 mg 230.00 USD Add To Cart
Product Specification
FORMULA: C11H12BrN5O
MW: 310.2
CAS NUMBER: 107019-95-4
SOURCE/HOST: Isolated from Hymeniacidon sp.
PURITY: ≥95%
APPEARANCE: Amorphous solid.
SOLUBILITY: Soluble in DMSO or 100 % ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
HAZARD: TOXIC. CYTOTOXIC.

Product Description
Antagonist of serotonergic receptors. Inhibitor of CDK5/p25 (IC50=4µM) and GSK-3β (IC50=12µM). 
Product Specific Literature References
A novel antagonist of serotonergic receptors, hymenidin, isolated from the Okinawan marine sponge Hymeniacidon sp: J. Kobayashi, et al.; Experientia 42, 1176 (1986) Abstract
Inhibition of cyclin-dependent kinases, GSK-3beta and CK1 by hymenialdisine, a marine sponge constituent: L. Meijer, et al.; Chem. Biol. 7, 51 (2000)
Brominated pyrrole alkaloids from marine Agelas sponges reduce depolarization-induced cellular calcium elevation: U. Bickmeyer, et al.; Toxicon. 44, 45 (2004) Abstract
Marine compounds for the therapeutic treatment of neurological disorders: D. Alonso, et al.; Expert Opininon on Therapeutic Patents 15, 1377 (2005)
 
 
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-350-298 Revised 03-Apr-08
Betulinic acid (~95%)
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SYNONYMS 3β-Hydroxy-20(29)-lupaene-28-oic acid
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Antitumor Reagents
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ALX-350-298-M100   100 mg 55.00 USD Add To Cart
ALX-350-298-M500   500 mg 180.00 USD Add To Cart
ALX-350-298-G001   1 g 290.00 USD Add To Cart
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Product Specification
FORMULA: C30H48O3
MW: 456.7
CAS NUMBER: 472-15-1
SOURCE/HOST: Isolated from Platanus acerifolia (plane tree) bark.
PURITY: ≥95% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
Antitumor and anti-HIV agent. Induces apoptosis by activating mitochondrial permeability transition (MPT). Inhibits NF-κB activation and NF-κB-regulated gene expression induced by carcinogens and inflammatory stimuli. Decreases expression of Bcl-2 and cyclin D1. Potent proteasome activator.
Product Specific Literature References
Anti-AIDS agents, 11. Betulinic acid and platanic acid as anti-HIV principles from Syzigium claviflorum, and the anti-HIV activity of structurally related triterpenoids: T. Fujioka, et al.; J. Nat. Prod. 57, 243 (1994) Abstract
Discovery of betulinic acid as a selective inhibitor of human melanoma that functions by induction of apoptosis: E. Pisha, et al.; Nat. Med. 1, 1046 (1995) Abstract
Betulinic acid and dihydrobetulinic acid derivatives as potent anti-HIV agents: Y. Kashiwada, et al.; J. Med. Chem. 39, 1016 (1996) Abstract
Betulinic acid triggers CD95 (APO-1/Fas)- and p53-independent apoptosis via activation of caspases in neuroectodermal tumors: S. Fulda, et al.; Cancer Res. 57, 4956 (1997) Abstract
Anti-AIDS agents--XXVII. Synthesis and anti-HIV activity of betulinic acid and dihydrobetulinic acid derivatives: F. Hashimoto, et al.; Bioorg. Med. Chem. 5, 2133 (1997) Abstract
Betulinic acid induces apoptosis in human neuroblastoma cell lines: M.L. Schmidt, et al.; Eur. J. Cancer 33, 2007 (1997) Abstract
Induction of p53 without increase in p21WAF1 in betulinic acid-mediated cell death is preferential for human metastatic melanoma: M. Rieber & M. Strasberg Rieber; DNA Cell Biol. 17, 399 (1998) Abstract
Activation of mitochondria and release of mitochondrial apoptogenic factors by betulinic acid: S. Fulda, et al.; J. Biol. Chem. 273, 33942 (1998) Abstract; Full Text
Betulinic acid inhibits aminopeptidase N activity: M.F. Melzig & H. Bormann; Planta Med. 64, 655 (1998) Abstract
Correspondence re: S. Fulda et al., Betulinic acid triggers CD95 (Apo1/Fas)- and p53-independent apoptosis via activation of caspases in neuroectodermal tumors. Cancer Res., 57: 4956, 1997: M. Rieber & M. Strasberg Rieber; Cancer. Res. 58, 5876 (1998) Abstract
Betulinic acid: a new cytotoxic agent against malignant brain-tumor cells: S. Fulda, et al.; Int. J. Cancer 82, 435 (1999) Abstract
Betulinic acid-induced apoptosis in glioma cells: A sequential requirement for new protein synthesis, formation of reactive oxygen species, and caspase processing: W. Wick, et al.; J Pharmacol. Exp. Ther. 289, 1306 (1999) Abstract; Full Text
Effects of betulinic acid alone and in combination with irradiation in human melanoma cells: E. Selzer, et al.; J. Invest. Dermatol. 114, 935 (2000) Abstract
Betulinic acid suppresses carcinogen-induced NF-kappa B activation through inhibition of I kappa B alpha kinase and p65 phosphorylation: abrogation of cyclooxygenase-2 and matrix metalloprotease-9: Y. Takada & B.B. Aggarwal; J. Immunol. 171, 3278 (2003) Abstract
Chemistry, biological activity, and chemotherapeutic potential of betulinic acid for the prevention and treatment of cancer and HIV infection: R.H. Cichewicz & S.A. Kouzi; Med. Res. Rev. 24, 90 (2004), Review Abstract
Betulinic acid-induced apoptosis in leukemia cells: H. Ehrhardt, et al.; Leukemia 18, 1406 (2004) Abstract
Betulinic acid and its derivatives: a review on their biological properties: P. Yogeeswari & D. Sriram; Curr. Med. Chem. 12, 657 (2005), Review Abstract
Betulinic acid decreases expression of bcl-2 and cyclin D1, inhibits proliferation, migration and induces apoptosis in cancer cells: W. Rzeski, et al.; Naunyn Schmiedebergs Arch. Pharmacol. 374, 11 (2006) Abstract
Activation and inhibition of the proteasome by betulinic acid and its derivatives: L. Huang, et al.; FEBS Lett. 581, 4955 (2007) Abstract