DC72554 |
PKI(5-22)amide |
PKI(5-22)amide is the active inhibitory fragment of the inhibitor of the cyclic AMP-dependent protein kinase (PKA). PKI(5-22)amide inhibits PKA activation, but fails to attenuate homologous desensitization of CRF1 receptors. |
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DC72741 |
BGB 15025
Featured
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BGB-15025 is a potent and selective HPK1 inhibitor. It is used in the treatment of various cancers. |
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DC72742 |
SB 706504 |
SB 706504 is a potent p38 MAPK inhibitor that inhibits Lipopolysaccharides-stimulated inflammatory gene expression in macrophages in chronic obstructive pulmonary disease (COPD). |
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DC72743 |
Spiclomazine hydrochloride |
Spiclomazine hydrochloride (APY-606) is an antipsychotic and antitumor agent. Spiclomazine hydrochloride inhibits KRas. Spiclomazine hydrochloride induces cancer cell apoptosis. |
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DC72744 |
(S)-JDQ-443 |
(S)-JDQ-443 is an isomer of JDQ-443. JDQ-443 is an orally active, potent, selective, and covalent KRAS G12C inhibitor (extracted from patent WO2021120890A1). JDQ-443 shows antitumor activity. |
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DC72745 |
ARS-2102 |
ARS-2102 is a potent covalent KRAS G12C inhibitor for use in cancer research. |
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DC72783 |
DDO3711 |
DDO3711, a PP5-recruiting phosphatase recruitment chimeras (PHORCs), is formed by connecting a small molecular apoptosis signal-regulated kinase 1 (ASK1) inhibitor to a PP5 activator through a chemical linker. DDO3711 specifically inhibits ASK1 (IC50 =164.1 nM) not ASK2 (IC50>20 μM). DDO3711 significantly dephosphorylates p-ASK1T838 by recruiting PP5 and shows the ASK1-dependent antiproliferative activity. DDO3711 has anti-cancer activity and has the potential for abnormally phosphorylated oncoproteins research. |
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DC72791 |
Sp-cAMPS triethylamine |
Sp-cAMPS triethylamine, a cAMP analog, is potent activator of cAMP-dependent PKA I and PKA II. Sp-cAMPS triethylamine is also a potent, competitive phosphodiesterase (PDE3A) inhibitor with a Ki of 47.6 µM. Sp-cAMPS triethylamine binds the PDE10 GAF domain with an EC50 of 40 μM. |
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DC72792 |
4′-Demethylnobiletin |
4′-Demethylnobiletin is a bioactive metabolite that activates the PKA/ERK/CREB signaling pathway, enhances CRE-mediated transcription in hippocampal neurons, and reverses memory impairment associated with NMDA receptor antagonism by stimulating ERK signaling. |
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DC72793 |
Sp-5,6-DCl-cBIMPS |
Sp-5,6-DCl-cBIMPS is a potent and specific cAMP-dependent protein kinases (cAMP-PK) activator. Sp-5,6-DCl-cBIMPS stimulates insulin release. Sp-5,6-DCl-cBIMPS inhibits U46619-induced activation of Rho, Gq and G12/G13 in platelets. |
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DC72816 |
EB1 |
EB1 is the inhibitor of kinases MNK with IC50s of 0.69 μM (MNK1) and 9.4 μM (MNK2). EB1 selectively inhibits the growth of cancer cells, but not normal cells. EB1 also increases cell apoptosis and suppresses eIF4E phosphorylation. |
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DC74332 |
YL5084 |
YL5084 (YL 5084) is a potent, selective and covalent JNK2/3 inhibitor with IC50 of 70 nM (JNK2), displays selectivity (>30-fold) for JNK2 over JNK1. |
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DC74333 |
BAY-405
Featured
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BAY-405 is a potent and selective MAP4K1 inhibitor with IC50 of 6 nM. BAY-405 potentiates in vitro and in vivo antitumor T-cell reactivity which overcomes the suppression by TGFβ and PGE2. |
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DC74334 |
F389-0746 |
F389-0746 is a potent, selective and orally active MAP4K4 inhibitor with IC50 of 120.7 nM. |
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DC74335 |
MMI-0100 |
MMI-0100 is a cell-permeant peptide inhibitor of MAPKAP kinase 2 (MK2), inhibits MK2 and downstream fibrosis and inflammation. |
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DC74336 |
Darizmetinib
Featured
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Darizmetinib (HRX-0215, HRX0215) is a potent, selective inhibitor of MKK4 (MAP2K4/SEK1), shows potential for promoting liver regeneration or reducing or preventing hepatocyte death. |
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DC74337 |
DK2403 |
DK2403 (DK-2403) is a highly potent, selective and covalent MAP2K7 (MEK7) inhibitor with IC50 of 10 nM, covalently engages the unique Cys218 residue within the active site. |
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DC74338 |
DS03090629 |
DS03090629 is a potent, selective, ATP-competitive and orally available MEK1/2 inhibitor, shows high affinity for the MEK protein regardless of its phosphorylation status (npMEK (inactive) Kd=0.11 nM, and pMEK (active) Kd=0.15 nM). |
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DC74339 |
HRX-0233
Featured
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HRX-0233 (HRX0233) is a potent, selective MAP2K4 (MKK4) inhibitor, HRX-0233 is synergistic with RAS inhibitors in KRAS-mutant cancers. |
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DC74340 |
KZ-001 |
KZ-001 is a highly potent and selective MEK 1/2 inhibitor with IC50 values of 7.4/64 nM, respectively, exhibits greater inhibition against BRAF- and KRAS-mutant tumor cells than AZD6244. |
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DC74341 |
NFX-179
Featured
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NFX-179 (Nedometinib, NFX179) is a potent, specific, topical, metabolically labile MEK1/2 inhibitor with biochemical IC50 of 135 nM (MEK1). |
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DC74342 |
IACS-52825 |
IACS-52825 is a potent, selective dual leucine zipper kinase (DLK, MAP3K12) inhibitor with binding Kd of 1.3 nM, and IC50 of 107 nM in p-c-Jun cell assays. |
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DC74343 |
IKAM-1 |
IKAM-1 (Compound 39-100) is an orally bioavailable, small-molecule IKKβ activation modulator (IKAM) that selectively targets MAP3K1, inhibits TNF-α-induced IKKβ-mediated NF-κB activation in A549 cells with IC50 of 4.7 uM. |
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DC74344 |
KC-130 |
KC-130 (KC130, ZAK inhibitor 8) is a potent, selective and covalent leucine-zipper and sterile-α motif kinase (ZAK) inhibitor with IC50 of 11.5 nM. |
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DC74345 |
TC13172 |
TC13172 (TC 13172) is a highly potent necroptosis inhibitor targeting the mixed lineage kinase domain-like protein (MLKL), inhibits necroptosis with IC50 of 2 nM in TSZ-induced necroptosis assays in HT-29 cells. |
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DC74346 |
DCZ19931 |
DCZ19931 is a novel multi-targeting kinase inhibitor, exhibits anti-angiogenic effects in vitro and inhibits ocular neovascularization in vivo. |
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DC74347 |
NC-p38i NC-37
Featured
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Non-canonical p38α inhibitor NC-37 (NC-p38i NC-37) is a potent, highly selective, non-canonical inhibitor of p38α, inhibits TAB1-induced p38α autophosphorylation in vitro with IC50 of 0.27 uM. |
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DC74348 |
NC-p38i NC-38 |
Non-canonical p38α inhibitor NC-38 (NC-p38i NC-38) is a potent, highly selective, non-canonical inhibitor of p38α, inhibits TAB1-induced p38α autophosphorylation in vitro with IC50 of 0.27 uM. |
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DC74349 |
NuP-3 |
NuP-3 is a potent, selective MAPK13 and MAPK14 inhibitor with IC50 of 7 and 14 nM, respectively. |
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DC74350 |
VCP979 |
VCP979 (VCP-979) is a novel selective small molecule p38 MAPK inhibitor with a significantly greater affinity for the active form of p38 MAPK, has significant anti-fibrotic effects in vitro and in vivo. |
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