INK128 0.2μM R02 exp70 [The Human Chemical-Genetic Interaction Map Project]

Inhibits mTORC1 and mTORC2, ATP-competitive

Class / Subclass 1: Signal Transduction / Kinase Inhibitor
Class / Subclass 2: Proteostasis / mTOR inhibitor

Compound References

PubChem Name: Sapanisertib
Synonyms: INK-128; MLN0128; TAK-228
CAS #: 1224844-38-5
PubChem CID: 45375953
IUPAC: 5-(4-amino-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-3-yl)-1,3-benzoxazol-2-amine
INCHI Name: InChI=1S/C15H15N7O/c1-7(2)22-14-11(13(16)18-6-19-14)12(21-22)8-3-4-10-9(5-8)20-15(17)23-10/h3-7H,1-2H3,(H2,17,20)(H2,16,18,19)
INCHI Key: GYLDXIAOMVERTK-UHFFFAOYSA-N
Molecular Weight: 309.33
Canonical SMILES: CC(C)N1C2=NC=NC(=C2C(=N1)C3=CC4=C(C=C3)OC(=N4)N)N
Isomeric SMILES: N/A
Molecular Formula: C15H15N7O

Compound Supplier

Supplier Name: Selleck Chemicals
Catalog #: S2811
Lot #: N/A

Compound Characterization

HRMS (ESI-TOF) m/z: (M+H)+ Calcd for C15H15N7O 310.14108; found 310.1415

Dose Response Curve

Platform ID: INK128
Min: -13.2131; Max: 80.1073

IC	Concentration (µM)
IC10	N/A
IC20	0.0967
IC30	0.1748
IC40	0.2838
IC50	0.4429
IC60	N/A
IC70	N/A
IC80	N/A
IC90	N/A

Screen Summary

Round: 02
Dose: 200nM
Days of incubation: 8
Doublings: 3.4
Numbers of reads: 9512731

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

Gene	CRANKS Score	FDR
RRAGA	-2.75	0.12
THAP1	-2.74	0.12
BIRC2	-2.62	0.12
RNF38	-2.58	0.12
SLC1A2	-2.42	0.12
LAMTOR4	-2.38	0.13
AQP10	-2.32	0.49
GINS2	-2.22	0.58
ZXDB	-2.11	0.47
LAMTOR2	-2.10	0.47
TRAPPC8	-2.10	0.58
SIN3A	-2.09	0.47
NOP58	-2.08	0.58
GPC1	-2.05	0.49
XPO1	-2.05	0.78
TRIM3	-2.03	0.49
FAM219A	-2.02	0.58
NRAS	-2.00	0.58
KCTD5	-1.98	0.58
TIPRL	-1.98	0.58
C6orf118	-1.98	0.58
HEXIM1	-1.97	0.58
U2AF2	-1.97	0.58
AKT1	-1.95	0.58
LAMC2	-1.94	0.58
ICA1L	-1.91	0.58
OR5P3	-1.89	0.58
PDGFRB	-1.89	0.58
VTA1	-1.88	0.58
C3orf43	-1.86	0.58
TCTE3	2.05	0.31
DIAPH3	2.08	0.37
BTK	2.09	0.31
ADIPOR1	2.09	0.21
FAM136A	2.10	0.34
TRIAP1	2.10	0.34
DHX35	2.10	0.21
EIF2AK3	2.12	0.21
NFATC3	2.13	0.27
EIF4A1	2.14	0.27
DNAJC2	2.20	0.39
UBE2H	2.20	0.16
PTEN	2.23	0.15
RREB1	2.24	0.21
POLRMT	2.24	0.15
LDHB	2.27	0.20
EIF4EBP1	2.30	0.14
SON	2.31	0.17
TNC	2.38	0.10
ZFC3H1	2.41	0.14
PGM3	2.43	0.14
MEIG1	2.45	0.34
KIAA0195	2.63	0.06
PSMD7	2.63	0.40
RPE	2.63	0.06
AKT1S1	2.83	0.01
DAZAP1	2.90	<0.01
FIBP	4.09	<0.01
PPP3CA	4.22	<0.01
PPP3R1	4.73	<0.01

Screen	Correlation	Plot
Torin1 0.08μM R02 exp82	0.116	View
KU-0063794 3.8μM R02 exp71	0.094	View
Rapamycin 10μM R00 exp30	0.058	View
Rapamycin 1μM R00 exp29	0.057	View

GO Term	Fold Change	Genes
GTPase activator complex	184.27	RRAGA,LAMTOR4,LAMTOR2
enzyme activator complex	122.84	RRAGA,LAMTOR4,LAMTOR2
positive regulation of TORC1 signaling	49.14	RRAGA,LAMTOR4,LAMTOR2,AKT1

GO Term	Fold Change	Genes
calcineurin-NFAT signaling cascade	118.46	PPP3R1,PPP3CA,NFATC3
calcineurin-mediated signaling	97.55	PPP3R1,PPP3CA,NFATC3
calcium-mediated signaling	17.95	PPP3R1,PPP3CA,NFATC3,EIF2AK3,BTK

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