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MedKoo Cat#: 574863 | Name: Ro 5-3335
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

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

Ro 5-3335
Ro 5-3335
CAS#30195-30-3

Theoretical Analysis

MedKoo Cat#: 574863

Name: Ro 5-3335

CAS#: 30195-30-3

Chemical Formula: C13H10ClN3O

Exact Mass: 259.0512

Molecular Weight: 259.69

Elemental Analysis: C, 60.13; H, 3.88; Cl, 13.65; N, 16.18; O, 6.16

Price and Availability

Size Price Availability Quantity
10mg USD 600.00 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/
Solvent mg/mL mM
Solubility
DMSO 26.0 100.00
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

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.
1: Deng M, Guo J, Ling Z, Zhang C, He L, Fan Z, Cheng B, Xia J. KRAS mutations upregulate Runx1 to promote occurrence of head and neck squamous cell carcinoma. Mol Carcinog. 2023 Sep;62(9):1284-1294. doi: 10.1002/mc.23563. Epub 2023 May 24. PMID: 37222390. 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. 3: Mei HY, Mack DP, Galan AA, Halim NS, Heldsinger A, Loo JA, Moreland DW, Sannes-Lowery KA, Sharmeen L, Truong HN, Czarnik AW. Discovery of selective, small-molecule inhibitors of RNA complexes--I. The Tat protein/TAR RNA complexes required for HIV-1 transcription. Bioorg Med Chem. 1997 Jun;5(6):1173-84. doi: 10.1016/s0968-0896(97)00064-3. PMID: 9222511. 4: Kira T, Hashimoto K, Baba M, Okamoto T, Shigeta S. 2-Glycineamide-5-chlorophenyl 2-pyrryl ketone, a non-benzodiazepin Tat antagonist, is effective against acute and chronic HIV-1 infections in vitro. Antiviral Res. 1996 Oct;32(2):55-62. doi: 10.1016/0166-3542(95)00980-9. PMID: 8891164. 5: Silvestri R, Artico M, Pagnozzi E, Stefancich G, Massa S, La Colla P, Loi AG, Spiga MG, Corrias S, Lichino D. Synthesis and anti-HIV activity of 10,11-dihydropyrrolo [1,2-b][1,2,5]benzothiadiazepine-11-acetic acid 5,5-dioxide derivatives and related compounds. Farmaco. 1996 Jun;51(6):425-30. PMID: 8766226. 6: 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. 7: Desai-Yajnik V, Hadzic E, Modlinger P, Malhotra S, Gechlik G, Samuels HH. Interactions of thyroid hormone receptor with the human immunodeficiency virus type 1 (HIV-1) long terminal repeat and the HIV-1 Tat transactivator. J Virol. 1995 Aug;69(8):5103-12. doi: 10.1128/JVI.69.8.5103-5112.1995. PMID: 7609079; PMCID: PMC189328. 8: Thormar H, Balzarini J, Debyser Z, Witvrouw M, Desmyter J, De Clercq E. Inhibition of visna virus replication and cytopathic effect in sheep choroid plexus cell cultures by selected anti-HIV agents. Antiviral Res. 1995 May;27(1-2):49-57. doi: 10.1016/0166-3542(94)00082-j. PMID: 7486958. 9: Cupelli LA, Hsu MC. The human immunodeficiency virus type 1 Tat antagonist, Ro 5-3335, predominantly inhibits transcription initiation from the viral promoter. J Virol. 1995 Apr;69(4):2640-3. doi: 10.1128/JVI.69.4.2640-2643.1995. PMID: 7884917; PMCID: PMC188946. 10: Dunne AL, Siregar H, Mills J, Crowe SM. HIV replication in chronically infected macrophages is not inhibited by the Tat inhibitors Ro-5-3335 and Ro-24-7429. J Leukoc Biol. 1994 Sep;56(3):369-73. doi: 10.1002/jlb.56.3.369. PMID: 8083610. 11: Popik W, Pitha PM. Differential effect of tumor necrosis factor-alpha and herpes simplex virus type 1 on the Tat-targeted inhibition of human immunodeficiency virus type 1 replication. Virology. 1994 Aug 1;202(2):521-9. doi: 10.1006/viro.1994.1374. PMID: 8030218. 12: Braddock M, Cannon P, Muckenthaler M, Kingsman AJ, Kingsman SM. Inhibition of human immunodeficiency virus type 1 Tat-dependent activation of translation in Xenopus oocytes by the benzodiazepine Ro24-7429 requires trans-activation response element loop sequences. J Virol. 1994 Jan;68(1):25-33. doi: 10.1128/JVI.68.1.25-33.1994. PMID: 8254735; PMCID: PMC236260. 13: Kiso Y, Kisanuki S. [Anti-HIV compounds]. Nihon Rinsho. 1993 Sep;51 Suppl:235-40. Japanese. PMID: 8271390. 14: Hsu MC, Dhingra U, Earley JV, Holly M, Keith D, Nalin CM, Richou AR, Schutt AD, Tam SY, Potash MJ, et al. Inhibition of type 1 human immunodeficiency virus replication by a tat antagonist to which the virus remains sensitive after prolonged exposure in vitro. Proc Natl Acad Sci U S A. 1993 Jul 15;90(14):6395-9. doi: 10.1073/pnas.90.14.6395. PMID: 8341644; PMCID: PMC46938. 15: Camsonne R, Bigot MC, Fusibet H, Moulin MA. Potentiel thérapeutique du Ro 5-3335. Une nouvelle benzodiazépine active in vitro contre les virus HIV-1 résistants ou non à l'AZT [Therapeutic potential of Ro 5-3335. New active benzodiazepine in vitro against HIV-1 viruses resistant or non-resistant to AZT]. Therapie. 1993 Mar-Apr;48(2):105-7. French. Erratum in: Therapie 1993 May- Jun;48(3):280. PMID: 8351676. 16: Witvrouw M, Pauwels R, Vandamme AM, Schols D, Reymen D, Yamamoto N, Desmyter J, De Clercq E. Cell type-specific anti-human immunodeficiency virus type 1 activity of the transactivation inhibitor Ro5-3335. Antimicrob Agents Chemother. 1992 Dec;36(12):2628-33. doi: 10.1128/AAC.36.12.2628. PMID: 1282790; PMCID: PMC245518. 17: Potash MJ, Bentsman G, McKinley G, Volsky DJ. A Tat antagonist inhibits HIV-1 induction in naturally infected and experimentally infected T cells. Biochem Biophys Res Commun. 1992 Nov 30;189(1):250-6. doi: 10.1016/0006-291x(92)91551-z. PMID: 1449479. 18: Shahabuddin M, Volsky B, Hsu MC, Volsky DJ. Restoration of cell surface CD4 expression in human immunodeficiency virus type 1-infected cells by treatment with a Tat antagonist. J Virol. 1992 Nov;66(11):6802-5. doi: 10.1128/JVI.66.11.6802-6805.1992. PMID: 1404619; PMCID: PMC240182. 19: Town C, Chang D, Henderson L, Garland WA. Disposition of the human immunodeficiency virus Tat inhibitor, Ro 5-3335, in rats and dogs. Drug Metab Dispos. 1992 Nov-Dec;20(6):954-7. PMID: 1362952. 20: Hsu MC, Schutt AD, Holly M, Slice LW, Sherman MI, Richman DD, Potash MJ, Volsky DJ. Discovery and characterization of an HIV-1 Tat antagonist. Biochem Soc Trans. 1992 May;20(2):525-31. doi: 10.1042/bst0200525. PMID: 1397654.