Anpirtoline hydrochloride is a hydrochloride of anpirtoline. Anpirtoline is a agonist of 5-HT1B[1].
Ac-Glu-Asp(EDANS)-Lys-Pro-Ile-Leu-Phe-Phe-Arg-Leu-Gly-Lys(DABCYL)-Glu-NH2 is a cathepsin D substrate, that can be used for cathepsin D FRET assay[1].
sEH/AChE-IN-3 (compound (−)-15) is a potent and BBB-penetrated dual inhibitor of sEH (soluble epoxide hydrolase) and AChE (acetylcholinesterase), with IC50 values of 0.4 nM (hsEH), 1.94 nM (hAChE), 615 (hBChE, human butyrylcholinesterase), 4.3 nM (msEH), and 2.61 nM (mAChE), respectively[1].
HPK1-IN-19 is a hematopoietic progenitor kinase 1 (HPK1) inhibitor extracted from patent WO2018102366A1 compound I-47[1].
(2S,3S)-Pterosin C is a natural sesquiterpenoid compound[1].
Endothelin-1 (1-31) (Human) is a potent vasoconstrictor and hypertensive agent. Endothelin-1 (1-31) (Human) is derived from the selective hydrolysis of big ET-1 by chymase[1].
IQTub4P is a potent microtubule (MT) inhibitor. IQTub4P has the cytotoxicity in in HeLa cells, with EC50 of 170 nM. IQTub4P inhibits microtubule structure and function. IQTub4P is well-tolerated in vivo[1].
Eugenitol (Compound 3) is an antifungal metabolite isolated and purified from Diaporthe eucalyptorum. Eugenitol has inhibitory effect on four plant pathogenic fungi (Alternaria solani, Botrytis cinerea, Fusarium solani and Gibberella saubinettii)[1].
Allopregnanolone is a progesterone metabolite. Allopregnanolone is an allosteric modulator of the GABA receptor.
PD-1/PD-L1-IN 5 is a PD-1/PD-L1 protein/protein interaction inhibitor extracted from patent WO2017222976A1, compound Example 1, has an IC50 of ≤100 nM[1].
Tubulin inhibitor 35 (compound 6b) is a dual inhibitor of topoisomerase I (IC50=~50 μM) and tubulin polymerization (IC50=5.69 μM). Tubulin inhibitor 35 inhibits migration and invasion of MGC-803 and RKO cell lines，and induces apoptosis via arresting cell cycle at G2/M phase. Tubulin inhibitor 35 exhibis potent efficacy in gastrointestinal tumor inhibiton (inhibits MGC-803 (IC50=0.09 μM) and RKO (IC50=0.2 μM) cell lines)[1].
Sardomozide is an S-adenosylmethionine decarboxylase (SAMDC) inhibitor with an IC50 of 5 nM.
Decanoyl-RVKR-CMK (DecRVKRcmk) inhibits over-expressed gp160 processing and HIV-1 replication[1].
6RK73 is a covalent irreversible and specific UCHL1 inhibitor with an IC50 of 0.23 µM. 6RK73 shows almost no inhibition of UCHL3 (IC50=236 µM). 6RK73 specifically inhibit UCHL1 activity in breast cancer[1].
SPC-180002 is a SIRT1/3 dual inhibitor, with IC50 values of 1.13 and 5.41 μM, respectively. SPC-180002 disturbs redox homeostasis via ROS generation, which leads to an increase in both p21 protein stability and mitochondrial dysfunction. SPC-180002 strongly inhibits cell cycle progression and cancer cell growth. SPC-180002 activates the Nrf2 signaling pathway[1].
Palmatine hydroxide is an orally active and irreversible indoleamine 2,3-dioxygenase 1 (IDO-1) inhibitor with IC50s of 3 μM and 157μM against HEK 293-hIDO-1 and rhIDO-1, respectively. Palmatine hydroxide can also inhibit West Nile virus (WNV) NS2B-NS3 protease in an uncompetitive manner with an IC50 of 96 μM. Palmatine hydroxide shows anti-cancer, anti-oxidation, anti-inflammatory, neuroprotection, antibacterial, anti-viral activities[1][2][3][4][5].
HDAC-IN-42 (compound 14f) is a potent and selective HDAC inhibitor with IC50 values of 0.19 and 4.98 µM for HDAC1 and HDAC6, respectively. HDAC-IN-42 shows anticancer and anti-proliferative activity. HDAC-IN-42 induces apoptosis and cell cycle arrest at G2/M phase[1].
11-Oxomogroside IIIE is a cucurbitane triterpene glycoside isolated from Lo Han Kuo (Siraitia grosvenori)[1].
PPARα/γ agonist 2 is an orally active PPARα full agonist and PPARγ partial agonist. PPARα/γ agonist 2 activates PPARα and PPARγ with EC50 values of 0.95 μM and 0.91 μM respectively. PPARα/γ agonist 2 is also a PTP1B inhibitor. PPARα/γ agonist 2 is an anti-diabetic agent[1].
FR-167653 is a selective p38 MAPK inhibitor.
SB-334867 free base is a selective non-peptide orexin OX1 receptor antagonist with a pKb value of 7.2.IC50 value: 7.2 (pKb) [1]Target: orexin OX1 receptor in vitro: SB-334867-A inhibited the orexin-A (10 nM) and orexin-B (100 nM)-induced calcium responses (pK(B)=7.27+/-0.04 and 7.23+/-0.03 respectively, n=8), but had no effect on the UTP (3 microM)-induced calcium response in CHO-OX(1) cells. SB-334867-A (10 microM) also inhibited OX(2) mediated calcium responses (32.7+/-1.9% versus orexin-A) [1].in vivo: Single-unit recordings in anesthetized rats demonstrated the central effects of the selective orexin-1 receptor antagonist SB-334867 (2 mg/kg, intravenous), as it reversed the excitatory effects of orexin-A administration (6 microg, intracerebroventricular) on the activity of locus coeruleus (LC) cells [2]. The ICV injection of SB-334867 alone had no effect on the formalin-induced nociceptive behaviors. Pre-treatment with SB-334867 at a dose of 0.5 nmol significantly attenuated the analgesia induced by morphine (at dose 1.5mg/kg of morphine; interphase and phase 2B and at dose 3mg/kg of morphine just phase 2B of formalin test) [3]. Administered alone, SB-334867 (30 mg/kg, but not lower doses) significantly reduced food intake and most active behaviours (eating, grooming, sniffing, locomotion and rearing), while increasing resting. Pretreatment with SB-334867 dose-dependently blocked these effects of orexin-A, with significant antagonism evident at dose levels (3-10 mg/kg) below those required to produce intrinsic behavioural effects under present test conditions in rats [4].Toxicity: Acute systemic treatment with the selective orexin-1 (OX1R) antagonist SB-334867 reduces food intake in rats, an effect associated with an acceleration in behavioural satiety and unrelated to gross behavioural disruption, alterations in palatability, or toxicity.
c-Fms-IN-6 is a potent inhibitor of c-FMS, with an IC50 of ≤10 nM for unphosphorylated c-FMS, also weakly inhibits unphosphorylated c-KIT and PDGFR (IC50, > 1 μM). Used in the research of autoimmune diseases[1].
Galanin (1-29)(rat, mouse) is a non-selective galanin receptor agonist, with Kis of 0.98, 1.48 and 1.47 nM for GAL1, GAL2 and GAL3 respectively. Anticonvulsant effect[1][2].
MK-7145 is a ROMK inhibitor, with an IC50 of 0.045 μM.
Thalidomide-O-amido-C6-NH2 hydrochloride, a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker, can be used in the synthesis of PROTACs[1].
(-)-Zeylenol, isaolated from stems of Uvaria grandiflora, possesses anti-inflammatory and anticancer activities[1].
Tabituximab barzuxetan (OTSA101-DTPA-90Y) is a radioimmunoconjugate composed of a humanized monoclonal antibody targeting FZD-10 (OTSA-101), and labeled with Yttrium 90. Tabituximab barzuxetan shows antineoplastic activity. Tabituximab barzuxetan can be used for synovial sarcoma research[1].
Bevacizumab, as a humanized vascular endothelial growth factor (VEGF) antibody, is a highly effective monoclonal antibody. Bevacizumab can be used for the research of cancer[1][2].
THP-PEG4-Pyrrolidine(N-Boc)-CH2OH is a PEG-based PROTAC linker can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523)[1].
Rubratoxin B is a hepatotoxic mycotoxin that can be found in Penicillium rubrum Stoll. Rubratoxin B shows antitumor activity[1][2].