Gracillin is a kind of steroidal saponin isolated from the root bark of wild yam Dioscorea nipponica with antitumor agent.Gracillin could induce cell cycle arrest, oxidative stress, and apoptosis in HL60 cells.[1]
Gardiquimod trifluoroacetate is a specific TLR7 agonist which can also inhibit HIV-1 reverse transcriptase.
FMF-06-098-1 is a highly multitargeted depressant. FMF-06-098-1 can be used to target degradation kinases which degrades AAK1, AΒL2, AURKA, AURKB, BUBIB, CDC7, CDK1, CDK12, CDK13, CDK2, CDK4, CDk6, CDK7, CDK9, CHEK1, CSNKID, EPHA1, PER, FGFR1, GAK, IRAK4, ITK, LIMK2, MAP4K2, MAP4K3, MAPK6, MAPK7, MARK4, MELK, PKN3, PLK4, PRKAA1, PTK2, PTK6, RPS6KA4, S1K2, STK35, TNK2, UHMK1, ULK1, and WEE1[1].
CDK7-IN-22 (compound 101) is an CDK7 inhibitor with antitumor activity. CDK7-IN-22 shows selectivity on CDK7[1].
Devextinetug (IXT-M200) is a chimeric anti-methamphetamine, mouse-derived IgG2κ antibody[1].
TLR7/8 agonist 4 hydroxy-PEG6-acid is a Drug-Linker Conjugates for ADC. TLR7/8 agonist 4 hydroxy-PEG6-acid consists of TLR7/8 agonist 4 (HY-139017) and a linker Hydroxy-PEG6-acid (HY-133050), and can be used for synthesis of ADCs[1].
PHA-793887 is a potent, ATP-competitive CDK inhibitor, can inhibit Cdk2, Cdk1, Cdk4, and Cdk9 with IC50s of 8 nM, 60 nM, 62 nM and 138 nM, respectively, and also inhibits glycogen synthase kinase 3β with an IC50 of 79 nM.
BCL2-IN-1 is a potent Bcl-2 inhibitor. BCL2-IN-1 binds Bcl-2 with a Ki of <0.01 nM[1].
PI3K-IN-46 (Intermediate 4) is an intermediate in the synthesis of PI3K inhibitor (2-imino-azolinone-vinyl fused-benzene derivative) that can be used for the research of autoimmune disorders, cardiovascular diseases, and neurodegenerative diseases[1].
KM04416, an isothiazolone derivative, is a potent glycerol-3-phosphate dehydrogenase (GPD2) inhibitor. KM04416 significantly inhibits PNT1A cell proliferation[1][2].
KG-548 is an ARNT/TACC3 disruptor and a HIF-1α inhibitor. KG-548 directly interferes with ARNT/TACC3 complex formation by competing with TACC3 for binding to the ARNT PAS-B domain. ARNT is the aryl hydrocarbon receptor nuclear translocator, also known as HIF-β[1][2].
N3-PEG4-C2-Pfp ester is a nonclaevable 4-unit PEG linker used in the synthesis of antibody-drug conjugates (ADCs).
GRP (porcine) (Porcine gastrin-releasing peptide 27) is the putative mammalian analog of Bombesin (HY-P0195). GRP (porcine) activates the release of a number of gastroenteropancreatic (GEP) peptides into the peripheral circulation. GRP (porcine) stimulates gastrin release and exocrine pancreatic secretion. GRP (porcine) is a useful marker of neuroendocrine differentiation in many tumors[1][2].
S63845 is a potent and selective myeloid cell leukemia 1 (MCL1) inhibitor with a Kd of 0.19 nM for human MCL1.
ATR-IN-9 is a potent inhibitor of Ataxia-telangiectasia and RAD-3-related protein kinase (ATR) extracted from patent WO2020087170A1, compound 59, has an IC50 of 10 nM[1].
1-(alpha-L-Threofuranosyl)cytosine 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].
Chk2-IN-1 (compound 1) is a potent and selective inhibitor of checkpoint kinase 2 (Chk2), with IC50s of 13.5 nM and 220.4 nM for Chk2 and Chk1, respectively. Chk2-IN-1 can elicit a strong ataxia telangiectasia mutated (ATM)-dependent Chk2-mediated radioprotection effect[1].
JKE-1674 is an orally active glutathione peroxidase 4 (GPX4) inhibitor. JKE-1674 kills cells in a manner that is equipotent to ML210 and is completely rescued by ferroptosis inhibitors[1].
Cbl-b-IN-12 (Example 10) is a casitas B-lineage lymphoma-b (CBL-B) inhibitor with an IC50 of <100 nM[1].
UNC8153 TFA is a potent and selective nuclear receptor-binding SET domain-containing 2 (NSD2)-targeted degrader with a Kd of 24 nM. UNC8153 TFA reduces the cellular levels of both NSD2 protein and the H3K36me2 chromatin mark. UNC8153 TFA contains a simple warhead that confers proteasome-dependent degradation of NSD2[1].
FLI-06 is an inhibitor of Notch signaling with an EC50 of 2.3 μM.
Dexamethasone-d4 is deuterium labeled Dexamethasone. Dexamethasone (Hexadecadrol) is a glucocorticoid receptor agonist. Dexamethasone also significantly decreases CD11b, CD18, and CD62L expression on neutrophils, and CD11b and CD18 expression on monocytes. Dexamethasone is highly effective in the control of COVID-19 infection. Dexamethasone inhibits production of exosomes containing inflammatory microRNA-155 in lipopolysaccharide-induced macrophage inflammatory responses.
Lucanthone-d4 hydrochloride is the deuterium labeled Lucanthone. Lucanthone is an endonuclease inhibitor of Apurinic endonuclease-1 (APE-1)[1][2].
TH588 hydrochloride is first-in-class nudix hydrolase family inhibitor that potently and selectively engage and inhibit the MTH1(IC50= 5 nM) in cells.IC50 value: 5 nM [1]Target: MTH1 inhibitorTH588 is highly selective towards MTH1, with no relevant inhibition of other members of the nudix protein family or a panel of 87 enzymes, GPCRs, kinases, ion channels and transporter. TH588 has been shown to selectively kill a variety of cancer cell lines and with in vivo activity shown for TH588 in SW480 colorectal and MCF7 breast tumour xenografts.
Autophagy-IN-C1 not only induces apoptosis but also blocks autophagy in hepatocellular carcinoma (HCC) cells.
Eupalinolide B is a germacrane sesquiterpene isolated from Eupatorium lindleyanum. Eupalinolide B demonstrates potent cytotoxicity against A-549, BGC-823 and HL-60 tumour cell lines[1].
MALT1-IN-7 (compound 142b) is a potent MALT1 protease inhibitor. MALT1-IN-7 has the potential for cancer research[1].
3-O-(E)-Coumaroylbetulin (3-(E)-Trans coumaroylbetulin) (compound 6) is a potent antitumor agent[1].
C6-ceramide, a ceramide pathway activator, shows activity against a variety of cancer cell lines. C6-ceramide can be used as an adjuvant for chemotherapeutic agents, to enhance anti-tumor effects[1][2].
5’-O-Acetyl-2’,3’-dideoxy-2’,3’-didehydro-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].