Catalog No.S3603 Synonyms: ALS-357
Molecular Weight(MW): 456.7
Betulinic acid, a pentacyclic triterpenoid from Syzigium claviflorum, is a inhibitor of HIV-1 with EC50 of 1.4 μ M. Phase 1/2.
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3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.
|Description||Betulinic acid, a pentacyclic triterpenoid from Syzigium claviflorum, is a inhibitor of HIV-1 with EC50 of 1.4 μ M. Phase 1/2.|
Betulinic acid shows anti-HIV activity by blocking HIV replication in H9 lymphocytes with an EC50 value of 1.4 μM and inhibiting uninfected H9 cell growth with an IC50 value of 13 μM.  Betulinic acid also acts as anti-melanoma agent through inhibiting aminopeptidase N activity with IC50 of 7.3 μM.  In addition, Betulinic acid inhibits eukaryotic topoisomerase I activity with IC50 of 5 μM and can be exploited as a strong candidate for anti-tumor drug. 
|In vivo||Betulinic acid inhibits prostate cancer cell and tumor (xenograft) growth in athymic nude mice bearing LNCaP cells and this is due, in part, to proteasome-dependent downregulation of Sp1, Sp3, Sp4 and several Sp-regulated genes. |
Topoisomerase I-DNA interaction:Annealed 25-mer duplex of oligonucleotide-1 and oligonicleotide-2 is incubated with 25 or 50 units of rat liver topoisomerase I at 8 °C for 15 min in the presence or absence of betulinic acid in binding buffer. After incubation the reaction mixtures are electrophoresed in 7% non-denaturing polyacrylamide gel at 4 °C in 0.167 × TBE buffer and DNA bands are stained with ethidium bromid
|In vitro||DMSO||20 mg/mL (43.79 mM)|
|Ethanol||10 mg/mL (21.89 mM)|
* 1 mg/ml means slightly soluble or insoluble.
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT00346502||Suspended||Dysplastic Nevus Syndrome||University of Illinois at Chicago||January 2006||Phase 1|Phase 2|
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