Pioglitazone (U 72107) potassium is an orally active and selective PPARγ (peroxisome proliferator-activated receptor) agonist with high affinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 μM and 0.99 μM for human and mouse PPARγ, respectively. Pioglitazone potassium can be used in diabetes research[2][3][4].
(E)-3-AP is the E configuration of 3-AP. 3-AP is a potent ribonucleotide reductase inhibitor. 3-AP shows anti-proliferative activity. 3-AP shows anticancer activity in L1210 leukemia model. 3-AP inhibits RR activity and DNA synthesis[1][2].
Nicaraven is a novel chemically synthesized hydroxyl radical-specific scavenger.
ML264 is an antitumor agent that potently and selectively inhibits Krüppel-like factor five (KLF5) expression.
LRE1 is a specific and allosteric inhibitor of soluble adenylyl cyclase.
Azido-PEG2-C2-amine (N3-PEG2-CH2CH2NH2) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1]. Azido-PEG2-C2-amine is also a non-cleavable 2 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[2].
KDM5B-IN-3 (Compound 5) is a histone lysine specific demethylase 5B (KDM5B/JARID1B) inhibitor with an IC50 of 9.32 μM. KDM5B-IN-3 can be used for the research of gastric cancer[1].
D-Ribose-d is the deuterium labeled D-Ribose. D-Ribose is an energy enhancer, and acts as a sugar moiety of ATP, and widely used as a metabolic therapy supplement for chronic fatigue syndrome or cardiac energy metabolism. D-Ribose is active in protein gly
CDK4/6-IN-5 is a potent CDK4 and CDK6 inhibitor with Kis of 0.2 and 4.4 nM for CDK4/Cyclin D1 and CDK6/Cyclin D3, respectively[1]. (from patent WO2019207463A1 example A93).
Ninerafaxstat (IMB-1018972) trihydrochloride is a cardiac mitotrope agent. Ninerafaxstat trihydrochloride increases myocardial metabolic efficiency by shifting substrate utilization towards glucose through reducing fatty acid oxidation (inhibiting 3-ketoacyl CoA thiolase)[1].
Hypocretin (70-98), human is a polypeptide that is capable of binding to an orexin receptor OX1R and promotes Apoptosis[1].
Quisinostat (JNJ-26481585) is an orally available, potent HDAC inhibitor with an IC50 of 0.11 nM for HDAC1.
VX-984 (M9831) is a selective DNA-dependent protein kinase (DNA-PK) inhibitor with IC50 of 88±64 nM for A549 lung cancer cells.
PAD4-IN-3 (compound 4B) is a PAD4 inhibitor with antitumor activity in vitro and in vivo. PAD4-IN-3 was covalently linked to RGD sequence peptide-modified chitosan (K-CRGDV), resulting in an enhanced oxidative stress-responsive nanoagent. K-CRGDV-PAD4-IN-3 can actively target tumors, inhibit PAD4 activity, block the formation of neutrophil extracellular traps (NETs), and improve the tumor immune microenvironment in response to the tumor microenvironment[1].
2’-Deoxy-2’-fluoro-3’,5’-bis-O-TBDMS-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].
Trimetrexate (CI-898) isethionate is an antibiotic, also a potent and orally active dihydrofolate reductase (DHFR) inhibitor, reducing the production of DNA and RNA precursors and leading to cell death, with IC50 values of 4.74 nM and 1.35 nM for human DHFR and Toxoplasma gondii DHFR. Trimetrexate isethionate can also inhibit the growth of various cancer cells. Trimetrexate isethionate can be used for researching Pneumocystis carinii pneumonia (PCP) and cancer[1][2][3][4][5].
N6-(3-Trifluoromethylbenzyl)-2’-C-methyl 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].
2-Amino-2’-deoxy-N6,N6-dimethyl-2’-adenosine 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].
GSA-10 is a potent agonist of Smoothened (Smo) receptor with an EC50 of 1.2 μM. GSA-10 is a novel quinolinecarboxamide derivative. GSA-10 acts at Smo to promote the differentiation of multipotent mesenchymal progenitor cells into osteoblasts. GSA-10 mediates Hedgehog (Hh) signaling which may have researching interests in regenerative medicine for cancer disease[1][2].
HPB (HDAC6 inhibitor HPB) is a selective HDAC6 inhibitor with an IC50 of 31 nM. HPB exhibits >30-flod selectivity for HDAC6 over HDAC1[1].
SP-2-225 is a selective HDAC6 inhibitor. SP-2-225 enhance the production of cancer-associated antigens and macrophage antigen cross-presentation to T cells. SP-2-225 reduces the tumor volume in a syngeneic SM1 melanoma model[1].
MDM2-p53-IN-16 is a MDM2-p53 complex inhibitor with an IC50 value of 4.3 nM to dissociate human p53/MDM2 complex. MDM2-p53-IN-16 reactivates p53, and induces Glioblastoma Multiforme (GBM) cell apoptosis and cell-cycle arrest. MDM2-p53-IN-16 can be used for the cancer research[1].
3’-O-Propargyladenosine 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].
CD73-IN-5 is a potent and selective non-nucleotide small molecule inhibitor of CD73 (IC50 = 19 nM).
D-Mannitol-13C,d2 is the deuterium and 13C labeled D-Mannitol.
MI-3 is a Menin-MLL interaction inhibitor with IC50 value of 648 ± 25 nM.IC50 value: 648 ± 25 nM [1]Target: Menin-MLLin vitro: The menin-MLL inhibitors very effectively blocked proliferation of MLL-AF9 and MLL-ENL transduced BMC, with GI50 values of about 5 μM for MI-2 and MI-3. MI-2 and MI-3 showed only a small effect on the cell growth of E2A-HLF transduced BMC (GI50 > 50 μM). MI-2 and MI-3 substantially and specifically reduce the immortalization potential of cells transformed with MLL fusion oncoproteins [1].in vivo: MLL-AF9 transformed BMC that remained viable after 7 days of treatment with MI-2 and MI-3 showed substantial changes in morphology, indicative of monocytic differentiation, as evidenced by increased cell size, lower nuclear to cytoplasmic ratio and highly vacuolated cytoplasm. Consistent with the change in cell morphology, the expression of CD11b was substantially increased on MLL-AF9 transformed BMC after 7 days of treatment with MI-2 and MI-3 [1].
Mps1-IN-2 is a potent, selective and ATP-competitive dual Mps1/Plk1 inhibitor, with an IC50 and a Kd of 145 nM and 12 nM for Mps1 and a Kd of 61 nM for Plk1.
N-Boc-N-bis(PEG4-OH) is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
Fulvestrant S enantiomer is the S enantiomer of Fulvestrant. Fulvestrant is a selective estrogen receptor (ER) antagonist which can be used to treat breast cancer.
DC4SMe, a phosphate prodrug of cytotoxic DNA alkylator DC4, can be used in the synthesis of Antibody-drug Conjugate (ADC). DC4SMe exhibits IC50s of 1.9 nM, 2.9 nM, and 1.8 nM for Ramos, Namalwa, and HL60/s cancer cells, respectively. DC4SMe can be used for the targeted treatment of cancer[1].