DU145 |
Growth inhibition assay |
5 uM |
96 hrs |
Growth inhibition of human DU145 cells at 5 uM after 96 hrs |
18249125 |
DU145 |
Growth inhibition assay |
10 uM |
96 hrs |
Growth inhibition of human DU145 cells at 10 uM after 96 hrs |
18249125 |
PANC1 |
Function assay |
0.2 uM |
24 hrs |
Inhibition of Hh/GLI1-mediated PTCH mRNA expression in human PANC1 cells at 0.2 uM after 24 hrs by RT-PCR |
20450170 |
PANC1 |
Function assay |
0.4 uM |
24 hrs |
Inhibition of Hh/GLI1-mediated PTCH mRNA expression in human PANC1 cells at 0.4 uM after 24 hrs by RT-PCR |
20450170 |
Shh Light2 |
Function assay |
6.25 uM |
30 hrs |
Inhibition of N-palmitoylated Shh in mouse Shh Light2 cells at 6.25 uM after 30 hrs by firefly luciferase reporter gene assay |
19151731 |
U87MG |
Function assay |
10 uM |
4 hrs |
Inhibition of Hedgehog signaling pathway in human U87MG cells assessed as down regulation of Gli1 at 10 uM after 4 hrs by RT-PCR analysis |
22226657 |
HEK293 |
Function assay |
5 uM |
10 hrs |
Displacement of BODIPY-cyclopamine from human Smo expressed in HEK293 cells at 5 uM measured after 10 hrs by DAPI staining based fluorescence microscopic assay |
27736063 |
HEK293 |
Function assay |
5 uM |
10 hrs |
Displacement of BODIPY-cyclopamine from human Smo expressed in HEK293 cells at 5 uM measured after 10 hrs by FACS analysis |
27736063 |
U2OS |
Function assay |
5 uM |
6 hrs |
Antagonist activity at chimeric Smo 633 mutant expressed in U2OS cells coexpressing beta arrestin2-GFP assessed as inhibition of intracellular beta arrestin2-GFP aggregate formation at 5 uM after 6 hrs by confocal microscopy |
23063522 |
C3H10T1/2 |
Function assay |
55.5 to 4500 nM |
|
Competitive inhibition of Smo in mouse C3H10T1/2 cells assessed as inhibition of SAG-induced Gli1 transcriptional activity at 55.5 to 4500 nM by qPCR analysis |
23074541 |
U2OS |
Function assay |
|
2 hrs |
Displacement of [3H]cyclopamine from wild type Smo expressed in U2OS cells after 2 hrs by scintillation counting, Ki = 0.0127 μM. |
23063522 |
TM3 |
Function assay |
|
48 hrs |
Inhibition of Hedgehog signaling pathway in mouse TM3 cells bearing pTA-8xGli-Luc reporter construct assessed as transcriptional modulation of Gli after 48 hrs by luciferase assay, IC50 = 0.046 μM. |
19091559 |
HEK293 |
Function assay |
|
2 hrs |
Displacement of BODIPY-labelled cyclopamine from human Smo receptor expressed in HEK293 cells after 2 hrs by fluorescence microscopy, IC50 = 0.064 μM. |
22268551 |
Shh Light2 |
Function assay |
|
30 hrs |
Inhibition of hedgehog signaling pathway in mouse Shh Light2 cells assessed as inhibition of sonic hedgehog-induced GLI1-mediated transcriptional activity measured after 30 hrs by dual luciferase reporter gene assay, IC50 = 0.0741 μM. |
27567371 |
DaOY |
Function assay |
|
48 hrs |
Inhibition of Hedgehog signaling in human DaOY cells assessed as downregulation of Gli1 mRNA expression after 48 hrs by RT-PCR analysis, IC50 = 0.16 μM. |
24900716 |
U2OS |
Function assay |
|
2 hrs |
Displacement of [3H]cyclopamine from Smo D473H mutant expressed in U2OS cells after 2 hrs by scintillation counting, Ki = 0.232 μM. |
23063522 |
Shh Light2 |
Function assay |
|
40 hrs |
Inhibition of SHH pathway in mouse Shh Light2 cells after 40 hrs by Gli-dependent luciferase reporter gene assay, IC50 = 0.3 μM. |
21592788 |
M210B4 |
Function assay |
|
24 hrs |
Inhibition of Hedgehog signaling in mouse M210B4 cells assessed as downregulation of Ptch mRNA expression after 24 hrs by RT-PCR analysis, IC50 = 0.43 μM. |
24900716 |
Shh-Light 2 |
Function assay |
|
2 days |
Antagonist activity at Smo in mouse Shh-Light 2 cells assessed as inhibition of Shh-induced Gli1-reporter activity after 2 days by dual-luciferase reporter gene method, IC50 = 0.484 μM. |
23063522 |
C3H10T1/2 |
Function assay |
|
6 hrs |
Inhibition of SAG-induced differentiation of mouse mesenchymal pluripotent C3H10T1/2 cells to alkaline phosphatase positive oeseoblasts after 6 hrs, IC50 = 0.62 μM. |
22268551 |
ASZ001 |
Function assay |
|
48 hrs |
Inhibition of Hedgehog signaling in mouse ASZ001 cells assessed as downregulation of Gli1 mRNA expression after 48 hrs by RT-PCR analysis, IC50 = 0.66 μM. |
24900716 |
M210B4 |
Function assay |
|
24 hrs |
Inhibition of Hedgehog signaling in mouse M210B4 cells assessed as downregulation of Gli1 mRNA expression after 24 hrs by RT-PCR analysis, IC50 = 0.8 μM. |
24900716 |
Shh-Light2 |
Function assay |
|
48 hrs |
Inhibition of SHH in mouse Shh-Light2 cells after 48 hrs by Gli1 reporter gene assay in presence of SAG, IC50 = 1.312 μM. |
19541490 |
MEF |
Function assay |
|
30 hrs |
Inhibition of Smo in mouse Ptch-deficient MEF cells assessed as inhibition of Shh-induced Gli-responsive betagalactosidase activity after 30 hrs by BetaGLo assay, IC50 = 1.9 μM. |
23074541 |
U87MG |
Antiproliferative assay |
|
72 hrs |
Antiproliferative activity against human U87MG cells after 72 hrs by MTS assay, IC50 = 22.5 μM. |
22226657 |
KALS-1 |
Growth Inhibition Assay |
|
|
IC50=115.941 μM |
SANGER |
NCCIT |
Growth Inhibition Assay |
|
|
IC50=112.529 μM |
SANGER |
NCI-H82 |
Growth Inhibition Assay |
|
|
IC50=110.976 μM |
SANGER |
NCI-H1770 |
Growth Inhibition Assay |
|
|
IC50=108.784 μM |
SANGER |
MOLT-16 |
Growth Inhibition Assay |
|
|
IC50=104.986 μM |
SANGER |
KS-1 |
Growth Inhibition Assay |
|
|
IC50=101.639 μM |
SANGER |
LB2518-MEL |
Growth Inhibition Assay |
|
|
IC50=100.789 μM |
SANGER |
BV-173 |
Growth Inhibition Assay |
|
|
IC50=100.325 μM |
SANGER |
GCIY |
Growth Inhibition Assay |
|
|
IC50=99.0954 μM |
SANGER |
BE-13 |
Growth Inhibition Assay |
|
|
IC50=99.0477 μM |
SANGER |
KARPAS-45 |
Growth Inhibition Assay |
|
|
IC50=84.6992 μM |
SANGER |
HCC1599 |
Growth Inhibition Assay |
|
|
IC50=84.2837 μM |
SANGER |
LP-1 |
Growth Inhibition Assay |
|
|
IC50=82.8731 μM |
SANGER |
OCI-AML2 |
Growth Inhibition Assay |
|
|
IC50=76.9369 μM |
SANGER |
D-247MG |
Growth Inhibition Assay |
|
|
IC50=73.5442 μM |
SANGER |
MRK-nu-1 |
Growth Inhibition Assay |
|
|
IC50=73.4705 μM |
SANGER |
MHH-PREB-1 |
Growth Inhibition Assay |
|
|
IC50=72.8441 μM |
SANGER |
D-542MG |
Growth Inhibition Assay |
|
|
IC50=68.4135 μM |
SANGER |
KE-37 |
Growth Inhibition Assay |
|
|
IC50=66.2668 μM |
SANGER |
OVCAR-4 |
Growth Inhibition Assay |
|
|
IC50=63.5657 μM |
SANGER |
MV-4-11 |
Growth Inhibition Assay |
|
|
IC50=60.6538 μM |
SANGER |
IST-MES1 |
Growth Inhibition Assay |
|
|
IC50=60.5493 μM |
SANGER |
GI-1 |
Growth Inhibition Assay |
|
|
IC50=56.6149 μM |
SANGER |
DJM-1 |
Growth Inhibition Assay |
|
|
IC50=56.3391 μM |
SANGER |
LOXIMVI |
Growth Inhibition Assay |
|
|
IC50=53.5884 μM |
SANGER |
SK-NEP-1 |
Growth Inhibition Assay |
|
|
IC50=53.3923 μM |
SANGER |
ML-2 |
Growth Inhibition Assay |
|
|
IC50=52.9195 μM |
SANGER |
D-502MG |
Growth Inhibition Assay |
|
|
IC50=51.6271 μM |
SANGER |
CTV-1 |
Growth Inhibition Assay |
|
|
IC50=51.074 μM |
SANGER |
MS-1 |
Growth Inhibition Assay |
|
|
IC50=50.9351 μM |
SANGER |
RS4-11 |
Growth Inhibition Assay |
|
|
IC50=49.0938 μM |
SANGER |
CESS |
Growth Inhibition Assay |
|
|
IC50=44.2232 μM |
SANGER |
NTERA-S-cl-D1 |
Growth Inhibition Assay |
|
|
IC50=42.7074 μM |
SANGER |
A388 |
Growth Inhibition Assay |
|
|
IC50=42.5848 μM |
SANGER |
LC4-1 |
Growth Inhibition Assay |
|
|
IC50=40.8716 μM |
SANGER |
no-11 |
Growth Inhibition Assay |
|
|
IC50=40.5521 μM |
SANGER |
D-392MG |
Growth Inhibition Assay |
|
|
IC50=40.2215 μM |
SANGER |
IST-SL2 |
Growth Inhibition Assay |
|
|
IC50=38.224 μM |
SANGER |
BC-1 |
Growth Inhibition Assay |
|
|
IC50=37.9746 μM |
SANGER |
BB30-HNC |
Growth Inhibition Assay |
|
|
IC50=34.3306 μM |
SANGER |
NOS-1 |
Growth Inhibition Assay |
|
|
IC50=34.2956 μM |
SANGER |
LAMA-84 |
Growth Inhibition Assay |
|
|
IC50=32.5211 μM |
SANGER |
L-363 |
Growth Inhibition Assay |
|
|
IC50=31.7461 μM |
SANGER |
ATN-1 |
Growth Inhibition Assay |
|
|
IC50=31.2329 μM |
SANGER |
EVSA-T |
Growth Inhibition Assay |
|
|
IC50=27.5561 μM |
SANGER |
COLO-829 |
Growth Inhibition Assay |
|
|
IC50=26.8483 μM |
SANGER |
697 |
Growth Inhibition Assay |
|
|
IC50=26.6155 μM |
SANGER |
SR |
Growth Inhibition Assay |
|
|
IC50=23.6715 μM |
SANGER |
DEL |
Growth Inhibition Assay |
|
|
IC50=20.1471 μM |
SANGER |
NALM-6 |
Growth Inhibition Assay |
|
|
IC50=19.0167 μM |
SANGER |
EoL-1-cell |
Growth Inhibition Assay |
|
|
IC50=18.5948 μM |
SANGER |
RPMI-8402 |
Growth Inhibition Assay |
|
|
IC50=15.8537 μM |
SANGER |
8-MG-BA |
Growth Inhibition Assay |
|
|
IC50=13.1123 μM |
SANGER |
ALL-PO |
Growth Inhibition Assay |
|
|
IC50=11.7734 μM |
SANGER |
LS-513 |
Growth Inhibition Assay |
|
|
IC50=11.3547 μM |
SANGER |
no-10 |
Growth Inhibition Assay |
|
|
IC50=9.9039 μM |
SANGER |
DOHH-2 |
Growth Inhibition Assay |
|
|
IC50=9.35689 μM |
SANGER |
OS-RC-2 |
Growth Inhibition Assay |
|
|
IC50=5.8666 μM |
SANGER |
LB2241-RCC |
Growth Inhibition Assay |
|
|
IC50=116.679 μM |
SANGER |
HH |
Growth Inhibition Assay |
|
|
IC50=117.395 μM |
SANGER |
HD-MY-Z |
Growth Inhibition Assay |
|
|
IC50=118.488 μM |
SANGER |
EB-3 |
Growth Inhibition Assay |
|
|
IC50=123.094 μM |
SANGER |
BL-70 |
Growth Inhibition Assay |
|
|
IC50=123.127 μM |
SANGER |
K-562 |
Growth Inhibition Assay |
|
|
IC50=126.245 μM |
SANGER |
HT-144 |
Growth Inhibition Assay |
|
|
IC50=133.164 μM |
SANGER |
PF-382 |
Growth Inhibition Assay |
|
|
IC50=134.361 μM |
SANGER |
RPMI-8226 |
Growth Inhibition Assay |
|
|
IC50=135.045 μM |
SANGER |
NCI-H1355 |
Growth Inhibition Assay |
|
|
IC50=135.587 μM |
SANGER |
LXF-289 |
Growth Inhibition Assay |
|
|
IC50=139.781 μM |
SANGER |
NCI-H69 |
Growth Inhibition Assay |
|
|
IC50=142.932 μM |
SANGER |
SK-MEL-1 |
Growth Inhibition Assay |
|
|
IC50=147.13 μM |
SANGER |
KARPAS-299 |
Growth Inhibition Assay |
|
|
IC50=149.12 μM |
SANGER |
GB-1 |
Growth Inhibition Assay |
|
|
IC50=149.322 μM |
SANGER |
CMK |
Growth Inhibition Assay |
|
|
IC50=149.515 μM |
SANGER |
MPP-89 |
Growth Inhibition Assay |
|
|
IC50=156.035 μM |
SANGER |
KU812 |
Growth Inhibition Assay |
|
|
IC50=161.902 μM |
SANGER |
REH |
Growth Inhibition Assay |
|
|
IC50=162.125 μM |
SANGER |
NEC8 |
Growth Inhibition Assay |
|
|
IC50=165.026 μM |
SANGER |
KP-N-YS |
Growth Inhibition Assay |
|
|
IC50=168.395 μM |
SANGER |
Ramos-2G6-4C10 |
Growth Inhibition Assay |
|
|
IC50=169.915 μM |
SANGER |
Becker |
Growth Inhibition Assay |
|
|
IC50=174.18 μM |
SANGER |
LB647-SCLC |
Growth Inhibition Assay |
|
|
IC50=175.845 μM |
SANGER |
LU-139 |
Growth Inhibition Assay |
|
|
IC50=178.019 μM |
SANGER |
QIMR-WIL |
Growth Inhibition Assay |
|
|
IC50=179.646 μM |
SANGER |
NCI-H1395 |
Growth Inhibition Assay |
|
|
IC50=179.996 μM |
SANGER |
NOMO-1 |
Growth Inhibition Assay |
|
|
IC50=182.85 μM |
SANGER |
GI-ME-N |
Growth Inhibition Assay |
|
|
IC50=187.969 μM |
SANGER |
KMS-12-PE |
Growth Inhibition Assay |
|
|
IC50=189.273 μM |
SANGER |
Daudi |
Growth Inhibition Assay |
|
|
IC50=191.128 μM |
SANGER |
LB996-RCC |
Growth Inhibition Assay |
|
|
IC50=191.699 μM |
SANGER |
NCI-H2107 |
Growth Inhibition Assay |
|
|
IC50=193.739 μM |
SANGER |
SK-PN-DW |
Growth Inhibition Assay |
|
|
IC50=194.719 μM |
SANGER |
MC-CAR |
Growth Inhibition Assay |
|
|
IC50=202.253 μM |
SANGER |
SNB75 |
Growth Inhibition Assay |
|
|
IC50=221.94 μM |
SANGER |
ES4 |
Growth Inhibition Assay |
|
|
IC50=223.783 μM |
SANGER |
KARPAS-422 |
Growth Inhibition Assay |
|
|
IC50=228.352 μM |
SANGER |
NCI-H1648 |
Growth Inhibition Assay |
|
|
IC50=229.489 μM |
SANGER |
ES6 |
Growth Inhibition Assay |
|
|
IC50=239.43 μM |
SANGER |
KNS-81-FD |
Growth Inhibition Assay |
|
|
IC50=241.197 μM |
SANGER |
JAR |
Growth Inhibition Assay |
|
|
IC50=256.225 μM |
SANGER |
NB1 |
Growth Inhibition Assay |
|
|
IC50=260.516 μM |
SANGER |
D-336MG |
Growth Inhibition Assay |
|
|
IC50=260.698 μM |
SANGER |
BC-3 |
Growth Inhibition Assay |
|
|
IC50=265.178 μM |
SANGER |
HCC2218 |
Growth Inhibition Assay |
|
|
IC50=266.415 μM |
SANGER |
TE-9 |
Growth Inhibition Assay |
|
|
IC50=266.627 μM |
SANGER |
LB1047-RCC |
Growth Inhibition Assay |
|
|
IC50=266.753 μM |
SANGER |
CTB-1 |
Growth Inhibition Assay |
|
|
IC50=269.973 μM |
SANGER |
NB7 |
Growth Inhibition Assay |
|
|
IC50=271 μM |
SANGER |
ST486 |
Growth Inhibition Assay |
|
|
IC50=277.412 μM |
SANGER |
HCC1187 |
Growth Inhibition Assay |
|
|
IC50=282.811 μM |
SANGER |
NCI-SNU-16 |
Growth Inhibition Assay |
|
|
IC50=284.248 μM |
SANGER |
COR-L279 |
Growth Inhibition Assay |
|
|
IC50=291.584 μM |
SANGER |
ES8 |
Growth Inhibition Assay |
|
|
IC50=294.182 μM |
SANGER |
U-698-M |
Growth Inhibition Assay |
|
|
IC50=298.243 μM |
SANGER |
HEL |
Growth Inhibition Assay |
|
|
IC50=309.149 μM |
SANGER |
KINGS-1 |
Growth Inhibition Assay |
|
|
IC50=310.674 μM |
SANGER |
KY821 |
Growth Inhibition Assay |
|
|
IC50=336.595 μM |
SANGER |
MZ1-PC |
Growth Inhibition Assay |
|
|
IC50=345.618 μM |
SANGER |
LS-411N |
Growth Inhibition Assay |
|
|
IC50=354.66 μM |
SANGER |
SIG-M5 |
Growth Inhibition Assay |
|
|
IC50=359.782 μM |
SANGER |
HT |
Growth Inhibition Assay |
|
|
IC50=367.711 μM |
SANGER |
HC-1 |
Growth Inhibition Assay |
|
|
IC50=367.787 μM |
SANGER |
NCI-H1694 |
Growth Inhibition Assay |
|
|
IC50=372.934 μM |
SANGER |
BB65-RCC |
Growth Inhibition Assay |
|
|
IC50=376.245 μM |
SANGER |
HAL-01 |
Growth Inhibition Assay |
|
|
IC50=379.838 μM |
SANGER |
ARH-77 |
Growth Inhibition Assay |
|
|
IC50=394.008 μM |
SANGER |
MZ7-mel |
Growth Inhibition Assay |
|
|
IC50=397.233 μM |
SANGER |
SIMA |
Growth Inhibition Assay |
|
|
IC50=403.933 μM |
SANGER |
DG-75 |
Growth Inhibition Assay |
|
|
IC50=415.698 μM |
SANGER |
HUTU-80 |
Growth Inhibition Assay |
|
|
IC50=419.185 μM |
SANGER |
KNS-42 |
Growth Inhibition Assay |
|
|
IC50=425.815 μM |
SANGER |
SH-4 |
Growth Inhibition Assay |
|
|
IC50=427.565 μM |
SANGER |
L-540 |
Growth Inhibition Assay |
|
|
IC50=431.031 μM |
SANGER |
NB10 |
Growth Inhibition Assay |
|
|
IC50=441.234 μM |
SANGER |
ES1 |
Growth Inhibition Assay |
|
|
IC50=452.753 μM |
SANGER |
KMOE-2 |
Growth Inhibition Assay |
|
|
IC50=456.711 μM |
SANGER |
MC116 |
Growth Inhibition Assay |
|
|
IC50=458.116 μM |
SANGER |
RCC10RGB |
Growth Inhibition Assay |
|
|
IC50=460.005 μM |
SANGER |
RL95-2 |
Growth Inhibition Assay |
|
|
IC50=460.237 μM |
SANGER |
Raji |
Growth Inhibition Assay |
|
|
IC50=468.143 μM |
SANGER |
CAS-1 |
Growth Inhibition Assay |
|
|
IC50=472.073 μM |
SANGER |
Calu-6 |
Growth Inhibition Assay |
|
|
IC50=475.265 μM |
SANGER |
KG-1 |
Growth Inhibition Assay |
|
|
IC50=478.44 μM |
SANGER |
LB771-HNC |
Growth Inhibition Assay |
|
|
IC50=482.232 μM |
SANGER |
ACN |
Growth Inhibition Assay |
|
|
IC50=493.599 μM |
SANGER |
KM12 |
Growth Inhibition Assay |
|
|
IC50=496.589 μM |
SANGER |
U2OS |
Function assay |
|
|
Binding affinity to wild type Smo expressed in U2OS cells by scintillation counting, Kd = 0.0124 μM. |
23063522 |
HCC827 |
Function assay |
|
|
Displacement of [3H]-cyclopamine from SMO V404M mutant in gefitinib resistant human HCC827 cells by scintillation counting, Ki = 0.051 μM. |
28787156 |
U2OS |
Function assay |
|
|
Binding affinity to Smo D473H mutant expressed in U2OS cells by scintillation counting, Kd = 0.116 μM. |
23063522 |
CHO |
Function assay |
|
|
Antagonist activity at human Smo receptor expressed in CHO cells by [3H]Hh-Ag binding assay, IC50 = 0.28 μM. |
19091559 |
Shh-light2 |
Function assay |
|
|
Inhibition of Smo-mediated Hh signaling in human Shh-light2 cells by luciferase reporter gene assay, IC50 = 0.3 μM. |
22268551 |
Shh Light2 |
Function assay |
|
|
Inhibition of SHH in mouse Shh Light2 cells by GLI-responsive firefly luciferase reporter gene assay, EC50 = 0.5 μM. |
19309080 |
C3H10T1/2 |
Function assay |
|
|
Inhibition of N-terminal SHH activated pathway in mouse C3H10T1/2 cells assessed as SAG-induced cell differentiation by alkaline phosphatase assay, IC50 = 0.6 μM. |
21592788 |
medulloblastoma cells |
Antiproliferative assay |
|
|
Antiproliferative activity against mouse medulloblastoma cells harboring heterozygous ptch1 gene by MTT assay, EC50 = 1 μM. |
17417631 |
CHO |
Function assay |
|
|
Antagonist activity at mouse Smo receptor expressed in CHO cells by [3H]Hh-Ag binding assay, IC50 = 1.2 μM. |
19091559 |
MEF |
Function assay |
|
|
Inhibition of Smo in mouse Ptch-deficient MEF cells assessed as inhibition of Shh-induced Gli1 transcriptional activity, IC50 = 1.5 μM. |
23074541 |
neural precursor cells |
Antiproliferative assay |
|
|
Antiproliferative activity against mouse neural precursor cells by colony formation assay, EC50 = 13.44 μM. |
17417631 |
U87 |
Cytotoxicity assay |
|
|
Cytotoxicity against human U87 cells assessed as viability in presence of beta glucuronidase, IC50 = 15.5 μM. |
20116904 |
A549 |
Anticancer assay |
|
|
Anticancer activity against human A549 cells by MTS assay, IC50 = 49 μM. |
18221872 |
HEK293 |
Function assay |
|
|
Inhibition of beta galactosidase in HEK293 cells |
17494766 |
22Rv |
Function assay |
|
|
Reduction of expression of PTCH mRNA in human 22Rv cells |
17494766 |