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

Hodoodo CAT#: H563074

CAS#: 496794-70-8

Description: HhAntag is a GLI1-mediated transcription inhibitor. It acts as an inhibitor of the Shh pathway.

Chemical Structure

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HhAntag
CAS# 496794-70-8
Instruction

Theoretical Analysis

Hodoodo Cat#: H563074
Name: HhAntag
CAS#: 496794-70-8
Chemical Formula: C24H23ClN4O3
Exact Mass: 450.15
Molecular Weight: 450.923
Elemental Analysis: C, 63.93; H, 5.14; Cl, 7.86; N, 12.43; O, 10.64

Price and Availability

Size Price Availability Quantity
10mg USD 250 2 Weeks
25mg USD 450 2 Weeks
50mg USD 750 2 Weeks
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Synonym: HhAntag; Hh-Antag; Hh Antag;

IUPAC/Chemical Name: N-[4-Chloro-3-[6-(dimethylamino)-1H-benzimidazol-2-yl]phenyl]-3,5-dimethoxybenzamide

InChi Key: UBHJFPVTEATUFS-UHFFFAOYSA-N

InChi Code: InChI=1S/C24H23ClN4O3/c1-29(2)16-6-8-21-22(12-16)28-23(27-21)19-11-15(5-7-20(19)25)26-24(30)14-9-17(31-3)13-18(10-14)32-4/h5-13H,1-4H3,(H,26,30)(H,27,28)

SMILES Code: O=C(NC1=CC=C(Cl)C(C2=NC3=CC=C(N(C)C)C=C3N2)=C1)C4=CC(OC)=CC(OC)=C4

Appearance: Solid powder

Purity: >95% (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).

HS Tariff Code: 2934.99.9001

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 450.92 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:
In vitro protocol:
In vivo protocol:

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1: Kurio N, Saunders C, Bechtold TE, Salhab I, Nah HD, Sinha S, Billings PC, Pacifici M, Koyama E. Roles of Ihh signaling in chondroprogenitor function in postnatal condylar cartilage. Matrix Biol. 2018 Apr;67:15-31. doi: 10.1016/j.matbio.2018.02.011. Epub 2018 Feb 12. PubMed PMID: 29447948; PubMed Central PMCID: PMC5910228.

2: Bechtold TE, Saunders C, Decker RS, Um HB, Cottingham N, Salhab I, Kurio N, Billings PC, Pacifici M, Nah HD, Koyama E. Osteophyte formation and matrix mineralization in a TMJ osteoarthritis mouse model are associated with ectopic hedgehog signaling. Matrix Biol. 2016 May-Jul;52-54:339-354. doi: 10.1016/j.matbio.2016.03.001. Epub 2016 Mar 3. Review. PubMed PMID: 26945615; PubMed Central PMCID: PMC4875867.

3: Mundy C, Bello A, Sgariglia F, Koyama E, Pacifici M. HhAntag, a Hedgehog Signaling Antagonist, Suppresses Chondrogenesis and Modulates Canonical and Non-Canonical BMP Signaling. J Cell Physiol. 2016 May;231(5):1033-44. doi: 10.1002/jcp.25192. Epub 2015 Sep 22. PubMed PMID: 26363135.

4: Heiden KB, Williamson AJ, Doscas ME, Ye J, Wang Y, Liu D, Xing M, Prinz RA, Xu X. The sonic hedgehog signaling pathway maintains the cancer stem cell self-renewal of anaplastic thyroid cancer by inducing snail expression. J Clin Endocrinol Metab. 2014 Nov;99(11):E2178-87. doi: 10.1210/jc.2014-1844. Epub 2014 Jul 31. PubMed PMID: 25078145; PubMed Central PMCID: PMC5393503.

5: Kunkalla K, Liu Y, Qu C, Leventaki V, Agarwal NK, Singh RR, Vega F. Functional inhibition of BCL2 is needed to increase the susceptibility to apoptosis to SMO inhibitors in diffuse large B-cell lymphoma of germinal center subtype. Ann Hematol. 2013 Jun;92(6):777-87. doi: 10.1007/s00277-013-1684-6. Epub 2013 Feb 1. PubMed PMID: 23370596; PubMed Central PMCID: PMC3648611.

6: Zeng J, Aziz K, Chettiar ST, Aftab BT, Armour M, Gajula R, Gandhi N, Salih T, Herman JM, Wong J, Rudin CM, Tran PT, Hales RK. Hedgehog pathway inhibition radiosensitizes non-small cell lung cancers. Int J Radiat Oncol Biol Phys. 2013 May 1;86(1):143-9. doi: 10.1016/j.ijrobp.2012.10.014. Epub 2012 Nov 20. PubMed PMID: 23182391; PubMed Central PMCID: PMC4145860.

7: Zhang Y, Pullambhatla M, Laterra J, Pomper MG. Influence of bioluminescence imaging dynamics by D-luciferin uptake and efflux mechanisms. Mol Imaging. 2012 Nov-Dec;11(6):499-506. PubMed PMID: 23084250; PubMed Central PMCID: PMC4332814.

8: Shi Y, Moura U, Opitz I, Soltermann A, Rehrauer H, Thies S, Weder W, Stahel RA, Felley-Bosco E. Role of hedgehog signaling in malignant pleural mesothelioma. Clin Cancer Res. 2012 Sep 1;18(17):4646-56. doi: 10.1158/1078-0432.CCR-12-0599. Epub 2012 Jun 25. PubMed PMID: 22733539.

9: Chenna V, Hu C, Pramanik D, Aftab BT, Karikari C, Campbell NR, Hong SM, Zhao M, Rudek MA, Khan SR, Rudin CM, Maitra A. A polymeric nanoparticle encapsulated small-molecule inhibitor of Hedgehog signaling (NanoHHI) bypasses secondary mutational resistance to Smoothened antagonists. Mol Cancer Ther. 2012 Jan;11(1):165-73. doi: 10.1158/1535-7163.MCT-11-0341. Epub 2011 Oct 25. PubMed PMID: 22027695; PubMed Central PMCID: PMC3256300.

10: Brechbiel JL, Ng JM, Curran T. PTHrP treatment fails to rescue bone defects caused by Hedgehog pathway inhibition in young mice. Toxicol Pathol. 2011 Apr;39(3):478-85. doi: 10.1177/0192623311399788. Epub 2011 Mar 16. PubMed PMID: 21411723; PubMed Central PMCID: PMC3576833.

11: Katoh Y, Katoh M. Hedgehog target genes: mechanisms of carcinogenesis induced by aberrant hedgehog signaling activation. Curr Mol Med. 2009 Sep;9(7):873-86. Review. PubMed PMID: 19860666.

12: Kimura H, Ng JM, Curran T. Transient inhibition of the Hedgehog pathway in young mice causes permanent defects in bone structure. Cancer Cell. 2008 Mar;13(3):249-60. doi: 10.1016/j.ccr.2008.01.027. PubMed PMID: 18328428.

13: Hayhurst M, Gore BB, Tessier-Lavigne M, McConnell SK. Ongoing sonic hedgehog signaling is required for dorsal midline formation in the developing forebrain. Dev Neurobiol. 2008 Jan;68(1):83-100. PubMed PMID: 17948241.

14: Sasai K, Romer JT, Kimura H, Eberhart DE, Rice DS, Curran T. Medulloblastomas derived from Cxcr6 mutant mice respond to treatment with a smoothened inhibitor. Cancer Res. 2007 Apr 15;67(8):3871-7. Epub 2007 Apr 5. PubMed PMID: 17413002.

15: Sasai K, Romer JT, Lee Y, Finkelstein D, Fuller C, McKinnon PJ, Curran T. Shh pathway activity is down-regulated in cultured medulloblastoma cells: implications for preclinical studies. Cancer Res. 2006 Apr 15;66(8):4215-22. PubMed PMID: 16618744.

16: Romer JT, Kimura H, Magdaleno S, Sasai K, Fuller C, Baines H, Connelly M, Stewart CF, Gould S, Rubin LL, Curran T. Suppression of the Shh pathway using a small molecule inhibitor eliminates medulloblastoma in Ptc1(+/-)p53(-/-) mice. Cancer Cell. 2004 Sep;6(3):229-40. PubMed PMID: 15380514.