KCNQ2/3 activator-1 is an activator of Kv7.2/Kv7.3 (KCNQ2/3) potassium channel. KCNQ2/3 activator-1 has the potential in relieving pain (the main problem from medical treatment) (extracted from patent WO2021113757A1, compound A)[1].
HPK1-IN-24 (example 51) is a hematopoietic progenitor kinase 1 (HPK1) inhibitor with a Ki of 100 nM. HPK1-IN-24 has the potential for cancer research[1].
GBD-9 is a double-mechanism degrader that efficiently degrades BTK and GSPT1 by recruiting the E3 ligase cereblon (CRBN). GBD-9 acts both as a PROTAC molecule to induce the degradation of BTK and as a molecular glue to degrade GSPT1. GBD-9 effectively inhibits cancer cell growth[1].
KRCA-0008 is a potent and selective ALK/Ack1 inhibitor with IC50 of 12 nM/4 nM for ALK and Ack1 respectively; displays drug-like properties without hERG liability.IC50 value: 12 nM/4 nM(ALK/Ack1) [1]Target: ALK/Ack1 inhibitorKRCA-0008 retains good drug-like properties: good water-solubility (54 μM in 5% DMSO–water, 150 μM in 5% DMSO–PBS buffer) with moderate plasma protein binding (93% in rat) and low brain exposure (Cbrain/Cplasma = ～0.02). It has good liver microsomal stability (% remaining after 30 min: 52% in mouse, 89% in rat, 72% in human) and little to no CYP inhibition (1A2, 2C9, 2D6, 3A4 @ 10 μM). It does not appear to cause hERG blockade (patch clamp IC50 = 30 μM) and is negative on Ames test (1000 μg/plate), chromosomal aberration assay and micronucleus assay.KRCA-0008 also shows promising pharmacokinetic parameters in both mice and rat (oral bioavailability = 66–94.5%). KRCA-0008 shows a modest tumor growth inhibition in vivo activity in H3122 human lung cancer bearing mice model comparable to Crizotinib without significant body weight change. It is important to mention the KRCA-0008 25 mpk and 50 mpk groups did not show dose-dependent tumor growth inhibition.
Proglumide hemicalcium is a nonpeptide and orally active cholecystokinin (CCK)-A/B receptors antagonist. Proglumide hemicalcium selective blocks CCK’s effects in the central nervous system (CNS). Proglumide hemicalcium has ability to inhibit gastric secretion and to protect the gastroduodenal mucosa. Proglumide hemicalcium also has antiepileptic and antioxidant activities[1][2][3][4][5].
AZD2932 is a potent and multi-targeted kinase inhibitor VEGFR2, PDGFβ, Flt-3 and c-Kit with IC50s of 8, 4, 7 and 9 nM in cell assay, respectively.
VER-50589 is a Hsp90 inhibitor, with an IC50 of 21 nM and a Kd of 4.5 nM.
Physagulide J is a kind of withanolides compound that can be isolated from Physalis angulata L.. Many kinds of active ingredients of Physalis angulata L. shows anti-inflammatory and anti-tumor activity[1].
Sesamol is a constituent of sesame oil. Sesamol shows a free radical scavenging activity. Sesamol shows an IC50=5.95±0.56 μg/mL in the DPPH assay. Anti-oxidant activities[1]. Anticancer activities[2].
Boc-Aminooxy-PEG4-azide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
DC41-SMe is a DC1 derivative, shows cytotoxicity in Ramos, Namalwa, and HL60/s cells with IC50s ranging from 18-25 pM. DC1, a simplified analogue of CC-1065, is an antibody conjugate of cytotoxic DNA alkylators for the targeted treatment of cancer[1][2].
Withaphysalin R (compound 5) is a Withanolide that can be isolated from the Solanaceae. Withanolide is a steroid ester with an ergosterol skeleton, and some of these compounds have some significant activities, including cytotoxic and immunosuppressive, antitumor, anti-inflammatory, anticonvulsive, and antioxidant[1].
NSC 694621 is a potent PCAF inhibitor, with an IC50 of 5.71 µM (PCAF/H31-21). NSC 694621 exhibits good activity of inhibiting the proliferation of cancer cells[1].
sEH/AChE-IN-4 (compound (+)-15) is a potent and BBB-penetrated dual inhibitor of sEH (soluble epoxide hydrolase) and AChE (acetylcholinesterase), with IC50 values of 3.1 nM (hsEH), 1660 nM (hAChE), 179 nM (hBChE, human butyrylcholinesterase), 14.5 nM (msEH), and 102 nM (mAChE), respectively[1].
Ipatasertib dihydrochloride (GDC-0068 dihydrochloride) is a highly selective pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 5/18/8 nM, 620-fold selectivity over PKA.
https://pubmed.ncbi.nlm.nih.gov/1624543/
KWAR23 is an anti-human SIRPα antibody. KWAR23 binds human SIRPα with high affinity and disrupts its binding to CD47. KWAR23 shows antitumor activity in combination with tumor-opsonizing antibodies and can be used in cancer immunotherapy research[1].
CL67 is a potent hypoxia-inducible factor (HIF) pathway inhibitor. CL67 interferes G-quadruplex structures within promoter sequences. CL67 can be used in research of renal cancer[1].
S07-2005 racemic is a potent and selective aldo-keto reductase 1C3 (AKR1C3) inhibitor with an IC50 value of 0.13 μM and 0.75 μM for AKR1C3 and AKR1C4, respectively. S07-2005 racemic has potential as a chemotherapeutic potentiator for cancer drug resistance[1].
PROTAC SMARCA2 degrader-2 is a potent and selective SMARCA2/4 PROTAC degrader with an IC50 of <0.1 μΜ in HeLa HiBiT assay. PROTAC SMARCA2 degrader-2 is extracted from patent WO2023287787A1 and has the potential for SMARCA4-related or deficient cancer research[1].
Mps1-IN-1 is a potent, selective and ATP-competitive Mps1 kinase inhibitor, with an IC50 and a Kd of 367 nM and 27 nM.
Ro-3306 is a potent and selective inhibitor of CDK1, with Kis of 20 nM, 35 nM and 340 nM for CDK1, CDK1/cyclin B1 and CDK2/cyclin E, respectively.
Telratolimod is a toll like receptors 7/8 (TLR7/8) agonist, with antitumor activity.
NCGC00029283 is a werner syndrome helicase-nuclease (WRN) helicase inhibitor with IC50s of 2.3 μM, 12.5 μM, and 3.4 μM for WRN, BLM and FANCJ helicase, respectively[1].
LY2603618 is a potent and selective inhibitor of Chk1 with an IC50 of 7 nM.
Tarlatamab (AMG-757) is a bispecific T-cell engager (BiTE) antibody targeting delta-like ligand 3 (DLL3). DLL3 is a target that is selectively expressed in small-cell lung cancer (SCLC) tumors, but with minimal normal tissue expression. Tarlatamab has the KDs of 0.64 nM and 0.50 nM for human and nonhuman primate (NHP) DLL3, respectively. Tarlatamab has the KDs of 14.9 nM and 12 nM for human and NHP CD3, respectively. Tarlatamab is a first-in-class HLE BiTE immuno-oncology therapy targeting DLL3 and has the potential for SCLC research[1].
N-Desmethyl Apalutamide is an active metabolite of Apalutamide. N-Desmethyl Apalutamide is a less potent antagonist of the androgen receptor and is responsible for one-third of the activity of Apalutamide. The formation of N-Desmethyl Apalutamide mediated predominantly by CYP2C8 and CYP3A4. N-Desmethyl Apalutamide is moderate to strong CYP3A4 and CYP2B6 inducer and has an excellent plasma-proteins bound concentration[1][2][3].
Dimethylenastron is a potent Eg5 inhibitor, with an IC50 of 200 nM.
Osimertinib mesylate (AZD-9291 mesylate) is an irreversible and mutant selective EGFR inhibitor with IC50s of 12 and 1 nM against EGFRL858R and EGFRL858R/T790M, respectively.
E3 ligase Ligand 12 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 12 can be connected to the ligand for protein by a linker to form PROTACs or SNIPERs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins[1].