3-epi-Azido-3-deoxythymidine 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].
Thalidomide-NH-(CH2)3-NH-Boc is a Boc-modified Thalidomide (HY-14658), which acts as a Cereblon ligand to recruit CRBN protein. The Boc protecting group at the end of Thalidomide-NH-(CH2)3-NH-Boc can be removed under acidic conditions to participate in the synthesis of PROTAC molecules. Thalidomide-NH-(CH2)3-NH-Boc is a key intermediate in the synthesis of CRBN-based designed PROTAC molecules targeting 11β-substituted estradiol.
SNT-207707 is a selective, potent and orally active melanocortin MC-4 receptor antagonist with an IC50 of 8 nM (binding) and 5 nM (function) on the MC-4 receptor.
VEGFR-IN-1 (compound 3) is a potent angiogenesis inhibitor with IC50s of 0.02, 0.18, 0.24 7.3, and 7 µM for KDR, Flt-1, c-Kit, EGF-R, and c-Src, respectively[1].
Obrindatamab is a humanized anti-B7-H3/CD3 bispecific antibody. Obrindatamab binds to B7-H3 and CD3, thereby mediating redirected cytotoxic T-lymphocyte (CTL) activity against B7-H3-expressing cancer cells. Obrindatamab can be used in research of cancer[1].
Moroidin (1) is a bicyclic octapeptide belonging to the Urticaceae-type cyclopeptide family. Moroidin (1) has a potent inhibitory effect on purified tubulin polymerization. Moroidin (1) has cytotoxic effects for several cancer cells, and can induce apoptosis in A549 human lung cancer cells[1].
Sphinganine 1-phosphate (D-erythro-Dihydrosphingosine 1-phosphate) is a polar sphingolipid metabolite that regulates cell migration, differentiation, survival and complex physiological processes[1].
Gemnelatinib is a tyrosine kinase inhibitor (WO2018077227, implementation example 1). Gemnelatinib can be used for the research of cancer[1].
Delmitide (RDP58) acetate is an orally active d-isomer decapeptide with potent anti-inflammatory activity. Delmitide acetate inhibits production of TNF-α, IFN-γ, and interleukin (IL)-12, and up-regulates heme oxygenase 1 activity. Delmitide acetate can be used for the research of ulcerative colitis[1][2].
TW-37 is a potent Bcl-2 inhibitor with Ki values of 260, 290 and 1110 nM for Mcl-1, Bcl-2 and Bcl-xL, respectively.
HSD17B13-IN-2 (compound 1) is a potent hydroxysteroid 17ß-dehydrogenase 13 (HSD17B13) inhibitor. HSD17B13-IN-2 has cell experimental activity[1].
3’,5’-Di-O-acetyl-2’-deoxy-2’-fluoro-5-iodouridine 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].
S516 (Compound 22) is an active metabolite of CKD-516 and a potent tubulin polymerization inhibitor with an IC50 of 4.29 μM. S516 has marked antitumor activity[1].
(R)-Exatecan Intermediate 1 is an isomer of Exatecan Intermediate 1 (HY-42487). Exatecan Intermediate 1 (compound 6) is an intermediate of Exatecan (HY-13631), a camptothecin-based anticancer agent. Exatecan inhibits tumor growth by interfering with the proliferation and division of tumor cells by interacting with DNA. Exatecan is primarily used in research into a variety of cancers including ovarian, lung and breast cancer[1][2].
Emeramide is a novel lipid-soluble, thiol-redox antioxidant and heavy metal chelator.
WNK463 is an orally bioavailable pan-WNK-kinase inhibitor with IC50s of 5, 1, 6, and 9 nM for WNK1, WNK 2, WNK 3, and WNK 4, respectively.
DCZ0415, a potent TRIP13 inhibitor, impairs nonhomologous end joining repair and inhibits NF-κB activity. DCZ0415 induces anti-myeloma activity in vitro, in vivo, and in primary cells derived from drug-resistant myeloma patients[1].
Talazoparib tosylate (BMN 673ts) is a novel, potent and orally available PARP1/2 inhibitor with an IC50 of 0.57 nM for PARP1.
8-Aminoadenosine (8-NH2-Ado), a RNA-directed nucleoside analogue, reduces cellular ATP levels and inhibits mRNA synthesis. 8-Aminoadenosine blocks Akt/mTOR signaling and induces autophagy and apoptosis in a p53-independent manner. 8-Aminoadenosine has antitumor activity[1][2][3].
N6-Benzoyl-5'-O-(4,4'-dimethoxytrityl)-3'-O-(2-methoxyethyl)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].
ErSO is a selective anticipatory unfolded protein response (a-UPR) activator. ErSO acts through ERα to elicit strong and sustained cytotoxic activation of the a-UPR. ErSO can be used for the research of cancer[1].
Ipatasertib-NH2 dihydrochloride is a ligand for target protein AKT for PROTAC (INY-03-041). INY-03-041 is composed of Ipatasertib-NH2, a ten-hydrocarbon linker, and a CRBN ligand Lenalidomide for E3 ubiquitin ligase[1].
BMS-986205 is a selective indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor.
Tinlorafenib (PF-07284890) (compound 10) is an orally active BRAF kinase inhibitor, with IC50s of 4.25 and 2.7 nM for BRAFV600E/V600K respectively. Tinlorafenib demonstrates CNS penetration and can be used in the research of BRAF-associated malignant and benign tumors of the CNS as well as extracranial malignancies[1].
Pentetreotide is a diethylenetriaminopentaacetic (DTPA) conjugate of Octreotide. Pentetreotide is an indium-labelled somatostatin analog and can be uesd to nuclear medicine imaging. Somatostatin receptor scintigraphy with Pentetreotide is effective in visualizing neuroendocrine tumors, and its metastasis[1][2].
L-6-Diazo-5-oxonorleucine (L-6-Diazo-5-oxonorleucine) is a glutaminases antagonist with a Ki of 6 μM. L-6-Diazo-5-oxonorleucine exhibits analgesic, antibacterial, antiviral and anticancer properties. L-6-Diazo-5-oxonorleucine displays genetic toxicity in vitro. L-6-Diazo-5-oxonorleucine decreases the self-renewal potential and metastatic ability of tumor cell[1][2][3][4].
CPS-11 (N-(Hydroxymethyl)thalidomide) a Thalidomide analogue, is a potent anti-cancer agent. CPS-11 inhibits NF-κB, activates NFAT, and repress cytokine expression through elevated ROS. CPS-11 exhibits a wider activity spectrum and higher potency against MM (multiple myeloma) cell lines[1][2][3].
9-ING-41 is a potent glycogen synthase kinase-3 (GSK-3) inhibitor[1]. 9-ING-41 induces apoptosis and cell cycle arrest at prophase by targeting centrosomes and microtubule-bound GSK-3β. 9-ING-41 has anticancer activity[2].
Banoxantrone D12 (AQ4N D12) is the deuterium labeled banoxantrone. Banoxantrone is a novel bioreductive agent that can be reduced to a stable, DNA-affinic compound AQ4, which is a potent topoisomerase II inhibitor.
PD-1/PD-L1-IN-36 (Compound 2k) is a PD-1/PD-L1 complex inhibitor (IC50: 15 nM). PD-1/PD-L1-IN-36 can be used for research of cancer immunotherapy[1].