Cyclopamine

Catalog No.S1146 Synonyms: 11-deoxojervine

Cyclopamine Chemical Structure

Molecular Weight(MW): 411.62

Cyclopamine is a specific Hedgehog (Hh) signaling pathway antagonist of Smoothened (Smo) with IC50 of 46 nM in TM3Hh12 cells.

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Cited by 22 Publications

Purity & Quality Control

Choose Selective Hedgehog/Smoothened Inhibitors

Biological Activity

Description Cyclopamine is a specific Hedgehog (Hh) signaling pathway antagonist of Smoothened (Smo) with IC50 of 46 nM in TM3Hh12 cells.
Targets
Smoothened [1]
(TM3Hh12 cells)
46 nM
In vitro

Cyclopamine inhibits the Hedgehog signaling pathway with an IC50 of 46 nM, and blocks the activity of human Smo receptor expressed in CHO-K1 cells in [3H]Hh-Ag binding assay with an IC50 of 280 nM. [1] Cyclopamine significantly inhibits Hedgehog pathway activity in a dose-dependent manner in gut-derived tumor cell lines expressing Patched (PTCH) mRNA, and induces growth inhibition of those tumor cell lines by 75-95% at the concentration of 3 μM, but ineffective towards the colon tumor cells without PTCH mRNA expression, suggesting the effects of Cyclopamine treatment are Hedgehog pathway related rather than generally cytotoxic. [2] By blocking Hedgehog signaling through direct interaction with Smo, Cyclopamine (10 μM) inhibits the proliferation of SMOhigh Cyclopamine-responsive cell lines L3.6sl and Panc 05.04 by 75-80%, and increases the apoptosis by 2.5- to 3.5-fold, without affecting the BxPC3-SMOlow cell line. [3] Cyclopamine treatment significantly decreases of Snail mRNA and increasea E-cadherin transcripts in the E3LZ10.7 cell line. Independent of inhibition of cell growth, Cyclopamine treatment significantly inhibits the invasive phenotype of Hedgehog-dependent L3.6pl cells, causing a >500-fold reduction in the number of transmigrating cells, but not that of the Hedgehog-independent cell line Panc-1. [4]
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
OS-RC-2 MojoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmLSTWM2OD13Lki2OlYh|ryP MXLTRW5ITVJ?
DOHH-2 NEPFdFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUDid4FtUUN3ME25MlM2Pjh7IN88US=> MlT4V2FPT0WU
no-10 NUPmVnJ{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWnvN|lDUUN3ME25MlkxOzlizszN MmPGV2FPT0WU
LS-513 NFfVZWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn2zTWM2OD1zMT6zOVQ4KM7:TR?= MnPlV2FPT0WU
ALL-PO NH;hS|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3X6cGlEPTB;MUGuO|c{PCEQvF2= MkTQV2FPT0WU
8-MG-BA NHLweoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4i1fmlEPTB;MUOuNVEzOyEQvF2= MnTrV2FPT0WU
RPMI-8402 NFzFT5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHq3eZRKSzVyPUG1Mlg2OzdizszN NIDsblRUSU6JRWK=
EoL-1-cell M2\De2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoPwTWM2OD1zOD61PVQ5KM7:TR?= NUTYV282W0GQR1XS
NALM-6 MmLmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;5SFM1UUN3ME2xPU4xOTZ5IN88US=> MmnkV2FPT0WU
DEL MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXTJR|UxRTJyLkG0O|Eh|ryP MVvTRW5ITVJ?
SR NV\5N5F7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M130Z2lEPTB;MkOuOlcyPSEQvF2= M17JPXNCVkeHUh?=
697 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn24TWM2OD1{Nj62NVU2KM7:TR?= MV3TRW5ITVJ?
COLO-829 NI\KVpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmH3TWM2OD1{Nj64OFg{KM7:TR?= Mkj0V2FPT0WU
EVSA-T MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1XGVWlEPTB;MkeuOVU3OSEQvF2= M2joTHNCVkeHUh?=
ATN-1 M{DnWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHnqO2RKSzVyPUOxMlI{OjlizszN NIXFRZVUSU6JRWK=
L-363 NWThTWFPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEewb2RKSzVyPUOxMlc1PjFizszN MULTRW5ITVJ?
LAMA-84 NUjnUYRRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnLLTWM2OD1|Mj61NlEyKM7:TR?= M3:5OnNCVkeHUh?=
NOS-1 NYXKNXZOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUnJR|UxRTN2LkK5OVYh|ryP NX;rcHY4W0GQR1XS
BB30-HNC MoXoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX7JR|UxRTN2LkOzNFYh|ryP NXjOeYVwW0GQR1XS
BC-1 NVn2UVFmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1foc2lEPTB;M{euPVc1PiEQvF2= MoXPV2FPT0WU
IST-SL2 M2nVb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYDJR|UxRTN6LkKyOEDPxE1? MUPTRW5ITVJ?
D-392MG NYHwPZh6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGSwWJhKSzVyPUSwMlIzOTVizszN NWPaZ2x2W0GQR1XS
no-11 NXPNSpVqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUjaS4NIUUN3ME20NE42PTJzIN88US=> M37ySHNCVkeHUh?=
LC4-1 NXzGUIg6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2rpSWlEPTB;NECuPFcyPiEQvF2= MVjTRW5ITVJ?
A388 NELFRpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHr1eFNKSzVyPUSyMlU5PDhizszN NXrBXpVkW0GQR1XS
NTERA-S-cl-D1 MmqwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUjJR|UxRTR{LkewO|Qh|ryP MUDTRW5ITVJ?
CESS NWDjV3J3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MY\JR|UxRTR2LkKyN|Ih|ryP MYLTRW5ITVJ?
RS4-11 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2n1RWlEPTB;NEmuNFk{QCEQvF2= M37uN3NCVkeHUh?=
MS-1 NVHMSmZxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXrJR|UxRTVyLkmzOVEh|ryP M2\HeXNCVkeHUh?=
CTV-1 NXnVR2tiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX\JR|UxRTVzLkC3OEDPxE1? M1LsOXNCVkeHUh?=
D-502MG NHv0enVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHjkXnNKSzVyPUWxMlYzPzFizszN NYK1fWlSW0GQR1XS
ML-2 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{\MfmlEPTB;NUKuPVE6PSEQvF2= MlPEV2FPT0WU
SK-NEP-1 NWLEPGdtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX7JR|UxRTV|LkO5NlMh|ryP MV7TRW5ITVJ?
LOXIMVI M1r3Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkDPTWM2OD13Mz61PFg1KM7:TR?= M3rQUnNCVkeHUh?=
DJM-1 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1LLV2lEPTB;NU[uN|M6OSEQvF2= NEH0WXRUSU6JRWK=
GI-1 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYr6WVY1UUN3ME21Ok43OTR7IN88US=> M2XjXXNCVkeHUh?=
IST-MES1 MnfXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NInPXldKSzVyPU[wMlU1QTNizszN NXrNSpFxW0GQR1XS
MV-4-11 MmrsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX3JR|UxRTZyLk[1N|gh|ryP M3HRZXNCVkeHUh?=
OVCAR-4 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXr5e2NiUUN3ME22N{42PjV5IN88US=> NUfsdJFQW0GQR1XS
KE-37 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGnOU4ZKSzVyPU[2MlI3PjhizszN NH[2VGVUSU6JRWK=
D-542MG NFW5UFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX\tU2FrUUN3ME22PE41OTN3IN88US=> MWDTRW5ITVJ?
MHH-PREB-1 M1jqSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGLGfY1KSzVyPUeyMlg1PDFizszN NWruVFY4W0GQR1XS
MRK-nu-1 NXjBPWxLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1vxNWlEPTB;N{OuOFcxPSEQvF2= NHuxV3NUSU6JRWK=
D-247MG MoXtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWHJR|UxRTd|LkW0OFIh|ryP M2rNVXNCVkeHUh?=
OCI-AML2 NF[xeVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1rYemlEPTB;N{[uPVM3QSEQvF2= M2XS[HNCVkeHUh?=
LP-1 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnzCTWM2OD16Mj64O|MyKM7:TR?= MmDyV2FPT0WU
HCC1599 MmHGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoLQTWM2OD16ND6yPFM4KM7:TR?= NGXXVVNUSU6JRWK=
KARPAS-45 M2jtVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXXJR|UxRTh2Lk[5PVIh|ryP MoHaV2FPT0WU
BE-13 NVvnPWJjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF25W5VKSzVyPUm5MlA1PzdizszN MVXTRW5ITVJ?
GCIY NVu3b5FnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2PKVmlEPTB;OUmuNFk2PCEQvF2= MXfTRW5ITVJ?
BV-173 NVK5d4RIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFLQenFKSzVyPUGwNE4{OjVizszN Mn63V2FPT0WU
LB2518-MEL NYrRe5F7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M33rRmlEPTB;MUCwMlc5QSEQvF2= MkjwV2FPT0WU
KS-1 NHjSXFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF\UcFdKSzVyPUGwNU43OzlizszN MVnTRW5ITVJ?
MOLT-16 NI\GTGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1jJc2lEPTB;MUC0Mlk5PiEQvF2= NGTFfmdUSU6JRWK=
NCI-H1770 M3;aPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MknVTWM2OD1zMEiuO|g1KM7:TR?= MnzWV2FPT0WU
NCI-H82 MnnkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX:5TGhvUUN3ME2xNVAvQTd4IN88US=> NXXFd4pbW0GQR1XS
NCCIT MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3fLWWlEPTB;MUGyMlUzQSEQvF2= NHHETHZUSU6JRWK=
KALS-1 NF31V5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFHhZmpKSzVyPUGxOU46PDFizszN M2[wXXNCVkeHUh?=
LB2241-RCC M1uzVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUfsdVBVUUN3ME2xNVYvPjd7IN88US=> MlPmV2FPT0WU
HH NETwXldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUDJR|UxRTFzNz6zPVUh|ryP MnnqV2FPT0WU
HD-MY-Z MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1;ZbmlEPTB;MUG4MlQ5QCEQvF2= M1nJRnNCVkeHUh?=
EB-3 M{\qfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlTjTWM2OD1zMkOuNFk1KM7:TR?= NFn3dodUSU6JRWK=
BL-70 NVK2OHlKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmC3TWM2OD1zMkOuNVI4KM7:TR?= NGPwcJVUSU6JRWK=
K-562 NHq1WZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV7LT2FkUUN3ME2xNlYvOjR3IN88US=> M3raUXNCVkeHUh?=
HT-144 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVfJR|UxRTF|Mz6xOlQh|ryP MWjTRW5ITVJ?
PF-382 M3LpUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2f2dWlEPTB;MUO0MlM3OSEQvF2= NF\j[5VUSU6JRWK=
RPMI-8226 NYf4TotUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlTVTWM2OD1zM{WuNFQ2KM7:TR?= M33yTnNCVkeHUh?=
NCI-H1355 NWL0T5pyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3f0ZWlEPTB;MUO1MlU5PyEQvF2= NEPaZYNUSU6JRWK=
LXF-289 M2mwTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWTJc|RHUUN3ME2xN|kvPzhzIN88US=> MlfCV2FPT0WU
NCI-H69 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYnJR|UxRTF2Mj65N|Ih|ryP M3XMTXNCVkeHUh?=
SK-MEL-1 NYrtV21FT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUXJR|UxRTF2Nz6xN{DPxE1? M3jkc3NCVkeHUh?=
KARPAS-299 NVmzW4FST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGrlUHJKSzVyPUG0PU4yOiEQvF2= MmLlV2FPT0WU
GB-1 NGTsWGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHrJNFFKSzVyPUG0PU4{OjJizszN NWOwNlBJW0GQR1XS
CMK NYCzUVRMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIjSTnFKSzVyPUG0PU42OTVizszN MVnTRW5ITVJ?
MPP-89 NETGUVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2rt[2lEPTB;MUW2MlA{PSEQvF2= MWjTRW5ITVJ?
KU812 M4HMSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV\JR|UxRTF4MT65NFIh|ryP NEj2[JJUSU6JRWK=
REH MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoXKTWM2OD1zNkKuNVI2KM7:TR?= NInmOFlUSU6JRWK=
NEC8 NF7NRnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1vHRWlEPTB;MU[1MlAzPiEQvF2= MlTBV2FPT0WU
KP-N-YS M{S1U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2P6VGlEPTB;MU[4MlM6PSEQvF2= MWHTRW5ITVJ?
Ramos-2G6-4C10 NUjaOHRTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mk\xTWM2OD1zNkmuPVE2KM7:TR?= MVHTRW5ITVJ?
Becker MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHXINpJKSzVyPUG3OE4yQCEQvF2= MojpV2FPT0WU
LB647-SCLC NVvqT48yT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUDRZY93UUN3ME2xO|UvQDR3IN88US=> M{jkdnNCVkeHUh?=
LU-139 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn[0TWM2OD1zN{iuNFE6KM7:TR?= NIjNZodUSU6JRWK=
QIMR-WIL NWfmU29mT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnKwTWM2OD1zN{muOlQ3KM7:TR?= MYHTRW5ITVJ?
NCI-H1395 Ml3qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4n2bWlEPTB;MUe5Mlk6PiEQvF2= NITnZ4NUSU6JRWK=
NOMO-1 M{XJZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV;ZOZdiUUN3ME2xPFIvQDVizszN MmPnV2FPT0WU
GI-ME-N M2Pqfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXHJR|UxRTF6Nz65Olkh|ryP M3nt[nNCVkeHUh?=
KMS-12-PE NUnlVmtGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mof3TWM2OD1zOEmuNlc{KM7:TR?= NFfSXVJUSU6JRWK=
Daudi Ml\qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4D4XmlEPTB;MUmxMlEzQCEQvF2= NWfOWnJUW0GQR1XS
LB996-RCC NYjHVldVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFK1fW1KSzVyPUG5NU43QTlizszN MlnaV2FPT0WU
NCI-H2107 M{jTS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2HBRmlEPTB;MUmzMlc{QSEQvF2= M{nzUXNCVkeHUh?=
SK-PN-DW NIHCSZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGnXR4FKSzVyPUG5OE44OTlizszN NIXW[o5USU6JRWK=
MC-CAR MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;5TWM2OD1{MEKuNlU{KM7:TR?= NH2xeodUSU6JRWK=
SNB75 MnXjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEj0TGxKSzVyPUKyNU46PCEQvF2= MnzkV2FPT0WU
ES4 NWXLc3VmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEX4XJlKSzVyPUKyN{44QDNizszN MW\TRW5ITVJ?
KARPAS-422 NVjBdVI3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUL2UmU4UUN3ME2yNlgvOzV{IN88US=> NIXPdGRUSU6JRWK=
NCI-H1648 NXfhO|hGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYPJR|UxRTJ{OT60PFkh|ryP NEPPVHFUSU6JRWK=
ES6 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1XyfmlEPTB;MkO5MlQ{KM7:TR?= NFjaS4dUSU6JRWK=
KNS-81-FD NI\ac4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlXLTWM2OD1{NEGuNVk4KM7:TR?= NFG2[lRUSU6JRWK=
JAR M13ZTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXvJR|UxRTJ3Nj6yNlUh|ryP MV3TRW5ITVJ?
NB1 NF\obmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGXpNVFKSzVyPUK2NE42OTZizszN MVTTRW5ITVJ?
D-336MG NWnkbmJET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1SxcmlEPTB;Mk[wMlY6QCEQvF2= NUn0TFM3W0GQR1XS
BC-3 MmTjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnXCTWM2OD1{NkWuNVc5KM7:TR?= Mn3WV2FPT0WU
HCC2218 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NE\aOolKSzVyPUK2Ok41OTVizszN MYDTRW5ITVJ?
TE-9 M1nib2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX3PZ4tnUUN3ME2yOlYvPjJ5IN88US=> MljpV2FPT0WU
LB1047-RCC NU\SSoltT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{fzU2lEPTB;Mk[2Mlc2OyEQvF2= MmDqV2FPT0WU
CTB-1 MnjFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo\MTWM2OD1{NkmuPVc{KM7:TR?= M2HYSXNCVkeHUh?=
NB7 M{DGVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{\IfGlEPTB;MkexJO69VQ>? NEDkcnVUSU6JRWK=
ST486 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2HaWmlEPTB;Mke3MlQyOiEQvF2= Ml7OV2FPT0WU
HCC1187 MoTzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYDJR|UxRTJ6Mj64NVEh|ryP MVrTRW5ITVJ?
NCI-SNU-16 NUfOVolYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NITSXphKSzVyPUK4OE4zPDhizszN MW\TRW5ITVJ?
COR-L279 MmHES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3fodGlEPTB;MkmxMlU5PCEQvF2= MXXTRW5ITVJ?
ES8 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4Xo[2lEPTB;Mkm0MlE5OiEQvF2= NHnPT4NUSU6JRWK=
U-698-M M1zwUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWHaUWp3UUN3ME2yPVgvOjR|IN88US=> MnvQV2FPT0WU
HEL NX20UG5HT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWDJR|UxRTNyOT6xOFkh|ryP NFjPNIxUSU6JRWK=
KINGS-1 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXjFbIRqUUN3ME2zNVAvPjd2IN88US=> NVXjWpFwW0GQR1XS
KY821 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXXJR|UxRTN|Nj61PVUh|ryP MoTTV2FPT0WU
MZ1-PC NHHxVFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3ztcGlEPTB;M{S1MlYyQCEQvF2= M4HMT3NCVkeHUh?=
LS-411N MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\hfFV1UUN3ME2zOVQvPjZizszN Ml61V2FPT0WU
SIG-M5 M4rRZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlnyTWM2OD1|NUmuO|gzKM7:TR?= NUHFOYF[W0GQR1XS
HT NUjVOZpXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVHJR|UxRTN4Nz63NVEh|ryP MoPvV2FPT0WU
HC-1 M4O5fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWLJR|UxRTN4Nz63PFch|ryP MXnTRW5ITVJ?
NCI-H1694 MkO2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnrzTWM2OD1|N{KuPVM1KM7:TR?= MkDMV2FPT0WU
BB65-RCC Ml75S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3HOcWlEPTB;M{e2MlI1PSEQvF2= MnzQV2FPT0WU
HAL-01 NEDQZ2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mme4TWM2OD1|N{muPFM5KM7:TR?= NV\5RnRIW0GQR1XS
ARH-77 NXzGbFdVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWfQ[|lRUUN3ME2zPVQvODB6IN88US=> MnrKV2FPT0WU
MZ7-mel NUfx[GhXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUT0O5hvUUN3ME2zPVcvOjN|IN88US=> M4KyS3NCVkeHUh?=
SIMA M13qcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlHoTWM2OD12MEOuPVM{KM7:TR?= M{fWPXNCVkeHUh?=
DG-75 NYOzclN[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVWzZ4FoUUN3ME20NVUvPjl6IN88US=> NUnwXWFXW0GQR1XS
HUTU-80 NF3I[XlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVPM[nFZUUN3ME20NVkvOTh3IN88US=> NVG1fI16W0GQR1XS
KNS-42 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWK0b5dxUUN3ME20NlUvQDF3IN88US=> M{C2dnNCVkeHUh?=
SH-4 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NE\LS|NKSzVyPUSyO{42PjVizszN MmD5V2FPT0WU
L-540 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MonzTWM2OD12M{GuNFMyKM7:TR?= MkmzV2FPT0WU
NB10 M2\GbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHT3cJRKSzVyPUS0NU4zOzRizszN NVHveVF5W0GQR1XS
ES1 NGjXPYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUjHV|d2UUN3ME20OVIvPzV|IN88US=> M4n5PXNCVkeHUh?=
KMOE-2 M{nmbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGDXe2NKSzVyPUS1Ok44OTFizszN M{SzU3NCVkeHUh?=
MC116 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmrtTWM2OD12NUiuNVE3KM7:TR?= MnLLV2FPT0WU
RCC10RGB NYG4e2pqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF22XnBKSzVyPUS2NE4xODVizszN MUPTRW5ITVJ?
RL95-2 M3HtXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2TEXmlEPTB;NE[wMlI{PyEQvF2= M2nteHNCVkeHUh?=
Raji MkLhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoPCTWM2OD12NkiuNVQ{KM7:TR?= M3LaOnNCVkeHUh?=
CAS-1 M3O0[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnHRTWM2OD12N{KuNFc{KM7:TR?= NU\pT|VmW0GQR1XS
Calu-6 M3nxVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWHQTpRCUUN3ME20O|UvOjZ3IN88US=> M1m1O3NCVkeHUh?=
KG-1 M1zUXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX;JR|UxRTR5OD60OEDPxE1? MVzTRW5ITVJ?
LB771-HNC NX3ER5BFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVXOSG1UUUN3ME20PFIvOjN{IN88US=> MWDTRW5ITVJ?
ACN NYTXeXo2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{i2c2lEPTB;NEmzMlU6QSEQvF2= NF3jbmhUSU6JRWK=
KM12 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHSxNIhKSzVyPUS5Ok42QDlizszN M4HVO3NCVkeHUh?=

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot
NF-κB / Cyclin D1 / MMP2 / MMP9; 

PubMed: 23599805     


Whole cell lysates were prepared, and 50 μg proteins were resolved using SDS-PAGE, followed by immunoblotting with the indicated specific antibodies against NF-κB, cyclin D1, MMP2 and MMP9. 

Gli1 / TGF-β1 / CXCR4; 

PubMed: 26137001     


Western blotting demonstrated that Gli1, TGF-β1 and CXCR4 protein expression levels were downregulated in the AGS cells treated with cyclopamine for 24 h.

Snail / E-cadherin / Slug / Vimentin ; 

PubMed: 26859575     


SW1736 and WRO82 cells were incubated in the presence of vehicle (0.5% DMSO) or the indicated concentrations of cyclopamine or GANT61 for 72 hr. The cells were harvested and analyzed for the expression of several genes involved in EMT.

23599805 26137001 26859575
Immunofluorescence
Vimentin; 

PubMed: 24553082     


Vimentin protein expression was reduced following treatment with cyclopamine (20 μmol/L; 72 h), detected by immunocytochemistry.

PCNA / β-catenin; 

PubMed: 28747625     


Immunofluorescence images demonstrating the distribution of PCNA or β-catenin in EH cells pre-treated with cyclopamine in presence and absence of estrogen for 24 h. Experiments were repeated at least three times.

24553082 28747625
In vivo Administration of Cyclopamine at dose of 50 mg/kg/day for 22 days eradicates the HUCCT1 xenografts in mice with no obvious adverse effects. [2] Cyclopamine treatment at dose of 1.2 mg for 7 days induces significant apoptosis of tumor cells and decreases the tumor mass by 50-60% in Panc 05.04- and L3.6sl-derived tumors, respectively, but not in the BxPC3-SMOlow tumors. [3] Administration of Cyclopamine alone profoundly inhibits tumor metastases in xenografts of E3LZ10.7 and L3.6pl, and completely abrogates metastases when in combination of gemcitabine. [4]

Protocol

Kinase Assay:[1]
+ Expand

Hedgehog cell assay:

This assay measures the end stage of the Hh signaling pathway, that is, the transcriptional modulation of Gli, using Luciferase as readout (Gli-Luc assay). Cyclopamine is prepared for assay by serial dilution in DMSO and then added to empty assay plates. TM3Hh12 cells (TM3 cells containing Hh-responsive reporter gene construct pTA-8xGli-Luc) are resuspended in F12 Ham's/DMEM (1:1) containing 5% FBS and 15 mM Hepes pH 7.3, added to assay plates and incubated with Cyclopamine for approximately 30 minutes at 37 °C in 5% CO2. 1 nM Hh-Ag 1.5 is then added to assay plates and incubated at 37 °C in the presence of 5% CO2. After 48 hours, either Bright-Glo or MTS reagent is added to the assay plates and luminescence or absorbance at 492 nm is determined. IC50 value, defined as the inflection point of the logistic curve, is determined by non-linear regression of the Gli-driven luciferase luminescence or absorbance signal from MTS assay vs log10 (concentration) of Cyclopamine using the R statistical software pack
Cell Research:[2]
+ Expand
  • Cell lines: SEG1, OE33, KYAE, KYSE180, SNU1, AGS, SNU16, NCI-N-87, HUCCT1, PANC1, PL5, PL6, BXPC3, HS766T, KYSE150, GBD1, DLD1, and HCT116
  • Concentrations: Dissolved in DMSO, final concentration 3 μM
  • Incubation Time: 4 days
  • Method: Cells are exposed to Cyclopamine in 96-well plates. Cell viability is measured by MTS (soluble tetrazolium salt) assay. Viable cell mass is determined by optical density measurements at 490 nm (OD490) at 2 and 4 days using the CellTiter96 colorimetric assay. Relative growth is calculated as OD (day 4)﹣OD (day 2)/OD (day 2).
    (Only for Reference)
Animal Research:[2]
+ Expand
  • Animal Models: Athymic (nude) mice inoculated subcutaneously with HUCCT1 cells
  • Formulation: Dissolved in DMSO, and diluted in saline
  • Dosages: 50 mg/kg/day
  • Administration: Subcutaneous injection
    (Only for Reference)

Solubility (25°C)

In vitro DMF 10 mg/mL warmed (24.29 mM)
Ethanol 2 mg/mL warmed (4.85 mM)
DMSO Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 411.62
Formula

C27H41NO2
CAS No. 4449-51-8
Storage powder
in solvent
Synonyms 11-deoxojervine

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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Frequently Asked Questions

  • Question 1:

    How to reconstitute the compound for in vivo use in mice?

  • Answer:

    One paper dissolved this drug in DMSO, and diluted in saline: Berman DM, et al. Nature, 2003, 425(6960), 846-851. Alternatively, you can try this vehicle: 10% DMSO+30% PEG 300+5% Tween 80+ddH2O for P.O. When preparing the solution, please dissolve the compound in DMSO clearly first. Then add PEG300 and Tween, after they mixed well, dilute with water.

selleck catalog

Hedgehog/Smoothened Signaling Pathway Map

Hedgehog/Smoothened Inhibitors with Unique Features

  • Selective Smoothened inhibitor

    PF-5274857 : Smoothened-selective, IC50=5.8 nM.

  • Smoothened Inhibitor in Clinical Trial

    LDE225 (NVP-LDE225,Erismodegib) : Phase III for Hh-pathway activated relapsed Medulloblastoma (MB).

  • Newest Smoothened Inhibitor

    GANT61 : Inhibitor for GLI1 as well as GLI2-induced transcription, inhibits hedgehog with IC50 of 5 μM, displays selectivity over other pathways, such as TNF and glucocorticoid receptor gene transactivation.

  • Smoothened Activator

    Purmorphamine : Directly binds and activates Smoothened, and blocks BODIPY-cyclopamine binding to Smo with IC50 of ~ 1.5 μM.

Related Hedgehog/Smoothened Products4

  • Smoothened Agonist (SAG) HCl New

    Smoothened Agonist (SAG) HCl is a cell-permeable Smoothened (Smo) agonist with EC50 of 3 nM in Shh-LIGHT2 cells.

  • SB225002 New

    SB225002 is a potent, and selective CXCR2 antagonist with IC50 of 22 nM for inhibiting interleukin IL-8 binding to CXCR2, > 150-fold selectivity over the other 7-TMRs tested.

  • SB-334867 New

    SB-334867 is a selective orexin-1 (OX1) receptor antagonist.

  • Vismodegib (GDC-0449)

    Vismodegib (GDC-0449) is a potent, novel and specific hedgehog inhibitor with IC50 of 3 nM and also inhibits P-gp with IC50 of 3.0 μM in a cell-free assay.

  • GANT61

    GANT61 is an inhibitor for GLI1 as well as GLI2-induced transcription, inhibits hedgehog with IC50 of 5 μM in GLI1 expressing HEK293T cell, displays selectivity over other pathways, such as TNF and glucocorticoid receptor gene transactivation.

  • Purmorphamine

    Purmorphamine, which directly binds and activates Smoothened, blocks BODIPY-cyclopamine binding to Smo with IC50 of ~ 1.5 μM in HEK293T cell and also is an inducer of osteoblast differentiation with EC50 of 1 μM.

  • Sonidegib (Erismodegib, NVP-LDE225)

    Sonidegib (Erismodegib, NVP-LDE225) is a Smoothened (Smo) antagonist, inhibiting Hedgehog (Hh) signaling with IC50 of 1.3 nM (mouse) and 2.5 nM (human) in cell-free assays, respectively. Phase 3.

  • Taladegib (LY2940680)

    Taladegib (LY2940680) binds to the Smoothened (Smo) receptor and potently inhibits Hedgehog (Hh) signaling. Phase 1/2.

  • Glasdegib (PF-04449913)

    Glasdegib (PF-04449913) is a potent, and orally bioavailable Smoothened (Smo) inhibitor with IC50 of 5 nM. Phase 2.

  • SANT-1

    SANT-1 directly binds to Smoothened (Smo) receptor with Kd of 1.2 nM and inhibits Smo agonist effects with IC50 of 20 nM.

    Features:Attenuates SAG stimulation of Shh-LIGHT2 cells to a greater extent relative to other antagonists.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID