CHIR-99021 (CT99021) HCl

Catalog No.S2924

CHIR-99021 (CT99021) HCl Chemical Structure

Molecular Weight(MW): 501.8

CHIR-99021 HCl (CT99021) is hydrochloride of CHIR-99021, which is a GSK-3α/β inhibitor with IC50 of 10 nM/6.7 nM; CHIR-99021 shows greater than 500-fold selectivity for GSK-3 versus its closest homologs Cdc2 and ERK2.

Size Price Stock Quantity  
In DMSO USD 340 In stock
USD 90 In stock
USD 170 In stock
USD 570 In stock
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Cited by 70 Publications

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  • Differentiation induced by treatment with the Gsk3 inhibitor in hPSCs is β-catenin dependent. H9-7TGP cells were treated with 12 uM CH in mTeSR1 for 4 d. Immunofluorescent staining for Oct4, Isl1, and Nkx2.5 was compared with GFP expression. (Scale bars, 50 uM.)

    Proc Natl Acad Sci U S A 2012 109(27):E1848-57. CHIR-99021 (CT99021) HCl purchased from Selleck.

    Gpc4 regulates ESC response to Wnt/β-catenin signaling.  (E) Quantitative analysis of control and Gpc4-mutant beating foci exposed to the GSK3 inhibitor, CHIR 99021 (1 and 3 μM, from day 0 to day 5). Analysis was done at different time points. Gpc4- mutant cells treated with CHIR 99021 behave as controls (mean±SEM; n=2).

    Stem Cells 2012 30, 1863-1874. CHIR-99021 (CT99021) HCl purchased from Selleck.

  • Inhibition of GSK3 activity induces an autophagic response in human pancreatic cancer cells. PANC1 cells were treated for 24 h with DMSO, CHIR99021 (CHIR; 5 uM) or the mTOR inhibitor Torin1 (250 nM). Autophagosome (punctate LC3B) (D) and lysosome (E) labeling was visualized with a Zeiss LSM700 confocal microscope. Images were acquired with a 20x (D) or 63x (E) objective. Nuclei were stained with DAPI. Scale bars, 20 祄.

    J Biol Chem 2015 290(9), 5592-605 . CHIR-99021 (CT99021) HCl purchased from Selleck.

     

    Characterization of rES cells. A: image of normal rES cell colonies on feeder layers. B: rES colonies were positive for AP staining. CeE: rES colonies readily expressed pluripotent markers, Sox2 (C), Oct4 (D), and SSEA-1 (E). Blue, DAPI. Scale bars: 100 um.

    J Genet Genomics 2012 39, 643e651. CHIR-99021 (CT99021) HCl purchased from Selleck.

  •  

    Smad linker phosphorylation involves GSK3 in human melanoma lines. Inhibition of Smad2 and Smad3 linker phosphorylation in the presence of the specific GSK3 specific inhibitor, CT99021. 24 hours post seeding, WM793 and 1205LU cells were serum-starved for about 16 hours, and incubated in the absence (2) or presence (+) of 2 uM of CT99021 for two hours. Immunoblots were performed as in A. p: Phosphorylated. S: Serine; T: Threonine.

    PLoS One 2012 7, e47312. CHIR-99021 (CT99021) HCl purchased from Selleck.

    A. Vero cells were pretreated with the indicated concentrations of CHIR-99021 for 1 h and then infected with PEDV (MOI = 1) for 8 or 10 h. Cell lysates were prepared and analyzed using Western blotting.

    PLoS One, 2016, 11(8):e0161508. CHIR-99021 (CT99021) HCl purchased from Selleck.

  • SKOV3/DDP cells were treated with a range of concentration of (A) CHIR-99021 or in combination with 20 µM cisplatin for 48 h.

    Exp Ther Med, 2016, 12(6):3851-3858. CHIR-99021 (CT99021) HCl purchased from Selleck.

     

    PANC1 cells were treated with GSK3 inhibitors SB216763 (SB 10µM or SB 20µM) or CHIR99021 (CHIR 5µM) for 72h.

    CHIR-99021 (CT99021) HCl purchased from Selleck.

  •  

     Activity of canonical WNT/ β -CATENIN signals induced by CHIR 99021 in the developing human lung. Human lung tissue explants obtained at 15 weeks of gestation were exposed to 0, 5 and 10 μM CHIR 99021 in vitro for 72 h. (A-B) Western blot analysis showed expression of β -CATENIN in human lung tissues. Results are presented as the mean ± sem of three independent experiments. *P < 0.05, **P < 0.01. (C) qRT-PCR analysis detected a dose-dependent increase in WNT signaling transcription factors and target genes following exposure to CHIR 99021. Results are presented as the mean ± sem of three independent experiments. *P < 0.05, **P < 0.01. (D-K) Histology examination showed obvious morphogenetic changes of the airway epithelial cells associated with CHIR 99021 treated lung tubes. Scale bars: D-G =100 μm; H-K = 20 μm.

    CHIR-99021 (CT99021) HCl purchased from Selleck.

Purity & Quality Control

Choose Selective GSK-3 Inhibitors

Biological Activity

Description CHIR-99021 HCl (CT99021) is hydrochloride of CHIR-99021, which is a GSK-3α/β inhibitor with IC50 of 10 nM/6.7 nM; CHIR-99021 shows greater than 500-fold selectivity for GSK-3 versus its closest homologs Cdc2 and ERK2.
Targets
GSK-3β [1]
(Cell-free assay)
GSK-3α [1]
(Cell-free assay)
Tie-2 [1]
(Cell-free assay)
FLT1 [1]
(Cell-free assay)
KDR [1]
(Cell-free assay)
6.7 nM 10 nM >5 μM >5 μM >5 μM
In vitro

CHIR-99021 shows greater than 500-fold selectivity for GSK-3 versus its closest homologs CDC2 and ERK2, as well as other protein kinases. Furthermore, CHIR-99021 shows only weak binding to a panel of 22 pharmacologically relevant receptors and little inhibitory activity against a panel of 23 nonkinase enzymes. CHIR-99021 induces the activation of glycogen synthase (GS) in insulin receptor-expressing CHO-IR cells with EC50 of 0.763 μM. [1] In addition to simulating the actions of insulin, inhibition of GSK-3 by CHIR-99021 (3 μM) increases free cytosolic β-catenin by 1.9-fold, mimicking the canonical Wnt signaling pathway in 3T3-L1 preadipocytes. During any of the first 3 days of differentiation, CHIR-99021 treatment inhibits the preadipocyte differentiation with IC50 of 0.3 μM by blocking induction of CCAAT/enhancer-binding protein α (C/EBPα) and peroxisome proliferator-activated receptor γ (PPARγ). [2] Unlike lithium chloride and AR-A014418, CHIR-99021 treatment does not reduce the viability of INS-1E cells even at high concentrations. Instead, CHIR-99021 robustly increases the rate of proliferation of INS-1E cells in a dose-dependent manner, and significantly inhibits INS-E cell death induced by high glucose and high palmitate in a concentration-dependent manner. CHIR-99021 promotes primary beta cell replication in isolated rat islets at concentrations as low as 1 μM, with 2-3 fold increase of cell replication at 5 μM of CHIR-99021 treatment. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
3T3-L1 M4XnW2Z2dmO2aX;uJGF{e2G7 NXL0bY5xOyEQvF2= NH;rNW01KGh? M3G4R2ROW09? MkjNTY5pcWKrdIOgdJJm[WSrcH;jfZRmKGSrZn\ldoVvfGmjdHnvci=> NXPQW5h6OTJyNUWyNFA>
insulin receptor–expressing CHO-IR NVTXZpUxTnWwY4Tpc44hSXO|YYm= MWm1NFAhdk1? M1jTPVMxKG2rbh?= M{HTWWROW09? NHfrZpJC[3SrdnH0[ZMhT2y7Y3;n[Y4hW3mwdHjhd4UhMEeVKR?= NGiz[oUyOjZyNkS5Oy=>
H4IIE MWPGeY5kfGmxbjDBd5NigQ>? NY\uXYlWOTBizszN NHPqfI8zPCCq NWTKSohCTE2VTx?= MX;S[Yd2dGG2ZYOg{tIu[2G2ZX7pckBi[3Srdnn0fUBidmRiVFnSSUBkd262YXnubY5oKHC{b33veIVzKGGldHn2bZR6 Mo\3NVU{PTBzOUW=
Oct4/Sox2/Klf4-infected MEFs M{X2Z2Z2dmO2aX;uJGF{e2G7 MVyxNEDPxE1? NEf1[YYzQCCm NX7rXYIyTE2VTx?= Mly0VJJwdW:2ZYOgUWVHeyC{ZYDyc4dz[W2vaX7nJHRz[W6|ZIXj[YQh[nliT3P0OEwhW2:6MjygZY5lKEuuZkS= MofENVk5OzlyNUW=
Sca-1+ HPC NEP2dnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2q4bFIh|ryP M2[3V|Yh\A>? MlfmSG1UVw>? M2PLZnN6dmW{Z3nzeIlk[WyueTDwdo9ud3SnczDTZ4EuOSwEoFjQR{Bxem:uaX\ldoF1cW:wIHHu[EBkd2yxbomg[o9zdWG2aX;uJJRw\2W2aHXyJJdqfGhiRVfG MVuyNVYzPDN2OB?=
HMC1.2 NV7lWopKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoHHN|Ah|ryP MXu3NkBp MmjLSG1UVw>? M2f2WnJm\HWlZYOgZ4VtdCC|dYL2bZZidA>? MXOyNlA{QTNyMR?=
Endothelial cell(EC) MXzGeY5kfGmxbjDBd5NigQ>? NV\4W2V5OyEQvF2= Mnn4SG1UVw>? M1nUZXBzd22xdHXzJIVv\G:2aHXsbYFtKGOnbHygLGVEMSCmaX\m[ZJmdnSrYYTpc44> NIfJXnIzOjB3MkCwOi=>
PANC1 MmfURZBweHSxc3nzJGF{e2G7 M37N[OKhPSEQvF2= MXy3NkBp NHjjUmJFVVOR NX;yWIxEXHKrZ3fldpMh[W5iYYDvdJRwfGmlIILld5BwdnOn M4nWO|IzOjBzMUi2
INS-1E M4fYcGZ2dmO2aX;uJGF{e2G7 NEGxR44zNjVizszN NGmzNFUzPCCq NYLKXXdiTE2VTx?= NYrD[FJ4UW6mdXPld{BiKHKnZIXjeIlwdiCxZjDOVFEhd3[ncnX4dJJme3Orb36= MljiNlI1Ojd5MES=
hiPSC-NPs M4n6XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFe2UG4{6oDLzszN MoXOO|IhcA>? NHLPWWJFVVOR NIPsVHVKdmO{ZXHz[ZMh[2WubDDwdo9tcW[ncnH0bY9vyqB? MonHNlI3PDJ4OEe=
platelets NFPjZmRHfW6ldHnvckBCe3OjeR?= NGqyW|MyOCEQvF2= NUfW[Jg{OTVibXnu MYXEUXNQ NF;jUWhKdmO{ZXHz[ZMhfGi{b33ibY4udWWmaXH0[YQheGyjdHXs[ZQh[WepcnXnZZRqd25iYX7kJGFVWCC|ZXPy[ZRqd25? M4n5SFI{OjN7OEe3
DN3 MUfGeY5kfGmxbjDBd5NigQ>? M4fXVlExKM7:TR?= MVK5OkBp M2nONmROW09? M{nVV2lv[3KnYYPld{Bk\WyuIHTleoVtd3CvZX70JIFv\CCycn;sbYZmemG2aX;u NWf2XZNvOjN3Mk[5PFk>
embryonic stem cells (ESC) Mn7TSpVv[3Srb36gRZN{[Xl? Mn\RN{DDvU1? NXzGfGFpOTFiZB?= NGXmWpFFVVOR M3XQSXBzd22xdHXzJJNmdGZvcnXu[ZdidCCxZjDuZeOwfmVvdInw[UBud3W|ZTDlcYJzgW:waXOgd5RmdSClZXzsd{ApTVOFKR?= M362ZlI{QDR|M{Gy
H460 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn7LOUDDvU1? M4HKZlI1KGh? MXHEUXNQ NY\4dGRJWHKxbX;0[ZMh[2WubDDwdo9tcW[ncnH0bY9v MY[yOFM3PzZ6OB?=
H157 MkDyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXu1JOK2VQ>? M1\ke|I1KGh? MWTEUXNQ NY\3eXBQWHKxbX;0[ZMh[2WubDDwdo9tcW[ncnH0bY9v MXqyOFM3PzZ6OB?=
H460 MVXBdI9xfG:|aYOgRZN{[Xl? M2HTVlUhyrWP Mlu2NlQhcA>? M1vyfGROW09? MWTBeJRmdnWjdHXzJINmdGxiYYDvdJRwe2m| M4mzdlI1OzZ5Nki4
H157 M{TJRWFxd3C2b4Ppd{BCe3OjeR?= MVy1JOK2VQ>? NUHySphxOjRiaB?= M{nh[GROW09? M3jEV2Rw\XNibn;0JJNq\26rZnnjZY51dHliYX\m[YN1KGGyb4D0c5Nqew>? MmTUNlQ{Pjd4OEi=
A549 NXrGZ3R[SXCxcITvd4l{KEG|c3H5 M4rORlUhyrWP NXX1eHJ1OjRiaB?= M33hTWROW09? NVrKSYlDUW6lcnXhd4V{KGOnbHygZZBweHSxc3nz NVjZdpI2OjR|Nke2PFg>
Neural progenitor cells M{DPeGZ2dmO2aX;uJGF{e2G7 NHnpOJc{KM7:TR?= MV2xNEBl NYqy[HVpTE2VTx?= NHX6[YVKdmS3Y3XzJIdmdmW{YYTpc44hd2ZibnX1doFtKHC{b3flcol1d3JiY3XscJM> NXHyNodTOjR4M{iwN|Q>
ES-D3 M4C3SGN6fG:2b4jpZ{BCe3OjeR?= MXKxNOKh|ryP NVK5RYlZOyCm MYTEUXNQ NYTid5EzUW6mdXPld{Bud2SncnH0[UBkgXSxdH;4bYNqfHlid3n0bEBKSzVyIH;mJFQvQSEQvF2= MYOyOFc4QTN4NR?=
ES-CCE M1f6bWN6fG:2b4jpZ{BCe3OjeR?= M4PMWFExyqEQvF2= MojLN{Bl NWPmcJJWTE2VTx?= MVnJcoR2[2W|IH3v[IVz[XSnIHP5eI91d3irY3n0fS=> NIC5OHMzPDd5OUO2OS=>
ES-D3 NVPN[mdzTnWwY4Tpc44hSXO|YYm= NXm5dpNQPcLizszN NFfRboE{KGR? NYTHb|ZUTE2VTx?= M3HHVXN1em:wZ3z5JIlv\HWlZYOgeIhmKGGldHn2bZR6KG:oIGfueE9j\XSjLXPheIVvcW5icHH0bJdigQ>? Mkn0NlQ4Pzl|NkW=
ES-CCE M3;6bWZ2dmO2aX;uJGF{e2G7 M{DVZlXDqM7:TR?= NH\Gbo0{KGR? NGfwO|RFVVOR MlTTV5Rzd26pbImgbY5lfWOnczD0bIUh[WO2aY\peJkhd2ZiV370M4JmfGFvY3H0[Y5qdiCyYYToe4F6 MV2yOFc4QTN4NR?=
SW982 NWfPO4dGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWXJR|UxRTBwMkG0NVYh|ryP NGj1NYhUSU6JRWK=
GCT M4PnWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHjXVphKSzVyPUCuN|A3PzJizszN NX22Zoh[W0GQR1XS
769-P MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEDxcFhKSzVyPUCuOVg1QTlizszN NUjGdIdQW0GQR1XS
LOXIMVI NGf0UIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3q1emlEPTB;MD61PFg{OiEQvF2= M3H3VHNCVkeHUh?=
D-336MG M4jRfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MofMTWM2OD1yLki0OlIh|ryP M3LsOnNCVkeHUh?=
S-117 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MonOTWM2OD1yLkmyNVMyKM7:TR?= MVvTRW5ITVJ?
D-247MG NVTDPYhyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXPJR|UxRTBwOUS4OVIh|ryP MnvtV2FPT0WU
TYK-nu Mn\IS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlTPTWM2OD1zLkC3PVEzKM7:TR?= MmXSV2FPT0WU
A498 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVXNb2tEUUN3ME2xMlMxPDZ7IN88US=> NIrZfHhUSU6JRWK=
BCPAP NFLubFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWT1c3IyUUN3ME2xMlY3QDl6IN88US=> M2jvNnNCVkeHUh?=
KYSE-180 NF7ZbpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVTJR|UxRTFwN{K3PFgh|ryP NEjRXW5USU6JRWK=
MIA-PaCa-2 M4f1eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkXsTWM2OD1zLke1PVc4KM7:TR?= NXv3bHdSW0GQR1XS
HCC1395 M2TMcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{\ydmlEPTB;MT63PFI4OyEQvF2= MXjTRW5ITVJ?
RS4-11 NWi1NFh6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXrJR|UxRTFwOUW0NVUh|ryP NUPKdmh3W0GQR1XS
NCI-H2122 M3W1V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUjsSlRYUUN3ME2yMlI4Pjh2IN88US=> NWjs[nFNW0GQR1XS
SNU-423 NUHPWotrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn3JTWM2OD1{LkS5O|g4KM7:TR?= MlT1V2FPT0WU
SK-LMS-1 NVvxU3ZzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkHiTWM2OD1{Lk[0NVI5KM7:TR?= NWO2cnZbW0GQR1XS
RPMI-7951 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlvZTWM2OD1{LkewNVk{KM7:TR?= M3L6SHNCVkeHUh?=
COLO-829 MoDKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYTJR|UxRTJwN{[1OEDPxE1? MoH2V2FPT0WU
SCC-9 M3TRRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYHJR|UxRTJwOUW0PFUh|ryP MWPTRW5ITVJ?
A704 Ml\KS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGrmb29KSzVyPUOuNFgyOiEQvF2= NGLVN|lUSU6JRWK=
HOP-62 MnzvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVjJR|UxRTNwM{[wOVQh|ryP NY\KcYEyW0GQR1XS
HCC1569 MlToS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF23Z5JKSzVyPUOuOFg{ODVizszN MWnTRW5ITVJ?
A172 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWDJR|UxRTNwN{W0PVgh|ryP MkfkV2FPT0WU
MOLT-16 MmPHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXJR|UxRTNwOEi1OVYh|ryP MXrTRW5ITVJ?
TE-15 NIe0UolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUPJR|UxRTNwOUWzOFMh|ryP NIrYWFhUSU6JRWK=
OE19 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlHQTWM2OD1|Lkm2OFUyKM7:TR?= NXez[GI3W0GQR1XS
MHH-ES-1 M1TYNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkTZTWM2OD12LkC0OVQ2KM7:TR?= MWjTRW5ITVJ?
NKM-1 MnPsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFi5ZWdKSzVyPUSuNVM6PzFizszN NHe4UpdUSU6JRWK=
RCC10RGB MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFGwe4dKSzVyPUSuNlk1PzlizszN M{Cw[HNCVkeHUh?=
BxPC-3 M3vLOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHTu[HFKSzVyPUSuO|A{QTFizszN MkLxV2FPT0WU
ALL-PO M3PtTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVzJR|UxRTRwOEO4OVgh|ryP MmTVV2FPT0WU
SK-OV-3 NWrqN5I2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnnoTWM2OD12Lkm5N|Qh|ryP M{f0TnNCVkeHUh?=
SW1710 NXfMN2lMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4DMOmlEPTB;NT60NlQ2PiEQvF2= M3rwTnNCVkeHUh?=
NCI-H2452 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX3JR|UxRTVwNEW2Nlgh|ryP MmX6V2FPT0WU
D-392MG MmTXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmLoTWM2OD13LkS5NVQ2KM7:TR?= M1PzTXNCVkeHUh?=
LB2518-MEL MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2DwPGlEPTB;NT63NlYzPyEQvF2= M3;NU3NCVkeHUh?=
BL-41 MmT1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGj1cW1KSzVyPUWuPFEzPjZizszN NILHXohUSU6JRWK=
WM-115 MoLWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2K2UGlEPTB;NT64NVUxQSEQvF2= NYey[mVrW0GQR1XS
SK-MEL-2 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M17OSWlEPTB;Nj6zPFM1PCEQvF2= MXnTRW5ITVJ?
CGTH-W-1 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmjRTWM2OD14LkSxO{DPxE1? NEDhV25USU6JRWK=
BB65-RCC MoX2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1;D[mlEPTB;Nj61N|E6PSEQvF2= M1raVXNCVkeHUh?=
CAL-85-1 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2LLcWlEPTB;Nj62NFk{PiEQvF2= NXzrTHlJW0GQR1XS
RT-112 NGnvWI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVjJR|UxRTdwMU[0OVYh|ryP M3\ERXNCVkeHUh?=
MC116 NILoRWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYi4fFJOUUN3ME23MlI5PjlzIN88US=> NEjQdJBUSU6JRWK=
G-361 NVLj[4pwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYXJR|UxRTdwNE[1OlEh|ryP MX;TRW5ITVJ?
SW1417 NI\6cVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{Lub2lEPTB;Nz62OFU5PCEQvF2= NHP6RmFUSU6JRWK=
MV-4-11 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXi3SJI2UUN3ME24MlU1OzB2IN88US=> NHv0NYFUSU6JRWK=
CAL-72 NFS1N2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXr0NXBGUUN3ME24Mlc3OTF|IN88US=> NHuzfm9USU6JRWK=
MKN28 MknNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmXhTWM2OD16Lki4OVE3KM7:TR?= MVLTRW5ITVJ?
MEG-01 M1fKPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3vQPWlEPTB;OD65PVA1OyEQvF2= NGjCN5VUSU6JRWK=
ACHN MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXyxTos{UUN3ME25MlMxPTR4IN88US=> M3TFdXNCVkeHUh?=
NCI-H1755 Mk\sS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mnm4TWM2OD17LkO5PVg3KM7:TR?= NVrxc|BbW0GQR1XS
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LB996-RCC MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXfHfGh5UUN3ME25MlUzOzl5IN88US=> NHTjTW5USU6JRWK=
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NCI-H28 M{XIRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1vMXmlEPTB;MUCuOFQyOyEQvF2= M{DPVHNCVkeHUh?=
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HT-3 MkmxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mmi3TWM2OD1zMD62NVc6KM7:TR?= MYTTRW5ITVJ?
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NCI-H526 MoTSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo\wTWM2OD1zMT6xN|Y2KM7:TR?= M1ztNHNCVkeHUh?=
HEL NYTPSIxkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWLKO|VJUUN3ME2xNU43PTd7IN88US=> NWTvS2t1W0GQR1XS
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T98G NYDGUmZKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUnnV405UUN3ME2xN{41PzF5IN88US=> M2\1N3NCVkeHUh?=
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ST486 M{H2eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXXnZ2dqUUN3ME2xOE4zOjVzIN88US=> NGDUfYRUSU6JRWK=
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Daudi MlfzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mlj2TWM2OD1zNz62NVQ6KM7:TR?= MmHzV2FPT0WU
SIMA MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXPJR|UxRTF5LkmxNVgh|ryP MYnTRW5ITVJ?
8305C Mlq4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2DtT2lEPTB;MUiuOVMxPSEQvF2= MWjTRW5ITVJ?
EM-2 MmfjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWHYRVNRUUN3ME2xPE43OjR6IN88US=> Mn6wV2FPT0WU
SNU-449 MkLVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnLSTWM2OD1zOD63NVUh|ryP MYrTRW5ITVJ?
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Becker MlvnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1y4VWlEPTB;MkCuNVc4PyEQvF2= Mn25V2FPT0WU
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HCC1187 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIHjTYRKSzVyPUKwMlM2QDlizszN MX\TRW5ITVJ?
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TGBC24TKB NFrNOZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYLJR|UxRTJzLki5OVch|ryP NHr1d41USU6JRWK=
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LS-513 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{nPNmlEPTB;MkKuOlE6OiEQvF2= M3zaV3NCVkeHUh?=
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GI-1 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUDJR|UxRTJ{Lke4OFEh|ryP M320bnNCVkeHUh?=
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REH MnzzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnzZTWM2OD1{Mz6xOlk6KM7:TR?= M3TB[3NCVkeHUh?=
K5 MnfHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{i4VGlEPTB;MkOuOVQ5PiEQvF2= MXLTRW5ITVJ?
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NCI-H1770 M2XDOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVLHXI5QUUN3ME2yOk45QTh4IN88US=> MknkV2FPT0WU
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KLE M4rtTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXOx[HdJUUN3ME2yO{4zPTZ3IN88US=> NGrJOHhUSU6JRWK=
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LCLC-103H MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUHJR|UxRTNyLkKwOVkh|ryP M2T2fXNCVkeHUh?=
CAKI-1 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2L6RmlEPTB;M{CuNlY2PiEQvF2= MUfTRW5ITVJ?
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SK-MM-2 M{e5eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW\zRlk1UUN3ME2zNE46Pzl{IN88US=> MnXZV2FPT0WU
LB373-MEL-D Mo\hS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlzNTWM2OD1|MT6wNFQ4KM7:TR?= NYnxOlZ1W0GQR1XS
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SW948 NFjZbFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYmyNIlCUUN3ME2zNk44PTR6IN88US=> MXjTRW5ITVJ?
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PFSK-1 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4SxU2lEPTB;M{SuPVI1OSEQvF2= M4nUO3NCVkeHUh?=
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KM12 MlnNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIHmeINKSzVyPUO4MlU6QThizszN MnHFV2FPT0WU
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SK-CO-1 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYHPeG5kUUN3ME20NU44PzV3IN88US=> NXrkSFVzW0GQR1XS
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LB831-BLC MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYDJ[mp4UUN3ME20N{43QTdizszN NYP3PZNpW0GQR1XS
TE-8 NH;JcodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1P5U2lEPTB;NEOuO|g6PSEQvF2= M{TW[HNCVkeHUh?=
SR MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoLITWM2OD12Mz64Olc{KM7:TR?= MkTqV2FPT0WU
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KYSE-270 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3PzeGlEPTB;NEWuNFQ{PyEQvF2= Ml33V2FPT0WU
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UACC-62 MojjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVrZ[3lvUUN3ME20Ok45PjB6IN88US=> NYO2OVk2W0GQR1XS
D-542MG MkKzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWntR212UUN3ME20O{41PTh7IN88US=> M3e2c3NCVkeHUh?=
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NCI-H2030 M3fGfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1j5U2lEPTB;M{SxMlYxQSEQvF2= M4jhOnNCVkeHUh?=
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PF-382 NGTOfHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFjNXFJKSzVyPUO0OE41OjJizszN NFLJS2VUSU6JRWK=
NB13 M3[3WWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXnJR|UxRTN2NT61PEDPxE1? NGniXWJUSU6JRWK=
D-502MG NV3wUXlOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVj1dmlwUUN3ME2zOFUvQDF{IN88US=> NYS2flBoW0GQR1XS
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DMS-53 NGfvOXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFTReWpKSzVyPUO1PE44OTFizszN Mke2V2FPT0WU
NCI-H1838 NEPZeIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXfPRlNuUUN3ME2zOVkvQTh5IN88US=> M4rFUnNCVkeHUh?=
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ChaGo-K-1 MnfKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1mxOGlEPTB;M{[zMlkzPCEQvF2= MkLwV2FPT0WU
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NCI-H596 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYXJR|UxRTN6NT6zOEDPxE1? MlvOV2FPT0WU
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NCI-H716 NGTFdmNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MorETWM2OD12MUCuNFc2KM7:TR?= NI\yTZZUSU6JRWK=
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MDA-MB-134-VI M{fvfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWjJR|UxRTR|MT6wN|Mh|ryP M1rse3NCVkeHUh?=
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NCI-H1694 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYXaelhOUUN3ME21NVIvPDN7IN88US=> M1HsOXNCVkeHUh?=
NCI-H2171 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFPYTlFKSzVyPUWxNk44ODVizszN NHPzdIZUSU6JRWK=
Mo-T NVHVRZJ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmfkTWM2OD13MUWuNVE3KM7:TR?= NGraUGZUSU6JRWK=
HL-60 Mkm2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVHTSXA{UUN3ME21NlIvQTJ2IN88US=> NULrOYFGW0GQR1XS
NCI-H1436 M4j3S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2K4WmlEPTB;NUKzMlA3PCEQvF2= M2j6bXNCVkeHUh?=
NCI-H510A MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlX5TWM2OD13MkSuOlk3KM7:TR?= M3\3c3NCVkeHUh?=
NCI-H2081 NV3JfIs2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWjWbVg5UUN3ME21NlUvPTF|IN88US=> MnraV2FPT0WU
NB5 MlvlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4fTfGlEPTB;NUK2MlQ{KM7:TR?= NHj6SVFUSU6JRWK=
NCI-H2227 NHfXVWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX\JR|UxRTV|MD6yOVQh|ryP NHjhe5pUSU6JRWK=
HSC-4 NHPvXIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWXJR|UxRTV|OT6yPVMh|ryP NITGbppUSU6JRWK=
RL NWDTSGxkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVTpbolrUUN3ME21OFIvPDR{IN88US=> NVnleGRNW0GQR1XS
EVSA-T NHLFfVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF\sTJhKSzVyPUW0N{43QDRizszN M4LGXnNCVkeHUh?=
NCI-H889 MlPsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml7ITWM2OD13NEeuNlMh|ryP NHu2R2ZUSU6JRWK=
COLO-320-HSR MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NW\mb25{UUN3ME21OVEvOzVizszN M1nRXnNCVkeHUh?=
EW-11 NFTsSm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY\JR|UxRTV3Mj6zPVkh|ryP NYjhcmZNW0GQR1XS
UACC-812 M{f3WWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2rGcWlEPTB;NUW5MlM6OSEQvF2= M3PiXHNCVkeHUh?=
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ML-2 NXTCWWZvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWXzZpFZUUN3ME22NFYvPTd7IN88US=> MV;TRW5ITVJ?
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HT NWfx[3NuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3zCeWlEPTB;NkKyMlc5PSEQvF2= MUHTRW5ITVJ?
NCI-H226 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3PUcGlEPTB;NkK4MlM2OyEQvF2= NFXDdWRUSU6JRWK=
L-363 NGjIe|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnzQTWM2OD14NEiuNFY1KM7:TR?= M{nEWXNCVkeHUh?=
IM-9 Ml;4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4LNV2lEPTB;NkWxMlU1OSEQvF2= MmO5V2FPT0WU
TUR M3PlV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXjJR|UxRTZ5MT6zNlIh|ryP NXiyWGtoW0GQR1XS
NCI-SNU-16 NVTjOHh6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIfhZYdKSzVyPU[4NE41PjJizszN M1vqNXNCVkeHUh?=
NCI-SNU-1 MkLqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlfxTWM2OD14OUCuNVczKM7:TR?= Mk\0V2FPT0WU
U-87-MG NGLP[4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1;kbGlEPTB;Nkm0MlU5PSEQvF2= MWTTRW5ITVJ?
KM-H2 MoixS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUfN[mRGUUN3ME22PVkvODV7IN88US=> MoDWV2FPT0WU
DEL M2rMS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M37SNmlEPTB;N{CwMlg{QCEQvF2= MlrTV2FPT0WU
KARPAS-422 M4LQT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVrJR|UxRTd6OT6zNVUh|ryP NHnVeoRUSU6JRWK=
BC-3 Ml\DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1TTRWlEPTB;OEC1MlIxOyEQvF2= NVLjdm5LW0GQR1XS
NCI-H1155 M13HTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYDJR|UxRThzOD6wOVkh|ryP M4f3ZXNCVkeHUh?=
NCI-H1581 MoXuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{\3OmlEPTB;OUCwMlI{OSEQvF2= MnXaV2FPT0WU

... Click to View More Cell Line Experimental Data

In vivo Oral administration of CHIR-99021 at 30 mg/kg enhances glucose metabolism in a rodent model of type 2 diabetes, with a maximal plasma glucose reduction of nearly 150 mg/dl 3-4 hours after administration, while plasma insulin remains at or below control levels. Oral administration of CHIR-99021 at 16 or 48 mg/kg 1 hour before oral glucose challenges in ZDF rats significantly improves glucose tolerance with 14% and 33% reduction in plasma glucose at 16 mg/kg and 48 mg/kg, respectively, and the higher dose of CHIR-99021 also reduces hyperglycemia before the oral glucose challenge. [1] Administration of CHIR-99021 significantly augments hematopoietic repopulation in recipient mice transplanted with mouse or human hematopoietic stem cells (HSCs), suggesting that GSK-3 is a specific modulator of HSC activity. [4]

Protocol

Kinase Assay:

[1]

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Cell-free kinase assays:

Polypropylene 96-well plates are filled with 300 μL/well buffer (50 mM tris HCl, 10 mM MgCl2, 1 mM EGTA, 1 mM dithiothreitol, 25 mM β-glycerophosphate, 1 mM NaF, 0.01% BSA, pH 7.5) containing 27 nM GSK-3α or 29 nM GSK-3β, and 0.5 μM biotin-CREB peptide substrate. Various concentrations of CHIR-99021 are added in 3.5 μL of DMSO, followed by 50 μL of ATP stock to yield a final concentration of 1 μM ATP in all cell-free assays. After incubation, triplicate 100-μL aliquots are transferred to Combiplate eight plates containing 100 μL/well 50 μM ATP and 20 mM EDTA. After 1 hour, the wells are rinsed five times with PBS, filled with 200 μL of scintillation fluid, sealed, left 30 minutes, and counted in a scintillation counter. All steps are performed at room temperature.
Cell Research:

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  • Cell lines: INS-1E
  • Concentrations: Dissolved in DMSO, final concentrations ~ 20 μM
  • Incubation Time: 1, or 4 days
  • Method:

    Cells are maintained for 24 hours in starvation medium (culture medium with only 5 mM glucose, 1% fetal calf serum). Then cells are exposed to various concentrations of CHIR-99021 for 1, or 4 days. Cell number is measured by staining of cellular DNA with CyQuant dye, which becomes fluorescent when bound to DNA. Fluorescence is measured after 30 minutes of incubation using the FLUOstar Optima reader. Cell replication is determined by BrdUrd incorporation. BrdUrd labeling solution is added to the medium for the last 4 hours before the cells are fixed using FixDenat solution and incubated with monoclonal anti-BrdUrd-POD antibodies. After substrate solution is added to each well, the light emission is measured in a microplate luminometer using the Analyst HT detection system.


    (Only for Reference)
Animal Research:

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  • Animal Models: Female db/db mice or male ZDF rats with type 2 diabetes
  • Formulation: Formulated as solutions in 20 mM citrate-buffered 15% Captisol or as fine suspensions in 0.5% carboxymethylcellulose.
  • Dosages: ~48 mg/kg
  • Administration: Orally
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 93 mg/mL (185.33 mM)
Ethanol 2 mg/mL (3.98 mM)
Water <1 mg/mL
In vivo 5% DMSO+30% PEG 300+ddH2O 24mg/mL

* 1 mg/ml means slightly soluble or 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 501.8
Formula

C22H18Cl2N8.HCl

CAS No. 252917-06-9 (free base)
Storage powder
in solvent
Synonyms N/A

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 (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*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 )

  • C1
    V1
    C2
    V2

* 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):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

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

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID