IWR1 50μM R08 exp495 [The Human Chemical-Genetic Interaction Map Project]

Stabilizes axin complex, inhibits Wnt/β-catenin signaling, also inhibits tankyrase

Class / Subclass 1: Signal Transduction / Other Inhibitor

Compound References

PubChem Name: IWR-1-endo
Synonyms: endo-IWR 1; IWR-1-endo
CAS #: 1127442-82-3
PubChem CID: 44483163
IUPAC: 4-[(1S,2R,6S,7R)-3,5-dioxo-4-azatricyclo[5.2.1.02,6]dec-8-en-4-yl]-N-quinolin-8-ylbenzamide
INCHI Name: InChI=1S/C25H19N3O3/c29-23(27-19-5-1-3-14-4-2-12-26-22(14)19)15-8-10-18(11-9-15)28-24(30)20-16-6-7-17(13-16)21(20)25(28)31/h1-12,16-17,20-21H,13H2,(H,27,29)/t16-,17+,20-,21+
INCHI Key: ZGSXEXBYLJIOGF-ALFLXDJESA-N
Molecular Weight: 409.4
Canonical SMILES: C1C2C=CC1C3C2C(=O)N(C3=O)C4=CC=C(C=C4)C(=O)NC5=CC=CC6=C5N=CC=C6
Isomeric SMILES: C1[C@@H]2C=C[C@H]1[C@@H]3[C@H]2C(=O)N(C3=O)C4=CC=C(C=C4)C(=O)NC5=CC=CC6=C5N=CC=C6
Molecular Formula: KLTFYLKTLENAQAQQTTLSLAIF

Compound Supplier

Supplier Name: Med Chem Express
Catalog #: HY-12238
Lot #: 12245

Compound Characterization

HRMS (ESI-TOF) m/z: (M+H)+ Calcd for C25H19N3O3 410.14992; found 410.15127

Dose Response Curve

Platform ID: IWR1
Min: -6.6055; Max: 35.5116

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

Screen Summary

Round: 08
Dose: 50µM
Days of incubation: 8
Doublings: 4.4
Numbers of reads: 16401227

Sensitive/Resistant hits (FDR<0.05)	CRANKS	Score Plot	Top 30 Genes	Screen Similarity	Top 30 Sensitive GO terms	Top 30 Resistant GO terms
5/0	Scores	View	View	View	View	View

Gene	CRANKS Score	FDR
SLC7A5	-3.27	<0.01
KIAA1432	-2.91	0.02
SLC5A3	-2.88	0.02
PRKAA1	-2.78	0.02
RSRC2	-2.76	0.45
SPTLC2	-2.64	0.03
GRIA1	-2.28	0.21
OR56A4	-2.27	0.21
POLR2J2	-2.26	0.75
VPS25	-2.25	0.67
SCAP	-2.24	0.22
ATP2A2	-2.22	0.79
CKMT1B	-2.16	0.31
CALML4	-2.16	0.45
PLA2G4E	-2.14	0.31
DARS2	-2.13	0.64
PCMT1	-2.10	0.33
DDHD2	-2.08	0.33
RC3H1	-2.07	0.33
NIM1	-2.07	0.33
RNASE9	-2.06	0.33
FNTB	-2.04	0.45
PITPNB	-2.04	0.35
SNX18	-2.01	0.37
ALG5	-2.01	0.37
TAC4	-2.00	0.45
LSM1	-1.96	0.45
GLCE	-1.95	0.45
YTHDC2	-1.95	0.53
TCP11X2	-1.94	0.45
MZT2A	1.99	0.33
ELP6	1.99	0.33
CD19	1.99	0.39
NEK5	1.99	0.39
BCOR	2.01	0.33
SPI1	2.02	0.38
TBCC	2.02	0.79
F12	2.04	0.33
ASIC2	2.06	0.33
TDRD3	2.08	0.33
ARID4B	2.08	0.34
DNAH17	2.12	0.33
MIEN1	2.13	0.31
KIAA1210	2.14	0.31
PABPC1	2.14	0.33
KSR1	2.16	0.33
DLEC1	2.18	0.33
NDUFA13	2.19	0.36
RFC2	2.22	0.73
CTR9	2.22	0.33
MEIS3	2.24	0.24
NR2C2AP	2.32	0.27
SSX2IP	2.33	0.21
GLRX3	2.38	0.24
TBRG4	2.47	0.21
ANKRD40	2.52	0.24
TPX2	2.56	0.21
RPL11	2.62	0.33
CADPS	2.69	0.21
GLTSCR2	2.77	0.21

Last modified: 2026/01/15 21:36
by 127.0.0.1