Hh-Ag1.5, Hedgehog Agonist


Catalog No. size PriceQuantity
M60004-2D 10 mM in DMSO (0.380 mL) $139
M60004-2S 2 mg solid $139
M60004-10S 10 mg solid $563

Description

Hh-Ag1.5 is one of the most potent and selective small-molecule agonists of the Hedgehog pathway, targeting Smoothened (Smo) with an EC50 ~1 nM. Studies showed that it has more potent activity than the recombinant Hh protein in activating Smo and hedgehog pathway.

Product information

CAS Number: 612542-14-0

Molecular Weight: 526.04

Formula: C28H26ClF2N3OS

Synonym:

SAG1.5

SAG-1.5

SAG 1.5

Related CAS Number:

478688-75-4 (trans&cis)

Chemical Name: 3-chloro-4,7-difluoro-N-(4-(methylamino)cyclohexyl)-N-(3-(pyridin-4-yl)benzyl)benzo[b]thiophene-2-carboxamide

Smiles: CN[C@@H]1CC[C@H](CC1)N(CC1C=CC=C(C=1)C1C=CN=CC=1)C(=O)C1SC2=C(C=1Cl)C(F)=CC=C2F

InChiKey: RXZDWPYJFCAZCW-MEMLXQNLSA-N

InChi: InChI=1S/C28H26ClF2N3OS/c1-32-20-5-7-21(8-6-20)34(16-17-3-2-4-19(15-17)18-11-13-33-14-12-18)28(35)27-25(29)24-22(30)9-10-23(31)26(24)36-27/h2-4,9-15,20-21,32H,5-8,16H2,1H3/t20-,21-

Technical Data

Appearance: Solid Power.

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

Solubility: DMSO up to 50 mM

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

Hh-Ag1.5 was used at 25 nM to induce Hh pathway activation in the reporter gene assay. It was suggested to use at 0.1 µM to replace recombinant Hh protein.

References:

  1. Frank-Kamenetsky M, et al. Small-molecule modulators of Hedgehog signaling: identification and characterization of Smoothened agonists and antagonists. (2002) Journal of Biology (1): 10.2-10.19.
  2. Borzillo GV, et al. The Hedgehog Signaling Pathway as a Target for Anticancer Drug Discovery. (2005) Current Topics in Medicinal Chemistry (5), 147-157.
  3. Pan S, et al. Discovery of NVP-LDE225, a Potent and Selective Smoothened Antagonist. ACS Med. Chem. Lett., 2010, 1 (3), pp 130–134.

Products are for research use only. Not for human use.

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