1. Anti-infection Cell Cycle/DNA Damage
  2. HIV Reverse Transcriptase Telomerase Bacterial
  3. β-Rubromycin

β-Rubromycin, a quinone antibacterial agent, is a selective HIV-1 reverse transcriptase inhibitor with a Ki of 0.27 μM. β-Rubromycin is a potent telomerase inhibitor with an IC50 of 3 μM. β-Rubromycin inhibits the proliferation of both K-562 and HeLa cells with IC50 values of 19.5 µM and 22.7 µM, respectively.

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β-Rubromycin Chemical Structure

β-Rubromycin Chemical Structure

CAS No. : 27267-70-5

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Description

β-Rubromycin, a quinone antibacterial agent, is a selective HIV-1 reverse transcriptase inhibitor with a Ki of 0.27 μM. β-Rubromycin is a potent telomerase inhibitor with an IC50 of 3 μM. β-Rubromycin inhibits the proliferation of both K-562 and HeLa cells with IC50 values of 19.5 µM and 22.7 µM, respectively[1][2].

IC50 & Target

HIV-1

 

Cellular Effect
Cell Line Type Value Description References
A549 EC50
> 100 μM
Compound: 7
Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by alamar blue assay
Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by alamar blue assay
[PMID: 31833370]
HeLa IC50
1.32 μM
Compound: 1, beta-R
Inhibition of telomerase in human HeLa cells using 5'-AAT CCG TCG AGC AGA GTT-3' as substrate incubated for 15 mins prior to extension reaction by telomeric repeat amplification protocol
Inhibition of telomerase in human HeLa cells using 5'-AAT CCG TCG AGC AGA GTT-3' as substrate incubated for 15 mins prior to extension reaction by telomeric repeat amplification protocol
[PMID: 22413845]
HeLa IC50
1.53 μM
Compound: 1, beta-R
Inhibition of telomerase in human HeLa cells using 5'-AAT CCG TCG AGC AGA GTT-3' as substrate incubated for 15 mins prior to extension reaction followed by compound washout by spin-telomeric repeat amplification protocol
Inhibition of telomerase in human HeLa cells using 5'-AAT CCG TCG AGC AGA GTT-3' as substrate incubated for 15 mins prior to extension reaction followed by compound washout by spin-telomeric repeat amplification protocol
[PMID: 22413845]
K562 IC50
3.06 μM
Compound: 1, beta-R
Inhibition of telomerase in human K562 cells by modified telomeric repeat amplification protocol
Inhibition of telomerase in human K562 cells by modified telomeric repeat amplification protocol
[PMID: 22413845]
PC-3 EC50
> 100 μM
Compound: 7
Antiproliferative activity against human PC3 cells assessed as reduction in cell viability after 72 hrs by alamar blue assay
Antiproliferative activity against human PC3 cells assessed as reduction in cell viability after 72 hrs by alamar blue assay
[PMID: 31833370]
In Vitro

β-Rubromycin inhibits equipotently HIV-1 RT and avian myeloblastosis virus RT, in a concentration-dependent manner, and is significantly weaker as an inhibitor of calf thymus DNA polymerase α[1].
A kinetic study of the inhibition by β-Rubromycin revealed a competitive interaction with respect to the telomerase substrate primer, with a Ki of 0.74 μM, whereas a mixed type inhibition was observed with respect to the nucleotide substrate[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

536.44

Formula

C27H20O12

CAS No.
Appearance

Solid

Color

Brown to reddish brown

SMILES

O=C(C(O1)=CC(C=C(CC[C@@]2(OC(C3=O)=C(C(C4=C3C(O)=C(OC)C=C4OC)=O)C2)O5)C5=C6O)=C6C1=O)OC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 1 mg/mL (1.86 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8641 mL 9.3207 mL 18.6414 mL
5 mM --- --- ---
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation

Purity: 97.7%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8641 mL 9.3207 mL 18.6414 mL 46.6035 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
β-Rubromycin
Cat. No.:
HY-122482
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