SB-203580
CAS 152121-47-6
SB 203580 is a widely used p38 MAPK inhibitor with an IC50 of 0.3-0.5 μM. It shows more than 100-fold selectivity over PKB, LCK, and GSK-3β.
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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CHIR-99021 HCl
CAS 1797989-42-4
CHIR-99021 monohydrochloride is a GSK-3α/β inhibitor with IC50 of 10 nM/6.7 nM; > 500-fold selectivity for GSK-3 versus its closest homologs CDC2 and ERK2, as well as other protein kinases.
Bisindolylmaleimide X(Ro 31-8425)
CAS 1241725-89-2
Bisindolylmaleimide X is a cell-permeable, reversible, ATP-competitive protein kinase C (PKC) inhibitor (IC50 = 15 nM, rat brain PKC).
Ruxolitinib Phosphate
CAS 1092939-17-7
Ruxolitinib phosphate is a potent JAK1/2 inhibitor with IC50s of 3.3 nM/2.8 nM, respectively, showing more than 130-fold selectivity over JAK3.
Bohemine
CAS 189232-42-6
Bohemine is a purine analogue and is a synthetic and selective CDK inhibitor with IC50s of 4.6 μM, 83 μM, and 2.7 μM for Cdk2/cyclin E, Cdk2/cyclin A, and Cdk9/cyclin T1, respectively. Bohemine also inhibits ERK2 with an IC50 of 52 μM and has less inhibitory…
Vesnarinone(OPC8212)
CAS 81840-15-5
Vesnarinone is a quinolinone derivative, and its pharmacodynamic effects include inhibition of phosphodiesterase III (PDE3) activity, increases in calcium flux and decreases in potassium flux.
SB-505124
CAS 694433-59-5
SB-505124 is a selective inhibitor of TGFβR with IC50 of 129 nM and 47 nM for ALK4, ALK5, respectively, and it does not inhibits ALK1, 2, 3, or 6 but ALK7.
ARS-1620
CAS 1698055-85-4
ARS-1620 is an atropisomeric selective KRASG12C inhibitor with desirable pharmacokinetics.
Erdafitinib
CAS 1346242-81-6
Erdafitinib (JNJ-42756493) is a potent and orally available FGFR family inhibitor; inhibits FGFR1/2/3/4 with IC50s of 1.2, 2.5, 3.0 and 5.7 nM, respectively.
Dasatinib monohydrate
CAS 863127-77-9
Dasatinib monohydrate (BMS-354825 monohydrate) is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Ki values of 16 pM and 30 pM for Src and Bcr-Abl, respectively[1].
Tofacitinib
CAS 477600-75-2
Tofacitinib is a JAK1/2/3 inhibitor with IC50s of 1, 20, and 112 nM, respectively.
BIBW2992-MA2 (Afatinib dimaleate)
CAS 850140-73-7
Afatinib dimaleate 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.
JH-II-127
CAS 1700693-08-8
JH-II-127 is a highly potent, selective, and brain penetrant LRRK2 inhibitor, with IC50 of 6.6 nM, 2.2 nM ,47.7 nM for LRRK2-wild-type, LRRK2-G2019S, LRRK2-A2016T.IC50 value: 2.2 n(LRRK2-G2019S), 6.6 nM(LRRK2-wild-type), 47.7 nM (LRRK2-A2016T)Target:…
AZD-8055
CAS 1009298-09-2
AZD-8055 is a novel ATP-competitive inhibitor of mTOR kinase with an IC50 of 0.8 nM. AZD-8055 inhibits both mTORC1 and mTORC2.
LM22B-10
CAS 342777-54-2
LM22B-10 is an activator of TrkB/TrkC neurotrophin receptor, and can induce TrkB, TrkC, AKT and ERK activation in vitro and in vivo.
ENMD-2076 L-(+)-Tartaric acid
CAS 1453868-32-0
ENMD-2076 Tartrate is a multi-targeted kinase inhibitor with IC50s of 1.86, 14, 58.2, 15.9, 92.7, 70.8, 56.4 nM for Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα, respectively.
LENVATINIB MESYLATE
CAS 857890-39-2
Lenvatinib mesylate (E7080 mesylate), an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities[1][2].
ETC-159
CAS 1638250-96-0
ETC-159 is a potent, orally available PORCN inhibitor. It inhibits β-catenin reporter activity with an IC50 of 2.9 nM.
Tirofiban (hydrochloride monohydrate)
CAS 150915-40-5
Tirofiban hydrochloride monohydrate is a potent non-peptide, glycoprotein IIb/IIIa (integrins alphaIIbbetaIII) antagonistTirofiban hydrochloride monohydrate blocks platelet aggregation and thrombus formation. Tirofiban is an antithrombotic used in the…
TA-02
CAS 1784751-19-4
TA-02 is a p38 MAPK inhibitor with IC50 of 20 nM.IC50 value: 20 nMTarget: p38TA-02 is a novel compound with similar cardiogenic properties asSB203580 and SB202190. TA-02 especially inhibits TGFBR-2.
TA-01
CAS 1784751-18-3
TA-01 is a potent CK1 and p38 MAPK inhibitor, with IC50s of 6.4 nM, 6.8 nM, 6.7 nM for CK1ε, CK1δ and p38 MAPK, respectively.
Crizotinib (PF-2341066)
CAS 877399-52-5
Crizotinib is a potent inhibitor of c-Met and ALK with an IC50 of 11 nM and 24 nM in cell-based assays, respectively.
Alsterpaullone
CAS 237430-03-4
Alsterpaullone (9-Nitropaullone;NSC 705701) is a potent cyclin-dependent kinases (CDK) inhibitor, with IC50s of 35 nM, 15 nM, 200 nM and 40 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E and CDK5/p35, respectively. Alsterpaullone also competes with ATP…
Ensifentrine
CAS 1884461-72-6
Ensifentrine (RPL-554) is an inhaled first-in-class dual inhibitor of phosphodiesterase 3 (PDE3) and PDE4 with IC50s of 0.4 nM and 1479 nM, respectively. Ensifentrine has bronchoprotective and anti-inflammatory activities. Ensifentrine can be used for chronic…
Erlotinib hydrochloride
CAS 183319-69-9
Erlotinib hydrochloride inhibits purified EGFR kinase with an IC50 of 2 nM.
GANT61(NSC 136476)
CAS 500579-04-4
GANT 61 is an inhibitor of Gli1 and Gli2 targeting the Hedgehog/GLI pathway.
Takeda-6d
CAS 1125632-93-0
Takeda-6d has potent inhibitory activity in both B-RAF with an IC50 of 7.0 nM and VEGFR2 with an IC50 of 2.2 nM.
GNE 477
CAS 1032754-81-6
GNE-477 is a potent and efficacious dual PI3K (IC50=4 nM)/mTOR(Ki=21 nM) inhibitor.
NPS-1034
CAS 1221713-92-3
NPS-1034 is a dual inhibitor of AXL and MET with IC50s of 10.3 and 48 nM, respectively.
Repotrectinib(TPX-005)
CAS 1802220-02-5
Repotrectinib (TPX-0005) is a potent ALK/ROS1/TRK inhibitor, with IC50 of 5.3 nM, 1.01 nM, 1.26 nM and 1.08 nM for SRC, WT ALK, ALK G1202R and ALK L1196M, respectively.
STF-083010
CAS 307543-71-1
STF-083010 is an Ire1 inhibitor. STF-083010 inhibits Ire1 endonuclease activity, without affecting its kinase activity, after endoplasmic reticulum stress.
VPS34 inhibitor 1 (Compound 19, PIK-III analogue)
CAS 1383716-46-8
VPS34 inhibitor 1 (Compound 19, PIK-III analogue) is a potent and selective inhibitor of VPS34 with an IC50 of 15 nM.
GF 109203X
CAS 133052-90-1
Bisindolylmaleimide I (GF109203X) is a highly selective, cell-permeable, and reversible protein kinase C (PKC) inhibitor with a Ki of 14 nM.
PHT427
CAS 1191951-57-1
PHT-247 is an inhibitor of the pleckstrin homology (PH) domain of Akt, and it is also an inhibitor of PDPK1 with Kis of 2.7 µM and 5.2 µM and for Akt and PDPK1, respectively.
Skepinone-L
CAS 1221485-83-1
Skepinone-L is a selective p38 mitogen-activated protein kinase inhibitor. IC50 value:Target: p38MAPKskepinone-L, the first ATP-competitive p38 MAPK inhibitor with excellent in vivo efficacy and selectivity. Therefore, skepinone-L is a valuable probe for…
JSH-23
CAS 749886-87-1
JSH-23 is an NF-κB inhibitor which inhibits NF-κB transcriptional activity with an IC50 of 7.1 μM.
Olprinone (Hydrochloride)
CAS 119615-63-3
Olprinone Hcl(Loprinone Hcl) is a selective phosphodiesterase 3 (PDE3) inhibitor. Olprinone is used as cardiotonic agent with positive inotropic and vasodilating effects. Olprinone has been reported to improve microcirculation and attenuate inflammation.…
Bi 2536
CAS 755038-02-9
BI 2536 is a dual PLK1 and BRD4 inhibitor with IC50s of 0.83 and 25 nM, respectively.
Rolipram
CAS 61413-54-5
Rolipram is a selective phosphodiesterases PDE4 inhibitor with IC50s of 3 nM, 130 nM and 240 nM for PDE4A, PDE4B, and PDE4D, respectively.
Belizatinib(TSR-011)
CAS 1357920-84-3
Belizatinib is an oral, dual, potent inhibitor of ALK and TRKA, TRKB, and TRKC, with IC50 of 0.7 nM for wild-type recombinant ALK kinase.
TC-2153
CAS 1381769-23-8
TC-2153 is a specific, small moelcule inhibitor of neuron-specific tyrosine phosphatase STEP with IC50 of 24.6 nM; increases tyrosine phosphorylation of STEP substrates ERK1/2, Pyk2, and GluN2B, and exhibits no toxicity in cortical cultures, shows specificity…
Riociguat (BAY 63-2521)
CAS 625115-55-1
Riociguat is an oral stimulator of soluble guanylate cyclase (sGC) used in the treatment of pulmonary hypertension.
IRAK-1/4 Inhibitor
CAS 509093-47-4
IRAK-1-4 Inhibitor I is an inhibitor of interleukin-1 receptor-associated kinase 1/4 (IRAK 1/4) with IC50s of 0.2 μM and 0.3 μM, respectively.
URMC-099
CAS 1229582-33-5
URMC-099 is an orally bioavailable and potent mixed lineage kinase type 3 (MLK3) (IC50=14 nM) inhibitor with with excellent blood-brain barrier penetration properties.
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