Kinases & Cell Signaling

Sorafenib (BAY-43-9006)

CAS 475207-59-1

Sorafenib tosylate is a potent multikinase inhibitor, with IC50s of 6 nM, 20 nM, and 22 nM for Raf-1, B-Raf, and VEGFR-3, respectively.

Nilotinib

CAS 641571-10-0

Nilotinib is an orally available Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity.

PD0325901 (Mirdametinib)

CAS 391210-10-9

PD0325901 is a selective and cell permeable MEK inhibitor with an IC50 of 0.33 nM.

LEE011 hydrochloride

CAS 1211443-80-9

Ribociclib hydrochloride (LEE011 hydrochloride) is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex.

p38-α MAPK-IN-1

CAS 443913-15-3

p38-α MAPK-IN-1 is an inhibitor of MAPK14 (p38-α), with IC50 of 2300 nM in EFC displacement assay, and 5500 nM in HTRF assay.

Sildenafil

CAS 139755-83-2

Sildenafil is a potent phosphodiesterase type 5 (PDE5) inhibitor with IC50 of 5.22 nM.

BVT-948

CAS 39674-97-0

BVT948 is a protein tyrosine phosphatase (PTP) inhibitor which can also inhibit several cytochrome P450 (P450) isoforms and lysine methyltransferase SETD8.

IXA4

CAS 1185329-96-7

IXA4 is the most selective for the IRE1–XBP1s signaling pathway.IXA4 selectively activate IRE1–XBP1s signaling and reduces secretion of APP through IRE1 activation.

HG106

CAS 928712-10-1

HG106 is a potent SLC7A11 inhibitor and enhances ROS generation, ER stress, and ultimately growth arrest specifically in KRAS-mutant lung adenocarcinoma (LUAD).

GRK6 inhibitor 18

CAS 2677786-61-5

GRK6 inhibitor 18 is a potent, and selective GRK6 inhibitor with IC50 of 8 nM. GRK6 inhibitor 18 displays >1,000-fold selectivity over Aurora A, as well as high selectivity against a panel of 85 kinases. GRK6 inhibitor 18 has potent cellular target engagement…

Ezetimibe (Zetia)

CAS 163222-33-1

Ezetimibe (SCH 58235) is a Niemann-Pick C1-like1 (NPC1L1) inhibitor, and is a potent Nrf2 activator. Ezetimibe (SCH 58235) is a potent cholesterol absorption inhibitor.

CASIN

CAS 425399-05-9

CASIN is a selective GTPase Cdc42 inhibitor with IC50 of 2 uM.

Lanraplenib (GS-9876)

CAS 1800046-95-0

Lanraplenib (GS-9876) is a highly selective and oral SYK inhibitor (IC50=9.5 nM) in development for the treatment of inflammatory diseases. Lanraplenib (GS-9876) inhibits SYK activity in platelets via the glycoprotein VI (GPVI) receptor without prolonging…

3-Methyladenine

CAS 5142-23-4

3-Methyladenine is a PI3K inhibitor. 3-Methyladenine is a widely used inhibitor of autophagy via its inhibitory effect on class III PI3K.

Pyrrolidinedithiocarbamate ammonium;APDC, PDTC

CAS 5108-96-3

Pyrrolidinedithiocarbamate ammonium is a selective NF-κB inhibitor.

Larotrectinib (LOXO-101 sulfate)

CAS 1223405-08-0

Larotrectinib (LOXO-101) sulfate is an ATP-competitive oral, selective inhibitor of the tropomyosin-related kinase (TRK) family receptors, with low nanomolar 50% inhibitory concentrations against all three isoforms (TRKA, B, and C).

GAK inhibitor 12r

CAS 2241325-66-4

GAK inhibitor 12r is a higghly potent, selective inhibitor of cyclin G-associated kinase (GAK) with Kd of 89 nM; targets only 8 other kinases with greater than 90% inhibition in a diverse panel of 468 kinases; demonstrates broad-spectrum antiviral activity…

TrkA inhibitor compound 23（TrkA-IN-23）

CAS 1821484-84-7

TrkA-IN-23 is a highly potent, subtype selective, peripherally restricted, allosteric TrkA inhibitor with IC50 of 10 nM, 180-fold selective over TrkB and 70-fold selective over TrkC in cell based assays; exhibits exquisite TrkA selectivity with >95%…

NRPa-308

CAS 717863-53-1

NRPa-308 is a neuropilin-1 (NRP-1) antagonist, inhibits the VEGF-A165/NRP-1 binding with IC50 of 42 uM, exerts in vitro anti-angiogenic activity.

Brigatinib (AP-26113)

CAS 1197953-54-0

Brigatinib is a highly potent and selective ALK inhibitor, with an IC50 of 0.6 nM.

Dasatinib (BMS-354825)

CAS 302962-49-8

Description of Dasatinib: Dasatinib is an orally bioavailable synthetic small molecule-inhibitor of SRC-family protein-tyrosine kinases. Dasatinib binds to and inhibits the growth-promoting activities of these kinases. Apparently because of its less stringent…

Regorafenib monohydrate（BAY 73-4506）

CAS 1019206-88-2

Regorafenib monohydrate is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively.

VU 0465350

CAS 1414843-61-0

A potent, specific BMP receptor activin receptor-like kinase 3 (ALK3) antaognist with Ki of 92.3 nM; shows no activity for ALK2/4/5, also shows affinity for TGFBR2, VEGFR2 and AMPK; blocks SMAD phosphorylation in vitro and in vivo, and enhances liver…

JNK-IN-8

CAS 1410880-22-6

JNK-IN-8 is a potent JNK inhibitor with IC50s of 4.7 nM, 18.7 nM, and 1 nM for JNK1, JNK2, and JNK3, respectively.

GW-2580 (GW2580)

CAS 870483-87-7

GW2580 is an orally bioavailable inhibitor of c-Fms kinase which completely inhibits human cFMS kinase in vitro at 0.06 μM.

Neratinib (HKI-272)

CAS 698387-09-6

Neratinib is an orally available, irreversible tyrosine kinase inhibitor with IC50s of 59 nM and 92 nM for HER2 and EGFR, respectively.

UU-T03

CAS 1586007-00-2

UU-T03 is the ethyl ester derivative of UU-T02, which is a potent, selective inhibitor of β-catenin/Tcf4 interaction with Ki of 1.36 uM; exhibits growth inhibition of SW480 cells with IC50 of 10.77 uM; downregulates the transcription of AXIN2, LGR5, cyclin…

FN1-8

CAS 1419258-63-1

FN1-8 is a novel, synthetic small molecule that efficiently interferes with Gli/TAF9 interaction and downregulate Gli/TAF9-dependent transcriptional activity (at 15 uM); inhibits non-canonical Gli activation and acts downstream of the canonical Hh pathway;…

PRL-295

CAS 2377770-85-7

PRL-295 is a small molecule Keap1-Nrf2 protein–protein interaction inhibitor.PRL-295 binds to Keap1 in the cellular environment, disrupting its interaction with Nrf2, which leads to enhanced gene expression of the classical Nrf2 target NQO1 in cells and in…

SCB-4380

CAS 915-67-3

SCB-4380 (SCB 4380, SCB4380) is the first potent, selective inhibitor for PTPRZ (protein tyrosine phosphatase receptor-type Z) with IC50 of 0.4 uM against human Z-ICR-catalyzed hydrolysis. SCB-4380 also strongly inhibits PTPRG (IC50=0.4 uM), and shows little…

BCI(NSC 150117)

CAS 1245792-51-1

BCI is an allosteric inhibitor of dual specificity phosphatase (DUSP). BCI specifically inhibits DUSP6 and DUSP1 with EC50s of 13.3 and 8.0 μM in cells, respectively. BCI does not inhibit DUSP5[1].

TMX-4102

TMX-4102 (TMX4102) is a highly potent, selective PIP4K2C binder with KD of 0.45 nM, shows no affinity for PIP4K2B and PIP4K2A (KD>10 uM).

ACA-14

CAS 667437-56-1

ACA-14 is a small molecule direct inhibitor of KRAS, impedes the interaction of KRAS with its effector Raf and reduces both intrinsic and SOS-mediated nucleotide exchange rates.

Z271-0326

CAS 1243002-72-3

Z271-0326 is a first-in-class, potent and specifc inhibitor of NACK (Notch activation complex kinase) with SPR KD value of 0.89 uM, directly blocks NACK recruitment to the Notch ternary complex (NTC).

BioE-11979（BioE1197）

CAS 1268863-69-9

BioE-1197 is a novel Pask inhibitor. BioE-1197 is a compound that enhances T cell function. Functionally, treatment with BIOE-1197 significantly boosts the ability of effector T cells (such as CD8+, Th1, and Th2 cells) to produce lineage-specific cytokines…

Lipoic acid

CAS 62-46-4

For the detailed information of Lipoic acid, the solubility of Lipoic acid in water, the solubility of Lipoic acid in DMSO, the solubility of Lipoic acid in PBS buffer, the animal experiment（test） (test) of Lipoic acid, the cell expriment (test) of Lipoic…

DSF-102

CAS 197585-01-6

DSF-102 (DSF102) is a small molecule EGFR inhibitor that interacts with the extracellular domain (ECD) of EGFR, inhibits the interaction with the EGF instead of blocking the intracellular kinase activity, shows inhibition of EGFR dimerization with IC50 of

LB-102

CAS 1527483-97-1

LB102 demonstrates potent and selective inhibition of PP2A serine/threonine phosphatase activity, with half-maximal inhibitory concentration (IC50) of 400 nM.

GS-680

CAS 3057733-01-1

GS-680 (GS680) is a novel selective and ATP-competitive CaMKII inhibitor with biochemical IC50 of 2.3 and 15.9 nM against CaMKIIδ and CaMKIIα, respectively.GS-680 inhibited phospholamban phosphorylation in NRVM with an EC50 of 98.9 nM.GS-680 inhibits…

FRAX486

CAS 1232030-35-1

FRAX486 is a p21-activated kinase (PAK) inhibitor with IC50s of 14, 33 and 39 nM for PAK1, PAK2 and PAK3, respectively.

GYS32661

CAS 2589092-11-3

GYS32661 is a potent, small-molecule inhibitor of RAC1 and its isoform RAC1B, specifically designed to target the Sonic Hedgehog (Shh) signaling pathway in cancers like medulloblastoma and colorectal carcinoma. Distinguishing itself from other RAC1…

AZD-7624

CAS 1095004-78-6

AZD7624 is an inhaled p38 inhibitor, with potent anti-inflammatory activity.

K145 (hydrochloride)

CAS 1449240-68-9

K145 is a selective SphK2 inhibitor with an IC50 of 4.30±0.06 μM , while no inhibition of SphK1 at concentrations up to 10 μM.IC50 value: 4.3 uM [1]Target: SphK2in vitro: K145 inhibited the activity of SphK2 in a dose-dependent manner with an IC50 of…

Palbociclib (PD0332991 HCl)

CAS 827022-32-2

Palbociclib hydrochloride is a highly selective CDK4/6 inhibitor with IC50s of 11 nM and 16 nM, respectively.

Reversine

CAS 656820-32-5

Reversine is a novel class of ATP-competitive Aurora kinase inhibitor with IC50s of 400, 500 and 400 nM for Aurora A, Aurora B and Aurora C, respectively.

NVP-BSK805 dihydrochloride

CAS 1942919-79-0

NVP-BSK805 is an ATP-competitive JAK2 inhibitor, with IC50s of 0.48 nM, 31.63 nM, 18.68 nM, and 10.76 nM for JAK2 JH1 (JAK homology 1), JAK1 JH1, JAK3 JH1, and TYK2 JH1, respectively.

Cobimetinib(GDC-0973; XL518)

CAS 934660-93-2

Cobimetinib (GDC-0973, RG7420) is a potent, selective and oral MEK inhibitor with an IC50 of 4.2 nM for MEK1.

Lapatinib ditosylate monohydrate

CAS 388082-78-8

Lapatinib ditosylate monohydrate (GW572016 ditosylate monohydrate) is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively[1].