GW284543 (UNC10225170) is a selective MEK5 inhibitor[1].
PD 113270 (CL 1565-B) is an antitumor agent. PD 113270 exhibits inhibitory effects to yeasts[1].
3F8 is a potent and selective GSK-3β inhibitor that could be useful as new reagent and potential therapeutic candidate for GSK3 related diseases[1].
LSD1-IN-13 (compound 7e) is an orally active and potent LSD1 inhibitor, with an IC50 of 24.43 nM. LSD1-IN-13 can activate CD86 expression, with an EC50 of 470 nM. LSD1-IN-13 induces differentiation of AML (acute myeloid leukemia) cell lines[1].
Btk inhibitor 1 R enantiomer is a pyrazolo[3,4-d]pyrimidine derivative as a Btk kinase inhibitor.IC50 value:Target: BtkFrom PCT Int. Appl. (2012), WO 2012158843 A2 20121122.
Euscaphic acid, a DNA polymerase inhibitor, is a triterpene from the root of the R. alceaefolius Poir. Euscaphic inhibits calf DNA polymerase α (pol α) and rat DNA polymerase β (pol β) with IC50 values of 61 and 108 μM[1]. Euscaphic acid induces apoptosis[2].
MAX-40279 hydrochloride is a dual and potent inhibitor of FLT3 kinase and FGFR kinase. MAX-40279 hydrochloride has the potential for the research of acute myelogenous leukemia (AML) (extracted from patent WO2021180032)[1].
Dendrotoxin-I is a potent K+ channels blocker and targets voltage-gated potassium channel subunits KV1.1 and KV1.2. Dendrotoxin-I is a neurotoxin isolated from thevenom of Dendroaspis snakes[1][2][3].
N-Benzoyl-5'-O-dmtr-2'-O-(2-methoxyethyl)-adenosine is an adenosine analog. Adenosine analogs mostly act as smooth muscle vasodilators and have also been shown to inhibit cancer progression. Its popular products are adenosine phosphate, Acadesine (HY-13417), Clofarabine (HY-A0005), Fludarabine phosphate (HY-B0028) and Vidarabine (HY-B0277)[1].
Azido-PEG1-CH2CO2H is a PROTAC linker, which refers to the alkyl/ether composition. Azido-PEG1-CH2CO2H can be used in the synthesis of PROTAC BRD4 Degrader-1[1].
STAT3-IN-11 (7a) is a selective STAT3 inhibitor that inhibits the phosphorylation of STAT3 at site pTyr705. STAT3-IN-11 inhibits the phosphorylation of downstream genes (Survivin and Mcl-1) without affecting its upstream tyrosine kinases (Src and JAK2) levels and p-STAT1 expression. STAT3-IN-11 can induce cancer cell apoptosis, which is potential for the discovery of effective STAT3 inhibitors and antitumor agents against cancers[1].
Thalidomide-4-NH-PEG1-COOH TFA is an E3 Ligase Ligand-Linker Conjugate consisting of Thalidomide (HY-14658) and NH-PEG3-NH-Boc. Thalidomide-4-NH-PEG1-COOH TFA acts as a ligand for Cereblon to recruit CRBN protein. Thalidomide-4-NH-PEG1-COOH TFA is a key intermediate in the synthesis of CRBN-based PROTAC molecules.
CB07-Exatecan is an ADC drug-Linker conjugate that can be used for the synthesis of ADCs. ADC conjugated with CB07-Exatecan and trastuzumab inhibits the growth of HER2-positive cancer cells. CB07-Exatecan can be used in cancer research[1].
TNG-0746132 can be used for synthesis of the compound with anticancer activity[1].
BnO-PEG5-OH is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
Inauhzin is a dual SirT1/IMPDH2 inhibitor, and acts as an activator p53, used in the research of cancer.
Vitronectin is a multifunctional glycoprotein present in blood and in the extracellular matrix. Vitronectin binds glycosaminoglycans, collagen, plasminogen and the urokinase-receptor. Vitronectin also stabilizes the inhibitory conformation of plasminogen activation inhibitor-1. Vitronectin can be used for researching wound healing and in tumorprogression[1].
3’-Deoxy-2’,5’-di-O-acetyl-8-hydroxyguanosine 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].
Aristeromycin, an adenosine analog, is an antibiotic and a potent S-adenosylhomocysteine hydrolase (AHCY) inhibitor[1][2].
Propafenone (SA-79), a sodium-channel blocker, acts an antiarrhythmic agent. Propafenone also has high affinity for the β receptor (IC50=32 nM)[1]. Propafenone blocks the transient outward current (Ito) and the sustained delayed rectifier K current (Isus) with IC50 values of 4.9 μm and 8.6 μm, respectively[2]. Propafenone suppresses esophageal cancer proliferation through inducing mitochondrial dysfunction and induce apoptosis[3].
4-Hydroxylonchocarpin is a chalcone compound from an extract of Psoralea corylifolia. 4-Hydroxylonchocarpin increases phosphorylation of p38 MAPK, JNK and ERK. 4-Hydroxylonchocarpin has diverse pharmacological activities, including antibacterial, antifungal, anticancer, antireverse transcriptase, antitubercular, antimalarial, anti-inflammatory and antioxidant activities[1].
FHD-609 is an inhibitor and a degrader of BRD9 (bromodomain-containing protein 9). FHD-609 targets to ncBAF, can be used for research of wide range of cancers that contain a mutation in a BAF complex subunit. FHD-609 in combination with Telomelysin or INO5401, may play a role in adrenocortical carcinoma (ACC) treatment[1][2].
2’-O-Phthalimidopropyl uridine 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].
Telomerase-IN-1 is a Telomerase inhibitor with an IC50 of 0.19 μM.
Mitoxantrone is a topoisomerase II inhibitor; also inhibits protein kinase C (PKC) activity with an IC50 of 8.5 μM.
Toceranib phosphate is a multitargeted indolinone receptor tyrosine kinase (RTK) inhibitor with Kis of 5 and 6 nM for PDGFRβ and Flk-1/KDR, respectively.
STF-31 is an inhibitor of glucose transporter 1 (GLUT1, IC50 = 1 μM).IC50 value: 1 μMTarget: GLUT1in vitro: STF 31 is a glucose uptake inhibitor in RCC (renal cell carcinoma) 4 cells. By limiting glucose uptake in cancer cells, the immense energy requirements for the cancer cell is not met and the cell does not have the resources to rapidly proliferate.STF-31, which selectively kills RCCs by specifically targeting glucose uptake through GLUT1 and exploiting the unique dependence of these cells on GLUT1 for survival. STF-31 decreases glycolysis by decreasing glucose transport and not by inhibiting a particular glycolytic step or enzyme.[1]in vivo: STF-31 selectively targets the von Hippel-Lindau (VHL)-deficient kidney cancer cells. STF-31 inhibits VHL-deficient cancer cells by inhibiting Glut1. Daily intraperitoneal injection of a soluble analogue of STF-31 effectively reduces the growth of tumors of VHL-deficient cancer cells grafted on nude mice. On the other hand, STF-31 appears to be an inhibitor with a narrow cell target spectrum.[2]
THK01 is a potent ROCK2 inhibitor with IC50 values of 5.7 and 923 nM for ROCK2 and ROCK1, respectively. THK01 inhibits breast cancer metastasis through the ROCK2-STAT3 signaling pathway. THK01 can be used in research of breast cancer[1].
Thalidomide-O-PEG2-propargyl (E3 ligase Ligand-Linker Conjugates 32) is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and 2-unit PEG linker used in PROTAC technology[1].
Bromodomain inhibitor-10 (compound 128) is a potent bromodomain inhibitor with Kds of 15.0, 2500 nM for BRD4-1 and BRD4-2, respectively. Bromodomain inhibitor-10 inhibits the production of IL12p40[1].