HMS-I1 10μM R06 exp256

HMS-I1 10μM R06 exp256

Mechanism of Action

Inhibits HDAC

Class / Subclass 1: Uncharacterized Mechanism / Chemical Screen Hit

Technical Notes

Protein References

PubChem Name: 2-(2,3-Dihydro-1,4-benzodioxin-6-yl)-6-methylimidazo[1,2-a]pyridine
Synonyms: N/A
CAS #: 702636-92-8
PubChem CID: 2813456
IUPAC: 2-(2,3-dihydro-1,4-benzodioxin-6-yl)-6-methylimidazo[1,2-a]pyridine
INCHI Name: InChI=1S/C16H14N2O2/c1-11-2-5-16-17-13(10-18(16)9-11)12-3-4-14-15(8-12)20-7-6-19-14/h2-5,8-10H,6-7H2,1H3
INCHI Key: ZNAWJWFMKKSTJM-UHFFFAOYSA-N
Molecular Weight: 266.29
Canonical SMILES: CC1=CN2C=C(N=C2C=C1)C3=CC4=C(C=C3)OCCO4
Isomeric SMILES: N/A
Molecular Formula: C16H14N2O2

Protein Supplier

Supplier Name: Maybridge
Catalog #: HTS 07134
Lot #: N/A

Protein Characterization

HRMS (ESI-TOF) m/z: (M+H)+ Calcd for C16H14N2O2 267.1128; found 267.11196

Dose Response Curve

Platform ID: EMI1
Min: 1.1936; Max: 97.3773

IC	Concentration (µM)
IC10	N/A
IC20	0.5341
IC30	0.9549
IC40	1.5374
IC50	2.3801
IC60	N/A
IC70	N/A
IC80	N/A
IC90	N/A

Screen Summary

Round: 06
Dose: 10µM
Days of incubation: 8
Doublings: -0.6
Numbers of reads: 9286629

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
0/94	Scores	View	View	View	View	View

Gene	CRANKS Score	FDR
RPS19	-2.71	0.46
CUL4B	-2.66	0.38
QRICH1	-2.51	0.43
EXOSC6	-2.48	0.54
LIG4	-2.41	0.43
NAPA	-2.39	0.51
ADRM1	-2.35	0.43
CHAF1A	-2.33	0.50
NPC2	-2.29	0.43
PSTK	-2.22	0.46
PSMC2	-2.21	0.51
ACACA	-2.20	0.46
SMNDC1	-2.19	0.50
CFAP45	-2.16	0.65
USP17L2	-2.15	0.48
GDF9	-2.14	0.46
GREM2	-2.11	0.50
MIEF1	-2.11	0.46
FAM179B	-2.10	0.50
UPF2	-2.07	0.65
PKHD1	-2.06	0.46
OR5H6	-2.06	0.46
SMG7	-2.00	0.54
POLR1B	-2.00	0.67
UBXN1	-1.98	0.61
CDK12	-1.98	0.54
BACH2	-1.98	0.51
DPYD	-1.97	0.50
POTEH	-1.97	0.50
BRMS1	-1.97	0.54
AMZ1	2.82	<0.01
PPP5C	2.83	<0.01
ADCYAP1R1	2.84	<0.01
MAD2L1BP	2.84	<0.01
OSBPL3	2.84	<0.01
MPLKIP	2.86	<0.01
NFE2L3	2.89	<0.01
AGMO	2.99	0.00
RADIL	3.00	<0.01
INMT	3.00	0.00
IGFBP1	3.00	0.00
MAPKAP1	3.06	<0.01
MEOX2	3.09	0.00
PGAM2	3.23	0.00
CDC20	3.28	<0.01
TMED4	3.42	0.00
ZWILCH	3.64	0.00
ELAVL1	3.65	0.00
CDCA2	3.69	0.00
LRRC72	3.75	0.00
MAD2L1	4.08	0.00
FNTB	4.64	0.00
RBM14-RBM4	5.50	0.00
BUB3	5.54	0.00
MAD1L1	5.84	0.00
BUB1B	6.06	0.00
RBM14	6.07	0.00
ZW10	6.12	0.00
TRIP13	6.17	0.00
KNTC1	6.64	0.00

Screen	Correlation	Plot
Nocodazole 0.1μM R03 exp94	0.271	View
SB743921 0.001μM R05 exp244	0.216	View
Rotenone 2μM R00 exp33	0.211	View
Nocodazole 0.2μM R00 exp24	0.206	View
Vinblastine 0.015μM R05 exp208	0.189	View
R-DABN 8μM R03 exp111	0.189	View
Nocodazole 0.2μM R02 exp64	0.184	View
Vinblastine 0.2μM R03 exp108	0.065	View
DABN racemic mixture R03 exp93	0.246	View
BI-6727 0.04μM R03 exp98	0.089	View
Centrinone 0.5μM R07 exp343	0.059	View
DABN 20μM R00 exp17	0.056	View
BI-2536 0.02μM R03 exp96	0.055	View

GO Term	Fold Change	Genes
spindle assembly checkpoint signaling	177.56	KNTC1,TRIP13,ZW10,BUB1B,MAD1L1,BUB3,MAD2L1,ZWILCH,CDC20
mitotic spindle checkpoint signaling	177.56	KNTC1,TRIP13,ZW10,BUB1B,MAD1L1,BUB3,MAD2L1,ZWILCH,CDC20
mitotic spindle assembly checkpoint signaling	177.56	KNTC1,TRIP13,ZW10,BUB1B,MAD1L1,BUB3,MAD2L1,ZWILCH,CDC20
negative regulation of mitotic sister chromatid segregation	160.37	KNTC1,TRIP13,ZW10,BUB1B,MAD1L1,BUB3,MAD2L1,ZWILCH,CDC20
negative regulation of mitotic sister chromatid separation	160.37	KNTC1,TRIP13,ZW10,BUB1B,MAD1L1,BUB3,MAD2L1,ZWILCH,CDC20
spindle checkpoint signaling	152.39	KNTC1,TRIP13,ZW10,BUB1B,MAD1L1,BUB3,ZWILCH,CDC20
negative regulation of metaphase/anaphase transition of cell cycle	150.65	KNTC1,TRIP13,ZW10,BUB1B,MAD1L1,BUB3,MAD2L1,ZWILCH,CDC20
negative regulation of chromosome separation	150.65	KNTC1,TRIP13,ZW10,BUB1B,MAD1L1,BUB3,MAD2L1,ZWILCH,CDC20
negative regulation of chromosome segregation	150.65	KNTC1,TRIP13,ZW10,BUB1B,MAD1L1,BUB3,MAD2L1,ZWILCH,CDC20
negative regulation of sister chromatid segregation	142.55	KNTC1,TRIP13,ZW10,BUB1B,MAD1L1,BUB3,ZWILCH,CDC20
negative regulation of mitotic metaphase/anaphase transition	142.55	KNTC1,TRIP13,ZW10,BUB1B,MAD1L1,MAD2L1,ZWILCH,CDC20
negative regulation of nuclear division	108.08	KNTC1,TRIP13,ZW10,BUB1B,MAD1L1,BUB3,MAD2L1,ZWILCH,CDC20
regulation of mitotic sister chromatid segregation	93.80	KNTC1,TRIP13,ZW10,BUB1B,MAD1L1,BUB3,MAD2L1,ZWILCH,MAD2L1BP
regulation of mitotic sister chromatid separation	85.72	TRIP13,ZW10,BUB1B,MAD1L1,BUB3,MAD2L1,ZWILCH,CDC20,MAD2L1BP
regulation of chromosome separation	75.67	KNTC1,TRIP13,ZW10,BUB1B,MAD1L1,BUB3,MAD2L1,ZWILCH,CDC20,MAD2L1BP
regulation of mitotic metaphase/anaphase transition	62.07	KNTC1,TRIP13,ZW10,BUB1B,MAD1L1,BUB3,MAD2L1,ZWILCH,CDC20,MAD2L1BP
regulation of metaphase/anaphase transition of cell cycle	60.04	KNTC1,TRIP13,ZW10,BUB1B,MAD1L1,BUB3,MAD2L1,ZWILCH,CDC20,MAD2L1BP
regulation of mitotic nuclear division	51.94	KNTC1,TRIP13,ZW10,BUB1B,MAD1L1,BUB3,MAD2L1,CDCA2,ZWILCH,CDC20,MAD2L1BP
regulation of chromosome segregation	48.23	KNTC1,TRIP13,ZW10,BUB1B,MAD1L1,BUB3,MAD2L1,CDCA2,ZWILCH,CDC20,MAD2L1BP

Table of Contents

HMS-I1 10μM R06 exp256

Mechanism of Action

Technical Notes

Protein References

Protein Supplier

Protein Characterization

Dose Response Curve

Screen Summary

Screen Results