Chloroquine 32μM R08 exp470

Chloroquine 32μM R08 exp470

Mechanism of Action

Lysosomotropic agent, prevents sequestration of heme into hemozoin, forms toxic complex with heme, enhances hematin-induced red blood cell lysis, also intercalates into DNA

Class / Subclass 1: Infectious Disease / Antimalarial
Class / Subclass 2: DNA Damage, Repair and Replication / Intercalating Agent
Class / Subclass 3: Proteostasis / Autophagy Inhibitor

Technical Notes

Protein References

PubChem Name: Chloroquine phosphate
Synonyms: N/A
CAS #: 50-63-5
PubChem CID: 64927
IUPAC: 4-N-(7-chloroquinolin-4-yl)-1-N,1-N-diethylpentane-1,4-diamine;phosphoric acid
INCHI Name: 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)
INCHI Key: QKICWELGRMTQCR-UHFFFAOYSA-N
Molecular Weight: 515.9
Canonical SMILES: CCN(CC)CCCC(C)NC1=C2C=CC(=CC2=NC=C1)Cl.OP(=O)(O)O.OP(=O)(O)O
Isomeric SMILES: N/A
Molecular Formula: C18H32ClN3O8P2

Protein Supplier

Supplier Name: Med Chem Express
Catalog #: HY-17589
Lot #: 16566

Protein Characterization

Characterization data not available.

Dose Response Curve

Platform ID: Chloroquine
Min: -16.1830; Max: 87.3046

IC	Concentration (µM)
IC10	19.0600
IC20	24.1000
IC30	28.1600
IC40	32.0000
IC50	35.9900
IC60	40.4600
IC70	45.9800
IC80	53.7400
IC90	67.9500

Screen Summary

Round: 08
Dose: 32µM
Days of incubation: 8
Doublings: 5.2
Numbers of reads: 13747420

Screen Results

Sensitive/Resistant hits (FDR<0.05)	CRANKS	Score Plot	Top 30 Genes	Screen Similarity	Top 30 Sensitive GO terms	Top 30 Resistant GO terms
13/0	Scores	View	View	View	View	View

Gene	CRANKS Score	FDR
ODC1	-4.41	<0.01
SLC5A3	-3.88	<0.01
FLVCR1	-3.84	<0.01
MTMR4	-3.22	<0.01
DPAGT1	-3.13	<0.01
SLC7A6	-3.06	<0.01
CDIPT	-2.93	0.05
ADAMTS3	-2.70	0.01
BRD1	-2.69	0.01
RAB7A	-2.67	0.01
ALG9	-2.53	0.03
SHOC2	-2.51	0.05
F8A3	-2.50	0.03
KIAA2013	-2.47	0.06
F8A1	-2.47	0.03
F8A2	-2.45	0.04
COMMD2	-2.40	0.08
ANKH	-2.38	0.05
MGAT1	-2.34	0.09
SLC25A1	-2.33	0.06
ZBED4	-2.33	0.15
PROSER1	-2.33	0.10
PPCS	-2.31	0.10
WDR81	-2.29	0.11
MED31	-2.28	0.07
ARID4B	-2.26	0.12
TLR7	-2.25	0.08
TCF4	-2.23	0.09
AHCYL1	-2.21	0.14
GMPPB	-2.17	0.57
RCC2	2.11	0.14
MTO1	2.12	0.14
PTPN6	2.12	0.14
PET117	2.15	0.14
CRNKL1	2.16	0.25
NDUFA2	2.16	0.17
CNBD2	2.16	0.14
PNO1	2.17	0.43
SELRC1	2.17	0.14
FAM65A	2.21	0.15
VPREB3	2.22	0.13
YBEY	2.22	0.13
TMEM52B	2.26	0.14
FASTKD2	2.29	0.14
NDUFA1	2.32	0.14
CD72	2.33	0.10
KDM6A	2.34	0.10
DEPDC7	2.34	0.10
ALDH18A1	2.36	0.13
MALSU1	2.38	0.10
ACAD9	2.40	0.10
PDE12	2.45	0.11
CDK2	2.47	0.09
MRPL1	2.49	0.14
NDUFAF6	2.52	0.09
LRPPRC	2.58	0.11
SHMT2	2.60	0.11
KCND3	2.63	0.09
GNA13	2.66	0.07
HSP90B1	2.78	0.07

Screen	Correlation	Plot
Hydroxychloroquine 30μM R08 exp490	0.098	View
FTY720 3μM R08 exp483	0.093	View
NN-Dimethylsphingosine 2.5μM R08 exp508	0.079	View
Chlorpromazine 10μM R07 exp344	0.067	View
Thioridazine 5μM R08 exp530	0.065	View
Clomiphene 4.4μM R02 exp68	0.057	View
iCRT14 30μM R08 exp492	0.057	View
Nicotine 3000μM R08 exp510	0.055	View
LJH685 50μM R08 exp433	0.053	View
Trametinib 10μM R02 exp83	0.052	View
Vemurafenib 6.6μM R08 exp434	0.051	View
Ibrutinib 10μM R08 exp442	0.051	View
Bafilomycin-A1 0.009μM R08 exp454	0.088	View
Azithromycin 100μM R08 exp452	0.072	View
B02 10μM R08 exp453	0.057	View
BS-181 20μM R08 exp461	0.052	View

GO Term	Fold Change	Genes
mitochondrial RNA catabolic process	368.20	LRPPRC,PDE12
regulation of mitochondrial gene expression	78.90	SHMT2,LRPPRC,MALSU1,FASTKD2
regulation of mitochondrial translation	69.04	SHMT2,LRPPRC,MALSU1
mitochondrial RNA metabolic process	51.38	LRPPRC,PDE12,FASTKD2,MTO1
mitochondrial respiratory chain complex I assembly	42.48	NDUFAF6,ACAD9,NDUFA1,NDUFA2
NADH dehydrogenase complex assembly	42.48	NDUFAF6,ACAD9,NDUFA1,NDUFA2
mitochondrial respiratory chain complex assembly	31.74	NDUFAF6,ACAD9,NDUFA1,NDUFA2,PET117
organelle inner membrane	8.66	SHMT2,LRPPRC,NDUFAF6,MRPL1,ACAD9,ALDH18A1,NDUFA1,NDUFA2
mitochondrial inner membrane	8.44	SHMT2,NDUFAF6,MRPL1,ACAD9,ALDH18A1,NDUFA1,NDUFA2

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