BH3I-1
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MedKoo CAT#: 406839

CAS#: 300817-68-9

Description: BH3I-1 is a Bcl-2 family inhibitor. BH3I-1 appeared to induce a dose- and time-dependent apoptosis in H460 and H1792 cells, regardless of p53 status. After 2 days of BH3I-1 treatment, the cells that remained attached were exposed to ionizing radiation. Followed by clonogenic assay, BH3I-1 treatment enhanced the radiation sensitivity of H1792 surviving cells with mutant p53, but not in H460 cells with wild-type p53. A transient time-dependent cell cycle blockade at G2-M phase was identified for H1792 cells without subsequent modification of cell cycle distribution.


Price and Availability

Size
Price

1g
USD 2650
Size
Price

2g
USD 3950
Size
Price

5g
Ask price

BH3I-1, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 406839
Name: BH3I-1
CAS#: 300817-68-9
Chemical Formula: C15H14BrNO3S2
Exact Mass: 398.9598
Molecular Weight: 400.305
Elemental Analysis: C, 45.01; H, 3.53; Br, 19.96; N, 3.50; O, 11.99; S, 16.02


Synonym: BH3I-1; BH 3I-1; BH-3I-1; BH3I1; BH 3I1; BH-3I1.

IUPAC/Chemical Name: 5-[(4-bromophenyl)methylene]-a-(1-methylethyl)-4-oxo-2-thioxo-3-thiazolidineacetic acid

InChi Key: COHIEJLWRGREHV-YRNVUSSQSA-N

InChi Code: InChI=1S/C15H14BrNO3S2/c1-8(2)12(14(19)20)17-13(18)11(22-15(17)21)7-9-3-5-10(16)6-4-9/h3-8,12H,1-2H3,(H,19,20)/b11-7+

SMILES Code: O=C(O)C(C(C)C)N(C/1=O)C(SC1=C\C2=CC=C(Br)C=C2)=S


Technical Data

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:
>2 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).

Harmonized System Code:
293490


References

1: Varadarajan S, Vogler M, Butterworth M, Dinsdale D, Walensky LD, Cohen GM. Evaluation and critical assessment of putative MCL-1 inhibitors. Cell Death Differ. 2013 Nov;20(11):1475-84. doi: 10.1038/cdd.2013.79. Epub 2013 Jul 5. PubMed PMID: 23832116; PubMed Central PMCID: PMC3792441.

2: Porter JR, Helmers MR, Wang P, Furman JL, Joy ST, Arora PS, Ghosh I. Profiling small molecule inhibitors against helix-receptor interactions: the Bcl-2 family inhibitor BH3I-1 potently inhibits p53/hDM2. Chem Commun (Camb). 2010 Nov 14;46(42):8020-2. doi: 10.1039/c0cc02969f. Epub 2010 Sep 20. PubMed PMID: 20856941; PubMed Central PMCID: PMC4576826.

3: Krishnamoorthy J, Yu VC, Mok YK. Auto-FACE: an NMR based binding site mapping program for fast chemical exchange protein-ligand systems. PLoS One. 2010 Feb 18;5(2):e8943. doi: 10.1371/journal.pone.0008943. PubMed PMID: 20174626; PubMed Central PMCID: PMC2823773.

4: Füllbeck M, Gebhardt N, Hossbach J, Daniel PT, Preissner R. Computer-assisted identification of small-molecule Bcl-2 modulators. Comput Biol Chem. 2009 Dec;33(6):451-6. doi: 10.1016/j.compbiolchem.2009.10.001. Epub 2009 Oct 12. PubMed PMID: 19889579.

5: Lartigue L, Medina C, Schembri L, Chabert P, Zanese M, Tomasello F, Dalibart R, Thoraval D, Crouzet M, Ichas F, De Giorgi F. An intracellular wave of cytochrome c propagates and precedes Bax redistribution during apoptosis. J Cell Sci. 2008 Nov 1;121(Pt 21):3515-23. doi: 10.1242/jcs.029587. Epub 2008 Oct 7. PubMed PMID: 18840646.

6: Wang L, Kong F, Kokoski CL, Andrews DW, Xing C. Development of dimeric modulators for anti-apoptotic Bcl-2 proteins. Bioorg Med Chem Lett. 2008 Jan 1;18(1):236-40. Epub 2007 Oct 30. PubMed PMID: 18023349; PubMed Central PMCID: PMC2266893.

7: Mitsiades CS, Hayden P, Kotoula V, McMillin DW, McMullan C, Negri J, Delmore JE, Poulaki V, Mitsiades N. Bcl-2 overexpression in thyroid carcinoma cells increases sensitivity to Bcl-2 homology 3 domain inhibition. J Clin Endocrinol Metab. 2007 Dec;92(12):4845-52. Epub 2007 Sep 11. PubMed PMID: 17848408.

8: Zhang YH, Bhunia A, Wan KF, Lee MC, Chan SL, Yu VC, Mok YK. Chelerythrine and sanguinarine dock at distinct sites on BclXL that are not the classic BH3 binding cleft. J Mol Biol. 2006 Dec 1;364(3):536-49. Epub 2006 Sep 14. PubMed PMID: 17011577.

9: Roa W, Chen H, Alexander A, Gulavita S, Thng J, Sun XJ, Petruk K, Moore R. Enhancement of radiation sensitivity with BH3I-1 in non-small cell lung cancer. Clin Invest Med. 2005 Apr;28(2):55-63. PubMed PMID: 15909480.