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 24 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? MWXJR|UxRTVwOE[2OkDPxE1? M2\CXXNCVkeHUh?=
DOHH-2 NW\vZZV6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYXJR|UxRTlwM{W2PFkh|ryP MmDCV2FPT0WU
no-10 NFTDOWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUjleJFvUUN3ME25MlkxOzlizszN NXG5OmE4W0GQR1XS
LS-513 MoH2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3v6W2lEPTB;MUGuN|U1PyEQvF2= Mn;hV2FPT0WU
ALL-PO NV31dYxyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3LCXGlEPTB;MUGuO|c{PCEQvF2= NGjPO|hUSU6JRWK=
8-MG-BA MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHvC[ZlKSzVyPUGzMlEyOjNizszN MYjTRW5ITVJ?
RPMI-8402 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1\VeWlEPTB;MUWuPFU{PyEQvF2= NYf1dXpEW0GQR1XS
EoL-1-cell MnXES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml30TWM2OD1zOD61PVQ5KM7:TR?= M2rSSnNCVkeHUh?=
NALM-6 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{nMN2lEPTB;MUmuNFE3PyEQvF2= M4fB[nNCVkeHUh?=
DEL MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoX5TWM2OD1{MD6xOFcyKM7:TR?= Ml\1V2FPT0WU
SR MnjQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1TMXWlEPTB;MkOuOlcyPSEQvF2= NVK0TllzW0GQR1XS
697 NIWwT5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVHnN3AxUUN3ME2yOk43OTV3IN88US=> M{DtfHNCVkeHUh?=
COLO-829 NXOySIc2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmXwTWM2OD1{Nj64OFg{KM7:TR?= NGTDeJNUSU6JRWK=
EVSA-T M3XHT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYjJR|UxRTJ5LkW1OlEh|ryP M3voXnNCVkeHUh?=
ATN-1 NWO0NVJZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFO1dGVKSzVyPUOxMlI{OjlizszN Mk\sV2FPT0WU
L-363 NXT2V2N4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M17kXWlEPTB;M{GuO|Q3OSEQvF2= MYTTRW5ITVJ?
LAMA-84 NHG2THlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX7USItJUUN3ME2zNk42OjFzIN88US=> MWPTRW5ITVJ?
NOS-1 M3[ybWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYDiWplkUUN3ME2zOE4zQTV4IN88US=> MYDTRW5ITVJ?
BB30-HNC Mln2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPJTWM2OD1|ND6zN|A3KM7:TR?= NI\MSGxUSU6JRWK=
BC-1 M{\keGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MofiTWM2OD1|Nz65O|Q3KM7:TR?= MV\TRW5ITVJ?
IST-SL2 MkjTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVnuZYdsUUN3ME2zPE4zOjRizszN NFzPUYZUSU6JRWK=
D-392MG NXTGR4IzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MULJR|UxRTRyLkKyNVUh|ryP NGnQflRUSU6JRWK=
no-11 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmWyTWM2OD12MD61OVIyKM7:TR?= MljYV2FPT0WU
LC4-1 NUjCXoZRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWfJR|UxRTRyLki3NVYh|ryP MnzTV2FPT0WU
A388 Mnz4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXjJR|UxRTR{LkW4OFgh|ryP NXHGdZZFW0GQR1XS
NTERA-S-cl-D1 MkjGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIf3eIJKSzVyPUSyMlcxPzRizszN MVjTRW5ITVJ?
CESS M4HkdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoXnTWM2OD12ND6yNlMzKM7:TR?= NWDJOHlVW0GQR1XS
RS4-11 MnXSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF;hUZFKSzVyPUS5MlA6OzhizszN M{LSZXNCVkeHUh?=
MS-1 NIG2PZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2r3WmlEPTB;NUCuPVM2OSEQvF2= M2LTV3NCVkeHUh?=
CTV-1 NVvWUpVMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF\KNplKSzVyPUWxMlA4PCEQvF2= NIHB[HFUSU6JRWK=
D-502MG M2nw[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX3JR|UxRTVzLk[yO|Eh|ryP Ml\vV2FPT0WU
ML-2 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWi4R5pCUUN3ME21Nk46OTl3IN88US=> NYT6VJI2W0GQR1XS
SK-NEP-1 M3nrSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGrjXXBKSzVyPUWzMlM6OjNizszN NXnpdJV3W0GQR1XS
LOXIMVI M{HPOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2X3c2lEPTB;NUOuOVg5PCEQvF2= NV\vblNLW0GQR1XS
DJM-1 NYD4b|hZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVLJR|UxRTV4LkOzPVEh|ryP NVvpRoh2W0GQR1XS
GI-1 M13F[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4jm[GlEPTB;NU[uOlE1QSEQvF2= M3PCOnNCVkeHUh?=
IST-MES1 Mmq4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFj0OYtKSzVyPU[wMlU1QTNizszN MYXTRW5ITVJ?
MV-4-11 M4TncGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVHIWYhSUUN3ME22NE43PTN6IN88US=> MUTTRW5ITVJ?
OVCAR-4 M1W1Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoXITWM2OD14Mz61OlU4KM7:TR?= MWTTRW5ITVJ?
KE-37 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUTke|drUUN3ME22Ok4zPjZ6IN88US=> NHXYWIRUSU6JRWK=
D-542MG MkP3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVHJR|UxRTZ6LkSxN|Uh|ryP NGrq[o5USU6JRWK=
MHH-PREB-1 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1P1WGlEPTB;N{KuPFQ1OSEQvF2= NYTafZUzW0GQR1XS
MRK-nu-1 M2DqUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWXJR|UxRTd|LkS3NFUh|ryP NFjlPGVUSU6JRWK=
D-247MG NYC3SVJ7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUeyUGdUUUN3ME23N{42PDR{IN88US=> NVrsU41TW0GQR1XS
OCI-AML2 NE\VUXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWrLfVZ2UUN3ME23Ok46OzZ7IN88US=> M1LLb3NCVkeHUh?=
LP-1 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkjKTWM2OD16Mj64O|MyKM7:TR?= MWnTRW5ITVJ?
HCC1599 MlzFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{HnR2lEPTB;OESuNlg{PyEQvF2= NGW0RWFUSU6JRWK=
KARPAS-45 NYfH[|VkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{nFd2lEPTB;OESuOlk6OiEQvF2= MnTIV2FPT0WU
BE-13 M{LkZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX;XcYJJUUN3ME25PU4xPDd5IN88US=> MlLMV2FPT0WU
GCIY NGnVSnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3XITGlEPTB;OUmuNFk2PCEQvF2= M1zQOXNCVkeHUh?=
BV-173 MoT3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{ezRWlEPTB;MUCwMlMzPSEQvF2= MUPTRW5ITVJ?
LB2518-MEL NXvBVZFmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVPJR|UxRTFyMD63PFkh|ryP MojXV2FPT0WU
KS-1 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXLPOVk3UUN3ME2xNFEvPjN7IN88US=> MmXrV2FPT0WU
MOLT-16 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXvJR|UxRTFyND65PFYh|ryP NGW5SJVUSU6JRWK=
NCI-H1770 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmrUTWM2OD1zMEiuO|g1KM7:TR?= NFj3fVZUSU6JRWK=
NCI-H82 Mo\0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnrZTWM2OD1zMUCuPVc3KM7:TR?= NXjtTmo1W0GQR1XS
NCCIT NF;0eo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVrJR|UxRTFzMj61Nlkh|ryP NH;G[odUSU6JRWK=
KALS-1 MkPQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1rBXWlEPTB;MUG1Mlk1OSEQvF2= NIe3ZWNUSU6JRWK=
LB2241-RCC M{Da[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYHoSpZZUUN3ME2xNVYvPjd7IN88US=> MXTTRW5ITVJ?
HH M{PhO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmHaTWM2OD1zMUeuN|k2KM7:TR?= MkWxV2FPT0WU
HD-MY-Z NYLMSndoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2jSU2lEPTB;MUG4MlQ5QCEQvF2= NVW3TnliW0GQR1XS
EB-3 NYPPe|hQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3vXZmlEPTB;MUKzMlA6PCEQvF2= M1LwW3NCVkeHUh?=
BL-70 MkO2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2GxcGlEPTB;MUKzMlEzPyEQvF2= MX\TRW5ITVJ?
K-562 M2r5b2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlvDTWM2OD1zMk[uNlQ2KM7:TR?= M3;5RnNCVkeHUh?=
HT-144 NF\qUZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV3NO5UxUUN3ME2xN|MvOTZ2IN88US=> NXn0d4xnW0GQR1XS
PF-382 M3\ofWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHTsPFJKSzVyPUGzOE4{PjFizszN MUPTRW5ITVJ?
RPMI-8226 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXexS49OUUN3ME2xN|UvODR3IN88US=> MnPDV2FPT0WU
NCI-H1355 M17KPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3jZSGlEPTB;MUO1MlU5PyEQvF2= MX7TRW5ITVJ?
LXF-289 MoWwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHy3dJVKSzVyPUGzPU44QDFizszN NV:yWFBCW0GQR1XS
NCI-H69 MlrFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVmwSGJHUUN3ME2xOFIvQTN{IN88US=> NX3XTFJxW0GQR1XS
SK-MEL-1 M1i2dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MornTWM2OD1zNEeuNVMh|ryP MVfTRW5ITVJ?
KARPAS-299 NGTMWVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkO4TWM2OD1zNEmuNVIh|ryP MVvTRW5ITVJ?
GB-1 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF2zPIZKSzVyPUG0PU4{OjJizszN M1fzXnNCVkeHUh?=
CMK MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHPMN45KSzVyPUG0PU42OTVizszN NXHxV4ZnW0GQR1XS
MPP-89 NUHzfVN7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlPKTWM2OD1zNU[uNFM2KM7:TR?= NEPDZ3NUSU6JRWK=
KU812 NULMSFFST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmrKTWM2OD1zNkGuPVAzKM7:TR?= NFTKcIdUSU6JRWK=
REH MkHWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUPJR|UxRTF4Mj6xNlUh|ryP MmHaV2FPT0WU
NEC8 NF;XS|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{HRV2lEPTB;MU[1MlAzPiEQvF2= MXvTRW5ITVJ?
KP-N-YS MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXv6d4p[UUN3ME2xOlgvOzl3IN88US=> MnLwV2FPT0WU
Ramos-2G6-4C10 MkDzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF7EdoZKSzVyPUG2PU46OTVizszN NIH4RYhUSU6JRWK=
Becker NUPEdlMxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnfETWM2OD1zN{SuNVgh|ryP NY\0[JpxW0GQR1XS
LB647-SCLC MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkC2TWM2OD1zN{WuPFQ2KM7:TR?= NWrsW3NpW0GQR1XS
LU-139 NYXob3d6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF3LUYZKSzVyPUG3PE4xOTlizszN M2fQUHNCVkeHUh?=
QIMR-WIL NF3pO5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml75TWM2OD1zN{muOlQ3KM7:TR?= MUHTRW5ITVJ?
NCI-H1395 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVvMPIZ{UUN3ME2xO|kvQTl4IN88US=> M330N3NCVkeHUh?=
NOMO-1 NGTYSXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVXhU4o3UUN3ME2xPFIvQDVizszN MnO2V2FPT0WU
GI-ME-N M2nXOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlP3TWM2OD1zOEeuPVY6KM7:TR?= MWDTRW5ITVJ?
KMS-12-PE NX;pSVFNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYPBZ5pLUUN3ME2xPFkvOjd|IN88US=> MYLTRW5ITVJ?
Daudi MmTTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH3ROVJKSzVyPUG5NU4yOjhizszN M3OzeXNCVkeHUh?=
LB996-RCC NFv1TJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWPvW4Q6UUN3ME2xPVEvPjl7IN88US=> M3XHZnNCVkeHUh?=
NCI-H2107 NIW1VXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFvYbZhKSzVyPUG5N{44OzlizszN MYLTRW5ITVJ?
SK-PN-DW Mn;US5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF\DZ5NKSzVyPUG5OE44OTlizszN NGLqfpNUSU6JRWK=
MC-CAR NHfmTXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWPJR|UxRTJyMj6yOVMh|ryP M4HDTnNCVkeHUh?=
SNB75 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX;JR|UxRTJ{MT65OEDPxE1? NHj4VlhUSU6JRWK=
ES4 Ml7LS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUjJR|UxRTJ{Mz63PFMh|ryP NHHldm5USU6JRWK=
KARPAS-422 M1zvVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVPJR|UxRTJ{OD6zOVIh|ryP NIXZU4FUSU6JRWK=
NCI-H1648 NIjKTHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoXTTWM2OD1{MkmuOFg6KM7:TR?= MVfTRW5ITVJ?
ES6 NXzzcnpyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFrjOINKSzVyPUKzPU41OyEQvF2= NFjUOGxUSU6JRWK=
KNS-81-FD M1HIUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2DrTmlEPTB;MkSxMlE6PyEQvF2= NX7tS3p6W0GQR1XS
JAR NIiwV3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{Cy[GlEPTB;MkW2MlIzPSEQvF2= M{jCSXNCVkeHUh?=
NB1 Mm\FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXHJR|UxRTJ4MD61NVYh|ryP MoG0V2FPT0WU
D-336MG M3rBdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmH2TWM2OD1{NkCuOlk5KM7:TR?= NG[0PYFUSU6JRWK=
BC-3 M{K2bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2O3ZmlEPTB;Mk[1MlE4QCEQvF2= M3vJcXNCVkeHUh?=
HCC2218 NEG4XFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{mwWGlEPTB;Mk[2MlQyPSEQvF2= MoXBV2FPT0WU
TE-9 NGnU[ldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVzvS29WUUN3ME2yOlYvPjJ5IN88US=> MWrTRW5ITVJ?
LB1047-RCC Ml3pS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYLJR|UxRTJ4Nj63OVMh|ryP NWfKcJBjW0GQR1XS
CTB-1 M4HQRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXvJR|UxRTJ4OT65O|Mh|ryP M1\ae3NCVkeHUh?=
NB7 MlHSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV3JR|UxRTJ5MTFOwG0> Mn;hV2FPT0WU
ST486 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX7JR|UxRTJ5Nz60NVIh|ryP MWTTRW5ITVJ?
HCC1187 NWfieVF3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnvJTWM2OD1{OEKuPFEyKM7:TR?= NIDySJdUSU6JRWK=
NCI-SNU-16 NWfncFdGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEewWIVKSzVyPUK4OE4zPDhizszN NH\hc5hUSU6JRWK=
COR-L279 M{j5Wmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYDJR|UxRTJ7MT61PFQh|ryP NWjhfpdxW0GQR1XS
ES8 M1v0U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{PnPGlEPTB;Mkm0MlE5OiEQvF2= MkjMV2FPT0WU
U-698-M NEXqSotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHLnTVZKSzVyPUK5PE4zPDNizszN MkTZV2FPT0WU
HEL NXz2RW9ET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI\ROVlKSzVyPUOwPU4yPDlizszN NV;jS2J3W0GQR1XS
KINGS-1 Mn7LS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYfJR|UxRTNzMD62O|Qh|ryP M3HUUXNCVkeHUh?=
KY821 NWrWcFR6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFHw[XVKSzVyPUOzOk42QTVizszN NUOxNHFFW0GQR1XS
MZ1-PC NF7B[HVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX7JR|UxRTN2NT62NVgh|ryP M{HCbnNCVkeHUh?=
LS-411N Mm\nS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MluxTWM2OD1|NUSuOlYh|ryP M1XNWHNCVkeHUh?=
SIG-M5 M3u0SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUXJR|UxRTN3OT63PFIh|ryP NYTBcJcxW0GQR1XS
HT NXTOVHlFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkG1TWM2OD1|NkeuO|EyKM7:TR?= NYfKXG5EW0GQR1XS
HC-1 NWe3UXpjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{T4WGlEPTB;M{[3Mlc5PyEQvF2= Ml3nV2FPT0WU
NCI-H1694 NX3KOnM5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGOye3ZKSzVyPUO3Nk46OzRizszN M1[yfnNCVkeHUh?=
BB65-RCC MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWnQc2l3UUN3ME2zO|YvOjR3IN88US=> M{CxfHNCVkeHUh?=
HAL-01 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV;JR|UxRTN5OT64N|gh|ryP Mmm5V2FPT0WU
ARH-77 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn7pTWM2OD1|OUSuNFA5KM7:TR?= MX7TRW5ITVJ?
MZ7-mel NI\UfoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUDJR|UxRTN7Nz6yN|Mh|ryP M4rwOXNCVkeHUh?=
SIMA Mm\VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF:zWm1KSzVyPUSwN{46OzNizszN MWnTRW5ITVJ?
DG-75 NXu4V4ptT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUnzclJXUUN3ME20NVUvPjl6IN88US=> M1XONXNCVkeHUh?=
HUTU-80 NXzVOmUzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3fsU2lEPTB;NEG5MlE5PSEQvF2= NX6yPGZ7W0GQR1XS
KNS-42 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1mxT2lEPTB;NEK1MlgyPSEQvF2= MlHLV2FPT0WU
SH-4 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGThRZBKSzVyPUSyO{42PjVizszN NHnkUW5USU6JRWK=
L-540 M13oRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4\hVmlEPTB;NEOxMlA{OSEQvF2= Mn34V2FPT0WU
NB10 M4Xkd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkfLTWM2OD12NEGuNlM1KM7:TR?= MkH2V2FPT0WU
ES1 NHvGNlNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NITXSW1KSzVyPUS1Nk44PTNizszN NYLUTGtDW0GQR1XS
KMOE-2 NEW4R29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M37KWGlEPTB;NEW2MlcyOSEQvF2= NH;rZo5USU6JRWK=
MC116 M{Dkd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVXJR|UxRTR3OD6xNVYh|ryP NXH4R4ZEW0GQR1XS
RCC10RGB NVTjUlB4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml;STWM2OD12NkCuNFA2KM7:TR?= NF;3bldUSU6JRWK=
RL95-2 NH\sVI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFjF[5RKSzVyPUS2NE4zOzdizszN MnHIV2FPT0WU
Raji MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4Xzd2lEPTB;NE[4MlE1OyEQvF2= M3XEVnNCVkeHUh?=
CAS-1 MnzPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4PMWGlEPTB;NEeyMlA4OyEQvF2= NE\uSnhUSU6JRWK=
Calu-6 NYm0[FVUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlLGTWM2OD12N{WuNlY2KM7:TR?= NX;IdZYzW0GQR1XS
KG-1 NXqzVYpvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWH1N5dsUUN3ME20O|gvPDRizszN MXLTRW5ITVJ?
LB771-HNC MlT0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXiyfodHUUN3ME20PFIvOjN{IN88US=> M1frbHNCVkeHUh?=
ACN M4j0Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlrpTWM2OD12OUOuOVk6KM7:TR?= NH7ZUWVUSU6JRWK=
KM12 M1XuZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF\Lfo1KSzVyPUS5Ok42QDlizszN NYWyZ4RFW0GQR1XS

... 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

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

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Dilution Calculator

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

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

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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 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