Gilvetmab is a potent caninized antiPD-1 monoclonal antibody. gilvetmab blocks the interaction between PD-1 and its ligand PDL-1[1].
MKC9989 is a Hydroxy aryl aldehydes (HAA) inhibitor and also inhibits IRE1α with an IC50 of 0.23 to 44 μM.
Bafetinib is a Lyn and Bcr-Abl tyrosine kinase inhibitor with potential antineoplastic activity.
NSC-658497 is an effective inhibitor of Ras-GEF, SOS1. NSC-658497 binds to SOS1, competitively suppresses SOS1-Ras interaction, and dose-dependently inhibits SOS1 GEF activity. NSC-658497 showed dose-dependent efficacy in inhibiting Ras, downstream signaling activities, and associated cell proliferation[1].
6-Chloro-9-(2,3,5-tri-O-benzoyl-2-C-methyl-beta-D-ribofuranosyl)-9H-purine dibenzoate 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].
COH34 is a potent and specific poly(ADP-ribose) glycohydrolase (PARG) inhibitor with an IC50 of 0.37 nM. COH34 binds to the catalytic domain of PARG (Kd=0.547 μM), thereby prolonging PARylation at DNA lesions and trapping DNA repair factors[1].
Cdc7-IN-3 (compound I-A) is a potent Cdc7 kinase inhibitor extracted from patent WO2019165473A1, compound I-B. Cdc7 is a serine-threonine protein kinase enzyme which is essential for the initiation of DNA replication in the cell cycle[1].
5β-Hydroxybufotalin (compound 6) is an anticancer agent that can effectively inhibit the growth activity of cancer cells. 5β-Hydroxybufotalin is also a natural product obtained from the chinese traditional drug Ch'an Su[1].
KRIBB11 is an inhibitor of Heat shock factor 1 (HSF1), with IC50 of 1.2 μM.
erythro-Austrobailignan-6 is an orally active anti-cancer agent. erythro-Austrobailignan-6 inhibits DNA topoisomerase I and II activity. erythro-Austrobailignan-6 induces cell apoptosis and increases phosphorylation of p38 and JNK[1][2].
SirReal2 is a potent, isotype-selective Sirt2 inhibitor with an IC50 value of 140 nM and has very little effect on the activities of Sirt3-5. SirReal2 leads to tubulin hyperacetylation in HeLa cells and induces destabilization of the checkpoint protein BubR1[1].
D5261 is a potent, type III allosteric tropomyosin-related kinase A (TrkA) inhibitor[1].
MI-538 is an inhibitor of the interaction between menin and MLL fusion proteins with an IC50 of 21 nM.
Germanicol is a selective antineoplastic agent against human colon cancer cell lines HCT-116 and HT29 . Germanicol induces apoptosis via chromatin condensation and DNA damage[1].
CCCI-01 is a centrosome clustering inhibitor. CCCI-01 has selective effects on cancer. CCCI-01 can be used for the research of non-cross-resistant anti-cancer agents with blocking centrosome clustering[1].
ATM Inhibitor-5 [formula (1)] is a potent inhibitor of serine/threonine protein kinase ATM (extracted from patent WO2022058351A1)[1].
Telomerase-IN-3 is a telomerase inhibitor, which directly targets hTERT promoter activity. hTERT is the key component for maintenance of telomerase activity[1].
Protopine hydrochloride, an isoquinoline alkaloid, is a specific reversible and competitive inhibitor of acetylcholinesterase. Protopine hydrochloride exhibits anti-inflammation, anti-microbial, anti-angiogenic and anti-tumour activity[1][2].
Manzamine A hydrochloride, an orally active beta-carboline alkaloid, inhibits specifically GSK-3β and CDK-5 with IC50s of 10.2 and 1.5μM, respectively. Manzamine A hydrochloride targets vacuolar ATPases and inhibits autophagy in pancreatic cancer cells. Manzamine A hydrochloride has antimalarial and anticancer activities. Manzamine A hydrochloride also shows potent activity against HSV-1[1][2][3][4].
PAK1-IN-1 is a potent and selective PAK1 inhibitor with an IC50 of 9.8 nM. PAK1-IN-1 inhibits the migration and invasion of PAK1-related tumour cells in a dose-dependent manner[1].
DGKα-IN-6 is a DGKα inhibitor with the IC50 of 1.377 nM, extracted from patent WO2022271650 (compound 143). DGKα-IN-6 has the potential for cancer study.
CB-1158 is a potent and orally bioavailable inhibitor of arginase, with IC50s of 86 and 296 nM for recombinant human arginase 1 and 2, respectively.
Gresonitamab (AMG 910) is a half-life extended (HLE) bispecific T-cell engager (BiTE) antibody targets CD3-positive T cells and CLDN18.2-expressing tumor cells. Gresonitamab can be used for the research of adenocarcinoma[1].
Mcl-1 inhibitor 12 (Example 10) is a MCL-1 inhibitor (Ki: 0.22 nM). Mcl-1 inhibitor 12 can be used for the research of cancers[1].
JSH-23 is an NF-κB inhibitor which inhibits NF-κB transcriptional activity with an IC50 of 7.1 μM.
Fatostatin A is a inhibitor of SREBP that directly binds SCAP and blocks its ER-to-Golgi transport with IC50 of 2.5 and 10 μM in mammalian cellstarget: SREBPIC50: 2.5 ~10 μMIn vitro: Fatostatin A suppress cell proliferation and anchorage-independent colony formation in both androgen-responsive LNCaP and androgen-insensitive C4-2B prostate cancer cells. [1] Fatostatin potently inhibited cell growth.[2]In vivo: Fatostatin A cause G2/M cell cycle arrest and induce apoptosis by increasing caspase-3/7 activity and the cleavages of caspase-3 and PARP. [1] μCT analyses show that fatostatin A treatment preserve bone mass and structure in the proximal tibial trabecular bone in the mouse RANKL-induced bone loss model.[3]
NMS-P118 is a potent, orally available, and highly selective PARP-1 Inhibitor for cancer therapy.
Tyrphostin 25 (AG82) is a specific inhibitor of the EGFR tyrosine kinase. Tyrphostin 25 is also a GPR35 agonist with an IC50 of 0.94 µM and an EC50 of 5.3 µM[1][2].
Uvarigrin, isolated from the roots of Uvaria calamistrata, induces tumor multidrug resistance cell apoptosis and triggers Caspase-9 activation[1][2].
(Z)-Semaxanib (compound (z)-1) is a potent tyrosine kinase inhibitor. (Z)-Semaxanib shows cytotoxicity for TAMH and HepG2 cells with IC50s of 6.28 µM and 8.17 µM, respectively[1].