CZC-25146
CAS 1191911-26-8
CZC-25146 is a potent, selective and metabolically stable LRRK2 inhibitor with IC50 of 4.76 nM/6.87 nM for wild type LRRK2 and G2019S LRRK2 respectively.
Kinases & Cell Signaling
Kinase inhibitors and modulators of intracellular signaling pathways.
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Other Research Tools (75) · Additional reagents, building blocks and specialized research tools.
Kinases & Cell Signaling products
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B-Raf IN 1
CAS 950736-05-7
B-Raf IN 1 is a potent and selective B-Raf kinase inhibitor with an IC50 of 24 nM.
AZD-1208
CAS 1204144-28-4
AZD1208 is a novel, orally bioavailable, highly selective PIM kinases inhibitor.
AS703026（Pimasertib）
CAS 1236699-92-5
Pimasertib (AS703026) is a highly selective, potent, ATP non-competitive allosteric inhibitor of MEK1/2, used for cancer treatment.
FGF401( Roblitinib)
CAS 1708971-55-4
FGF-401 is an inhibitor of FGFR4 extracted from patent WO2015059668A1, compound example 83; has an IC50 of 1.9 nM.
SB 415286
CAS 264218-23-7
SB 415286 is a potent and selective cell permeable inhibitor of GSK-3α, with an IC50 of 77.5 nM, and a Ki of 30.75 nM; SB 415286 is equally effective at inhibiting human GSK-3α and GSK-3β.
Pexidartinib(PLX3397)
CAS 1029044-16-3
Pexidartinib (PLX-3397) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 13 nM, 27 nM, and 11 nM for CSF1R, c-Kit, and FLT3, respectively.
PHA-739358 (danusertib)
CAS 827318-97-8
Description of Danusertib: Danusertib is a small-molecule 3-aminopyrazole derivative with potential antineoplastic activity. Aurora kinase inhibitor PHA-739358 binds to and inhibits the Aurora kinases, which may result in cell growth arrest and apoptosis in…
SLx-2119(KD-025,Belumosudil )
CAS 911417-87-3
SLx-2119 is a selective inhibitor of ROCK2 with an IC50 of 105 nM.
WHI-P180(Janex 3)
CAS 211555-08-7
WHI-P180 (Janex 3) is a multi-kinase inhibitor; inhibits RET, KDR and EGFR with IC50s of 5 nM, 66 nM and 4 μM, respectively.
PQR-309(Bimiralisib)
CAS 1225037-39-7
Bimiralisib is a potent, brain-penetrant, orally bioavailable, pan-class I PI3K/mTOR inhibitor with IC50s of 33 nM, 451 nM, 661 nM, 708 nM and 89 nM for PI3Kα, PI3Kδ, PI3Kβ, PI3Kγ and mTOR, respectively. Bimiralisib is an mTORC1 and mTORC2 inhibitor.
Solcitinib（GLPG0778）
CAS 1206163-45-2
Solcitinib is an orally active, competitive, potent, selective JAK1 inhibitor, with an IC50 of 9.8 nM, and 11-, 55- and 23-fold selectivity over JAK2, JAK3 and TYK2, respectively; Solcitinib is used in the research of moderate-to-severe plaque-type psoriasis.
WHI-P258
CAS 21561-09-1
WHI-P258, a quinazoline compound, binds to the active site of JAK3 with an estimated Ki of 72 µM. WHI-P258 does not inhibit JAK3 and does not affect the thrombin-induced aggregation of platelets even at 100 μM[1][2].
Vardenafil hydrochloride trihydrate
CAS 330808-88-3
Vardenafil is a PDE5 inhibitor used for treating erectile dysfunction.Vardenafil specifically inhibited the hydrolysis of cGMP by PDE5 with an IC50 of 0.7 nM (6.6 nM). In contrast, the IC50 of vardenafil for PDE1 was 180 nM; for PDE6, 11 nM; for PDE2, PDE3…
NVP-ACC-789
CAS 300842-64-2
NVP-ACC789 is an inhibitor of human VEGFR-1, VEGFR-2 (mouse VEGFR-2), VEGFR-3 and PDGFR-β with IC50s of 0.38, 0.02 (0.23), 0.18, 1.4 μM, respectively.
R788 disodium (Fostamatinib)
CAS 1025687-58-4
Fostamatinib Disodium (R788 Disodium), a prodrug of the active metabolite R406, is a potent Syk inhibitor with IC50 of 41 nM.
GW806742X
CAS 579515-63-2
GW806742X is a Mixed Lineage Kinase Domain-Like (MLKL) inhibitor which binds the MLKL pseudokinase domain with a Kd value of 9.3 μM and anti-necroptosis activity. GW806742X has activity against VEGFR2[1][2].
Lonafarnib
CAS 193275-84-2
Lonafarnib is an orally bioavailable farnesyl protein transferase (FPTase) inhibitor for H-ras, K-ras and N-ras with IC50 of 1.9 nM, 5.2 nM and 2.8 nM, respectively.
GW-5074
CAS 220904-83-6
GW 5074 is a potent and selective c-Raf inhibitor with IC50 of 9 nM, and has no effect on the activities of JNK1/2/3, MEK1, MKK6/7, CDK1/2, c-Src, p38 MAP, VEGFR2 or c-Fms.
RAF709
CAS 1628838-42-5
RAF709 is a potent, selective, and efficacious RAF inhibitor with IC50s of 0.4 nM and 0.5 nM for BRAF and CRAF, respectively[1]. Antitumor efficacy[1].
α-Amyloid Precursor Protein Modulator(TPPB)
CAS 497259-23-1
α-Amyloid Precursor Protein Modulator(TPPB) is a cell-permeable benzolactam-derived protein kinase C (PKC) activator with a Ki of 11.9 nM.
Torin1
CAS 1222998-36-8
Torin 1 is a potent inhibitor of mTOR with an IC50 of 3 nM. Torin 1 inhibits both mTORC1/2 complexes with IC50 values between 2 and 10 nM.
SAR131675
CAS 1433953-83-3
SAR131675 is a potent and selective VEGFR3 inhibitor with an IC50 of 23 nM.
EW-7197
CAS 1352608-82-2
Vactosertib (EW-7197) is an ATP-competitive inhibitor of ALK5 with an IC50 of 12.9 nM. It also inhibits ALK2 and ALK4 at nanomolar concentrations.
Selonsertib（GS-4997）
CAS 1448428-04-3
Selonsertib is an apoptosis signal-regulating kinase 1 (ASK1) inhibitor with a pIC50 of 8.3±0.07.
RKI-1447
CAS 1342278-01-6
RKI-1447 is a potent small molecule inhibitor of ROCK1 and ROCK2 with IC50 values of 14.5 nM and 6.2 nM, respectively.
WP1130(Degrasyn)
CAS 856243-80-6
Degrasyn (WP1130) is a cell-permeable deubiquitinase (DUB) inhibitor, directly inhibiting DUB activity of USP9x, USP5, USP14, and UCH37. Degrasyn has been shown to downregulate the antiapoptotic proteins Bcr-Abl and JAK2.
Dovitinib (TKI258, CHIR258)
CAS 405169-16-6
Dovitinib is a multi-targeted tyrosine kinase inhibitor with IC50s of 1, 2, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, FGFR1/3, VEGFR1/2/3 and PDGFRα/β, respectively.
GSK2982772
CAS 1622848-92-3
GSK2982772 is a potent and ATP competitive RIP1 inhibitor with an IC50 of 16 nM.
Semaxanib (SU5416)
CAS 204005-46-9
Semaxinib (SU5416) is a potent and selective inhibitor of the vascular endothelial growth factor receptor (Flk-1/KDR) with an IC50 of 1.23 μM.
Bay 11-7085
CAS 196309-76-9
BAY 11-7085 is an inhibitor of NF-κB activation and phosphorylation of IκBα; it stabilizes IκBα with an IC50 of 10 μM.
SC-514 (GK 01140)
CAS 354812-17-2
SC-514 is a selective IKK-2 inhibitor (IC50=11.2±4.7 μM), which does not inhibit other IKK isoforms or other serine-threonine and tyrosine kinases.
LY-303511(Nv-128)
CAS 154447-38-8
LY303511 is a structural analogue of LY294002. LY303511 does not inhibit PI3K. LY303511 enhances TRAIL sensitivity of SHEP-1 neuroblastoma cells. LY303511 reversibly blocks K+ currents (IC50=64.6±9.1 μM) in MIN6 insulinoma cells.
AICAR (Acadesine)
CAS 2627-69-2
AICAR is a cell-permeable AMP-activated protein kinase (AMPK) activator.
Darapladib
CAS 356057-34-6
Darapladib is a potent inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2) with IC50 of 0.25 nM.
Upadacitinib
CAS 1310726-60-3
Upadacitinib (ABT-494) is a potent and selective Janus kinase (JAK) 1 inhibitor with an IC50 of 43 nM, being developed for the treatment of several autoimmune disorders.
VX-745
CAS 209410-46-8
Neflamapimod (VX-745) is a potent and selective inhibitor of p38α, and possesses anti-inflammatory activity.
SD-208
CAS 627536-09-8
SD-208 is a selective TGF-βRI (ALK5) inhibitor with IC50 of 48 nM, and > 100-fold selectivity over TGF-βRII.
GSK2983559 active metabolite
CAS 1423186-80-4
GSK2983559 active metabolite is a receptor interacting protein-2 (RIP2) kinase inhibitor extracted from patent WO/2014043446 A1, compound example 1.
SU 5214
CAS 186611-04-1
SU5214 is a potent VEGFR2 inhibitor extracted from patent US5834504A, SU5214, has the IC50s of 14.8 µM (FLK-1) and 36.7 µM (EGFR), respectively[1].
AZD5438
CAS 602306-29-6
AZD-5438 is a potent inhibitor of CDK1/2/9 with IC50 of 16 nM/6 nM/20 nM in cell-free assays. It also inhibits GSK3β, but is less potent to CDK5/6.
GS9973（Entospletinib）
CAS 1229208-44-9
Entospletinib (GS-9973) is an orally bioavailable, selective?Syk inhibitor with an IC50 of 7.7 nM.
GSK1838705A
CAS 1116235-97-2
GSK1838705A is a small-molecule kinase inhibitor that inhibits IGF-IR and IR (insulin receptor) with IC50s of 2.0 and 1.6 nM, respectively . GSK1838705A blocks the in vitro proliferation of cell lines derived from solid and hematologic malignancies, inclu
PKC-412 (Midostaurin)
CAS 120685-11-2
Midostaurin (CGP41231; PKC412) is a multi-targeted protein kinase inhibitor which inhibits PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/2 with IC50 ranging from 16-500 nM.
c-Kit-IN-1(DCC-2618)
CAS 1225278-16-9
c-Kit-IN-1 is a potent inhibitor of c-Kit and c-Met with IC50s of <200 nM.
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