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AB142116

Chloroquine diphosphate, apoptosis and autophagy inhibitor

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(15 Publications)

MW 515.9 Da, Purity >98%. Antimalarial agent. Inhibits tumor cell growth and metastasis and induces apoptosis in vitro. Binds to Fe(II)-protoporphyrin IX (FP) to form FP-chloroquine complex resulting in cell lysis and parasite cell autodigestion.

View Alternative Names

ACEE, ACES_HUMAN, ACLS, AIS, ANDR_HUMAN, AR, AR8, ARACHE, Acetylcholinesterase, Androgen nuclear receptor variant 2, Androgen receptor, Androgen receptor (dihydrotestosterone receptor; testicular feminization; spinal and bulbar muscular atrophy; Kennedy disease), Apoptosis related acetylcholinesterase, CAR, CAR BETA, CARA, Car 1, Constitutive activator of retinoid response, Constitutive active response, Constitutive androstane receptor, DHTR, DNA binding protein, Dihydro testosterone receptor, Dihydrotestosterone receptor (DHTR), GCPS, GLI Kruppel family member GLI 3, GLI Kruppel family member GLI3 (Greig cephalopolysyndactyly syndrome), GLI family zinc finger 3, GLI3 C-terminally truncated form, GLI3 form of 190 kDa, GLI3 form of 83 kDa, GLI3 full length protein, GLI3-190, GLI3-83, GLI3FL, GLI3_HUMAN, Glioma associated oncogene family zinc finger 3, HUMARA, HYSP1, KD, Kennedy disease (KD), MB67, MGC97144, N-ACHE, NR1I3_HUMAN, NR3C3, NR3C4, Nuclear receptor subfamily 1 group I member 3, Nuclear receptor subfamily 3 group C member 3, Nuclear receptor subfamily 3 group C member 4, Nuclear receptor subfamily 3 group C member 4 (NR3C4), Oncogene GLI3, Orphan nuclear receptor MB67, Orphan nuclear receptor NR1I3, PAP A, PAPB, PGR, PPD IV, PR, PRA, PRB, PRGR_HUMAN, Progesterone receptor, Progestin receptor form A, Progestin receptor form B, SBMA, SMAX1, Spinal and bulbar muscular atrophy, Spinal and bulbar muscular atrophy (SBMA), TFM, Testicular Feminization (TFM), Transcriptional activator GLI3, Transcriptional repressor GLI3R, YT, YT blood group, Zinc finger protein GLI 3, androgen receptor splice variant 4b, constitutive active receptor, constitutive androstane nuclear receptor variant 2, constitutive androstane nuclear receptor variant 3, constitutive androstane nuclear receptor variant 4, constitutive androstane nuclear receptor variant 5, orphan nuclear hormone receptor

2 Images
Immunocytochemistry - Chloroquine diphosphate, apoptosis and autophagy inhibitor (AB142116)
  • ICC

Lab

Immunocytochemistry - Chloroquine diphosphate, apoptosis and autophagy inhibitor (AB142116)

ab240635 staining SQSTM1 in wild-type Hap1 cells and SQSTM1 knockout Hap1 cells treated with chloroquine (ab142116, 50μM for 24 hrs). The cells were fixed with 100% methanol (5 min) then permeabilized with 0.1% Triton X-100 for 5 minutes and then blocked with 1% BSA/10% normal goat serum/0.3M glycine in 0.1% PBS-Tween for 1h. The cells were then incubated with ab240635 at 1μg/ml concentration and ab7291 (Mouse monoclonal to alpha Tubulin) at 1/1000 dilution overnight at 4°C followed by a further incubation at room temperature for 1h with a goat secondary antibody to rabbit IgG (Alexa Fluor® 488) (ab150081) at 2 μg/ml (shown in green) and a goat secondary antibody to mouse IgG (Alexa Fluor® 594) (ab150120) at 2 μg/ml (shown in red). Nuclear DNA was labelled in blue with DAPI.
Image was taken with a confocal microscope (Leica-Microsystems TCS SP8).

Chemical Structure - Chloroquine diphosphate, apoptosis and autophagy inhibitor (AB142116)
  • Chemical Structure

Lab

Chemical Structure - Chloroquine diphosphate, apoptosis and autophagy inhibitor (AB142116)

2D chemical structure image of ab142116, Chloroquine diphosphate, apoptosis and autophagy inhibitor

Key facts

CAS number

50-63-5

Purity

>98%

Form

Solid

form

Molecular weight

515.9 Da

Molecular formula

C<sub>1</sub><sub>8</sub>H<sub>3</sub><sub>2</sub>ClN<sub>3</sub>O<sub>8</sub>P<sub>2</sub>

PubChem

64927

Nature

Synthetic

Solubility

Soluble in water to 100 mM

Biochemical name

Chloroquine phosphate

Biological description

Antimalarial agent. Inhibits tumor cell growth and metastasis and induces apoptosis in vitro. Binds to Fe(II)-protoporphyrin IX (FP) to form FP-chloroquine complex resulting in cell lysis and parasite cell autodigestion.

Canonical smiles

CCN(CC)CCCC(C)NC1=C2C=CC(=CC2=NC=C1)Cl.OP(=O)(O)O.OP(=O)(O)O

InChi

InChI=1S/C18H26ClN3.2H3O4P/c1-4-22(5-2)12-6-7-14(3)21-17-10-11-20-18-13-15(19)8-9-16(17)18;2*1-5(2,3)4/h8-11,13-14H,4-7,12H2,1-3H3,(H,20,21);2*(H3,1,2,3,4)

InChiKey

QKICWELGRMTQCR-UHFFFAOYSA-N

IUPAC Name

4-N-(7-chloroquinolin-4-yl)-1-N,1-N-diethylpentane-1,4-diamine;phosphoric acid

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Properties and storage information

Shipped at conditions
Ambient - Can Ship with Ice
Appropriate short-term storage conditions
-20°C
Appropriate long-term storage conditions
-20°C
Storage information
Store under desiccating conditions|The product can be stored for up to 12 months
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Supplementary information

This supplementary information is collated from multiple sources and compiled automatically.

Progesterone receptor often called PR or NR3C3 acts as a ligand-activated transcription factor. It has a molecular weight ranging from 93 to 116 kDa depending on isoforms. PR is typically expressed in reproductive tissues like uterus and mammary glands. The acetylcholinesterase enzyme (AChE) breaks down acetylcholine in neuromuscular junctions and brain synapses with a mass of about 65 kDa. Gli3 a zinc finger transcription factor weighing roughly 160 kDa is active mainly in the developing brain and limbs. Androgen receptor (AR) important for male sexual development weighs approximately 110 kDa and expresses mostly in male reproductive organs. Constitutive androstane receptor (CAR) a nuclear receptor with about 40 – 50 kDa expresses significantly in liver and intestine.
Biological function summary

These proteins engage in distinct yet sometimes overlapping roles. PR regulates expression of genes critical for female reproductive processes. AChE facilitates termination of synaptic transmission not existing as part of a larger protein complex. Gli3 functions in limb and central nervous system development often as part of the hedgehog signaling complex. AR modulates transcription of androgen-responsive genes playing a role in male characteristics and fertility. CAR activates detoxification pathways including metabolism of drugs and toxins in the liver.

Pathways

These proteins integrate into various important biological processes. PR participates in steroid hormone signaling pathways interacting with estrogen receptor. AChE is central to the cholinergic neurotransmission pathway connecting with nicotinic and muscarinic receptors. Gli3 associates with sonic hedgehog (Shh) pathway influencing limb patterning and brain structure alongside other Gli family members. AR involves in growth regulation pathways frequently intersecting with insulin-like growth factor 1 (IGF-1). CAR contributes to drug metabolism pathways working in conjunction with the pregnane X receptor (PXR).

These proteins are linked to significant health concerns. PR abnormalities connect with breast cancer where estrogen receptor plays a central role. Defects in AChE relate to neuromuscular disorders like myasthenia gravis. Mutations in Gli3 may cause disorders such as Greig cephalopolysyndactyly syndrome often involving other Shh pathway proteins. Dysfunctional AR can lead to androgen insensitivity syndrome and prostate cancer with key links to genes regulating cell growth. CAR variations associate with liver diseases influencing response to drugs and environmental toxins with the PXR as a related factor.
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Product protocols

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Publications (15)

Recent publications for all applications. Explore the full list and refine your search

iScience 27:109510 PubMed38660406

2024

The activation of LBH-CRYAB signaling promotes cardiac protection against I/R injury by inhibiting apoptosis and ferroptosis.

Applications

Unspecified application

Species

Unspecified reactive species

Anbiao Wu,Chongbin Zhong,Xudong Song,Wen Yuan,Mintian Tang,Tao Shu,Houda Huang,Pingzhen Yang,Qicai Liu

Virus research 345:199379 PubMed38643859

2024

The varicella-zoster virus ORF16 protein promotes both the nuclear transport and the protein abundance of the viral DNA polymerase subunit ORF28.

Applications

Unspecified application

Species

Unspecified reactive species

Huang-Shen Lin,Cheng-Han Li,Lee-Wen Chen,Shie-Shan Wang,Li-Yu Chen,Chien-Hui Hung,Chun-Liang Lin,Pey-Jium Chang

Archives of virology 168:147 PubMed37115342

2023

Repurposing of artesunate, an antimalarial drug, as a potential inhibitor of hepatitis E virus.

Applications

Unspecified application

Species

Unspecified reactive species

Neha Bhise,Megha Agarwal,Nidhi Thakur,P S Akshay,Sarah Cherian,Kavita Lole

The Journal of cell biology 222: PubMed36239631

2022

Convergence of secretory, endosomal, and autophagic routes in trans-Golgi-associated lysosomes.

Applications

Unspecified application

Species

Unspecified reactive species

Lingjian Zhou,Xutong Xue,Ke Yang,Zhi Feng,Min Liu,José C Pastor-Pareja

Frontiers in oncology 12:911615 PubMed35712465

2022

Carnosol Induces p38-Mediated ER Stress Response and Autophagy in Human Breast Cancer Cells.

Applications

Unspecified application

Species

Unspecified reactive species

Halima Alsamri,Aysha Alneyadi,Khalid Muhammad,Mohammed Akli Ayoub,Ali Eid,Rabah Iratni

iScience 24:102849 PubMed34381974

2021

Intestinal microbiota modulates adrenomedullary response through Nod1 sensing in chromaffin cells.

Applications

Unspecified application

Species

Unspecified reactive species

Chen Xiang,Peihua Chen,Qin Zhang,Yinghui Li,Ying Pan,Wenchun Xie,Jianyuan Sun,Zhihua Liu

Frontiers in oncology 11:664403 PubMed34055630

2021

Carnosol Is a Novel Inhibitor of p300 Acetyltransferase in Breast Cancer.

Applications

Unspecified application

Species

Unspecified reactive species

Halima Alsamri,Hussain El Hasasna,Bincy Baby,Aysha Alneyadi,Yusra Al Dhaheri,Mohammed Akli Ayoub,Ali H Eid,Ranjit Vijayan,Rabah Iratni

Autophagy 18:142-160 PubMed33966599

2021

Lipotoxicity reduces DDX58/Rig-1 expression and activity leading to impaired autophagy and cell death.

Applications

Unspecified application

Species

Unspecified reactive species

Karla K Frietze,Alyssa M Brown,Dividutta Das,Raymond G Franks,Jessie Lee Cunningham,Michael Hayward,Joseph T Nickels

Nature biomedical engineering 5:815-829 PubMed33941899

2021

A human-airway-on-a-chip for the rapid identification of candidate antiviral therapeutics and prophylactics.

Applications

Unspecified application

Species

Unspecified reactive species

Longlong Si,Haiqing Bai,Melissa Rodas,Wuji Cao,Crystal Yuri Oh,Amanda Jiang,Rasmus Moller,Daisy Hoagland,Kohei Oishi,Shu Horiuchi,Skyler Uhl,Daniel Blanco-Melo,Randy A Albrecht,Wen-Chun Liu,Tristan Jordan,Benjamin E Nilsson-Payant,Ilona Golynker,Justin Frere,James Logue,Robert Haupt,Marisa McGrath,Stuart Weston,Tian Zhang,Roberto Plebani,Mercy Soong,Atiq Nurani,Seong Min Kim,Danni Y Zhu,Kambez H Benam,Girija Goyal,Sarah E Gilpin,Rachelle Prantil-Baun,Steven P Gygi,Rani K Powers,Kenneth E Carlson,Matthew Frieman,Benjamin R tenOever,Donald E Ingber

Frontiers in oncology 10:1138 PubMed32766148

2020

Chloroquine Triggers Cell Death and Inhibits PARPs in Cell Models of Aggressive Hepatoblastoma.

Applications

Unspecified application

Species

Unspecified reactive species

Katja Eloranta,Stefano Cairo,Emmi Liljeström,Tea Soini,Antti Kyrönlahti,Jean-Gabriel Judde,David B Wilson,Markku Heikinheimo,Marjut Pihlajoki
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