Mdivi-1 15μM R05 exp217

Mdivi-1 15μM R05 exp217

Mechanism of Action

Inhibits GTPase dynamin-related protein 1 (Drp1), impairs mitochondrial fission, also inhibits respiratory complex I

Class / Subclass 1: Organelle Function / Mitochondrial Inhibitor

Technical Notes

Protein References

PubChem Name: 3-(2,4-Dichloro-5-methoxyphenyl)-2-sulfanyl-4(3H)-quinazolinone
Synonyms: Mitochondrial division inhibitor 1
CAS #: 338967-87-6
PubChem CID: 3825829
IUPAC: 3-(2,4-dichloro-5-methoxyphenyl)-2-sulfanylidene-1H-quinazolin-4-one
INCHI Name: InChI=1S/C15H10Cl2N2O2S/c1-21-13-7-12(9(16)6-10(13)17)19-14(20)8-4-2-3-5-11(8)18-15(19)22/h2-7H,1H3,(H,18,22)
INCHI Key: NZJKEVWTYMOYOR-UHFFFAOYSA-N
Molecular Weight: 353.2
Canonical SMILES: COC1=C(C=C(C(=C1)N2C(=O)C3=CC=CC=C3NC2=S)Cl)Cl
Isomeric SMILES: N/A
Molecular Formula: C15H10Cl2N2O2S

Protein Supplier

Supplier Name: Sigma-Aldrich
Catalog #: M0199
Lot #: N/A

Protein Characterization

HRMS (ESI-TOF) m/z: (M+H)+ Calcd for C15H10Cl2N2O2S 352.99128; found 352.99118

Dose Response Curve

Platform ID: Mdivi-1
Min: -12.2946; Max: 89.1505

IC	Concentration (µM)
IC10	N/A
IC20	11.9377
IC30	14.5586
IC40	17.1308
IC50	19.8894
IC60	N/A
IC70	N/A
IC80	N/A
IC90	N/A

Screen Summary

Round: 05
Dose: 15µM
Days of incubation: 8
Doublings: 4.8
Numbers of reads: 17266778

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
38/66	Scores	View	View	View	View	View

Gene	CRANKS Score	FDR
YPEL5	-4.80	<0.01
SGOL2	-4.42	<0.01
TCF4	-3.88	<0.01
TRIP13	-3.84	<0.01
ASPM	-3.61	<0.01
SEPHS1	-3.48	<0.01
CALM2	-3.39	<0.01
EDF1	-3.37	<0.01
KNTC1	-3.31	<0.01
TSC1	-3.28	<0.01
BRD1	-3.21	<0.01
CNOT8	-3.18	<0.01
MSI2	-3.06	<0.01
TUBB4B	-2.97	<0.01
TACC3	-2.93	<0.01
WDR26	-2.93	<0.01
KIF18A	-2.89	<0.01
QRICH1	-2.89	0.01
GTSE1	-2.86	<0.01
ZWILCH	-2.72	<0.01
DNTTIP1	-2.71	<0.01
TSC2	-2.70	<0.01
GSK3B	-2.67	<0.01
ESCO2	-2.67	<0.01
CDK2	-2.65	<0.01
ATP2B1	-2.59	0.02
UBE4B	-2.56	0.01
PPIL1	-2.55	0.02
MAPRE1	-2.51	0.03
PSME4	-2.49	0.03
HAUS6	2.74	<0.01
TMEM161B	2.75	<0.01
MEF2C	2.78	<0.01
CBX3	2.80	<0.01
PPP2R5C	2.80	<0.01
TIPRL	2.83	<0.01
PPP1CC	2.84	<0.01
NSD1	2.85	<0.01
SNRK	2.87	<0.01
CELF1	2.97	<0.01
KATNA1	2.97	<0.01
SEC63	2.98	<0.01
DCUN1D1	3.01	<0.01
PHF15	3.04	<0.01
ATAT1	3.09	<0.01
PPME1	3.24	<0.01
KIF2A	3.25	<0.01
TUBB	3.70	<0.01
KATNB1	3.92	<0.01
NUMA1	4.12	<0.01
CLASP1	4.23	<0.01
HAUS3	4.27	<0.01
CCNF	4.29	<0.01
PPP2R1A	4.53	<0.01
CLASP2	4.86	<0.01
KIF4A	4.97	<0.01
TP53	5.44	<0.01
KIF2C	5.88	<0.01
LCMT1	6.45	<0.01
KIF18B	7.96	<0.01

Screen	Correlation	Plot
UMK57 1μM R01 exp59	0.216	View
UM131593 0.2μM R03 exp106	0.133	View
Taxol 0.004μM R03 exp103	0.104	View
Vincristine 0.0005μM R04 exp190	0.097	View
Quercetin 20μM R08 exp517	0.095	View
Vinblastine 0.002μM R01 exp60	0.09	View
RO-3307 4.7μM R02 exp80	0.066	View
UMK57 0.6μM R03 exp107	0.059	View
S-trityl-L-cysteine 0.5μM R05 exp243	0.058	View
Nutlin-3A 1.6μM R06 exp294	0.054	View
Milciclib 2μM R08 exp502	0.051	View
BML-284 0.09μM R08 exp460	0.207	View
2-Methoxyestradiol 0.55 to 1μM on day4 R07 exp312	0.121	View
Demecolcine 0.03μM R05 exp228	0.12	View
BVD-523 15μM R02 exp67	0.118	View
2-Methoxyestradiol 0.55 to 0.75μM on day4 R07 exp311	0.105	View
Colchicine 0.009μM R05 exp215	0.098	View
Combretastatin A4 0.002 to 0.003μM day4 R04 exp179	0.097	View
HMS-I1 1μM R01 exp46	0.085	View
2-Methoxyestradiol 0.55μM R07 exp310	0.084	View
Ixabepilone 0.004 to 0.005μM on day4 R04 exp184	0.083	View
Epothilone-B 0.0015μM R05 exp231	0.065	View
BI-6727 0.0125μM R03 exp97	0.061	View
Docetaxel 0.002μM R01 exp45	0.051	View

GO Term	Fold Change	Genes
kinetochore microtubule	95.23	KNTC1,KIF18A,ZWILCH
mitotic spindle checkpoint signaling	61.22	TRIP13,KNTC1,ZWILCH
mitotic spindle assembly checkpoint signaling	61.22	TRIP13,KNTC1,ZWILCH
spindle assembly checkpoint signaling	61.22	TRIP13,KNTC1,ZWILCH
spindle checkpoint signaling	59.11	TRIP13,KNTC1,ZWILCH
spindle microtubule	36.63	CALM2,KNTC1,KIF18A,ZWILCH,MAPRE1
cytoplasmic microtubule	27.21	TUBB4B,KIF18A,GTSE1,MAPRE1
mitotic cell cycle checkpoint signaling	23.42	TRIP13,KNTC1,GTSE1,ZWILCH,CDK2
spindle pole	20.17	YPEL5,ASPM,CALM2,KNTC1,TACC3,MAPRE1
mitotic spindle	19.37	YPEL5,ASPM,TUBB4B,TACC3,KIF18A,MAPRE1
cell cycle checkpoint signaling	18.31	TRIP13,KNTC1,GTSE1,ZWILCH,CDK2
spindle	12.42	YPEL5,ASPM,CALM2,KNTC1,TUBB4B,TACC3,KIF18A,ZWILCH,MAPRE1
chromosome segregation	12.23	SGO2,TRIP13,ASPM,KNTC1,KIF18A,ESCO2,MAPRE1
microtubule	10.53	ASPM,CALM2,KNTC1,TUBB4B,KIF18A,GTSE1,ZWILCH,MAPRE1
mitotic cell cycle process	9.93	TRIP13,CALM2,KNTC1,TACC3,KIF18A,GTSE1,ZWILCH,CDK2,MAPRE1
mitotic cell cycle	9.49	TRIP13,CALM2,KNTC1,TUBB4B,TACC3,KIF18A,GTSE1,ZWILCH,CDK2,MAPRE1
cell division	7.90	SGO2,ASPM,KNTC1,TACC3,ZWILCH,CDK2,MAPRE1
cell cycle process	7.85	SGO2,TRIP13,ASPM,CALM2,KNTC1,TACC3,KIF18A,GTSE1,ZWILCH,ESCO2,CDK2,MAPRE1
polymeric cytoskeletal fiber	6.92	ASPM,CALM2,KNTC1,TSC1,TUBB4B,KIF18A,GTSE1,ZWILCH,MAPRE1

GO Term	Fold Change	Genes
spindle microtubule	56.65	KIF18B,KIF4A,CLASP2,HAUS3,CLASP1,NUMA1,KIF2A,HAUS6
spindle assembly	35.47	KIF4A,CLASP2,HAUS3,CLASP1,NUMA1,KIF2A,HAUS6
mitotic sister chromatid segregation	32.49	KIF18B,KIF2C,KIF4A,CLASP2,PPP2R1A,CLASP1,KATNB1,KIF2A
sister chromatid segregation	31.56	KIF18B,KIF2C,KIF4A,CLASP2,PPP2R1A,CLASP1,KATNB1,KIF2A
spindle organization	28.90	KIF4A,CLASP2,PPP2R1A,HAUS3,CLASP1,NUMA1,TUBB,KIF2A,HAUS6
mitotic spindle	28.08	KIF18B,CLASP2,HAUS3,CLASP1,NUMA1,TUBB,ATAT1,KATNA1,HAUS6
microtubule binding	20.84	KIF18B,KIF2C,KIF4A,CLASP2,CLASP1,NUMA1,KATNB1,KIF2A,KATNA1,HAUS6
chromosome segregation	20.27	KIF18B,KIF2C,KIF4A,CLASP2,PPP2R1A,HAUS3,CLASP1,NUMA1,KATNB1,TUBB,KIF2A,HAUS6
nuclear chromosome segregation	20.18	KIF18B,KIF2C,KIF4A,CLASP2,PPP2R1A,CLASP1,KATNB1,KIF2A
spindle	18.68	KIF18B,KIF2C,KIF4A,CLASP2,HAUS3,CLASP1,NUMA1,KATNB1,TUBB,KIF2A,ATAT1,KATNA1,CBX3,HAUS6
microtubule	16.54	KIF18B,KIF2C,KIF4A,CLASP2,HAUS3,CLASP1,NUMA1,KATNB1,TUBB,KIF2A,ATAT1,KATNA1,HAUS6
cell division	15.28	KIF18B,KIF2C,KIF4A,CLASP2,CCNF,HAUS3,CLASP1,NUMA1,KATNB1,TUBB,KIF2A,KATNA1,PPP1CC,HAUS6
tubulin binding	15.09	KIF18B,KIF2C,KIF4A,CLASP2,CLASP1,NUMA1,KATNB1,KIF2A,KATNA1,HAUS6
microtubule cytoskeleton organization	14.35	KIF18B,KIF2C,KIF4A,CLASP2,PPP2R1A,HAUS3,CLASP1,NUMA1,KATNB1,TUBB,KIF2A,ATAT1,KATNA1,HAUS6
mitotic cell cycle process	13.86	KIF18B,LCMT1,KIF2C,TP53,KIF4A,CLASP2,PPP2R1A,CCNF,CLASP1,NUMA1,KATNB1,KIF2A,PPME1
mitotic cell cycle	12.84	KIF18B,LCMT1,KIF2C,TP53,KIF4A,CLASP2,PPP2R1A,CCNF,CLASP1,NUMA1,KATNB1,TUBB,KIF2A,PPME1
cell cycle process	10.11	KIF18B,LCMT1,KIF2C,TP53,KIF4A,CLASP2,PPP2R1A,CCNF,HAUS3,CLASP1,NUMA1,KATNB1,TUBB,KIF2A,PPME1,HAUS6
microtubule-based process	9.91	KIF18B,KIF2C,KIF4A,CLASP2,PPP2R1A,HAUS3,CLASP1,NUMA1,KATNB1,TUBB,KIF2A,ATAT1,KATNA1,HAUS6
polymeric cytoskeletal fiber	9.66	KIF18B,KIF2C,KIF4A,CLASP2,HAUS3,CLASP1,NUMA1,KATNB1,TUBB,KIF2A,ATAT1,KATNA1,HAUS6

Table of Contents

Mdivi-1 15μM R05 exp217

Mechanism of Action

Technical Notes

Protein References

Protein Supplier

Protein Characterization

Dose Response Curve

Screen Summary

Screen Results