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 77 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 NEPqb2ZJTUtvQnz1[UBk\Wyucx?= MonxRY51[WexbnnzeEBi[3Srdnn0fUBifCCqdX3hckBVVFJ7IHX4dJJme3OnZDDpckBJTUtvQnz1[UBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iQ4DHRk1qdmS3Y3XkJG5HNWujcIDhRkBt\X[nbIOgZYZ1\XJiMkSgbJJ{KGK7IIPw[YN1em:yaH;0c41mfHKrYzDhcoFtgXOrczygTWM2OCB;IECuNVEh|ryPLh?= MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJ7Mki5Okc,OzB{OUK4PVY9N2F-
Antiviral assay M{POWnZmem9iRU[gZ4VtdHN? NIfnR3A1QCCq NI\xXlFKSzVyIH\vdkBidnSrdnnyZYwh[WO2aY\peJkh[WejaX7zeEBUSVKVLVPvWk0zKGmwIITo[UBX\XKxIFW2JINmdGxibHnu[UBifCB2ODDoJIJ6KGmvbYXuc4ZtfW:{ZYPj[Y5k\S2kYYPl[EBie3OjeTCo[IV1\WO2aX7nJJRp\SC4aYLhcEBPWCCycn;0[YlvKGmwIITo[UBvfWOuZYXzJI9nKHSqZTDW[ZJwKEV4IHPlcIx{MS5uIFnDOVAhRSByLk[3OlA5KM7:TT6= MmrRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzJ|NUO4OVkoRjN{M{WzPFU6RC:jPh?=
Function assay M2\CZmhGUy2EbIXlJINmdGy| MYDBcpRi\2:waYP0JIFkfGm4aYT5JIF1KGi3bXHuJHRNWjdiZYjwdoV{e2WmIHnuJGhGUy2EbIXlJINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiCFTEK2OE1qdmS3Y3XkJG5HNWujcIDhRkBt\X[nbIOgZYZ1\XJiMkSgbJJ{KGK7IIPw[YN1em:yaH;0c41mfHKrYzDhcoFtgXOrczygTWM2OCB;IECuPEDPxE1w MnfUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{OUK4PVYoRjNyMkmyPFk3RC:jPh?=
Function assay NUTxdFQyUEWNMkmzJINmdGy| M1vpc4hGWkdiYnnu[Ilv\yCjc4PhfZM7KESrc4DsZYNmdWWwdDDv[kBcO0ifLVTv[oV1cWyrZHWgLFUhdk1iZnnuZYwqKG[{b32gbGVTTyCvZX3idoFv\XNib3L0ZYlv\WRiZoLvcUBJTUt{OUOgZ4VtdHNuIFvpJF0hOi53MUG4PUDPxE1w NIe1[lg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MkO1N|g2QSd-M{KzOVM5PTl:L3G+
Antiviral assay MXvW[ZJwKEV4IHPlcIx{ MkGxTWM6OCCob4KgZY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgV2FTWy2Fb2[tNkBqdiC2aHWgWoVzdyCHNjDj[YxtKGyrbnWgZpkhdWWjc4XybY5oKGmwZnXjeIlwfXNidnnyZYwhfGm2ZYKgc4Yhe3WyZYLuZZRmdnRiZoLvcUBkd22yb4Xu[E11emWjdHXkJHZmem9iRU[gZ4VtdHNiYomgUYVlcWGwIGTpd5N2\SCFdXz0eZJmKEmwZnXjeIlwfXNiRH;z[UApXEOLRDm1NEBjgSC2aHWgcYV1cG:mIH;mJHJm\WRiYX7kJG12\W6laDygTWM6OCB;IEWuO|gh|ryPLh?= NFj2OoM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MkO1N|g2QSd-M{KzOVM5PTl:L3G+
Antiproliferative assay MlvURphRSzNiY3XscJM> MnfPO|IhcHK| M2DmNmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQojQR|Mh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IGPSRkBu\XSqb3SsJGlEPTBiPTCzN{DPxE1w NVviXJB5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW2PVkyPTdpPkK1Olk6OTV5PD;hQi=>
qHTS assay M1fLfWE3PzNiY3XscJM> NUeyeYdFeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFG2O|Mh[2WubIO= M1jLbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
qHTS assay NGPnS2ZDXC1|NzDj[Yxtew>? MULxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhSlRvM{egZ4VtdHN? M{m2eVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
qHTS assay MnqxV2suVi2PQzDj[Yxtew>? MlvJdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFONLV6tUWMh[2WubIO= M3LmVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
qHTS assay M3vafW5DNUWEY{GgZ4VtdHN? M{K3c5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCQQj3FRoMyKGOnbHzz NYj5XnJCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
qHTS assay NXTtSItiVEGQLUWgZ4VtdHN? Mn7EdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEyDTj21JINmdGy| MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
Antiproliferative assay M1nnTGE2PDliY3XscJM> NXnXcm9{OjVidXevcYw> MoX0NlAhcHK| MnfCRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgbY4hcHWvYX6gRVU1QSClZXzsd{BifCB{NTD1[{9udCC3cDD0c{AzOCCqcoOgZpkhgEOHTFzp[4Vv[2ViUmTDRUBUWCCkYYPl[EBk\WyudXzhdkBqdXCnZHHuZ4Uh[W6jbInzbZM> MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDV5MEm3O{c,Ojh3N{C5O|c9N2F-
Antiproliferative assay MYrBOVQ6KGOnbHzz NEC0cIczPSC3Zz;tcC=> M3fhdVYxKGi{cx?= NG\VW2ZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBqdiCqdX3hckBCPTR7IHPlcIx{KGG2IEK1JJVoN22uIHHmeIVzKDZyIHjyd{BjgSC6Q1XMUIlo\W6lZTDSWGNCKFOSIHLhd4VlKGOnbHz1cIFzKGmvcHXkZY5k\SCjbnHsfZNqew>? NUfXZWM1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki1O|A6PzdpPkK4OVcxQTd5PD;hQi=>
Autophagy assay M1K5WW5EUS2KM{GyNkBk\Wyucx?= M{fD[lI2KHSxIEWwJJVO MnLVOkBpenN? MoTRTY5pcWKrdHnvckBw\iCjdYTvdIhi\3liaX6gbJVu[W5iTlPJMWg{OTJ{IHPlcIx{KGG|c3Xzd4VlKGG|IHnuZ5Jm[XOnIHnuJJB2dmO2YYTlJGxEOyCneIDy[ZN{cW:wIHH0JFI2KHSxIEWwJJVOKGGodHXyJFYhcHK|IHL5JIZtfW:{ZYPj[Y5k\SCvaXPyc5Nkd3CrYzDhcoFtgXOrcx?= MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTZ7OUG1O{c,OjV4OUmxOVc9N2F-
Apoptosis assay MomwTFQ3OCClZXzsdy=> NImweoQzPSC2bzC3OUB2VQ>? NG\USnAzPCCqcoO= NWLVWYY{UW6mdXP0bY9vKG:oIHHwc5B1d3OrczDpckBpfW2jbjDIOFYxKGOnbHzzJIF1KDJ3IITvJFc2KHWPIHHmeIVzKDJ2IHjyd{BjgSCjbn7lfIlvNVZic4ThbY5qdmdvYnHz[YQh\myxdzDjfZRwdWW2com= NF[z[G09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NU[5PVE2Pyd-MkW2PVkyPTd:L3G+
Autophagy assay MVTIOFYxKGOnbHzz MXeyOEBpenN? M{XSSWlvcGmkaYTpc44hd2ZiYYX0c5Bp[We7IHnuJIh2dWGwIFi0OlAh[2WubIOgZZN{\XO|ZXSgZZMhcW6lcnXhd4UhcW5iTFOzMVIhdGW4ZXygZZQhUUN3MDDh[pRmeiB{NDDodpMh[nliaX3teY5w[myxdDDhcoFtgXOrcx?= M3zJXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3Nkm5NVU4Lz5{NU[5PVE2PzxxYU6=
Antiviral assay NYr3N292XmW{bzDFOkBk\Wyucx?= MoDyNkBl[Xm| NIjPWVNCdnSrdnnyZYwh\W[oaXPhZ5kh[WejaX7zeEBUSVKVLVPvWk0zKCi|dILhbY4hSmG4UHH0NUkhcW5iVnXyc{BGPiClZXzsd{Bie3Onc4Pl[EBjgSCrbnjpZol1cW:wIH;mJJZqemGuIGLORUBz\XCuaXPheIlwdiCvZXHzeZJm\CCkeTDSWE1RS1JiYX\0[ZIhOiCmYYnzMEBGSzVyIE2gOE4yPyEQvF2u NEPZc5I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyPjlyLze+R4hGVUKOPD;hQi=>
Antiviral assay M3izXHZmem9iRU[gZ4VtdHN? NXTXVW1uOyCmYYnz NEjXTIpKSzVyIHTleIVzdWmwYYTpc44h[XRiTV;JJFAvODB2IIXzbY5oKEOnbHzUbZRmei1iR3zvJEhEXEdrIHHzd4F6NCCyZYLmc5Ju\WRiMzDkZZl{KHCxc4StbY5n\WO2aX;uJIlvKFODUmOtR49XNTJiaX7m[YN1\WRiVnXyc{BGPiClZXzsd{whUUN3MDC9JFkvOjFizszNMi=> NF7RPG89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyPjlyLze+R4hGVUKOPD;hQi=>
Antiviral assay MnvyWoVzdyCHNjDj[Yxtew>? NWLmR2RKOyCmYYnz NUH3dotGUUN3MDDk[ZRmem2rbnH0bY9vKGG2IF3PTUAxNjBzIIXzbY5oKEOnbHzUbZRmei1iR3zvJEhEXEdrIHHzd4F6NCCyZYLmc5Ju\WRiMzDkZZl{KHCxc4StbY5n\WO2aX;uJIlvKFODUmOtR49XNTJiaX7m[YN1\WRiVnXyc{BGPiClZXzsd{whUUN3MDC9JFEyNjF5IN88UU4> NXK3T2RNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTZ7MD:nQmNpTU2ETEyvZV4>
Antiviral assay M4\GOXZmem9iRU[gZ4VtdHN? MXqyJIRigXN? M3\mWWFvfGm4aYLhcEBm\m[rY3HjfUBi\2GrboP0JHNCWlNvQ3;WMVIhMHO2cnHpckBD[X[SYYSxLUBqdiCYZYLvJGU3KGOnbHzzJIF{e2W|c3XkJIJ6KGmwaHnibZRqd25ib3[geolz[WxiUl7BJJJmeGyrY3H0bY9vKG2nYYP1doVlKGK7IGLUMXBEWiCjZoTldkAzKGSjeYOsJGVEQTBiPTCyOU41QSEQvF2u Mo[4QIEhfGG{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

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)

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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 2022-08-01)

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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