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IGF-1R, Aurora, FGFR, ABL, SRC inhibitor
XL228 is a protein kinase inhibitor targeting IGF1R, the AURORA kinases, FGFR1-3, ABL and SRC family kinases. XL228 is an Aurora A inhibitor (IC50, f3 nmol/L) that has shown potent biochemical activity against ABL1 (Ki, 5 nmol/L), as well as the BCR-ABL1 T315I (Ki, 1.4 nmol/L) kinases. -
Chk2, KDR, FGFR, Aurora A & Cdk2 inhibitor
R1530 is a pyrazolobenzodiazepine small molecule with potential antiangiogenesis and antineoplastic activities. R1530 is also a mitosis-angiogenesis inhibitor (MAI) that inhibits multiple receptor tyrosine kinases involved in angiogenesis, such as vascular endothelial growth factor receptor (VEGFR)-1, -2, -3, platelet-derived growth factor receptor (PDGFR) beta? FMS-like tyrosine kinase (Flt)-3, and fibroblast growth factor receptor (FGFR) -1, -2.- Vijaya Bharti, .et al. , Cell Rep, 2022, Dec 20;41(12):111826 PMID: 36543138
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Ras/Raf/MEK inhibitor
Balamapimod, also known as MKI-822, is a Ras/Raf/MEK inhibitor. -
CDK inhibitor
RGB-286638 is a novel CDK inhibitor with IC50s of 1 nM/2 nM/3 nM/4 nM/5 nM for cyclin T1-CDK9/cyclin B1-CDK1/cyclin E-CDK2/cyclin D1-CDK4/cyclin E-CDK3/p35-CDK5 respectively; less potent against cyclin H-CDK7 and cyclin D3-CDK6. -
Kras-G12C inhibitor 1
KRas G12C inhibitor 1 is a compound that inhibits KRas G12C, extracted from patent US 20180072723 A1. -
RAD51 Inhibitor II
RI-1 is a small molecule that inhibits the central recombination protein RAD51. RI-1 specifically reduces gene conversion in human cells while stimulating single strand annealing. RI-1 binds covalently to the surface of RAD51 protein at cysteine 319 that likely destabilizes an interface used by RAD51 monomers to oligomerize into filaments on DNA. -
human A3 adenosine receptor antagonist /Aurora inhibitor
Reversine is a potent human A3 adenosine receptor antagonist with Ki of 0.66 μM, and a pan-aurora A/B/C kinase inhibitor with IC50 of 12 nM/13 nM/20 nM, respectively. Also used for stem cell dedifferentiation.- Amy H. Ide, .et al. , Mol Biol Cell, 2023, Jun 1;34(7):ar76 PMID: 37126397
- Hazheen K, .et al. , J Biol Chem, 2020, August 20
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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). -
CDK4/6 inhibitor
LEE011 is an orally available cyclin-dependent kinase (CDK) inhibitor targeting cyclin D1/CDK4 and cyclin D3/CDK6 cell cycle pathway, with potential antineoplastic activity.- Federico Antoniciello, .et al. , Front Mol Biosci, 2023, May 11;9:887564 PMID: 35647033
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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.) -
CDK inhibitor
BMS-863233, also known as XL-413, is an orally bioavailable cell division cycle 7 homolog (CDC7) kinase inhibitor with potential antineoplastic activity.- Gijs Zonderland, .et al. , Mol Cell, 2022, Sep 15;82(18):3350-3365 PMID: 36049481
- Wang C, .et al. , Nature, 2019, Oct 2 PMID: 31578521
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Chk1 inhibitor
LY2606368 is an inhibitor of checkpoint kinase 1 (chk1) with potential antineoplastic activity.- Yuri Tozaki, .et al. , Cancers (Basel), 2023, Jan 25;15(3):735 PMID: 36765693
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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. -
CDK4/6 inhibitor
PD 0332991 Isethionate is a highly selective inhibitor of CDK4/6 with IC50 of 11 nM/16 nM respectively. -
Rac family GTPase inhibitor
EHT 1864 is an antiproliferative chemical shown to inhibit Rac family GTPases.- Natalie J Jooss, .et al. , J Thromb Haemost, 2023, Aug;21(8):2260-2267 PMID: 37150294
- Kakoki M, .et al. , JCI Insight, 2019, Jun 20;4(12) PMID: 31217360
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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. -
CDK7 Inhibitor
THZ1 is a novel selective and potent covalent CDK7 inhibitor with IC50(binding affinity) of 3.2 nM; inhibits Jurkat cell's proliferation with IC50 of 50 nM- Guowang Li, .et al. , Life Sci Alliance, 2023, Apr 3;6(6):e202201854 PMID: 37012048
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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.