GI254023X

Catalog No.S8660 Synonyms: GI 4023, SRI028594

For research use only.

GI254023X (GI 4023, SRI028594) is a selective inhibitor of ADAM10 with 100-fold selectivity for ADAM10 over ADAM17. The IC50 values for recombinant ADAM10 amd ADAM17 are 5.3 nM and 541 nM, respectively.

GI254023X Chemical Structure

CAS No. 260264-93-5

Selleck's GI254023X has been cited by 6 Publications

Purity & Quality Control

Choose Selective Immunology & Inflammation related Inhibitors

Biological Activity

Description GI254023X (GI 4023, SRI028594) is a selective inhibitor of ADAM10 with 100-fold selectivity for ADAM10 over ADAM17. The IC50 values for recombinant ADAM10 amd ADAM17 are 5.3 nM and 541 nM, respectively.
Targets
ADAM10 [1]
(Cell-free assay)
5.3 nM
In vitro

In cell-based cleavage experiments GI254023X potently blocks the constitutive release of IL6R, CX3CL1 and CXCL16, which is in line with the reported involvement of ADAM10 but not ADAM17 in this process. By contrast, the compound does not affect the PMA-induced shedding[2]. In addition to ADAM10 and ADAM17, GI254023X is a moderate inhibitor of ADAM9 with an IC50 of 280 nM[1].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
L428 NVe4bpd4TnWwY4Tpc44h[XO|YYm= NHXCPJgzPCCqcoO= MYLJcohq[mm2aX;uJI9nKEGGQV2tNVAhcW5iaIXtZY4hVDR{ODDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4heGW{dnHuZYRifGVvaX7keYNm\CCWTl\hcJBp[SC|aHXk[Ilv\yCjZoTldkAzPCCqcoOgZpkhTUyLU1GsJGlEPTB;Nd88UU4> Mkn2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ6N{G2OlAoRjJ4OEexOlYxRC:jPh?=
L540 MoHYSpVv[3Srb36gZZN{[Xl? MkPENlQhcHK| MnPHTY5pcWKrdHnvckBw\iCDRFHNMVExKGmwIHj1cYFvKEx3NECgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKHCnco\hcoFl[XSnLXnu[JVk\WRiVF7GZYxxcGFic3jl[IRqdmdiYX\0[ZIhOjRiaILzJIJ6KEWOSWPBMEBKSzVyPUhOwG0v NUOz[YI1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[4O|E3PjBpPkK2PFcyPjZyPD;hQi=>
KM-H2 MnvUSpVv[3Srb36gZZN{[Xl? NXT6XpBPOjRiaILz M3i2XmlvcGmkaYTpc44hd2ZiQVTBUU0yOCCrbjDoeY1idiCNTT3INkBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5icHXyeoFv[WSjdHWtbY5lfWOnZDDUUmZidHCqYTDzbIVl\GmwZzDh[pRmeiB{NDDodpMh[nliRVzJV2EtKEmFNUC9NVDPxE1w M1uzXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4OEexOlYxLz5{Nki3NVY3ODxxYU6=
KM-H2 NYnBN|NETnWwY4Tpc44h[XO|YYm= M1LZSFI1KGi{cx?= NVjTO483UW6qaXLpeIlwdiCxZjDBSGFONTF5IHnuJIh2dWGwIFvNMWgzKGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDw[ZJ3[W6jZHH0[U1qdmS3Y3XkJJNwdHWkbHWgRWxESU1ic3jl[IRqdmdiYX\0[ZIhOjRiaILzJIJ6KEWOSWPBMEBKSzVyPUGw{txONg>? NGfB[VY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nki3NVY3OCd-Mk[4O|E3PjB:L3G+
KM-H2 NUPLRpgxTnWwY4Tpc44h[XO|YYm= MXWyOEBpenN? MoPmTY5pcWKrdHnvckBw\iCDRFHNMVExKGmwIHj1cYFvKEuPLViyJINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiCyZYL2ZY5i\GG2ZT3pcoR2[2WmIIPvcJVjdGViVVzCVFMhe2inZHTpcoch[W[2ZYKgNlQhcHK|IHL5JGVNUVODLDDJR|UxRTFyzszNMi=> NV[xOVZKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[4O|E3PjBpPkK2PFcyPjZyPD;hQi=>
L428 NYnPdWlbTnWwY4Tpc44h[XO|YYm= MnfnNlQhcHK| NV7vZpFxUW6qaXLpeIlwdiCxZjDBSGFONTF5IHnuJIh2dWGwIFy0Nlgh[2WubIOgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKGmwIIDldpZidmGmYYTlMYlv\HWlZXSgd49tfWKuZTDBUGNCVSC|aHXk[Ilv\yCjZoTldkAzPCCqcoOgZpkhTUyLU1GsJGlEPTB;MUFOwG0v NH63RZY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nki3NVY3OCd-Mk[4O|E3PjB:L3G+
L540 MXPGeY5kfGmxbjDhd5NigQ>? NUDsdpB7OjRiaILz NIrScYhKdmirYnn0bY9vKG:oIFHERW0uOTBiaX6gbJVu[W5iTEW0NEBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5icHXyeoFv[WSjdHWtbY5lfWOnZDDzc4x2[mynIGXMRnA{KHOqZXTkbY5oKGGodHXyJFI1KGi{czDifUBGVEmVQTygTWM2OD1zMN88UU4> MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjh5MU[2NEc,OjZ6N{G2OlA9N2F-
KM-H2 NUTGN2VwTnWwY4Tpc44h[XO|YYm= NY[we5V7OjRiaILz MYnJcohq[mm2aX;uJI9nKEGGQV2tNVAhcW5iaIXtZY4hU01vSEKgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKHCnco\hcoFl[XSnLXnu[JVk\WRic3;seYJt\SCPSVPCJJNp\WSmaX7nJIFnfGW{IEK0JIhzeyCkeTDFUGlUSSxiSVO1NF0yOs7:TT6= MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjh5MU[2NEc,OjZ6N{G2OlA9N2F-
L428 MnLqSpVv[3Srb36gZZN{[Xl? MWGyOEBpenN? MlexTY5pcWKrdHnvckBw\iCDRFHNMVExKGmwIHj1cYFvKEx2MkigZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKHCnco\hcoFl[XSnLXnu[JVk\WRic3;seYJt\SCPSVPCJJNp\WSmaX7nJIFnfGW{IEK0JIhzeyCkeTDFUGlUSSxiSVO1NF0yOs7:TT6= NUTieG5qRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[4O|E3PjBpPkK2PFcyPjZyPD;hQi=>
L540 NYj1Rlc3TnWwY4Tpc44h[XO|YYm= MUWyOEBpenN? MWPJcohq[mm2aX;uJI9nKEGGQV2tNVAhcW5iaIXtZY4hVDV2MDDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4heGW{dnHuZYRifGVvaX7keYNm\CC|b3z1ZoxmKE2LQ1Kgd4hm\GSrbnegZYZ1\XJiMkSgbJJ{KGK7IFXMTXNCNCCLQ{WwQVEz|ryPLh?= NXz2WppoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[4O|E3PjBpPkK2PFcyPjZyPD;hQi=>
L428 M4mzW2Z2dmO2aX;uJIF{e2G7 NXK4PJh7OjRiaILz NHnz[G9KdmirYnn0bY9vKG:oIFHERW0uOTBiaX6gbJVu[W5iTESyPEBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5icHXyeoFv[WSjdHWtbY5lfWOnZDDzc4x2[mynIGXMRnA{KHOqZXTkbY5oKGGodHXyJFI1KGi{czDifUBGVEmVQTygTWM2OD1zNd88UU4> M3jzU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4OEexOlYxLz5{Nki3NVY3ODxxYU6=
In vivo

Acute treatment with GI254023X in an AD mouse model substantially reduces brain LRP1 shedding and increases Aβ40 levels in the plasma, indicating enhanced Aβ transit from the brain to the periphery. Furthermore, both soluble and insoluble Aβ40 and Aβ42 brain levels are decreased following GI254023X treatment, but these effects lack statistical significance[5].

Protocol (from reference)

Cell Research:

[3]

  • Cell lines: HCA-7 cells
  • Concentrations: 3 μM
  • Incubation Time: 24 h
  • Method:

    HCA-7 cells are treated for 24 h with 0.1% DMSO, the metalloprotease inhibitors GI (GI254023X, ADAM10-selective, 3 µM) and GW (GW280264X, ADAM10- and ADAM17-selective, 3 µM), the pan-metalloprotease inhibitor Marimastat (MM; 10 µM), and the EGF-R kinase inhibitor AG1478 (10 µM). Cells stimulated with 100 ng/ml EGF served as positive control. Tyrosine-phosphorylated EGF-R and total EGF-R are assessed by Western blot analysis.

Animal Research:

[4]

  • Animal Models: BALB/c mice
  • Dosages: 200 mg/kg
  • Administration: i.p.

Solubility (25°C)

In vitro

DMSO 78 mg/mL
(199.23 mM)
Water Insoluble
Ethanol ''78 mg/mL

Chemical Information

Molecular Weight 391.50
Formula

C21H33N3O4

CAS No. 260264-93-5
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C(CCCC1=CC=CC=C1)C(=O)NC(C(=O)NC)C(C)(C)C)N(C=O)O

In vivo Formulation Calculator (Clear solution)

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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.

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Molarity Calculator

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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.

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