Ro 5-3335
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MedKoo CAT#: 574863

CAS#: 30195-30-3

Description: Ro 5-3335 is a Core Binding Factor (CBF) inhibitor that represses RUNX1/CBFβ-dependent transactivation in reporter assays and inhibits transcriptional regulation by RUNX1 and CBFβ.

Chemical Structure

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Ro 5-3335
CAS# 30195-30-3
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 574863
Name: Ro 5-3335
CAS#: 30195-30-3
Chemical Formula: C13H10ClN3O
Exact Mass: 259.05
Molecular Weight: 259.690
Elemental Analysis: C, 60.13; H, 3.88; Cl, 13.65; N, 16.18; O, 6.16

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10mg USD 410 2 Weeks
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Related CAS #: 139339-45-0   2328140-37-8   30195-30-3    

Synonym: CBFβ-Runx1 inhibitor II; Ro 5-3335

IUPAC/Chemical Name: 7-Chloro-1,3-dihydro-5-(1H-pyrrol-2-yl)-2H-1,4-benzodiazepin-2-one

InChi Key: XWNMORIHKRROGW-UHFFFAOYSA-N

InChi Code: InChI=1S/C13H10ClN3O/c14-8-3-4-10-9(6-8)13(11-2-1-5-15-11)16-7-12(18)17-10/h1-6,15H,7H2,(H,17,18)

SMILES Code: O=C1CN=C(C3=CC=CN3)C2=C(C=CC(Cl)=C2)N1

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >3 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Product Data:
Product Data
Instruction:
View handling instruction
Biological target: Ro 5-3335 preferentially kills human leukemia cell lines with CBF fusion proteins (IC50 = 1.1 μM). It represses RUNX1/CBFβ-dependent transactivation in reporter assays and inhibits transcriptional regulation by RUNX1 and CBFβ. Ro 5-3335 is also a Tat antagonist that inhibits HIV-1 replication in vitro.
In vitro activity: Ro5-3335 significantly inhibited the heat shock induced virus activation. This study infected the OM10.1 cell line with heat shock at 42 degrees C for 2 h and found that it resulted in a high level of HIV-1 production without the addition of any cytokines. Reference: Arch Virol. 1996;141(3-4):439-47. https://pubmed.ncbi.nlm.nih.gov/8645086/
In vivo activity: Treatment with Ro 5-3335 protected mice from lipopolysaccharide (LPS)-induced endotoxic shock and substantially reduced the IL-6 levels. Overexpression of RUNX1 promoted IL-1β and IL-6 production in response to LPS stimulation. These findings suggest that RUNX1 may be a new potential target for resolving TLR4-associated uncontrolled inflammation and preventing sepsis. Reference: J Biol Chem. 2016 Oct 14;291(42):22011-22020. https://pubmed.ncbi.nlm.nih.gov/27573239/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 26.0 100.00

Preparing Stock Solutions

The following data is based on the product molecular weight 259.69 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Hashimoto K, Baba M, Gohnai K, Sato M, Shigeta S. Heat shock induces HIV-1 replication in chronically infected promyelocyte cell line OM10.1. Arch Virol. 1996;141(3-4):439-47. doi: 10.1007/BF01718308. PMID: 8645086. 2. Luo MC, Zhou SY, Feng DY, Xiao J, Li WY, Xu CD, Wang HY, Zhou T. Runt-related Transcription Factor 1 (RUNX1) Binds to p50 in Macrophages and Enhances TLR4-triggered Inflammation and Septic Shock. J Biol Chem. 2016 Oct 14;291(42):22011-22020. doi: 10.1074/jbc.M116.715953. Epub 2016 Aug 29. PMID: 27573239; PMCID: PMC5063984.
In vitro protocol: 1. Hashimoto K, Baba M, Gohnai K, Sato M, Shigeta S. Heat shock induces HIV-1 replication in chronically infected promyelocyte cell line OM10.1. Arch Virol. 1996;141(3-4):439-47. doi: 10.1007/BF01718308. PMID: 8645086.
In vivo protocol: 1. Luo MC, Zhou SY, Feng DY, Xiao J, Li WY, Xu CD, Wang HY, Zhou T. Runt-related Transcription Factor 1 (RUNX1) Binds to p50 in Macrophages and Enhances TLR4-triggered Inflammation and Septic Shock. J Biol Chem. 2016 Oct 14;291(42):22011-22020. doi: 10.1074/jbc.M116.715953. Epub 2016 Aug 29. PMID: 27573239; PMCID: PMC5063984.

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1. Cunningham et al (2012) Identification of benzodiazepine Ro5-3335 as an inhibitor of CBF leukemia through quantitative high throughput screen against RUNX1-CBF beta interaction. Proc.Natl.Acad.Sci.USA 109 14592 PMID: 22912405

2. Cupelli et al (1995) The human immunodeficiency virus type 1 Tat antagonist, Ro 5-3335, predominantly inhibits transcription initiation from the viral promoter. J.Virol. 69 2640 PMID: 7884917

3. Okuda et al (2001) RUNX1/AML1: a central player in hematopoiesis. Int. J. Hematol. 74 252 PMID: 11721959