An agonist of the hedgehog pathway
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SAG 21k

Item No. 41121

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-chloro-4,7-difluoro-N-[[2-methoxy-5-(4-pyridinyl)phenyl]methyl]-N-[trans-4-(methylamino)cyclohexyl]-benzo[b]thiophene-2-carboxamide
CAS Number
946002-48-8
Molecular Formula
C29H28ClF2N3O2S
Formula Weight
556.1
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Slightly soluble: 0.1-1 mg/mlEthanol: Sparingly soluble: 1-10 mg/ml
SMILES
ClC(C1=C(F)C=C2)=C(C(N([C@H]3CC[C@@H](CC3)NC)CC4=C(OC)C=CC(C5=CC=NC=C5)=C4)=O)SC1=C2F
InChi Code
InChI=1S/C29H28ClF2N3O2S/c1-33-20-4-6-21(7-5-20)35(29(36)28-26(30)25-22(31)8-9-23(32)27(25)38-28)16-19-15-18(3-10-24(19)37-2)17-11-13-34-14-12-17/h3,8-15,20-21,33H,4-7,16H2,1-2H3/t20-,21-
InChi Key
YVIFQUJDZSAFKG-MEMLXQNLSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $193

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    10 mg

    $367

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    25 mg

    $867

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    50 mg

    $1,252

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    Product Description

    SAG 21k is an agonist of the hedgehog signaling pathway.1 It activates the Smoothened receptor (Smo) in a reporter assay using C3H/10T1/2 cells expressing Smo (EC50 = 0.3 nM). SAG 21k (1 nM) increases the levels of mRNA encoding Ki67, coiled-coil domain-containing protein 1 (Ccdc1), collagen II, alkaline phosphatase (ALP), nuclear glioma-associated oncogene 1 (Gli1), and Gli2, and decreases the levels of mRNA encoding matrix metalloproteinase-13 (MMP-13) in mouse primary chondrocytes.2 In vivo, SAG 21k (5 mg/kg per day), in combination with the PHD2 antagonist IOX2 (Item No. 11573), induces the formation of bone calluses and partial bone unions and increases total bone volume, but not total tissue volume, in a mouse model of surgery-induced non-healing bone fracture.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Brunton, S.A., Stibbard, J.H., Rubin, L.L., et al. Potent agonists of the Hedgehog signaling pathway. Bioorg. Med. Chem. Lett. 19(15), 4308-4311 (2009).

    2. Rundle, C.H., Gomez, G.A., Pourteymoor, S., et al. Sequential application of small molecule therapy enhances chondrogenesis and angiogenesis in murine segmental defect bone repair. J. Orthop. Res. 41(7), 1471-1481 (2023).