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R428 is a potent and selective inhibitor of Axl with IC50 value of 14 nM
2018-09-26 19:00
R428 (2μM) significantly interferes with mechanisms of migration and
invasion of Axlpos melanoma cells at levels comparable to Axl knockdo..
AP20187 is a cell-permeable molecule
2018-09-26 18:46
AP20187 is a cell-permeable molecule used to dimerize FK506-binding protein (FKBP) fusion proteins and initiate biological signaling c..
SHP099 hydrochloride is a potent, selective, orally available SHP2 inhibitor with an IC50 of 70 nM
2018-09-25 18:25
The X-ray co-crystal for SHP099 with SHP2 reveals a new interaction with
the basic amine and the Phe113 backbone carbonyl. SHP099 shows
..
LY2835219 a selective CDK4/6 inhibitor with IC50 values of 2 nM and 10 nM for CDK4 and CDK6
2018-09-25 18:18
LY2835219 reduces cell viability with the IC50 values ranging
from 0.5 μM to 0.7 μM, inhibits Akt and ERK signaling but not mTOR
activat..
OTX-015 is a new potent BRD2/3/4 inhibitor for cell adhesion with IC50 values
2018-09-24 19:11
OTX015 (500 nM) exposure induces a strong decrease of BRD2, BRD4 and c-MYC and increase of HEXIM1 proteins, while BRD3 expression is unchang..
GSK126 is a potent, highly selective inhibitor of EZH2
2018-09-24 17:59
GSK126 potently inhibits both wild-type and mutant EZH2 methyltransferase activity with similar potencies (Ki=0.5-3
nM) independent of sub..
ARS-853 is a selective, covalent KRASG12C inhibitor with IC50 of 2.5 μM
2018-09-20 22:33
ARS853 is designed to bind KRASG12C with high affinity. Treatment of KRASG12C-mutant
lung cancer cells with ARS853 reduces the level of GT..
ABT-199 is a highly potent, orally bioavailable and Bcl-2-selective inhibitor with Ki of <0.01 nM
2018-09-20 18:43
ABT-199 potently kills FL5.12-BCL-2 cells (EC50=4 nM), ABT-199 shows much weaker activity against FL5.12-BCL-XL cells (EC50=261 nM). ABT-199..
Olaparib is a potent PARP inhibitor with IC50 of 5 and 1 nM for PARP-1 and PARP-2
2018-09-19 22:37
Olaparib (AZD2281) is a single digit nanomolar inhibitor of both PARP-1
and PARP-2 that shows standalone activity against BRCA1-deficient ..
Motesanib Diphosphate is a potent ATP-competitive inhibitor of VEGFR1/2/3
2018-09-19 19:38
Motesanib Diphosphate is a potent ATP-competitive inhibitor of VEGFR1/2/3 with IC50s
of 2 nM/3 nM/6 nM, respectively, and has similar acti..
Navitoclax is a potent and orally bioavailable Bcl-2 family protein inhibitor that binds
2018-09-19 19:02
Navitoclax is a potent and orally bioavailable Bcl-2 family protein inhibitor that binds with high affinity (Ki < 1 nM) to multiple anti-..
Silvestrol is isolated from the fruits and twigs of Aglaia foveolata
2018-09-18 19:27
Silvestrol is a specific eIF4A-targeting translation inhibitor.
Silvestrol exhibits significant cytotoxic activity against many human
ca..
Elacestrant (RAD1901) is a selective and orally available estrogen receptor (ERR) degrader
2018-09-18 18:23
RAD1901 selectively binds to and degrades the ER and is a potent
antagonist of ER-positive breast cancer cell proliferation. RAD1901
tre..
Elafibranor is an agonist of the peroxisome proliferator-activated receptor-α
2018-09-17 23:43
Elafibranor is an agonist of the peroxisome proliferator-activated receptor-α (PPAR-α) and peroxisome proliferator-activated receptor-δ (PPA..
INCB 024360 is a potent and selective IDO1 inhibitor with IC50 of 71.8 nM±17.5 nM
2018-09-17 19:00
In cellular assays,INCB 024360 (INCB024360) selectively inhibits human IDO1 with IC50
values of approximately 10 nM, demonstrating little ..