Niraparib R-enantiomer (MK-4827 R-enantiomer) is an excellent PARP1 inhibitor with IC50 of 2.4 nM.
RET-IN-21 is an inhibitor of receptor tyrosine kinase (RET), with the IC50 of 4.4 μM, that has antitumor activity[1].
G3-C12 is a galectin-3 binding peptide, with Kd of 88 nM, and shows anticancer activity.
HER2-IN-14 (Compound 34) is an HER2 inhibitor with an IC50 of 18 nM. HER2-IN-14 also inhibits wt-EGFR with an IC50 of 6.3 μM[1].
AT13148 is an orally active and ATP-competitive, multi-AGC kinase inhibitor with IC50s of 38 nM/402 nM/50 nM, 8 nM, 3 nM, and 6 nM/4 nM for Akt1/2/3, p70S6K, PKA, and ROCKI/II, respectively.
GNE-886 is a potent and selective CECR2 bromodomain inhibitor with IC50 of 16 nM; shows a wide selectivity over the 40 bromodomains, >100-fold selectivity over BRD9, BRD7, TAF1(2), and BRD4(1); has a highly favorable measured kinetic solubility of 122 uM and is an appropriate in vitro tool compound for the CECR2 bromodomain.
ATG7-IN-1 is a potent and selective inhibitor of ATG7 (IC50 = 62 nM).
OICR-0547 is a closely related derivative of OICR-9429. OICR-942 is a novel small-molecule antagonist of the Wdr5-MLL interaction, while OICR-0547 cannot bind to WDR5.
22-(tert-Butoxy)-22-oxodocosanoic acid is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). 22-(tert-Butoxy)-22-oxodocosanoic acid is also a alkyl chain-based PROTAC linker that can be used in t
GNE-493 is a potent, selective, and orally available dual pan-PI3-kinase/mTOR inhibitor with IC50s of 3.4 nM, 12 nM, 16 nM, 16 nM and 32 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ and mTOR.
VS 8 (Compound VS 8) is a potent, orally active VEGFR-2 inhibitor with significant anti-angiogenic effects. VS 8 induces cancer cell apoptosis and migration. VS 8 is active against CSCs (Cancer stem cells)[1].
3-(3-Phenoxybenzyl)amino-β-carboline is a potent tubulin inhibitor. 3-(3-Phenoxybenzyl)amino-β-carboline promotes selective degradation of αβ-tubulin heterodimers. 3-(3-Phenoxybenzyl)amino-β-carboline induces G2/M phase cell cycle arrest and apoptosis. 3-(3-Phenoxybenzyl)amino-β-carboline exhibits anticancer activity[1].
Koenimbine is an anticancer agent that can be obtained from the leaves and fruits of Murraya koenigii. Koenimbine can induce apoptosis and necrosis in HT-29 and SW48 cells. Koenimbine can be used in the research of cancer[1].
(-)-Irofulven (MGI 114), an Illudin S analog, is a DNA alkylating agent. (-)-Irofulven inhibits the replication of DNA, induces tumor cells apoptosis, and has potent antitumor activity[1][2].
2’,5’-Dideoxyuridine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
GNE-900 is a an ATP-competitive, selective, and orally active ChK1 inhibitor with IC50s of 0.0011, 1.5 µM for ChKl, ChK2, respectively. GNE-900 abrogates the G2-M checkpoint, enhances DNA damage, and induces Apoptosis. gemcitabine (HY-17026) and GNE-900 administration shows anti-tumor activity[1].
IACS-9439 is a potent, selective, and orally active CSF1R inhibitor with a Ki value of 1 nM inhibitor. IACS-9439 can be used for advanced solid tumors research[1].
Calyxin B can be extracted from the seeds of Alpinia blepharocalyx. Calyxin B has anti-proliferative activity and can be used in cancer research[1].
GSK'481 can inhibit RIP1 WT S166 phosphorylation in human vs mouse plasmids overexpressed in HEK293T cellsGSK'481 have approximately equivalent RIP1 FP potencies against human andcynomolgus monkey RIP1 but was >100-fold less potent against nonprimate RIP1
Fucosterol is isolated from E. stolonifera with anti-adipogenic, anti-diabetic and anti-cancer activities. Fucosterol regulates adipogenesis via modulation of PPARαand C/EBPαexpression.
20(R)-Ginsenoside Rh2, a matrix metalloproteinase (MMP) inhibitor, acts as a cell antiproliferator. It has anticancer effects via blocking cell proliferation and causing G1 phase arrest. 20(R)-Ginsenoside Rh2 induces apoptosis, and has anti-inflammatory and antioxidative activity[1][2][3].
Leu-AMS is a potent inhibitor of leucyl-tRNA synthetase (LRS) with an IC50 of 22.34 nM and inhibits the growth of bacteria.
CDK12-IN-5, a pyrazolotriazine, is a potent CDK12 inhibitor with an IC50 of 23.9 nM at high ATP (2 mM). CDK12-IN-5 has no effect on CDK2/Cyclin E (IC50=173 μM) and CDK9/Cyclin T1 (IC50=127 μM) at high ATP (2 mM) (WO2021116178A1)[1].
HDAC-IN-56 ((S)-17b) is an orally active class I histone deacetylase (HDAC) inhibitor with IC50 values of 56.0 ± 6.0, 90.0 ± 5.9, 422.2 ± 105.1, >10000 nM for HDAC1, HDAC2, HDAC3, and HDAC4-11, respectively. HDAC-IN-56 has potent inhibitory activity while strongly increasing intracellular levels of acetylhistone H3 and P21 and effectively inducing G1 cell cycle arrest and apoptosis.HDAC-IN-56 has antitumor activity [1].
PROTAC ER Degrader-3 is an intermediate for synthesis of PAC. PAC comprises an antibody conjugated via a linker to a PROTAC. PAC extracts from patent WO2017201449A1, compound LP2. PAC is a more marked estrogen receptor-alpha (ERα) degrader compared to PROTAC (without Ab).
3'-O-Acetylhamaudol, isolated from Angelica japonica roots, exhibits anti-tumor activity through dual actions, anti-angiogenesis and intestinal intraepithelial lymphocyte activation[1].
Multi-kinase-IN-2 (compound 7h) is an orally active and potent angiokinase inhibitor. Multi-kinase-IN-2 exhibits excellent inhibitory activity against angiokinases including VEGFR-1/2/3, PDGFRα/β, and FGFR-1, as well as LYN and c-KIT kinases. Multi-kinase-IN-2 significantly attenuates phosphorylation of AKT and ERK proteins. Multi-kinase-IN-2 induces cell apoptosis. Multi-kinase-IN-2 shows anticancer activity[1].
A potent PD-1/PD-L1 interaction inhibitor with IC50 of 2.25 nM in a homogenous time-resolved fluorescence binding assay.
IQ 1 has many functions such as decreasing Wnt-stimulated phosphorylation, maintaining the pluripotency of murine ESCs, preventing PP2A/Nkd interaction and so on.IQ 1 maintains the pluripotency of murine ESCs in long-term culture in a Wnt-dependent manner. IQ 1 decreased Wnt-stimulated phosphorylation of p300 at Ser-89.IQ-1 binds to serine/threonine phosphatase PP2A and prevents PP2A/Nkd interaction.The binding of IQ 1 to PR72/130 leads to decreased phosphorylation of the coactivator protein p300 at Ser-89. IQ 1 thereby diminishes the β-catenin/p300 interaction and prevents β-catenin coactivator switching from CBP to p300.
CUDC-101 is a potent inhibitor of HDAC, EGFR, and HER2 with IC50s of 4.4, 2.4, and 15.7 nM, respectively.