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 29 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 Ml\yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXjwZ3dOUUN3ME21Mlg3PjZizszN M4TU[3NCVkeHUh?=
DOHH-2 NIXEfVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlPVTWM2OD17LkO1Olg6KM7:TR?= MVjTRW5ITVJ?
no-10 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWTuW3hFUUN3ME25MlkxOzlizszN M3HCT3NCVkeHUh?=
LS-513 NE[xWpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnfVTWM2OD1zMT6zOVQ4KM7:TR?= NGC5fWFUSU6JRWK=
ALL-PO Ml;mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYXrRoxCUUN3ME2xNU44PzN2IN88US=> MWPTRW5ITVJ?
8-MG-BA MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mle4TWM2OD1zMz6xNVI{KM7:TR?= NWPCU2h7W0GQR1XS
RPMI-8402 M37PSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkT5TWM2OD1zNT64OVM4KM7:TR?= NXznW29{W0GQR1XS
EoL-1-cell NFLK[GpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXPINVZPUUN3ME2xPE42QTR6IN88US=> NHj1V4JUSU6JRWK=
NALM-6 MlzOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYPrVZIyUUN3ME2xPU4xOTZ5IN88US=> M{WwR3NCVkeHUh?=
DEL MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW\JR|UxRTJyLkG0O|Eh|ryP MkD0V2FPT0WU
SR MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYTJR|UxRTJ|Lk[3NVUh|ryP NHjjWWpUSU6JRWK=
697 NFzCTnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV;JR|UxRTJ4Lk[xOVUh|ryP NX\pT29sW0GQR1XS
COLO-829 MlXBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWrJR|UxRTJ4Lki0PFMh|ryP MmnQV2FPT0WU
EVSA-T NYPjUVk3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIDLVIRKSzVyPUK3MlU2PjFizszN NFnqWWRUSU6JRWK=
ATN-1 MlPYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVOycoI5UUN3ME2zNU4zOzJ7IN88US=> MU\TRW5ITVJ?
L-363 NHXNb5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFG0TlFKSzVyPUOxMlc1PjFizszN NV3BZVhNW0GQR1XS
LAMA-84 Mlz2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWnaVVFnUUN3ME2zNk42OjFzIN88US=> NXvzXG0zW0GQR1XS
NOS-1 NVfxO5ROT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIDCbHRKSzVyPUO0MlI6PTZizszN MYPTRW5ITVJ?
BB30-HNC Ml;PS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmfMTWM2OD1|ND6zN|A3KM7:TR?= NVLadHNsW0GQR1XS
BC-1 MkDXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MofzTWM2OD1|Nz65O|Q3KM7:TR?= MmXwV2FPT0WU
IST-SL2 M{n3[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYrJR|UxRTN6LkKyOEDPxE1? NVjwfoQ6W0GQR1XS
D-392MG MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEXhcHZKSzVyPUSwMlIzOTVizszN NEDMeVFUSU6JRWK=
no-11 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2TvcWlEPTB;NECuOVUzOSEQvF2= M4T3[HNCVkeHUh?=
LC4-1 M{PvXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX:2b2hTUUN3ME20NE45PzF4IN88US=> MUnTRW5ITVJ?
A388 NEnn[4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnfnTWM2OD12Mj61PFQ5KM7:TR?= MWjTRW5ITVJ?
NTERA-S-cl-D1 M37pcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHTkbINKSzVyPUSyMlcxPzRizszN NHzCPJpUSU6JRWK=
CESS MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4r0cWlEPTB;NESuNlI{OiEQvF2= M3mwfHNCVkeHUh?=
RS4-11 M{LH[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUHUd4JrUUN3ME20PU4xQTN6IN88US=> M4\weHNCVkeHUh?=
MS-1 M1jwfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVqyRlF3UUN3ME21NE46OzVzIN88US=> NXH0R2pFW0GQR1XS
CTV-1 NGLLU2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG\ZWXlKSzVyPUWxMlA4PCEQvF2= NGGxco9USU6JRWK=
D-502MG NF\mbVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MULJR|UxRTVzLk[yO|Eh|ryP NV2wcY1RW0GQR1XS
ML-2 NVHRVJl{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYDnNYVtUUN3ME21Nk46OTl3IN88US=> MmfjV2FPT0WU
SK-NEP-1 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mlq4TWM2OD13Mz6zPVI{KM7:TR?= NYjsOWk{W0GQR1XS
LOXIMVI MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1[zb2lEPTB;NUOuOVg5PCEQvF2= NVnibIl7W0GQR1XS
DJM-1 M3jlU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX3JR|UxRTV4LkOzPVEh|ryP M1PSW3NCVkeHUh?=
GI-1 Ml\xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXn5N2ttUUN3ME21Ok43OTR7IN88US=> NH6yXVFUSU6JRWK=
IST-MES1 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWLJR|UxRTZyLkW0PVMh|ryP MVjTRW5ITVJ?
MV-4-11 M2rneGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX36S4tqUUN3ME22NE43PTN6IN88US=> MoPuV2FPT0WU
OVCAR-4 M3vaO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnKwTWM2OD14Mz61OlU4KM7:TR?= NYfNUGRDW0GQR1XS
KE-37 NV3CdIg4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFPTVGRKSzVyPU[2MlI3PjhizszN MYHTRW5ITVJ?
D-542MG NGW0UZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkjnTWM2OD14OD60NVM2KM7:TR?= M2n3dHNCVkeHUh?=
MHH-PREB-1 NEXOeHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGXZXnVKSzVyPUeyMlg1PDFizszN NXnvbVdsW0GQR1XS
MRK-nu-1 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHz6TnFKSzVyPUezMlQ4ODVizszN NYLndI5tW0GQR1XS
D-247MG M3jXT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIHRVVRKSzVyPUezMlU1PDJizszN M{HEXHNCVkeHUh?=
OCI-AML2 M3zvOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXTJR|UxRTd4LkmzOlkh|ryP M3fiS3NCVkeHUh?=
LP-1 M{TacWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo\YTWM2OD16Mj64O|MyKM7:TR?= MXHTRW5ITVJ?
HCC1599 NGjW[4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn[0TWM2OD16ND6yPFM4KM7:TR?= Mn\rV2FPT0WU
KARPAS-45 NYrVSldZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4HXPGlEPTB;OESuOlk6OiEQvF2= MWTTRW5ITVJ?
BE-13 NVKzcWo{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NG[4S5RKSzVyPUm5MlA1PzdizszN M{jTS3NCVkeHUh?=
GCIY Mn;DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2PGTGlEPTB;OUmuNFk2PCEQvF2= NY\WSZh[W0GQR1XS
BV-173 NVHQO4JvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkPrTWM2OD1zMECuN|I2KM7:TR?= Mn3TV2FPT0WU
LB2518-MEL NXT1dpFUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{j0WGlEPTB;MUCwMlc5QSEQvF2= MojuV2FPT0WU
KS-1 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX3JR|UxRTFyMT62N|kh|ryP NH;X[mJUSU6JRWK=
MOLT-16 M4nGR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVfJR|UxRTFyND65PFYh|ryP NGrrVY1USU6JRWK=
NCI-H1770 NVyyVWloT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV7OfpJDUUN3ME2xNFgvPzh2IN88US=> NHvPTINUSU6JRWK=
NCI-H82 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlS3TWM2OD1zMUCuPVc3KM7:TR?= MYrTRW5ITVJ?
NCCIT MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1vQOmlEPTB;MUGyMlUzQSEQvF2= M3HLd3NCVkeHUh?=
KALS-1 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWDJR|UxRTFzNT65OFEh|ryP M{X0OXNCVkeHUh?=
LB2241-RCC MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFm3dpJKSzVyPUGxOk43PzlizszN MUTTRW5ITVJ?
HH MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXvHO5lXUUN3ME2xNVcvOzl3IN88US=> NFrDVW5USU6JRWK=
HD-MY-Z MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWDJR|UxRTFzOD60PFgh|ryP NVm1emliW0GQR1XS
EB-3 NX7VZWliT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnrLTWM2OD1zMkOuNFk1KM7:TR?= NVKwUHN1W0GQR1XS
BL-70 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVzSN5hDUUN3ME2xNlMvOTJ5IN88US=> NVrY[3BNW0GQR1XS
K-562 NX;6[|M3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2W1UGlEPTB;MUK2MlI1PSEQvF2= Mlj0V2FPT0WU
HT-144 NEXsdXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEj4OpBKSzVyPUGzN{4yPjRizszN M2jTXHNCVkeHUh?=
PF-382 NYPLdFNyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn;6TWM2OD1zM{SuN|YyKM7:TR?= NH\mfllUSU6JRWK=
RPMI-8226 M1fGXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFLaclNKSzVyPUGzOU4xPDVizszN MofWV2FPT0WU
NCI-H1355 M2ridGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1j1W2lEPTB;MUO1MlU5PyEQvF2= MlX3V2FPT0WU
LXF-289 M4HHSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2n0OWlEPTB;MUO5Mlc5OSEQvF2= M1HtcXNCVkeHUh?=
NCI-H69 M1q3V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1jRdWlEPTB;MUSyMlk{OiEQvF2= MUDTRW5ITVJ?
SK-MEL-1 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWHJR|UxRTF2Nz6xN{DPxE1? MkS2V2FPT0WU
KARPAS-299 MoHWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2LSSmlEPTB;MUS5MlEzKM7:TR?= MXvTRW5ITVJ?
GB-1 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnPzTWM2OD1zNEmuN|IzKM7:TR?= NXvMN49KW0GQR1XS
CMK M4XMZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoLKTWM2OD1zNEmuOVE2KM7:TR?= NXX0fFBEW0GQR1XS
MPP-89 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1f1U2lEPTB;MUW2MlA{PSEQvF2= NX\lZ3E5W0GQR1XS
KU812 MnrNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{X0eWlEPTB;MU[xMlkxOiEQvF2= MnvuV2FPT0WU
REH MmXtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVPzSmc3UUN3ME2xOlIvOTJ3IN88US=> NWLoOHZ6W0GQR1XS
NEC8 NGTtcGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYTJR|UxRTF4NT6wNlYh|ryP M3LrbnNCVkeHUh?=
KP-N-YS M4ryXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1W5bGlEPTB;MU[4MlM6PSEQvF2= M4jLTXNCVkeHUh?=
Ramos-2G6-4C10 NWfZRo5[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVvJR|UxRTF4OT65NVUh|ryP NXXHdpAyW0GQR1XS
Becker MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUPJR|UxRTF5ND6xPEDPxE1? NFXPe49USU6JRWK=
LB647-SCLC NV;vVGVjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV:zeHJiUUN3ME2xO|UvQDR3IN88US=> NWjQOoUxW0GQR1XS
LU-139 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MljUTWM2OD1zN{iuNFE6KM7:TR?= NV7UU|dpW0GQR1XS
QIMR-WIL NUXlTXl5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4fTPGlEPTB;MUe5MlY1PiEQvF2= MV;TRW5ITVJ?
NCI-H1395 MnzWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnfGTWM2OD1zN{muPVk3KM7:TR?= M4TpdHNCVkeHUh?=
NOMO-1 NG\Fb|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX7VPGRkUUN3ME2xPFIvQDVizszN MXHTRW5ITVJ?
GI-ME-N Ml2wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF\KUXhKSzVyPUG4O{46PjlizszN M4TBPXNCVkeHUh?=
KMS-12-PE MkXFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NInLOXZKSzVyPUG4PU4zPzNizszN MmHSV2FPT0WU
Daudi MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1LYXGlEPTB;MUmxMlEzQCEQvF2= M{XlTnNCVkeHUh?=
LB996-RCC NXrnNJBnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4XqN2lEPTB;MUmxMlY6QSEQvF2= MVLTRW5ITVJ?
NCI-H2107 MmTOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NI\1bGlKSzVyPUG5N{44OzlizszN MXrTRW5ITVJ?
SK-PN-DW M3rzdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV3hXJEyUUN3ME2xPVQvPzF7IN88US=> M4Xid3NCVkeHUh?=
MC-CAR NFP5N2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4HHUmlEPTB;MkCyMlI2OyEQvF2= MWHTRW5ITVJ?
SNB75 MoH4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW\JR|UxRTJ{MT65OEDPxE1? MnnsV2FPT0WU
ES4 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX3rdm9PUUN3ME2yNlMvPzh|IN88US=> MYDTRW5ITVJ?
KARPAS-422 M{n1Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY[zPFZ[UUN3ME2yNlgvOzV{IN88US=> MoPzV2FPT0WU
NCI-H1648 Mk\1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIi5fYNKSzVyPUKyPU41QDlizszN NEjmeI1USU6JRWK=
ES6 NXr2SnVXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXTjUmp6UUN3ME2yN|kvPDNizszN NETMZ|RUSU6JRWK=
KNS-81-FD M{DROWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX;JR|UxRTJ2MT6xPVch|ryP NHfRdlVUSU6JRWK=
JAR NIHt[G1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmrYTWM2OD1{NU[uNlI2KM7:TR?= MWjTRW5ITVJ?
NB1 NX\EOY1rT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXXJR|UxRTJ4MD61NVYh|ryP NGKyUm5USU6JRWK=
D-336MG NWHsTm1{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{Tj[GlEPTB;Mk[wMlY6QCEQvF2= NYi0NnRrW0GQR1XS
BC-3 MnrqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHXmNIhKSzVyPUK2OU4yPzhizszN MorwV2FPT0WU
HCC2218 NX63cVZuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFjwNpBKSzVyPUK2Ok41OTVizszN NEDudGlUSU6JRWK=
TE-9 MkC5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmXwTWM2OD1{Nk[uOlI4KM7:TR?= MVTTRW5ITVJ?
LB1047-RCC MnK0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NITkT5pKSzVyPUK2Ok44PTNizszN MXXTRW5ITVJ?
CTB-1 NF\wfWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVrJR|UxRTJ4OT65O|Mh|ryP NUnGXGZXW0GQR1XS
NB7 M1fId2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUDXe2FkUUN3ME2yO|Eh|ryP MVXTRW5ITVJ?
ST486 MlzhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHHNcodKSzVyPUK3O{41OTJizszN MoLZV2FPT0WU
HCC1187 MlvUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmPITWM2OD1{OEKuPFEyKM7:TR?= NWfsNJpSW0GQR1XS
NCI-SNU-16 NXy5cYd7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFPpXoRKSzVyPUK4OE4zPDhizszN MVfTRW5ITVJ?
COR-L279 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mmr4TWM2OD1{OUGuOVg1KM7:TR?= MVfTRW5ITVJ?
ES8 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVzJR|UxRTJ7ND6xPFIh|ryP MlT3V2FPT0WU
U-698-M MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4jZZmlEPTB;Mkm4MlI1OyEQvF2= MlXmV2FPT0WU
HEL MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoHJTWM2OD1|MEmuNVQ6KM7:TR?= NGTqXJpUSU6JRWK=
KINGS-1 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUnJR|UxRTNzMD62O|Qh|ryP Mmq2V2FPT0WU
KY821 NYrmOldQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXjEb3N6UUN3ME2zN|YvPTl3IN88US=> M3TOU3NCVkeHUh?=
MZ1-PC M4Pkdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUjJR|UxRTN2NT62NVgh|ryP NFWzRZZUSU6JRWK=
LS-411N MmKxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MonyTWM2OD1|NUSuOlYh|ryP NI\UOGhUSU6JRWK=
SIG-M5 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHq0OXJKSzVyPUO1PU44QDJizszN NWLhN451W0GQR1XS
HT Ml;iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2TRWmlEPTB;M{[3MlcyOSEQvF2= NVPOcVZnW0GQR1XS
HC-1 NITobnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXzib4FvUUN3ME2zOlcvPzh5IN88US=> MXLTRW5ITVJ?
NCI-H1694 M3[4NGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYPy[m55UUN3ME2zO|IvQTN2IN88US=> NYLCT5A1W0GQR1XS
BB65-RCC M4HUNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{LlNGlEPTB;M{e2MlI1PSEQvF2= Mn\YV2FPT0WU
HAL-01 NFzINm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlnHTWM2OD1|N{muPFM5KM7:TR?= M3nLTXNCVkeHUh?=
ARH-77 NGCyR4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIfGb|FKSzVyPUO5OE4xODhizszN M1HLeHNCVkeHUh?=
MZ7-mel M1ezUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIfpZ|BKSzVyPUO5O{4zOzNizszN NUWyTFl{W0GQR1XS
SIMA MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NE\WRWlKSzVyPUSwN{46OzNizszN MV\TRW5ITVJ?
DG-75 Mli4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWfJR|UxRTRzNT62PVgh|ryP M2XO[HNCVkeHUh?=
HUTU-80 NHnxTFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm\CTWM2OD12MUmuNVg2KM7:TR?= MYTTRW5ITVJ?
KNS-42 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX7HWJlEUUN3ME20NlUvQDF3IN88US=> Mm\oV2FPT0WU
SH-4 NIfqT3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MonlTWM2OD12MkeuOVY2KM7:TR?= NIDsUHZUSU6JRWK=
L-540 M1zsRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXjJR|UxRTR|MT6wN|Eh|ryP M2G0Z3NCVkeHUh?=
NB10 NYrUSFB{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoXFTWM2OD12NEGuNlM1KM7:TR?= NUTWWIZtW0GQR1XS
ES1 NVuyVnhiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXzJR|UxRTR3Mj63OVMh|ryP NXfwR3R1W0GQR1XS
KMOE-2 NFG0PGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH;aSHhKSzVyPUS1Ok44OTFizszN NETzS4hUSU6JRWK=
MC116 M37adGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVO1ZlhjUUN3ME20OVgvOTF4IN88US=> MX;TRW5ITVJ?
RCC10RGB M4XrNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXjKRZNLUUN3ME20OlAvODB3IN88US=> NXTSb5h[W0GQR1XS
RL95-2 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIm0Zo1KSzVyPUS2NE4zOzdizszN NXThW5VTW0GQR1XS
Raji MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\TRnBRUUN3ME20OlgvOTR|IN88US=> Mm\uV2FPT0WU
CAS-1 MkLkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3HkbGlEPTB;NEeyMlA4OyEQvF2= NFf4NYlUSU6JRWK=
Calu-6 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml\hTWM2OD12N{WuNlY2KM7:TR?= MUjTRW5ITVJ?
KG-1 MlXkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX\JR|UxRTR5OD60OEDPxE1? NH3Hc4FUSU6JRWK=
LB771-HNC NETJOFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX31UVlsUUN3ME20PFIvOjN{IN88US=> MoXnV2FPT0WU
ACN NYjEToNKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkLFTWM2OD12OUOuOVk6KM7:TR?= MUjTRW5ITVJ?
KM12 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXHJR|UxRTR7Nj61PFkh|ryP MUDTRW5ITVJ?

... 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]
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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]
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  • 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]
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  • 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 (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
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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).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
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    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

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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.

  • * Indicates a Required Field

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 Products

  • 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