BI-D1870

Catalog No.S2843

For research use only.

BI-D1870 is an ATP-competitive inhibitor of S6 ribosome for RSK1/2/3/4 with IC50 of 31 nM/24 nM/18 nM/15 nM in cell-free assays, respectively; 10- to 100-fold selectivity for RSK than MST2, GSK-3β, MARK3, CK1 and Aurora B. BI-D1870 exhibits anticancer attributes including the generation of reactive oxygen species (ROS) and increases in endoplasmic reticulum (ER) stress and autophagy.

BI-D1870 Chemical Structure

CAS No. 501437-28-1

Selleck's BI-D1870 has been cited by 45 publications

Purity & Quality Control

Choose Selective S6 Kinase Inhibitors

Other S6 Kinase Products

Biological Activity

Description BI-D1870 is an ATP-competitive inhibitor of S6 ribosome for RSK1/2/3/4 with IC50 of 31 nM/24 nM/18 nM/15 nM in cell-free assays, respectively; 10- to 100-fold selectivity for RSK than MST2, GSK-3β, MARK3, CK1 and Aurora B. BI-D1870 exhibits anticancer attributes including the generation of reactive oxygen species (ROS) and increases in endoplasmic reticulum (ER) stress and autophagy.
Targets
RSK4 [1]
(Cell-free assay)
RSK3 [1]
(Cell-free assay)
RSK2 [1]
(Cell-free assay)
RSK1 [1]
(Cell-free assay)
15 nM 18 nM 24 nM 31 nM
In vitro

BI-D1870 inhibits RSK1, RSK2, RSK3 and RSK4 with an IC50 of 10–30 nM, but does not significantly inhibit ten other AGC kinase members and over 40 other protein kinases tested at 100-fold higher concentrations. BI-D1870 is cell permeant and prevents the RSK-mediated phorbol ester- and EGF -induced phosphorylation of glycogen synthase kinase-3β and LKB1 in human embry-onic kidney 293 cells and Rat-2 cells. BI-D1870 does not affect the agonist-triggered phosphorylation of substrates for six other AGC kinases. Moreover, BI-D1870 does not suppress the phorbol ester- or EGF-induced phosphorylation of CREB. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
EW-3 M2XUWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWHtU5BSUW6qaXLpeIlwdiCxZjDoeY1idiCHVz2zJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUCgQUAxNjB|NUig{txONg>? MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1O|MyODdxJ{7TRW5ITVJ:L3G+
H9 MmrXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWLJcohq[mm2aX;uJI9nKGi3bXHuJGg6KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVAhRSByLkC2NFE6KM7:TT6= M13hflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU4OzFyNz:nQnNCVkeHUkyvZV4>
KARPAS-45 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV\Jcohq[mm2aX;uJI9nKGi3bXHuJGtCWlCDUz20OUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwJF0hOC5zNkWyOUDPxE1w NUP2NW13RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTd|MUC3M{c,W0GQR1XSQE9iRg>?
NCI-H720 Mm\FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWTJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KN{KwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUCgQUAxNjF5MUm0JO69VS5? M13LSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU4OzFyNz:nQnNCVkeHUkyvZV4>
CTV-1 NITpbXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkXsTY5pcWKrdHnvckBw\iCqdX3hckBEXFZvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyIE2gNE41Pzh5MjFOwG0v MmjlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVc{OTB5Lze+V2FPT0WUPD;hQi=>
DU-4475 M1XqSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn7OTY5pcWKrdHnvckBw\iCqdX3hckBFXS12NEe1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUCgQUAxNjVyNEG3JO69VS5? M1naTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU4OzFyNz:nQnNCVkeHUkyvZV4>
A172 NUj2fYhkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFzRRWNKdmirYnn0bY9vKG:oIHj1cYFvKEFzN{KgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3MDC9JFAvPTF5MEWg{txONg>? NV:5TVE6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTd|MUC3M{c,W0GQR1XSQE9iRg>?
EW-18 MnHuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mli4TY5pcWKrdHnvckBw\iCqdX3hckBGXy1zODDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyIE2gNE43OjJzMTFOwG0v MlewQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVc{OTB5Lze+V2FPT0WUPD;hQi=>
KU812 NWW5O4F7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1HMUGlvcGmkaYTpc44hd2ZiaIXtZY4hU1V6MUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3MDC9JFAvPjJ4MkOg{txONg>? MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1O|MyODdxJ{7TRW5ITVJ:L3G+
KP-N-YS NVzF[YEzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHjKd3hKdmirYnn0bY9vKG:oIHj1cYFvKEuSLV6tXXMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NEA:KDBwNkiyNlMh|ryPLh?= NEC5OXc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2PzNzMEevK|5USU6JRWK8M4E,
SBC-1 NWTTU|k6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2Wy[2lvcGmkaYTpc44hd2ZiaIXtZY4hW0KFLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3MDC9JFAvPjl3MkSg{txONg>? MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1O|MyODdxJ{7TRW5ITVJ:L3G+
ECC10 M3qzVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3LRSmlvcGmkaYTpc44hd2ZiaIXtZY4hTUOFMUCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3MDC9JFAvPzByOUSg{txONg>? M4r3c|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU4OzFyNz:nQnNCVkeHUkyvZV4>
GAMG NIrI[3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWPJcohq[mm2aX;uJI9nKGi3bXHuJGdCVUdiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OCB;IECuO|Q4OTdizszNMi=> M13hXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU4OzFyNz:nQnNCVkeHUkyvZV4>
NCI-H209 NEDufmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG[4W3lKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INlA6KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVAhRSByLke2PFIh|ryPLh?= M2nme|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU4OzFyNz:nQnNCVkeHUkyvZV4>
MC-IXC MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUPJcohq[mm2aX;uJI9nKGi3bXHuJG1ENUm[QzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyIE2gNE44QTV6OTFOwG0v NVHSRYNMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTd|MUC3M{c,W0GQR1XSQE9iRg>?
HSC-3 Ml3hS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVXONYZQUW6qaXLpeIlwdiCxZjDoeY1idiCKU1OtN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwJF0hOC56MUe2PUDPxE1w MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1O|MyODdxJ{7TRW5ITVJ:L3G+
IST-SL1 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX3Jcohq[mm2aX;uJI9nKGi3bXHuJGlUXC2VTEGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3MDC9JFAvQDR3N{Sg{txONg>? Ml\qQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVc{OTB5Lze+V2FPT0WUPD;hQi=>
LU-139 M4n4Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1GzOWlvcGmkaYTpc44hd2ZiaIXtZY4hVFVvMUO5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUCgQUAxNjh2OUW4JO69VS5? MkfQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVc{OTB5Lze+V2FPT0WUPD;hQi=>
ML-2 M1LNcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{\tSWlvcGmkaYTpc44hd2ZiaIXtZY4hVUxvMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyIE2gNE45PTV5NTFOwG0v NUfJ[m1ZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTd|MUC3M{c,W0GQR1XSQE9iRg>?
CAL-62 Mn3VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYnJcohq[mm2aX;uJI9nKGi3bXHuJGNCVC14MjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyIE2gNE45QDF3MjFOwG0v M{e1d|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU4OzFyNz:nQnNCVkeHUkyvZV4>
HL-60 MlrMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3z2NGlvcGmkaYTpc44hd2ZiaIXtZY4hUExvNkCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3MDC9JFAvQDh|NkKg{txONg>? M3[1cVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU4OzFyNz:nQnNCVkeHUkyvZV4>
KY821 NF;3VoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWrJcohq[mm2aX;uJI9nKGi3bXHuJGt[QDJzIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTBiPTCwMlg5QDF{IN88UU4> MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1O|MyODdxJ{7TRW5ITVJ:L3G+
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MV-4-11 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{DrTGlvcGmkaYTpc44hd2ZiaIXtZY4hVVZvND2xNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwJF0hOC57N{i5O{DPxE1w NEDTRVI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2PzNzMEevK|5USU6JRWK8M4E,
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LAMA-84 M3fPe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY[xO5F3UW6qaXLpeIlwdiCxZjDoeY1idiCOQV3BMVg1KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVAhRSBzLkGyO|k1KM7:TT6= NWHiflFRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTd|MUC3M{c,W0GQR1XSQE9iRg>?
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OAW-28 NYL6fXRrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV3Jcohq[mm2aX;uJI9nKGi3bXHuJG9CXy1{ODDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyIE2gN|g{NjR7MzFOwG0v MkO2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVc{OTB5Lze+V2FPT0WUPD;hQi=>
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CAPAN-1 NULGRXVlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWDJcohq[mm2aX;uJI9nKGi3bXHuJGNCWEGQLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3MDC9JFQyOS5{OUKg{txONg>? NX65T4hHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTd|MUC3M{c,W0GQR1XSQE9iRg>?
UACC-257 MnPUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYnGVldLUW6qaXLpeIlwdiCxZjDoeY1idiCXQVPDMVI2PyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxKD1iNEOzMlE2PSEQvF2u NFWzUnY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2PzNzMEevK|5USU6JRWK8M4E,
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Assay
Methods Test Index PMID
Western blot IRF4 / MYC / MCL-1 / PARP ; p-YB1 / YB1 / p-Bad / Bad / p-RSK / RSK ; p-GSK3 / p-ERK / ERK / p-CREB / CREB / p-S6 / p-LKB1 / LKB1 ; IRF4 / MYC / MCL-1 / PARP ; p-YB1 / YB1 / p-Bad / Bad / p-RSK / RSK ; p-GSK3 / p-ERK / ERK / p-CREB / CREB / p-S6 / p-LKB1 / LKB1 25395420 28415756 17040210
Immunofluorescence PDCD4 / F-actin ; PDCD4 / F-actin 25002506
Growth inhibition assay Cell viability ; Cell viability 28415756

Protocol (from reference)

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
5% DMSO+40% PEG 300+5% Tween 80+50% ddH2O
For best results, use promptly after mixing.

1.25mg/ml

Chemical Information

Molecular Weight 391.42
Formula

C19H23F2N5O2

CAS No. 501437-28-1
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1C(=O)N(C2=CN=C(N=C2N1CCC(C)C)NC3=CC(=C(C(=C3)F)O)F)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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Frequently Asked Questions

Question 1:
BI-D1870 (catalog No.S2843) is found as a racemic mixture?

Answer:
Yes, BI-D1870 (catalog No.S2843) is found as a racemic mixture.

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