Cat. No.: HY-108470

Ro5-3335

13 Cited Publications

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Based on 13 publication(s) in Google Scholar

Ro5-3335, a benzodiazepine, acts as an inhibitor of core binding factor (CBF) leukemia. Ro5-3335 is a RUNX1-CBFβ interaction inhibitor that represses RUNX1/CBFB-dependent transactivation.

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Pureté: 99.35%
CAS No.: 30195-30-3
Formule: C₁₃H₁₀ClN₃O
Masse moléculaire:259.69

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Ro5-3335 Chemical Structure

CAS No.: 30195-30-3

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (13)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

Ro5-3335, a benzodiazepine, acts as an inhibitor of core binding factor (CBF) leukemia. Ro5-3335 is a RUNX1-CBFβ interaction inhibitor that represses RUNX1/CBFB-dependent transactivation^[1].

IC₅₀ & Target

RUNX1

Voir tous les produits spécifiques à Isoform RUNX :

RUNX1
RUNX2

Cellular Effect

Cell Line	Type	Value	Description	References
H9	IC₅₀	0.6 μM Compound: 1	Inhibition of HIV replication in H9 cells. Inhibition of HIV replication in H9 cells.	[PMID: 7650672]
H9	IC₅₀	0.6 μM Compound: 1	Inhibition of HIV-1 replication in H9 cells infected with three different concentrations of HIV IIIB strain Inhibition of HIV-1 replication in H9 cells infected with three different concentrations of HIV IIIB strain	[PMID: 8410982]
SW480	IC₅₀	4 μM Compound: 1	The compound was tested for inhibition of HIV-1 replication in SW480 cells using HIV tat assay The compound was tested for inhibition of HIV-1 replication in SW480 cells using HIV tat assay	[PMID: 7650672]

In Vitro

Ro5-3335 has antiproliferative activity against human CBF leukemia cell lines, with IC₅₀s of 1.1 μM, 21.7 μM and 17.3 μM for ME-1, Kasumi-1 and REH, respectively^[1].
Ro5-3335 inhibits definitive hematopoiesis in zebrafish embryos^[1].
Ro5-3335 does not completely break apart RUNX1-CBFβ interaction, but changes the conformation of their complex or increases the distance between RUNX1 and CBFβ in the complex^[1].

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

In Vivo

Ro5-3335 is identified as an inhibitor of RUNX1–CBFβ function in zebrafish models^[1].
Ro5-3335 rescues preleukemic phenotype in a RUNX1-ETO transgenic zebrafish^[1].
Ro5-3335 (300 mg/kg/d; p.o; for 30 days) reduces leukemia burden in a mouse CBFB-MYH11 leukemia model^[1].

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

Animal Model:

C57BL/6 mice (leukemic model)^[1]
Dosage:

300 mg/kg
Administration:

Oral administration; daily; for 30 days
Result:

Reduced the number of c-kit⁺ cells in the transplanted mice and leukemic cell infiltration in the livers, bone marrow and spleen.

Chemical Information

CAS No. 30195-30-3
Appearance Solid
Masse moléculaire 259.69
Formule C₁₃H₁₀ClN₃O
Color Off-white to light yellow
SMILES

O=C1NC2=CC=C(Cl)C=C2C(C3=CC=CN3)=NC1
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (13)

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Journal Impact Factor

Nat Immunol

Tumor cell-released kynurenine biases MEP differentiation into megakaryocytes in individuals with cancer by activating AhR-RUNX1. [Abstract]

2023 Dec;24(12):2042-2052. PMID: 37919525

Ro5-3335 purchased from MedChemExpress. Usage Cited in: Nat Immunol. 2023 Dec;24(12):2042-2052. [Abstract]

MEPs were isolated from healthy C57BL/6J mice and treated with Kyn or Kyn combined with the RUNX1 inhibitor Ro5-3335 (2 μM) in collagen medium for 7 d, and a c.f.u. analysis was performed.
Nat Commun

Erythropoietin regulates energy metabolism through EPO-EpoR-RUNX1 axis. [Abstract]

2024 Sep 16;15(1):8114. PMID: 39284834

Ro5-3335 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Sep 16;15(1):8114. [Abstract]

Western blotting for scWAT RUNX1 protein in WT (dark gray) and Tg6 (red) mice treated with RUNX1 inhibitor Ro5-3335 (5 mg/kg; s.c.; every other day for six times) or DMSO control. Ro5-3335 attenuated the increase in RUNX1 protein in scWAT of Tg6-mice compared with WT-mice.

Ro5-3335 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Sep 16;15(1):8114. [Abstract]

Lipid metabolism gene expression (qPCR) in scWAT of WT and Tg6-mice treated with RUNX1 inhibitor Ro5-3335 (5 mg/kg; s.c.; every other day for six times). Ro5-3335 administration attenuated the changes observed in Tg6-mice associated with high EPO on expression of lipid metabolismgenes.
Theranostics

Methyl-CpG-binding 2 K271 lactylation-mediated M2 macrophage polarization inhibits atherosclerosis. [Abstract]

2024 Jul 8;14(11):4256-4277. PMID: 39113793

Ro5-3335 purchased from MedChemExpress. Usage Cited in: Theranostics. 2024 Jul 8;14(11):4256-4277. [Abstract]

ApoE^-/- mice receiving HFD for 8 weeks were treated with Ro5-3335 (25 mg/kg; i.p.; twice a week for 4 weeks; DMSO) or DMSO starting at week 8. Representative images and quantification of atherosclerotic area in cross-sections of aortic root of ApoE^-/- mice treated with Ro5-3335 and DMSO by HE, Oil Red O and Masson staining.

Ro5-3335 purchased from MedChemExpress. Usage Cited in: Theranostics. 2024 Jul 8;14(11):4256-4277. [Abstract]

Representative images of immunofluorescence co-staining for RUNX1 together with macrophage maker F4/80 and M2 macrophage marker CD206 in aortic root plaques from ApoE^-/- mice treated with Ro5-3335 (25 mg/kg; i.p.; twice a week for 4 weeks; DMSO) and DMSO, with quantification of immunofluorescence intensity.
Arch Pharm Res

Salvianolic acid A enhances Treg accumulation via the RUNX1/CBFβ/FOXP3 axis as a neuroprotective immunomodulator in ischemic stroke. [Abstract]

2025 Dec;48(11-12):1399-1419. PMID: 41201767
Free Radic Biol Med

Cannabidiol mitigates radiation-induced intestine ferroptosis via facilitating the heterodimerization of RUNX3 with CBFβ thereby promoting transactivation of GPX4. [Abstract]

2024 Sep:222:288-303. PMID: 38830513
Cell Rep

CDK12 inhibition reveals melanoma dependence on the RUNX1/CBFβ complex for genomic stability. [Abstract]

2025 Nov 25;44(11):116495. PMID: 41176765
Biochem Pharmacol

Scutellarin suppresses the metastasis of triple-negative breast cancer via targeting TNFα/TNFR2-RUNX1-triggered G-CSF expression in endothelial cells. [Abstract]

2023 Nov:217:115808. PMID: 37716622
Brain Res Bull

Dendrobine attenuates postoperative cognitive dysfunction by inhibiting Runx1-mediated NF-κB signaling pathway. [Abstract]

2026 Feb:235:111746. PMID: 41616945
Adv Ophthalmol Pract Res

2025 Nov 21.
J Immunol

TLR7-mediated immune response of renal myeloid-derived suppressor cells via RUNX1-KLF4 in systemic candidiasis. [Abstract]

2025 Aug 7:vkaf170. PMID: 40795213
J Dent Sci

Kartogenin potentially protects temporomandibular joints from collagenase-induced osteoarthritis via core binding factor β and runt-related transcription factor 1 binding - A rat model study. [Abstract]

2023 Oct;18(4):1553-1560. PMID: 37799879
bioRxiv

Impaired SOX17 Expression Causes Endothelial Dysfunction and Pulmonary Arterial Hypertension by Insufficient Suppression of RUNX1. [Abstract]

2026 May 15:2026.05.14.725187. PMID: 42182299
bioRxiv

Cholangiocyte RUNX1 Orchestrates Fibrogenic and Inflammatory Signaling to Drive Biliary Fibrosis. [Abstract]

2026 May 22:2026.05.20.726667. PMID: 42239059

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (385.07 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.8507 mL

19.2537 mL

38.5075 mL

5 mM

0.7701 mL

3.8507 mL

7.7015 mL

10 mM

0.3851 mL

1.9254 mL

3.8507 mL

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (9.63 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (9.63 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (282 KB)
SDS (393 KB)
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COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Cunningham L, et al. Identification of benzodiazepine Ro5-3335 as an inhibitor of CBF leukemia through quantitative high throughput screen against RUNX1-CBFβ interaction. Proc Natl Acad Sci U S A. 2012 Sep 4;109(36):14592-7. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.8507 mL	19.2537 mL	38.5075 mL	96.2686 mL
	5 mM	0.7701 mL	3.8507 mL	7.7015 mL	19.2537 mL
	10 mM	0.3851 mL	1.9254 mL	3.8507 mL	9.6269 mL
	15 mM	0.2567 mL	1.2836 mL	2.5672 mL	6.4179 mL
	20 mM	0.1925 mL	0.9627 mL	1.9254 mL	4.8134 mL
	25 mM	0.1540 mL	0.7701 mL	1.5403 mL	3.8507 mL
	30 mM	0.1284 mL	0.6418 mL	1.2836 mL	3.2090 mL
	40 mM	0.0963 mL	0.4813 mL	0.9627 mL	2.4067 mL
	50 mM	0.0770 mL	0.3851 mL	0.7701 mL	1.9254 mL
	60 mM	0.0642 mL	0.3209 mL	0.6418 mL	1.6045 mL
	80 mM	0.0481 mL	0.2407 mL	0.4813 mL	1.2034 mL
	100 mM	0.0385 mL	0.1925 mL	0.3851 mL	0.9627 mL

Keywords

Ro5-3335

13 Cited Publications

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Ro5-3335

Stem Cell Signaling Compound Library

TGF-beta/Smad Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Anti-Blood Cancer Compound Library

Transcription Factor-Targeted Library

Targeted Diversity Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

Anti-Aging Compound Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) Ro5-3335

Voir tous les produits spécifiques à Isoform RUNX

Activité biologique

Chemical Information

Publications (13)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Ro5-3335

Stem Cell Signaling Compound Library

TGF-beta/Smad Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Anti-Blood Cancer Compound Library

Transcription Factor-Targeted Library

Targeted Diversity Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

Anti-Aging Compound Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) Ro5-3335

Voir tous les produits spécifiques à Isoform RUNX

Activité biologique

Chemical Information

Publications (13)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Ro5-3335 Related Classifications

HY-108470 Related Classifications