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T21761 |
HNMPA
|
|
IGF-1R
|
|
HNMPA is a membrane impermeable inhibitor of insulin receptor tyrosine kinase. HNMPA inhibits tyrosine and serine autophosphorylation by the human insulin receptor. HNMPA exhibits no effect on cyclic AMP-dependent prote... |
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T36287 |
Pirtobrutinib
|
|
BTK
|
|
Pirtobrutinib (LOXO-305) is an advanced BTK inhibitor that displays high selectivity and operates through a non-covalent mechanism. This compound effectively inhibits various BTK C481 substitution mutations, leading to t... |
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T9564 |
IRE1α kinase-IN-1
|
|
IRE1
|
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IRE1α kinase-IN-1 is a highly selective IRE1α (ERN1) inhibitor, with an IC50 of 77 nM. It displays 100-fold selectivity for IRE1α over the IRE1β isoform. It inhibits ER stress-induced IRE1α oligomerization and autophosph... |
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T2655 |
CEP-37440
|
CEP37440 |
FAK
,
ALK
|
|
CEP-37440 is an effective and specific Dual FAK/ALK inhibitor with IC50s of 120 nM(ALK cellular in 75% human plasma) and 2.3 nM (FAK). |
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T1770 |
GNE-9605
|
|
LRRK2
|
|
GNE-9605 is a highly effective, specifical, and brain-penetrant LRRK2 inhibitor (IC50: 19 nM). |
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T22396 |
PF-6274484
|
PF 6274484 |
EGFR
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|
PF-6274484, a high affinity, irreversible covalent inhibitor of EGFR kinase with Ki of 0.14 nM, inhibits the autophosphorylation of wild-type EGFR in A549 cells and EGFRL858R/T790M in H1975 cells with IC50 of 5.8 nM and ... |
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T7673 |
ATH686
|
ATH 686 |
Apoptosis
,
FLT
|
|
ATH686 is an potent and selective Inhibitor of FLT3. |
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T38562 |
AKN-028
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FLT
|
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AKN-028 is an orally active and potent FLT3 tyrosine kinase inhibitor ( IC 50 = 6 nM). AKN-028 causes dose-dependent inhibition of FLT3 autophosphorylation. |
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T4327 |
Prexasertib dihydrochloride
|
LY2606368 (dihydrochloride),Prexasertib HCl,LY2606368 |
Apoptosis
,
Chk
,
S6 Kinase
|
|
Prexasertib dihydrochloride (LY2606368) is an ATP-competitive CHK1 inhibitor (Ki: 0.9 nmol/L). in the cell-free assay, its IC50 values are 8 nM and 9 nM for CHK2 and RSK, respectively. |
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T4205 |
AG-494
|
Tyrphostin AG-494,AG 494,Tyrphostin B48 |
EGFR
,
CDK
|
|
AG-494 (Tyrphostin B48) is an inhibitor of epidermal growth factor receptor kinase. |
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T4310 |
Prexasertib
|
LY2606368 |
Apoptosis
,
Chk
|
|
Prexasertib (LY2606368) is an inhibitor of checkpoint kinase 1 (chk1) with potential antineoplastic activity. |
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T1667 |
Tandutinib
|
MLN518,CT53518,NSC726292 |
Apoptosis
,
FLT
,
CSF-1R
,
PDGFR
,
Src
,
c-Kit
|
|
Tandutinib (CT53518) (MLN518, CT53518), an effective FLT3 antagonist (IC50: 0.22 μM), can also inhibit c-Kit and PDGFR, 15-20 fold higher potency for FLT3 versus CSF-1R and >100-fold selectivity for the same target versu... |
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T14137 |
AG 1295
|
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PDGFR
|
|
AG 1295, a selective inhibitor of platelet-derived growth factor receptor (PDGFR) tyrosine-kinase, effectively halts PDGFR autophosphorylation without impacting the autophosphorylation of the EGF receptor[1][2][3][4]. |
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T3545 |
RG13022
|
RG 13022,Tyrphostin RG13022 |
EGFR
|
|
RG13022 (Tyrphostin RG13022) is a tyrosine kinase inhibitor; inhibits the autophosphorylation reaction of the EGF receptor (IC50: 4 μM). |
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T6619 |
Desmethyl Erlotinib hydrochloride
|
OSI420,OSI-420,DesMethyl Erlotinib (CP-473420) HCl,CP-473420,Desmethyl Erlotinib,OSI 420 |
EGFR
,
Drug Metabolite
|
|
Desmethyl Erlotinib hydrochloride (OSI 420) is an active metabolite of erlotinib which is an orally active EGFR tyrosin kinase inhibitor with IC50 of 2 and 20 nM for human EGFR and EGFR autophosphorylation in tumor cells... |
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T4053 |
AST 487
|
NVP-AST 487 |
VEGFR
,
FLT
,
c-RET
,
Bcr-Abl
,
c-Kit
|
|
AST 487 (NVP-AST 487) is a RET kinase inhibitor, inhibiting RET autophosphorylation and activation of downstream effectors. It also can inhibit Flt-3. |
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T16550 |
PKR-IN-C16
|
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Others
|
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PKR-IN-C16 is a specific protein kinase (PKR) inhibitor. PKR-IN-C16 is able to inhibit the autophosphorylation of PKR and unlock the translation blockade induced by PKR in primary neuronal cultures.PKR-IN-C16 binds the A... |
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T3599 |
BFH772
|
BFH-722 |
VEGFR
|
|
BFH772, a structure analogue of BAW2881, is a potent and selective VEGF inhibitor. BFH772 is highly effective at targeting VEGFR2 kinase with an IC50 value of 3 nM. BFH772 inhibits the ligand induced autophosphorylation ... |
|
T30855 |
CGP77675
|
CGP-77675,1-(4-(4-amino-5-(3-methoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)phenethyl)piperidin-4-ol,ZINC1488120,CGP 77675 |
EGFR
,
VEGFR
,
Bcr-Abl
,
Src
|
|
CGP77675 (ZINC1488120) is a potent and selective inhibitor of Src family kinase with IC50s of 5-20 and 40 nM for the phosphorylation of peptide substrates and autophosphorylation of purified Src. CGP77675 exhibits antica... |
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T5168 |
EGFR-IN-12
|
EGFR Inhibitor |
Apoptosis
,
EGFR
|
|
EGFR-IN-12 (EGFR Inhibitor) is a cell permeable and selective inhibitor of EGFR kinase (IC50: 21 nM) and blocks receptor autophosphorylation in cells. |
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T3691 |
(Rac)-SAR131675
|
SAR131675 |
VEGFR
|
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(Rac)-SAR131675 is an effective and specific VEGFR-3 inhibitor. It inhibited VEGFR-3 tyrosine kinase activity (IC50: 20 nmol/L) and VEGFR-3 autophosphorylation (IC50: 45 nmol/L) in HEK cells, respectively. SAR131675 is h... |
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T69260 |
Genistein Diglucuronide
|
|
|
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Genistein Diglucuronide is a metabolite of Genistein which exhibits specific inhibitory activity against tyrosine kinases including autophosphorylation of epidermal growth factor receptor kinase. |
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T69863 |
Dihydrogenistein
|
|
|
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Dihydrogenistein is a derivative of Genistein -- a compound that exhibits specific inhibitory activity against tyrosine kinases including autophosphorylation of epidermal growth factor receptor kinase. |
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T22462 |
1,2,3,4,5,6-Hexabromocyclohexane
|
|
Others
|
|
The compound effectively and directly inhibits JAK2 tyrosine kinase autophosphorylation and specifically inhibits ligand-dependent JAK2 activation. It has no cytotoxicity at 100 μM. A 16-hour treatment with compound (1 μ... |
|
T39185 |
Pp60 (v-SRC) Autophosphorylation Site, Phosphorylated
|
pp60 (v-SRC) Autophosphorylation Site, Phosphorylated |
|
|
pp60 (v-SRC) Autophosphorylation Site, Phosphorylated is a phosphorylated peptide derived from an EGFR substrate. It serves as a valuable tool for quantifying phosphorylated substrates in screening EGFR Kinase inhibitors... |
|
T38841 |
IRE1α kinase-IN-2
|
IRE1α kinase-IN-2 |
|
|
IRE1α kinase-IN-2 is a highly potent inhibitor of IRE1α kinase, demonstrating an EC50 of 0.82 μM. It effectively impedes IRE1α kinase autophosphorylation with an IC50 of 3.12 μM. Additionally, IRE1α kinase-IN-2 effective... |
|
T12610L |
3-Hydroxy Midostaurin
|
CGP52421 |
FLT
|
|
3-Hydroxy Midostaurin (CGP 52421), a PKC412 metabolite, inhibits FMS-like tyrosine kinase-3 (FLT3) autophosphorylation with IC50 values of roughly 132 nM in culture medium and 9.8 μM in plasma. Though less selective, it ... |
|
T40785 |
Gefitinib impurity 1
|
|
|
|
Gefitinib impurity 1 is a compound derived from Gefitinib, a potent and selective EGFR tyrosine kinase inhibitor (IC 50 = 33 nM). This orally active compound selectively inhibits tumor cell growth stimulated by EGF (IC 5... |
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T19119 |
3-Hydroxy Midostaurin-D5
|
CGP52421-D5 |
Others
|
|
3-Hydroxy Midostaurin-D5 (CGP52421-D5) is a deuterium-labeled 3-Hydroxy Midostaurin which is a metabolite of PKC412. PKC412 effectively inhibits FMS-like tyrosine kinase-3 (FLT3) autophosphorylation (IC50s: 132 nM and 9.... |
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T73521 |
Nec-3a
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|
|
|
Nec-3a, an analogue of Necrostatin-3, acts as a RIP1 inhibitor with an inhibition concentration (IC50) of 0.44 μM. This compound successfully impedes the autophosphorylation activity within the RIP1 kinase domain. |
|
T78797 |
FHND5071
|
|
|
|
FHND5071, a potent and selective RET kinase inhibitor, exerts antitumor effects through the inhibition of RET autophosphorylation and may be utilized for tumor disease research [1]. |
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T36718 |
Tie2 Inhibitor 7
|
|
|
|
Tie2 Inhibitor 7 blocks Tie2 kinase activity with a Ki value of 1.3 μM.. It has been shown to inhibit angiopoietin 1-induced Tie2 autophosphorylation and downstream signaling with an IC50 value of 0.3 μM. This compound c... |
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T70444 |
Edicotinib HCl
|
|
|
|
Edicotinib, also known as JNJ-40346527, is a small molecule and orally available inhibitor of colony-stimulating factor-1 receptor (CSF1R; FMS) with potential antineoplastic activity. FMS tyrosine kinase inhibitor JNJ-40... |
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T63978 |
FAK-IN-2
|
|
|
|
FAK-IN-2 is a potent, orally active adherens spot kinase (FAK) inhibitor (IC50: 35 nM) that exhibits antitumour effects. FAK-IN-2 covalently inhibits FAK autophosphorylation in a dose-dependent manner and also inhibits t... |
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T62871 |
LRRK2-IN-6
|
|
|
|
LRRK2-IN-6 (compound 22) is an orally active, selective leucine-rich repeat protein kinase 2 gene (LRRK2) inhibitor with blood-brain barrier permeability that inhibits GS LRRK2 (IC50: 4.6 μM) and WT LRRK2 (IC50: 49 μM). ... |
|
T63057 |
LRRK2-IN-5
|
|
|
|
LRRK2-IN-5 (compound 25) is an oral active, blood-brain barrier penetrating, selective leucine-rich repeat protein kinase 2 (LRRK2) inhibitor, which is effective for GS LRRK2 (IC50: 1.2 μM) and WT LRRK2 (IC50:16 μM) had ... |
|
T1181L |
Gefitinib hydrochloride
|
|
|
|
Gefitinib hydrochloride (ZD1839 hydrochloride) is a potent and orally active EGFR tyrosine kinase inhibitor (EGFR-TKI) (IC 50 = 33 nM) that selectively inhibits EGF-stimulated tumor cell growth (IC 50 = 54 nM) and that b... |
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T61358 |
AKN-028 acetate
|
|
|
|
AKN-028 acetate, a novel tyrosine kinase (TK) inhibitor, is a potent, orally active FMS-like receptor tyrosine kinase 3 (FLT3) inhibitor with an IC 50 value of 6 nM. AKN-028 acetate inhibits FLT3 autophosphorylation. AKN... |
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T37468 |
Siamycin I
|
|
|
|
Siamycin I is a tricyclic peptide originally isolated from Streptomyces and has antiviral and antibacterial activities. It is active against laboratory strains and clinical isolates of HIV-1 (ED50s = 0.05-0.45 and 0.89-5... |
|
T63630 |
Gefitinib dihydrochloride
|
|
|
|
Gefitinib dihydrochloride is a potent, selective, orally active EGFR tyrosine kinase inhibitor (IC50: 33 nM). Gefitinib dihydrochloride selectively inhibits EGF-stimulated tumor cell growth with an IC50 value of 54 nM an... |
|
T69682 |
AEW541 HCl
|
|
|
|
AEW541, also known as NVP-AEW541, is a novel, potent IGF-IR kinase inhibitor. NVP-AEW541 is capable of distinguishing between the IGF-IR (IC50 = 0.086 microM) and the closely related InsR (IC50 = 2.3 microM) in cells. NV... |
|
T35915 |
Erlotinib-13C6
|
Erlotinib-13C6 |
|
|
Erlotinib-13C6 (CP-358774-13C6) is a 13C-labeled Erlotinib. Erlotinib is a directly acting EGFR tyrosine kinase inhibitor, with an IC50 of 2 nM for human EGFR[1].
Erlotinib reduces EGFR autophosphorylation in intact tumo... |
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T67442 |
CGP-53716
|
|
|
|
The growth factors, platelet-derived growth factor (PDGF) and basic fibroblast growth factor (bFGF) play major roles in enhanced smooth muscle cells growth in rodent blood vessels after vascular injury. Tyrosine kinase i... |
