| DC45187 |
(E)-Osmundacetone |
(E)-Osmundacetone is the isomer of Osmundacetone. Osmundacetone significantly suppresses the phosphorylation of MAPKs, including JNK, ERK, and p38 kinases. Osmundacetone has a neuroprotective effect against oxidative stress. |
|
| DC45326 |
CCG-100602
Featured
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CCG-100602 is a specific inhibitor of myocardin-related transcription factor A/serum response factor (MRTF-A/SRF) signaling. CCG-100602 specifically block MRTF-A nuclear localization and thus inhibit the fibrogenic transcription factor SRF. |
|
| DC45363 |
Andrograpanin |
Andrograpanin, a bioactive compound from Andrographis paniculata, exhibits anti-inflammatory and anti-infectious properties. |
|
| DC45688 |
Atrovastatin-PEG3-FITC
Featured
|
Atrovastatin-PEG3-FITC (compound S31) is a KRAS-PDEδ interaction inhibitor. Atrovastatin-PEG3-FITC acts as a ligand in fluorescence anisotropy assay. |
|
| DC45689 |
SAH-SOS1A TFA |
SAH-SOS1A TFA is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A TFA binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC50=106-175 nM), directly and independently blocks nucleotide association, impairs KRAS-driven cancer cell viability, and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS. |
|
| DC45946 |
Gypenoside L |
Gypenoside L is a saponin that can be found in Gynostemma pentaphyllum. Gypenoside L increases the SA-β-galactosidase activity, promotes the production of senescence-associated secretory cytokines. Gypenoside L also can activate p38 and ERK MAPK pathways and NF-κB pathway to induce senescence. Gypenoside L exhibits anti-tumor and anti-inflammatory activities. |
|
| DC46410 |
StRIP16 |
StRIP16, bioavailable StRIP3 analogue, is a double-stapled peptide which can bind to Rab8a GTPase, with a Kd of 12.7 μM. |
|
| DC46476 |
JTP10-△-TATi TFA |
JTP10-△-TATi TFA is a selective JNK2 peptide inhibitor, with an IC50 of 92 nM, exhibiting 10-fold selectivity for JNK2 over JNK1 and JNK3. |
|
| DC46479 |
AMG-548 hydrochloride |
AMG-548 hydrochloride, an orally active and selective p38α inhibitor (Ki=0.5 nM), shows slightly selective over p38β (Ki=36 nM) and >1000 fold selective against p38γ and p38δ. AMG-548 hydrochloride is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM). AMG-548 hydrochloride inhibits Wnt signaling by directly inhibiting Casein kinase 1 isoforms δ and ε. |
|
| DC46921 |
HPK1-IN-7
Featured
|
HPK1-IN-7 is a potent, orally active HPK1 (hematopoietic progenitor kinase 1, MAP4K1) inhibitor (IC50=2.6 nM) with excellent family and kinome selectivity. HPK1-IN-7 shows selectivity against IRAK4 (59 nM) and GLK (140 nM). HPK1-IN-7 shows robust efficacy against MC38 syngeneic tumor model in combination with anti-PD1. |
|
| DC46922 |
CC-99677
Featured
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CC-99677 is a potent, covalent, and irreversible inhibitor of the mitogen-activated protein (MAP) kinase-activated protein kinase-2 (MK2) pathway in both biochemical (IC50=156.3 nM) and cell based assays (EC50=89 nM). |
|
| DC46923 |
SKF-86002 dihydrochloride |
SKF-86002 dihydrochloride is an orally active p38 MAPK inhibitor, with anti-inflammatory, anti-arthritic and analgesic activities. SKF-86002 dihydrochloride inhibits lipopolysaccharide (LPS)-stimulate human monocyte IL-1 and TNF-α production (IC50 = 1 μM). SKF-86002 dihydrochloride inhibits lipoxygenase- and cyclooxygenase-mediated metabolism of arachidonic acid. |
|
| DC46924 |
MRTX849 acid |
MRTX849 acid, a derivative of MRTX849, can be used in the synthesis of PROTAC LC-2. LC-2 is a potent and first-in-class PROTAC capable of degrading endogenous KRAS G12C (DC50s between 0.25 and 0.76 μM).
|
|
| DC47035 |
Edaxeterkib |
Edaxeterkib is a potent extracellular signal-regulated kinase (ERK) inhibitor for the research of cancer. |
|
| DC47125 |
PKA-IN-1 |
PKA-IN-1 is a potent and selective cyclic AMP-dependent protein kinase (PKA) catalytic subunit (cAK) inhibitor with an IC50 of 0.03 μM. |
|
| DC47164 |
8-CPT-Cyclic AMP sodium |
8-CPT-Cyclic AMP (8-CPT-cAMP) sodium is a selective activator of cyclic AMP-dependent protein kinase (PKA). 8-CPT-Cyclic AMP sodium is also a potent inhibitor of the cyclic GMP-specific phosphodiesterase (PDE VA) with an IC50 of 0.9 μM. 8-CPT-Cyclic AMP sodium also inhibits PDE III and PDE IV with IC50Epac and is a potent Epac activator. |
|
| DC47181 |
MRTX1133 formic |
MRTX1133 is a highly selective, first-in-class inhibitor of KRAS G12D. MRTX1133 targets the KRAS G12D protein in both active and inactive states. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells. |
|
| DC47210 |
JDQ-443
Featured
|
JDQ443 (example 1a) is a covalent KRAS G12C inhibitor (extracted from patent WO2021120890A1). |
|
| DC47260 |
Zunsemetinib
Featured
|
Zunsemetinib (CDD-450) is an orally active and selective p38α mitogen-activated protein kinase-activated protein kinase 2 (MK2) pathway inhibitor. Zunsemetinib can be used for the research of immuno-inflammatory diseases. |
|
| DC47263 |
Zapnometinib |
Zapnometinib (PD0184264), an active metabolite of CI-1040, is a MEK inhibitor, with an IC50 of 5.7 nM. Zapnometinib exhibits antiviral activity against influenza virus and antibacterial activities. |
|
| DC47347 |
RSK4-IN-1 |
RSK4-IN-1 is identified with potent RSK4 inhibitory activity with an IC50 value of 9.5 nM. |
|
| DC47351 |
ASP2453
Featured
|
ASP2453 is a potent, selective and covalent KRAS G12C inhibitor. ASP2453 inhibits the Son of Sevenless (SOS)-mediated interaction between KRAS G12C and Raf with an IC50 value of 40 nM. |
|
| DC47352 |
KRAS mutant protein inhibitor 1 |
KRAS mutant protein inhibitor 1 is a KRAS mutant protein inhibitor for potential treatment in cancer. |
|
| DC47353 |
KRAS G12C inhibitor 18 |
KRAS G12C inhibitor 18 is a potent and orally active KRAS G12C inhibitor. Anti-tumor activities. |
|
| DC47354 |
RTIL 13 |
RTIL 13 is a potent inhibitor of dynamin GTPase, with an IC50 of 2.3 µM for dynamin I GTPase. RTIL 13 also targets pleckstrin homology lipid binding domain. RTIL 13 can inhibit receptor-mediated and synaptic vesicle endocytosis, with IC50s of 9.3 μM and 7.1 μM, respectively. |
|
| DC47355 |
RM-018 |
RM-018 is a potent, functionally distinct tricomplex KRASG12C active-state inhibitor. RM-018 retains the ability to bind and inhibit KRASG12C/Y96D and could overcome resistance. RM-018 binds specifically to the GTP-bound, active [“RAS(ON)”] state of KRASG12C. |
|
| DC47411 |
Anti-inflammatory agent 7 |
Anti-inflammatory agent 7 inhibits proinflammatory cytokines by blocking the NF-κB/MAPK signaling pathway in LPS-treated RAW 264.7 cells as well as mice. |
|
| DC47567 |
MNK1/2-IN-5 |
MNK1/2-IN-5 is a potent and selective MNK1/2 inhibitor as a therapeutic agent. |
|
| DC47569 |
MLKL-IN-1 |
MLKL-IN-1 is a covalent MLKL inhibitor with a KD of 50 μM. |
|
| DC47574 |
MEK4 inhibitor-1 |
MEK4 inhibitor-1 is a novel MEK4 inhibitor against pancreatic adenocarcinoma with an IC50 value of 61 nM. |
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