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Ro5-3335

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Catalog No. T4687Cas No. 30195-30-3
Alias Ro 5-3335, CBFβ-Runx1 inhibitor II

Ro5-3335 (CBFβ-Runx1 inhibitor II) is core binding factor (CBF) inhibitor; preferentially kills human leukemia cell lines with CBF fusion proteins (IC50 = 1.1 μM). Ro5-3335 represses RUNX1/CBFβ-dependent transactivation in reporter assays and inhibits transcriptional regulation by RUNX1 and CBFβ. Ro5-3335 also reduces the leukemia burden in a mouse model. Attenuates RUNX1-dependent hematopoiesis in zebrafish embryos. It also is a Tat antagonist and inhibits HIV-1 replication in vitro.

Ro5-3335

Ro5-3335

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Purity: 99.87%
Catalog No. T4687Alias Ro 5-3335, CBFβ-Runx1 inhibitor IICas No. 30195-30-3
Ro5-3335 (CBFβ-Runx1 inhibitor II) is core binding factor (CBF) inhibitor; preferentially kills human leukemia cell lines with CBF fusion proteins (IC50 = 1.1 μM). Ro5-3335 represses RUNX1/CBFβ-dependent transactivation in reporter assays and inhibits transcriptional regulation by RUNX1 and CBFβ. Ro5-3335 also reduces the leukemia burden in a mouse model. Attenuates RUNX1-dependent hematopoiesis in zebrafish embryos. It also is a Tat antagonist and inhibits HIV-1 replication in vitro.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$42In StockIn Stock
5 mg$97In StockIn Stock
10 mg$139In StockIn Stock
25 mg$272In StockIn Stock
50 mg$455In StockIn Stock
100 mg$596-In Stock
1 mL x 10 mM (in DMSO)$96In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:99.87%
Appearance:Solid
Color:White to Yellow
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Product Introduction

Ro5-3335 AI Summary
Ro5-3335 exhibits a variety of bioactivities, including the inhibition of HIV-1 replication, with IC50 values of 600.0 nM in H9 cells and 4000.0 nM in SW480 cells. It also inhibits the Tat-induced HIV1 LTR transactivation with an IC50 value of 100.0 nM and the nuclear regulatory protein Tat with an IC50 value of 4000.0 nM. The compound has a therapeutic index of 5.9 as determined by a whole cell assay. Beyond HIV-1, Ro5-3335 shows various other biological activities, such as acting as a modulator of miRNAs, inhibitor of the Menin-MLL interaction in MLL-related leukemias, BAZ2B inhibition, ELG1-dependent DNA repair inhibition, delayed death inhibition of the malarial parasite plastid, and uPA inhibition on cell surfaces. It also blocks the interaction between CBF-beta and RUNX1 for Acute Myeloid Leukemia treatment, induces DNA re-replication in colon adenocarcinoma cells, reduces ATXN expression, functions as a GLP-1 receptor inverse agonist, stimulates the gsp mutation responsible for Fibrous Dysplasia/McCune-Albright Syndrome, inhibits human tyrosyl-DNA phosphodiesterase 1 both without and with CPT, and inhibits AMA1-RON for antimalarial development. Moreover, it displays antibacterial activity against Klebsiella pneumoniae MDR, Staphylococcus aureus MRSA, and Acinetobacter baumannii, and exerts antifungal effects against Candida albicans and Cryptococcus neoformans, though the latter efficacy is relatively low..
Note: Summary generated by AI. Data source: ChEMBL
Bioactivity
Description
Ro5-3335 (CBFβ-Runx1 inhibitor II) is core binding factor (CBF) inhibitor; preferentially kills human leukemia cell lines with CBF fusion proteins (IC50 = 1.1 μM). Ro5-3335 represses RUNX1/CBFβ-dependent transactivation in reporter assays and inhibits transcriptional regulation by RUNX1 and CBFβ. Ro5-3335 also reduces the leukemia burden in a mouse model. Attenuates RUNX1-dependent hematopoiesis in zebrafish embryos. It also is a Tat antagonist and inhibits HIV-1 replication in vitro.
Targets&IC50
CBF:1.1 μM
SynonymsRo 5-3335, CBFβ-Runx1 inhibitor II
Chemical Properties
Molecular Weight259.69
FormulaC13H10ClN3O
Cas No.30195-30-3
SmilesClc1ccc2NC(=O)CN=C(c3ccc[nH]3)c2c1
Relative Density.1.46g/cm3
Storage & Solubility Information
StorageIn solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 60 mg/mL (231.04 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (7.7 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM3.8507 mL19.2537 mL38.5075 mL192.5373 mL
5 mM0.7701 mL3.8507 mL7.7015 mL38.5075 mL
10 mM0.3851 mL1.9254 mL3.8507 mL19.2537 mL
20 mM0.1925 mL0.9627 mL1.9254 mL9.6269 mL
50 mM0.0770 mL0.3851 mL0.7701 mL3.8507 mL
100 mM0.0385 mL0.1925 mL0.3851 mL1.9254 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

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