Ripasudil(K-115)
CAS 887375-67-9
Ripasudil (K-115) is a specific inhibitor of ROCK, with IC50s of 19 and 51 nM for ROCK2 and ROCK1, respectively.
Kinases & Cell Signaling
Kinase inhibitors and modulators of intracellular signaling pathways.
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Toceranib phosphate(SU 11654)
CAS 874819-74-6
Toceranib phosphate is a multitargeted indolinone receptor tyrosine kinase (RTK) inhibitor with Kis of 5 and 6 nM for PDGFRβ and Flk-1/KDR, respectively.
PP2(AGL 1879)
CAS 172889-27-9
PP2 is a reversible and ATP-competitive Src family kinases inhibitor with IC50s of 4 and 5 nM for Lck and Fyn, respectively.
PF-04691502
CAS 1013101-36-4
PF-04691502 is a potent and selective inhibitor of PI3K and mTOR. PF-04691502 binds to human PI3Kα, β, δ, γ and mTOR with Kis of 1.8, 2.1, 1.6, 1.9 and 16 nM, respectively.
WHI-P154
CAS 211555-04-3
WHI-P154 is a potent EGFR inhibitor, and also modestly blocks JAK3, with IC50s of 4 nM and 1.8 μM, respectively.
PF-299804 (Dacomitinib,PF-00299804)
CAS 1110813-31-4
Dacomitinib is a specific and irreversible inhibitor of the ERBB family of kinases with IC50s of 6 nM, 45.7 nM and 73.7 nM for EGFR, ERBB2, and ERBB4, respectively.
PF573228
CAS 869288-64-2
PF-573228 is a potent and selective FAK inhibitor with IC50 of 4 nM for purified recombinant catalytic fragment of FAK.
GZD824
CAS 1257628-77-5
GZD824 is a novel orally bioavailable Bcr-Abl inhibitor for Bcr-Abl(WT) and Bcr-Abl(T315I) with IC50 of 0.34 nM and 0.68 nM, respectively. IC50 Value: 0.34/0.68 nM(Bce-Abl wt/T315I) [1]Target: Bcr-Abl in vitro: GZD824 potently suppressed proliferation of…
Duvelisib (IPI-145, INK1197)
CAS 1201438-56-3
Duvelisib is a selectivite p100δ inhibitor with IC50 of 2.5 nM, 27.4 nM, 85 nM and 1602 nM for p110δ, P110γ, p110β and p110α, respectively.
Pelitinib (EKB-569; WAY-EKB 569)
CAS 257933-82-7
Pelitinib (EKB-569;WAY-EKB 569) is an irreversible inhibitor of EGFR with an IC50 of 38.5 nM; also slightly inhibits Src, MEK/ERK and ErbB2 with IC50s of 282, 800, and 1255 nM, respectively.
PLX-4720
CAS 918505-84-7
PLX-4720 is a potent and selective inhibitor of B-RafV600E with IC50 of 13 nM in a cell-free assay, equally potent to c-Raf-1(Y340D and Y341D mutations), and 10-fold selectivity for B-RafV600E than wild-type B-Raf.
Toceranib(SU 11654; PHA 291639)
CAS 356068-94-5
Toceranib is a multitargeted indolinone receptor tyrosine kinase (RTK) inhibitor with Kis of 5 and 6 nM for PDGFRβ and Flk-1/KDR, respectively.
Baricitinib (INCB28050, LY3009104)
CAS 1187594-09-7
Baricitinib is a selective and orally bioavailable JAK1 and JAK2 inhibitor with IC50s of 5.9 nM and 5.7 nM, respectively.
Go 6983
CAS 133053-19-7
Go 6983 is a pan-PKC inhibitor against for PKCα, PKCβ, PKCγ, PKCδ and PKCζ with IC50 of 7 nM, 7 nM, 6 nM, 10 nM and 60 nM, respectively.
Roxadustat(FG-4592)
CAS 808118-40-3
Roxadustat (FG-4592) is an oral hypoxia-inducible factor (HIF) prolyl hydroxylase inhibitor developed for the treatment of anemia.
Idelalisib (CAL-101,GS-1101)
CAS 870281-82-6
Idelalisib (CAL-101) is a highly selective and potent p110δ inhibitor with an IC50 of 2.5 nM, showing 40- to 300-fold selectivity for p110δ over other PI3K class I enzymes.
AZD1080
CAS 612487-72-6
AZD1080 is a potent and selective GSK3 inhibitor. AZD1080 inhibits recombinant human GSK3α and GSK3β with pKi (IC50) of 8.2 (6.9 nM) and 7.5 (31 nM), respectively.
OTS-964
CAS 1338545-07-5
OTS-964 is a potent TOPK inhibitor (IC50=28 nM), which inhibits TOPK kinase activity with high affinity and selectivity.
FIPI
CAS 939055-18-2
FIPI is a derivative of halopemide which potently inhibits both PLD1 and PLD2 with IC50s of 25 nM and 20 nM, respectively.
KN-93 Phosphate
CAS 1188890-41-6
KN-93 is a selective Ca2+/calmodulin-dependent protein kinase II inhibitor, which has been implicated in the regulation of smooth muscle contractility. CaM kinase II activation was inhibited by KN-93 pretreatment (IC50 ~1 μM). KN-93 inhibited…
Quizartinib (AC220)
CAS 950769-58-1
Quizartinib (AC220) is a potent Flt3 tyrosine kinase inhibitor with a Kd of 1.6±0.7 nM.
CZC-54252
CAS 1191911-27-9
CZC-54252 is a potent inhibitor of LRRK2 with IC50s of 1.28 nM and 1.85 nM for wild-type and G2019S LRRK2 respectively
MHY1485
CAS 326914-06-1
MHY1485 is a cell-permeable mTOR activator. MHY1485 has an inhibitory effect on the autophagic process by inhibition of fusion between autophagosomes and lysosomes.
PD 153035(AG-1517)
CAS 153436-54-5
PD153035 (ZM 252868;AG 1517;Tyrphostin AG 1517;SU 5271) is a potent EGFR inhibitor with Ki and IC50 of 6 and 25 pM, respectively.
Afuresertib HCl
CAS 1047645-82-8
Afuresertib hydrochloride is a potent and ATP-competitive specific Akt inhibitor.
Pilaralisib(XL-147; SAR245408)
CAS 934526-89-3
Pilaralisib (XL147; SAR245408) is a potent and highly selective class I PI3Ks inhibitor with IC50s of 39 nM, 383 nM, 23 nM and 36 nM for PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ.
SNS-032(BMS-387032)
CAS 345627-80-7
SNS-032 (BMS-387032) is a selective inhibitor of?CDK2, CDK7, and CDK9 with?IC50s?of 38 nM, 62 nM and 4 nM, respectively.
APY0201
CAS 1232221-74-7
APY0201 is a potent PIKfyve inhibitor, which inhibits the conversion of PtdIns3P to PtdIns(3,5)P2 in the presence of in the presence of [33P]ATP with an IC50 of 5.2 nM. APY0201 also inhibits IL-12/IL-23 production.
LDN-214117
CAS 1627503-67-6
LDN-214117 is a potent and selective ALK2 inhibitor with IC50 of 22 nM; > 100 fold selectivity for ALK5; also inhibits BMP6(IC50=100 nM).IC50 value: 22 nM(ALK2) [1]Target: ALK2 inhibitorLDN-214117 is a highly BMP selective compound, significantly biased…
Lapatinib
CAS 231277-92-2
Lapatinib (GW572016) is a potent EGFR and ErbB2 inhibitor with IC50s of 10.2 and 9.8 nM, respectively.
Afatinib
CAS 850140-72-6
Afatinib (BIBW 2992) is an irreversible EGFR family inhibitor with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively.
Smoothened Agonist (SAG) free base
CAS 912545-86-9
SAG is a potent Smo receptor agonist which activates the Hedgehog signaling pathway with a Kd of 59 nM.
Palbociclib
CAS 571190-30-2
Palbociclib (PD 0332991) is a selective CDK4 and CDK6 inhibitor with IC50s of 11 and 16 nM, respectively. Palbociclib is a drug for the treatment of ER-positive and HER2-negative breast cancer.
Palbociclib isethionate
CAS 827022-33-3
Palbociclib isethionate(PD-0332991 isethionate) is a highly specific inhibitor of Cdk4 (IC50=11 nM) and Cdk6 (IC50=16 nM), having no activity against a panel of 36 additional protein kinases.
Sorafenib free base (BAY-43-9006)
CAS 284461-73-0
Sorafenib (Bay 43-9006) is a potent multikinase inhibitor with IC50s of 6 nM, 20 nM, and 22 nM for Raf-1, B-Raf, and VEGFR-3, respectively.
CX-4945 (Silmitasertib)
CAS 1009820-21-6
CX-4945 is a potent, selective and oral casein kinase 2 (CK2) inhibitor with a Ki of 0.38 nM.
PHA-665752
CAS 477575-56-7
PHA-665752 is a potent, selective and ATP-competitive c-Met inhibitor with IC50 of 9 nM, >50-fold selectivity for c-Met than RTKs or STKs.
PF06463922(Lorlatinib)
CAS 1454846-35-5
Lorlatinib is a potent, dual ALK/ROS1 inhibitor, with Kis of 0.02 nM, 0.07 nM, and 0.7 nM for ROS1, wild type ALK, and ALK-L1196M, respectively.
PH-797804
CAS 586379-66-0
PH-797804 is a novel pyridinone inhibitor of p38α with IC50 of 26 nM; 4-fold more selective versus p38β and does not inhibit JNK2.
Sunitinib malate
CAS 341031-54-7
Sunitinib Malate (SU 11248 Malate) is a potent tyrosine kinase inhibitor targeting VEGFR2 and PDGFRβ with IC50s of 80 nM and 2 nM, respectively.
Trametinib
CAS 871700-17-3
Trametinib is a potent MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Due to the poor solubility of Trametinib, Trametinib DMSO solvate (Cat. No.: HY-10999A) is recommeded.
SDMA
CAS 30344-00-4
SDMA (Symmetric dimethylarginine) is an endogenous inhibitor of nitric oxide (NO) synthase activity.
MSC2530818
CAS 1883423-59-3
MSC2530818 is a potent, selective and orally available CDK8 inhibitor with an IC50 of 2.6 nM for CDK8.
T-5224
CAS 530141-72-1
T-5224 is a selective inhibitor of c-Fos/activator protein (AP)-1. It also inhibits MMP3/13 with IC50s of 10 nM.
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