Hydroxychloroquine Sulfate (NSC 4375)

Catalog No.S4430 Synonyms: HCQ

For research use only.

Hydroxychloroquine Sulfate (NSC 4375, HCQ) is an antimalarial agent used for the treatment of systemic lupus erythematosus, rheumatoid arthritis and other autoimmune, inflammatory and dermatologic conditions. Also acts as an inhibitor of autophagy and toll-like receptor (TLR) 7/9.

Hydroxychloroquine Sulfate (NSC 4375) Chemical Structure

CAS No. 747-36-4

Selleck's Hydroxychloroquine Sulfate (NSC 4375) has been cited by 74 publications

Purity & Quality Control

Choose Selective Autophagy Inhibitors

Biological Activity

Description Hydroxychloroquine Sulfate (NSC 4375, HCQ) is an antimalarial agent used for the treatment of systemic lupus erythematosus, rheumatoid arthritis and other autoimmune, inflammatory and dermatologic conditions. Also acts as an inhibitor of autophagy and toll-like receptor (TLR) 7/9.
Targets
TLR9 [5] Autophagy [1]
In vitro

Hydroxychloroquine Sulfate is a potent inhibitor of autophagy. It prevents lysosomal acidification, thereby interfering with a key step in the autophagic process.HCQ treatment inhibits RCC (renal cell cancer) cell growth, promotes apoptosis, inhibits mitochondrial oxygen consumption, and increases rates of glycolysis[2].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Function assay MUjISWsuSmy3ZTDj[Yxtew>? MXXBcpRi\2:waYP0JIFkfGm4aYT5JIF1KGi3bXHuJHRNWjliZYjwdoV{e2WmIHnuJGhGUy2EbIXlJINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiCFcFfCMYlv\HWlZXSgUmYuc2GycHHCJIxmfmWuczDh[pRmeiB{NDDodpMh[nlic4DlZ5Rzd3Cqb4TvcYV1emmlIHHuZYx6e2m|LDDJR|UxKD1iMD6xNUDPxE1w NF\RZnE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEK5Nlg6Pid-M{CyPVI5QTZ:L3G+
Antiviral assay Ml:zWoVzdyCHNjDj[Yxtew>? NGLMSWo1QCCq NE\QTphKSzVyIH\vdkBidnSrdnnyZYwh[WO2aY\peJkh[WejaX7zeEBUSVKVLVPvWk0zKGmwIITo[UBX\XKxIFW2JINmdGxibHnu[UBifCB2ODDoJIJ6KGmvbYXuc4ZtfW:{ZYPj[Y5k\S2kYYPl[EBie3OjeTCo[IV1\WO2aX7nJJRp\SC4aYLhcEBPWCCycn;0[YlvKGmwIITo[UBvfWOuZYXzJI9nKHSqZTDW[ZJwKEV4IHPlcIx{MS5uIFnDOVAhRSByLk[3OlA5KM7:TT6= Mn;jQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzJ|NUO4OVkoRjN{M{WzPFU6RC:jPh?=
Function assay MXzISWsuSmy3ZTDj[Yxtew>? NGruVmRCdnSjZ3;ubZN1KGGldHn2bZR6KGG2IHj1cYFvKFSOUkeg[ZhxemW|c3XkJIlvKEiHSz3CcJVmKGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDDUFI3PC2rbnT1Z4VlKE6ILXvhdJBiSiCuZY\lcJMh[W[2ZYKgNlQhcHK|IHL5JJNx\WO2cn;wbI91d22ndILpZ{BidmGueYPpd{whUUN3MDC9JFAvQCEQvF2u M2XwXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkmyPFk3Lz5|MEK5Nlg6PjxxYU6=
Function assay MmLOTGVMOjl|IHPlcIx{ M{\IWohGWkdiYnnu[Ilv\yCjc4PhfZM7KESrc4DsZYNmdWWwdDDv[kBcO0ifLVTv[oV1cWyrZHWgLFUhdk1iZnnuZYwqKG[{b32gbGVTTyCvZX3idoFv\XNib3L0ZYlv\WRiZoLvcUBJTUt{OUOgZ4VtdHNuIFvpJF0hOi53MUG4PUDPxE1w M{PHU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzN{M{WzPFU6Lz5|MkO1N|g2QTxxYU6=
Antiviral assay NGnvUXVX\XKxIFW2JINmdGy| NVXRWI1nUUN7MDDmc5Ih[W62aY\pdoFtKGGldHn2bZR6KGGpYXnud5QhW0GUUz3Dc3YuOiCrbjD0bIUhXmW{bzDFOkBk\WyuIHzpcoUh[nlibXXhd5VzcW6pIHnu[oVkfGmxdYOgeolz[WxidHn0[ZIhd2Zic4Xw[ZJv[XSnboSg[pJwdSClb33wc5Vv\C22cnXheIVlKF[ncn:gSVYh[2WubIOgZpkhVWWmaXHuJHRqe3O3ZTDDeYx1fXKnIFnu[oVkfGmxdYOgSI9{\SBqVFPJSEk2OCCkeTD0bIUhdWW2aH;kJI9nKFKnZXSgZY5lKE23ZX7jbEwhUUN7MDC9JFUvPzhizszNMi=> NIPsdXU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MkO1N|g2QSd-M{KzOVM5PTl:L3G+
Antiproliferative assay NVrF[GpXSniSQ{OgZ4VtdHN? NFThVmE4OiCqcoO= MX;BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEK6UFOzJINmdGy|IHHmeIVzKDd{IHjyd{BjgSCVUlKgcYV1cG:mLDDJR|UxKD1iM{Og{txONg>? NWXFcZVCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW2PVkyPTdpPkK1Olk6OTV5PD;hQi=>
qHTS assay M3TlTmE3PzNiY3XscJM> NFm1XZJyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiQU[3N{Bk\Wyucx?= MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
qHTS assay MXHCWE0{PyClZXzsdy=> NULBPIRIeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFLUMVM4KGOnbHzz NX[5OIFoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
qHTS assay MUDTT{1PNU2FIHPlcIx{ M1jwO5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVSz3OMW1EKGOnbHzz MkSyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
qHTS assay NFXPVHlPSi2HQnOxJINmdGy| M3;ifZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCQQj3FRoMyKGOnbHzz NFL0W3M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
qHTS assay NWf0VnBiVEGQLUWgZ4VtdHN? NYG4d|NoeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFzBUk02KGOnbHzz NXPkd|MyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
Antiproliferative assay M1fvTWE2PDliY3XscJM> MoWwNlUhfWdxbXy= MljrNlAhcHK| MVzBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDpckBpfW2jbjDBOVQ6KGOnbHzzJIF1KDJ3IIXnM41tKHWyIITvJFIxKGi{czDifUB5S0WOTHnn[Y5k\SCUVFPBJHNRKGKjc3XkJINmdGy3bHHyJIlueGWmYX7j[UBidmGueYPpdy=> NHzhO2Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEW3NFk4Pyd-Mki1O|A6Pzd:L3G+
Antiproliferative assay MXHBOVQ6KGOnbHzz NXvoWWdKOjVidXevcYw> NVnKWoFLPjBiaILz MYTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDpckBpfW2jbjDBOVQ6KGOnbHzzJIF1KDJ3IIXnM41tKGGodHXyJFYxKGi{czDifUB5S0WOTHnn[Y5k\SCUVFPBJHNRKGKjc3XkJINmdGy3bHHyJIlueGWmYX7j[UBidmGueYPpdy=> NH\4XJc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEW3NFk4Pyd-Mki1O|A6Pzd:L3G+
Autophagy assay NGTGfFVPS0lvSEOxNlIh[2WubIO= MWCyOUB1dyB3MDD1US=> MX:2JIhzew>? NHmzfmRKdmirYnn0bY9vKG:oIHH1eI9xcGGpeTDpckBpfW2jbjDOR2kuUDNzMkKgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5kemWjc3WgbY4heHWwY4TheIUhVEN|IHX4dJJme3Orb36gZZQhOjVidH:gOVAhfU1iYX\0[ZIhPiCqcoOgZpkh\my3b4Lld4NmdmOnIH3pZ5Jwe2OxcHnjJIFv[Wy7c3nz NV:yN29uRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW2PVkyPTdpPkK1Olk6OTV5PD;hQi=>
Apoptosis assay MlGxTFQ3OCClZXzsdy=> M3nQfVI2KHSxIEe1JJVO MkLhNlQhcHK| NYrrbINKUW6mdXP0bY9vKG:oIHHwc5B1d3OrczDpckBpfW2jbjDIOFYxKGOnbHzzJIF1KDJ3IITvJFc2KHWPIHHmeIVzKDJ2IHjyd{BjgSCjbn7lfIlvNVZic4ThbY5qdmdvYnHz[YQh\myxdzDjfZRwdWW2com= NIHnfnQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NU[5PVE2Pyd-MkW2PVkyPTd:L3G+
Autophagy assay NWLBUnEyUDR4MDDj[Yxtew>? NXXBcnRLOjRiaILz M2nGfWlvcGmkaYTpc44hd2ZiYYX0c5Bp[We7IHnuJIh2dWGwIFi0OlAh[2WubIOgZZN{\XO|ZXSgZZMhcW6lcnXhd4UhcW5iTFOzMVIhdGW4ZXygZZQhUUN3MDDh[pRmeiB{NDDodpMh[nliaX3teY5w[myxdDDhcoFtgXOrcx?= NGjRfGM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NU[5PVE2Pyd-MkW2PVkyPTd:L3G+
Antiviral assay NHjk[YxX\XKxIFW2JINmdGy| M{\EelIh\GG7cx?= NFPPRpBCdnSrdnnyZYwh\W[oaXPhZ5kh[WejaX7zeEBUSVKVLVPvWk0zKCi|dILhbY4hSmG4UHH0NUkhcW5iVnXyc{BGPiClZXzsd{Bie3Onc4Pl[EBjgSCrbnjpZol1cW:wIH;mJJZqemGuIGLORUBz\XCuaXPheIlwdiCvZXHzeZJm\CCkeTDSWE1RS1JiYX\0[ZIhOiCmYYnzMEBGSzVyIE2gOE4yPyEQvF2u NEDwblE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyPjlyLze+R4hGVUKOPD;hQi=>
Antiviral assay M{TJb3Zmem9iRU[gZ4VtdHN? MU[zJIRigXN? MmTMTWM2OCCmZYTldo1qdmG2aX;uJIF1KE2RSTCwMlAxPCC3c3nu[{BE\WyuVHn0[ZIuKEeubzCoR3RIMSCjc4PhfUwheGW{Zn;ycYVlKDNiZHH5d{Bxd3O2LXnu[oVkfGmxbjDpckBUSVKVLVPvWk0zKGmwZnXjeIVlKF[ncn:gSVYh[2WubIOsJGlEPTBiPTC5MlIyKM7:TT6= M13NfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE3QTBxJ{7DbGVOSkx:L3G+
Antiviral assay NVjGdmhjXmW{bzDFOkBk\Wyucx?= M2XnR|Mh\GG7cx?= NYjlWVBVUUN3MDDk[ZRmem2rbnH0bY9vKGG2IF3PTUAxNjBzIIXzbY5oKEOnbHzUbZRmei1iR3zvJEhEXEdrIHHzd4F6NCCyZYLmc5Ju\WRiMzDkZZl{KHCxc4StbY5n\WO2aX;uJIlvKFODUmOtR49XNTJiaX7m[YN1\WRiVnXyc{BGPiClZXzsd{whUUN3MDC9JFEyNjF5IN88UU4> NVLhNYpvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTZ7MD:nQmNpTU2ETEyvZV4>
Antiviral assay MnXKWoVzdyCHNjDj[Yxtew>? MoezNkBl[Xm| NWnwSGFXSW62aY\pdoFtKGWoZnnjZYN6KGGpYXnud5QhW0GUUz3Dc3YuOiBqc4TyZYlvKEKjdmDheFEqKGmwIG\ldo8hTTZiY3XscJMh[XO|ZYPz[YQh[nliaX7obYJqfGmxbjDv[kB3cXKjbDDSUmEhemWybHnjZZRqd25ibXXhd5Vz\WRiYomgVnQuWEOUIHHmeIVzKDJiZHH5d{whTUN7MDC9JFI2NjR7IN88UU4> MnPUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVY6OC9pPlPoSW1DVDxxYU6=
Assay
Methods Test Index PMID
Western blot p62 / LC3-I / LC3-II / GAPDH ; NLRP3 / β-actin ; p-NF-κB / β-actin ; NOX2 / β-actin 31268153 31775905 32260307
IHC HE staining of spleen tissue 29456648
Immunofluorescence ZO-1 32260307
In vivo The treatment of Hydroxychloroquine Sulfate reduces the infarct size in an in vivo rat model of I/R injury and the cardioprotective effect of Hydroxychloroquine is ERK1/2 dependent[3]. In addition, Hydroxychloroquine Sulfate shows an early vascular protective effect. HCQ seems to prevent the occurrence of endothelial dysfunction(ED) in treated animals[4].

Protocol (from reference)

Kinase Assay:[2]
  • In vitro kinase assays:

    with purified proteins, recombinant S6 protein and recombinant active P70S6K are incubated in 1x kinase buffer with various amount of HCQ or RAD001 in the presence (25 μM) or absence of ATP for 30 minutes at 30°C. Total and phosphorylated S6 at ser235/236 and ser240/244 are detected by western analysis using phosphospecific antibodies. Note that recombinant GST-tagged S6 (53 kd) is distinguished from endogenous S6 (32 kd) on the western blot.

Cell Research:[2]
  • Cell lines: Human RCC cell lines
  • Concentrations: 75 or 100 μM
  • Incubation Time: 48 h
  • Method: All cells are cultured in RPMI with 10% FBS, 1% glutamine, and 1% Pen/Strep. cells are seeded on the appropriated plates overnight and treated with HCQ (75 or 100 μM) for 48 hours.

Solubility (25°C)

In vitro

Water 67 mg/mL
(154.39 mM)
DMSO Insoluble
Ethanol Insoluble

Chemical Information

Molecular Weight 433.95
Formula

C18H28ClN3O5S

CAS No. 747-36-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCN(CCCC(C)NC1=C2C=CC(=CC2=NC=C1)Cl)CCO.OS(=O)(=O)O

In vivo Formulation Calculator (Clear solution)

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

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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
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Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04007562 Unknown status Drug: Hydroxychloroquine Sulfate LIPIN1 Deficiency Assistance Publique - Hôpitaux de Paris July 2019 --

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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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