GANT61

Catalog No.S8075 Synonyms: NSC 136476

For research use only.

GANT61 (NSC 136476) 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. GANT61 induces apoptosis and activates protective autophagy in LX-2 cells.

GANT61 Chemical Structure

CAS No. 500579-04-4

Selleck's GANT61 has been cited by 80 publications

Purity & Quality Control

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Biological Activity

Description GANT61 (NSC 136476) 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. GANT61 induces apoptosis and activates protective autophagy in LX-2 cells.
Targets
GLI1 [1]
(HEK293T cells expressing GLI1)
5 μM
In vitro

GANT61 is an inhibitor for GLI1 as well as GLI2-induced transcription. GANT61 inhibits the DNA binding ability of GLI1. GANT61 inhibits hedgehog signaling with IC50 of 5 μM, displays selectivity over other pathways, such as TNF signaling/NFκB activation, glucocorticoid receptor gene transactivation, and the Ras–Raf–Mek–Mapk cascade. GANT61 efficiently inhibited in vitro tumor cell proliferation in a GLI-dependent manner. [1] GANT61 induces apoptosis in chronic lymphocytic leukemia cells (CLL), but not in normal B lymphocytes. [2] GANT61 induces robust cytotoxicity and abolishs the clonogenicity in human colon carcinoma cell lines. [3] GANT61 induces inhibition of DNA replication in early S-phase in human colon carcinoma cell lines, leading to DNA damage signaling involving an ATM–Chk2 axis and induction of cell death. [4] GANT61 (30 μM) causes growth arrest and apoptosis in acute myeloid leukemia (AML) cells. [5]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Shh Light2 NIXtfWFHfW6ldHnvckBie3OjeR?= NHy0bIlKdmirYnn0bY9vKG:oIGPITEBqdiCvb4Xz[UBUcGhiTHnnbJQzKGOnbHzzJIJ6KEeOST3y[ZNxd26|aY\lJIZqemWobImgcJVkcW[ncnHz[UBz\XCxcoTldkBo\W6nIHHzd4F6NCCLQ{WwJF0hPSEQvF2u NV3afXBERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUmzNFkxQDBpPkG5N|A6ODhyPD;hQi=>
Shh-L2 MWXGeY5kfGmxbjDhd5NigQ>? MXfJcohq[mm2aX;uJI9nKEinZHflbI9oKHOrZ37hcIlv\yCrbjDoeY1idiCVaHitUFIh[2WubIOsJGlEPTBiPTC1JO69VS5? Ml;1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd2OUS3OlYoRjF5NEm0O|Y3RC:jPh?=
NIH 3T3 M3uz[mZ2dmO2aX;uJIF{e2G7 NFnaOlhKdmirYnn0bY9vKG:oIFjoJJNq\26jbHnu[{Bx[XSqd3H5JIlvKFOqaD3MTWdJXDJiaX7jc5Jxd3KjdHXkJI1wfXOnIF7JTEA{XDNiY3XscJMh[XO|ZYPz[YQh[XNiZH;3cpJm\3WuYYTpc44hd2ZiR3zpNUBo\W6nIHX4dJJme3Orb36gZpkhdHWlaX\ldoF{\SC{ZYDvdpRmeiCpZX7lJIF{e2G7LDDFR|UxKD1iNTFOwG0v NFvYbok9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nkm3OlIyPSd-Mk[5O|YzOTV:L3G+
HeLa NHTqeJVHfW6ldHnvckBie3OjeR?= NIL6d4U1NjViaILz M2TucGlvcGmkaYTpc44hd2ZiRXLvcIF3cXK3czDncJlkd3C{b4TlbY4wdWG2cnn4JJBzd3SnaX6gWnA1OCCnboTyfUBqdiCqdX3hckBJ\UyjIHPlcIx{KGGodHXyJFQvPSCqcoOgZoV1[S2uYXP0ZY1ie2VicnXwc5J1\XJiYYPzZZktKEmFNUCgQUA3Njh|IN88UU4> M1zzNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NkK0N|g4Lz5{OU[yOFM5PzxxYU6=
TM3 NW\sXHk6TnWwY4Tpc44h[XO|YYm= NYfNSI5QPDhiaILz M{LQOGlvcGmkaYTpc44hd2ZiSHigd4lodmGuaX7nJJBifGi5YYmgbY4hdW:3c3WgWG0{KGOnbHzzJIF{e2W|c3XkJIF{KGSxd37y[Yd2dGG2aX;uJI9nKEeuaUGg[4Vv\SCneIDy[ZN{cW:wIHHmeIVzKDR6IHjyd{BjgSCudXPp[oVz[XOnIILldI9zfGW{IHflcoUh[XO|YYmsJGVEPTBiPTC5MlI4KM7:TT6= MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjl5NkKxOUc,OjZ7N{[yNVU9N2F-
Rh30 NX33WVJwTnWwY4Tpc44h[XO|YYm= NYHzUIhUOjRiaILz MnzKTY5pcWKrdHnvckBw\iCqdX3hckBIdGlzLX3l[IlifGWmIITyZY5{[3KrcITpc45idCCjY4Tpeol1gSCrbjDoeY1idiCUaEOwJINmdGy|IHHmeIVzKDJ2IHjyd{BjgSCudXPp[oVz[XOnIILldI9zfGW{IHflcoUh[XO|YYmsJGlEPTBiPTC0NEDPxE1w MoK3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB4MEW3NlAoRjJyNkC1O|IxRC:jPh?=
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NIH3T3 NHvkc|ZHfW6ldHnvckBie3OjeR?= NV;LbHFpUW6qaXLpeIlwdiCxZjDHUGkyKGmwZIXj[YQhcGWmZ3Xoc4che2mpbnHsbY5oKGmwIH3veZNmKE6LSEPUN{Bk\Wyucx?= M4H6NFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5NEm0O|Y3Lz5zN{S5OFc3PjxxYU6=
HEK293 MXXGeY5kfGmxbjDhd5NigQ>? MofMTY5pcWKrdHnvckBw\iCkZYThJIdidGGldH;zbYRie2ViaX6gTGVMOjl|IHPlcIx{ MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzR7NEe2Okc,OTd2OUS3OlY9N2F-
MEF MV\GeY5kfGmxbjDhd5NigQ>? NXzLVZJ4WmWmdXP0bY9vKGmwIHX4dJJme3Orb36gc4YhUGWmZ3Xoc4chfGG{Z3X0JIdmdmViSHnwNUBqdiCVdX\1JIRm\mmlaXXueEBud3W|ZTDNSWYh[2WubIO= M2XnUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5NEm0O|Y3Lz5zN{S5OFc3PjxxYU6=
NIH3T3 MXvGeY5kfGmxbjDhd5NigQ>? MXOxNEB2VQ>? MkTpTY5pcWKrdHnvckBw\iCKZXTn[Yhw\y:JbHmxJI1m\GmjdHXkJJRz[W6|Zn;ycYF1cW:wIHnuJI1wfXOnIF7JTFNVOyClZXzsd{BifCBzMDD1US=> NHOwS4w9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{S5OFc3Pid-MUe0PVQ4PjZ:L3G+
PANC1 NGXHSG9HfW6ldHnvckBie3OjeR?= NWLMUYlQPSC3TR?= NX3LUIRKWmWmdXP0bY9vKGmwIFfMTVEh\XiycnXzd4lwdiCrbjDoeY1idiCSQV7DNUBk\WyuczDheEA2KHWP M1e2SlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5NEm0O|Y3Lz5zN{S5OFc3PjxxYU6=
PANC1 MlL3SpVv[3Srb36gZZN{[Xl? Ml\QOUB2VQ>? MXfS[YR2[3Srb36gbY4hWFSFSDDlfJBz\XO|aX;uJIlvKGi3bXHuJHBCVkNzIHPlcIx{KGG2IEWgeW0> NGHib5E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{S5OFc3Pid-MUe0PVQ4PjZ:L3G+
22Rv NIHvNWdHfW6ldHnvckBie3OjeR?= MmnROUB2VQ>? M{T5VnJm\HWldHnvckBqdiCJbFmxJIV5eHKnc4Ppc44hcW5iaIXtZY4hOjKUdjDj[YxteyCjdDC1JJVO NWLjbpZYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUe0PVQ4PjZpPkG3OFk1PzZ4PD;hQi=>
22Rv M{Xx[mZ2dmO2aX;uJIF{e2G7 MXe1JJVO MVLS[YR2[3Srb36gbY4hWFSFSDDlfJBz\XO|aX;uJIlvKGi3bXHuJFIzWnZiY3XscJMh[XRiNTD1US=> MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzR7NEe2Okc,OTd2OUS3OlY9N2F-
22Rv M4nV[mZ2dmO2aX;uJIF{e2G7 NV;ubHJMWmWmdXP0bY9vKG:oIHX4dJJme3Orb36gc4YhWFSFSDDtVm5CKGmwIHj1cYFvKDJ{Uo[gZ4VtdHN? NIPXW449[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{S5OFc3Pid-MUe0PVQ4PjZ:L3G+
HEK293 MkjTSpVv[3Srb36gZZN{[Xl? NFraR4FKdmirYnn0bY9vKG:oIH71Z4xm[XJiYXPjeY12dGG2aX;uJI9nKEeOSTDteZRidnRiaX6gTGVMOjl|IHPlcIx{ M3e0fVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5NEm0O|Y3Lz5zN{S5OFc3PjxxYU6=
HEK293 Ml;wSpVv[3Srb36gZZN{[Xl? NXz6e5VbUW6qaXLpeIlwdiCxZjDueYNt\WG{IHHjZ5VufWyjdHnvckBw\iC5aXzkJJR6eGViR1zJJIlvKEiHS{K5N{Bk\Wyucx?= Mn3OQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd2OUS3OlYoRjF5NEm0O|Y3RC:jPh?=
HEK293 MoTWSpVv[3Srb36gZZN{[Xl? NXPEOmZ4WmWmdXP0bY9vKG:oIFfMTVEhdWWmaXH0[YQhfHKjboPjdolxfGmxbjDpckBJTUt{OUOgZ4VtdHNiYomgcJVkcW[ncnHz[UBz\XCxcoTldkBie3OjeR?= NHm2cI49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{S5OFc3Pid-MUe0PVQ4PjZ:L3G+
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HEK293 M1LqT2Z2dmO2aX;uJIF{e2G7 NFTteXY{OCC3TR?= M37FXmlvcGmkaYTpc44hd2ZiR1zJJEh2dmuwb4fuJI9zcWerbjmg[ZhxemW|c3XkJIlvKEiHS{K5N{Bk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iR1zJMY1m\GmjdHXkJJRz[W6|Y4LpdJRqd25iYYSgN|AhfU1? NFLPRlE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUW4NVAyPyd-MkW1PFExOTd:L3G+
A673 NWj5c3RveUiWUzDhd5NigQ>? MVfxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhSTZ5MzDj[Yxtew>? NUC5VmtMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SK-N-MC NHLuXW1yUFSVIHHzd4F6 M1PGZZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVSz3OMW1EKGOnbHzz MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
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OHS-50 Mn\JdWhVWyCjc4PhfS=> MWXxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhV0iVLUWwJINmdGy| MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
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SK-N-FI M3LiZmN6fG:2b4jpZ4l1gSCjc4PhfS=> MoXWO|IhcHK| MU\DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTT{1PNU[LIHPlcIx{KGGodHXyJFczKGi{czDifUBndHWxcn;t[ZRzcWNibXnjdo9kfWy2dYLlJIN6fG:2b4jpZ4l1gSCjc4PhfUwhT0l3MDC9JFUvQDJizszNMi=> MkfKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFcyPzJ6Lze+R4hGVUKOPD;hQi=>
SK-N-AS NEPzOppEgXSxdH;4bYNqfHliYYPzZZk> NXT3Zm9wPzJiaILz NVfF[o1MS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW0tvTj3BV{Bk\WyuczDh[pRmeiB5MjDodpMh[nliZnz1c5JwdWW2cnnjJI1q[3KxY4XseJVz\SCleYTveI95cWOrdImgZZN{[XluIFfJOVAhRSB3LkiyJO69VS5? MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0O|E4OjhxJ{7DbGVOSkx:L3G+
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SK-N-BE(2) Mn[5R5l1d3SxeHnjbZR6KGG|c3H5 NX;Kfo5oPzJiaILz NVzGXJl1S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW0tvTj3CSUgzMSClZXzsd{Bi\nSncjC3NkBpenNiYomg[ox2d3KxbXX0dolkKG2rY4LvZ5VtfHW{ZTDjfZRwfG:6aXPpeJkh[XO|YYmsJGdKPTBiPTC1MlgzKM7:TT6= MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0O|E4OjhxJ{7DbGVOSkx:L3G+
SH-SY5Y NH;qcllEgXSxdH;4bYNqfHliYYPzZZk> MYm3NkBpenN? MVjDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTTE1UYTW\IHPlcIx{KGGodHXyJFczKGi{czDifUBndHWxcn;t[ZRzcWNibXnjdo9kfWy2dYLlJIN6fG:2b4jpZ4l1gSCjc4PhfUwhT0l3MDC9JFUvQDJizszNMi=> M12zSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQ4OTd{OD:nQmNpTU2ETEyvZV4>
Assay
Methods Test Index PMID
Western blot GLI1 / p-STAT3 / STAT3 / SOCS3 ; GLI2 / Bcl-2 27275540 25544756
Immunofluorescence Gli2 24533083
Growth inhibition assay Cell viability 27275540
In vivo In nude mice injected with GLI1-positive 22Rv1 prostate cancer cells, GANT61 induces growth regression until no tumor is palpable. [1] In nude mice carrying SK-N-AS neuroblastoma xenografts, GANT61 treatment (oral gavage, 50 mg/kg) significantly inhibits tumor growth at Day 12 , as the tumor volume is reduced to 63% compared with controls. [6]

Protocol (from reference)

Kinase Assay:[1]
  • Dual Luciferase Assay:

    HEK293 cells are transfected with GLI1 expression plasmid, together with the reporter plasmids 12×GliBSLuc and R-Luc on 10-cm plates (day 0). Twenty-four hours later, cells are seeded in white 96-well plates with clear bottom at a density of 15,000 cells per well. Cells are allowed to attach, and compounds are added at a final concentration of 10 μM in DMSO (0.5% final DMSO concentration) (day 1.5). Cells are grown for another 24 h, subsequently lysed, and then analyzed by using the Dual Luciferase kit.

Cell Research:[1]
  • Cell lines: PANC1 or 22Rv1
  • Concentrations: ~5 μM
  • Incubation Time: 48 h
  • Method: BrdU Incorporation Assay. Subconfluent cells are grown in reduced FBS (2.5%) for 48 h in the presence of 5 μM test compound (or DMSO) on white 96-well plates with clear bottom. Subsequently, cells are labeled for 2 h with BrdU, fixed, and analyzed.
Animal Research:[1]
  • Animal Models: BALB/c nude mice with 22Rv1 cell xenograft
  • Dosages: 50 mg/kg
  • Administration: s.c.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 429.6
Formula

C27H35N5

CAS No. 500579-04-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CN(C)C1=CC=CC=C1CN2CCCN(C2C3=CC=NC=C3)CC4=CC=CC=C4N(C)C

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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

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