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Ca2+ channel agonist/CDK2 inhibitor
Ca2+ channel agonist 1 is an agonist of N-type Ca2+ channel and an inhibitor of Cdk2, with EC50s of 14.23 μM and 3.34 μM, respectively, and is used as a potential treatment for motor nerve terminal dysfunction. -
Cdc42 GTPase inhibitor
ZCL-278 is a selective inhibitor of Cdc42. Targets the binding site of the Cdc42 guanine nucleotide exchange factor, intersectin (ITSN). Inhibits Cdc42-mediated cellular effects, including microspike formation in 3T3 fibroblasts and neuronal branching in primary neonatal cortical neurons. Also suppresses cell motility and migration in PC3 cells, without cytotoxic effects. -
CDK/JAK2/FLT3 inhibitor
SB1317 is a potent inhibitor of Cyclin dependent kinases (CDKs), FMS-like tyrosine kinase-3 (FLT3) and Janus kinase 2 (JAK2) with IC50 values of 13nM, 56nM and 73nM for CDK2, JAK2 and FLT3, respectively. -
Cdc25 inhibitor
NSC 663284 is a potent, cell-permeable, and irreversible inhibitor of all Cdc25 isoforms, with preference for Cdc25A (IC50 = 29, 95, and 89 nM for Cdc25A, Cdc25B2, and Cdc25C, respectively). -
Aurora kinase A inhibitor
TC-A-2317 hydrochloride is a potent Aurora kinase A inhibitor (Ki = 1.2 nM compared to 101 nM for inhibition of Aurora kinase B). Selective over 60 other kinases (IC50 values > 1000 nM). Exhibits good cell permeability and antitumor activity. -
ROCK inhibitor
Glycyl-H 1152 2HCl is a selective and potent ROCK inhibitor (IC50 values are 0.0118, 2.35, 2.57, 3.26, > 10 and >10 uM for ROCKII, Aurora A, CAMKII, PKG, PKA and PKC respectively.) -
PDE-KRAS inhibitor
Deltarasin is a novel small molecule inhibiting the KRAS PDEδ interaction and thus impairing oncogenic KRAS signalling. -
ROCK Inhibitor
HA-1077 inhibits vascular smooth muscle contraction by acting as an intracellular Ca2+ antagonist. -
Rac GTPase inhibitor
NSC 23766 is a cell-permeable, reversible inhibitor of Rac1 activation by the Rac-specific GEFs TrioN and Tiam 1 (IC50 = 50 uM). -
Aurora A/B inhibitor
SCH-1473759 is a novel sub-nanomolar Aurora A/B inhibitor with IC50 of 4 nM and 13 nM, respectively. -
K-Ras(G12C) inhibitor
K-Ras(G12C) inhibitor 6 is an irreversible inhibitor of oncogenic K-Ras(G12C), subverting the native nucleotide preference to favour GDP over GTP. -
K-Ras(G12C) inhibitor
K-Ras(G12C) inhibitor 12 is an allosteric inhibitor of oncogenic K-Ras(G12C). -
K-Ras inhibitor
6H05 is a selective, and allosteric inhibitor of oncogenic K-Ras(G12C). -
K-Ras(G12C) inhibitor
K-Ras(G12C) inhibitor 9 is an allosteric inhibitor of oncogenic K-Ras(G12C). -
BMI-1 inhibitor
PTC-209 HBr is the hydrobromide salt of PTC-209. PTC-209 is a potent and selective BMI-1 inhibitor with IC50 of 0.5 μM in HEK293T cell line, and results in irreversible reduction of cancer-initiating cells (CICs).
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Aurora Kinase inhibitor
SAR156497 is an exquisitely selective Aurora A, B, and C inhibitor with in vitro and in vivo efficacy with IC50 = 0.5 nM (Aurora A), 1 nM (Aurora B / incenp), 3 nM (Aurora C / incenp) respectively SAR156497 combines high in vitro potency with satisfactory metabolic stability and limited CYP3A4 and PDE3 inhibition. -
CDK inhibitor
Voruciclib is a flavone and cyclin dependent kinase (CDK) inhibitor with potential antineoplastic activity. -
PLK inhibitor
SBE 13 HCl is a selective inhibitor of PLK1 (IC50 values are 200 pM, 875 nM and 66 μM for PLK1, PLK3 and PLK2 respectively). -
CDK4/6 inhibitor
Trilaciclib is a potential first-in-class short-acting CDK4/6 inhibitor in development to preserve hematopoietic stem cells and enhance immune system function during chemotherapy. -
CDK8 inhibitor
SEL120-34A is a potent and selective CDK8 inhibitor active in AML cells with high levels of serine phosphorylation of STAT1 and STAT5 transactivation domains. -
c-Myc Inhibitor
10074-G5 is a c-Myc inhibitor by inhibiting c-Myc/Max heterodimer formation and inhibiting its transcriptional activity with IC50 value of 146 μM. 10074-G5 binds to and distorts the bHLH-ZIP domain of c-Myc, thereby inhibiting c-Myc/Max heterodimer formation and inhibiting its transcriptional activity. 10074-G5 is capable of binding and sequestering the intrinsically disordered amyloid-β (Aβ) peptide in its monomeric, soluble state. Our analysis reveals that this compound interacts with Aβ and inhibits both the primary and secondary nucleation pathways in its aggregation process.
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Ras inhibitor
Antineoplaston A 10 is a Ras inhibitor potentially for the treatment of glioma, lymphoma, astrocytoma and breast cancer. -
pan-RAS inhibitor
Ras-IN-3144 is a pan-RAS inhibitor which inhibits RAS signaling pathways in cancer cells and prevents the growth of RAS mutant mouse cancer xenografts.

