GLI antagonist-1 is a potent GLI antagonist with an IC50 value of 1.1 µM. GLI antagonist-1 shows anti-proliferative activity. GLI antagonist-1 decreases the GLI1 mRNA expression. GLI antagonist-1 inhibits colony formation in a dose-dependent manner[1].
(R)-TAPI-2 is the isomer of TAPI-2 (HY-100211A). TAPI-2 (TNF Protease Inhibitor 2) is a broad-spectrum inhibitor of matrix metalloprotease (MMP), tumour necrosis factorα-converting enzyme (TACE) and a disintegrin and metalloproteinase (ADAM), with an IC50 of 20 μM for MMP[1]. TAPI-2 blocks the entry of infectious SARS-CoV[2].
CDK8-IN-6 (compound 9) is a potent cyclin-dependent kinase 8 (CDK8) inhibitor with an Kd of 13 nM. CDK8-IN-6 shows cytotoxicity for MOLM-13, OCI-AML3, MV4-11, NRK and H9c2 cells with IC50s of 11.2, 7.5, 8.6, 20.5, 12.5-25 µM, respectively. CDK8-IN-6 has the potential for the research of AML-cancer[1].
Chloroquine (diphosphate) is an antimalarial and anti-inflammatory drug widely used to treat malaria and rheumatoid arthritis. Chloroquine is an inhibitor of autophagy and toll-like receptors (TLRs).
Modified MMAF, an ADC cytotoxin, can be used in the synthesis of Antibody-drug Conjugate (ADC). Modified MMAF can be used for the targeted treatment of cancer[1].
7ACC2 is a new potent MCT inhibitor with IC50 of 11 nM for inhibition of [14C]-lactate influx; new antitumor treatment targeting lactate transport in cancer cells.IC50 value: 11 nM ([14C]-lactate influx) [1]Target: MCT inhibitor; lactate transport inhibitor7ACC2 did not influence the prothrombin time which, together with a good in vitro ADME profile, supports the potential of this new family of compounds to act as anticancer drugs through inhibition of lactate flux.
MS67 is a potent and selective WD40 repeat domain protein 5 (WDR5) degrader with a Kd of 63 nM. MS67 is inactive against other protein methyltransferases, kinases, GPCRs, ion channels, and transporters. MS67 shows potent acticancer effects[1].
AZA197 is a selective small molecule inhibitor of Cdc42.AZA197 suppresses colon cancer cell proliferation, cell migration, invasion and increases apoptosis by down-regulating the PAK1 and ERK signaling pathways in vitro. AZA197 reduces tumor growth and significantly increases mouse survival in SW620 tumor xenografts[1].
β-Glycerol phosphate disodium salt pentahydrate is a Phosphatase and tensin homolog (PTEN) inhibitor extracted from patent US 20110002877 A1.
5’-Azido-5’-deoxy-2’-O-(2-methoxyethyl)-5-methyluridine 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].
Target Protein-binding moiety 8 is a compound binding to BCR-ABL, and used for inhibiting BCR-ABL activity.
KGP-94 is a potent, selective cathepsin L inhibitor with IC50 of 189 nM, shows no significant inhibitory effect on cathepsin B (IC50>10 uM); significantly decreases the activity of cathepsin L toward human type I collagen, and impeds both migration and invasion of MDA-MB-231 human breast cancer cells; shows tumor growth retardation in a C3H mouse mammary carcinoma model.
Envonalkib citrate is a potent and orally active inhibitor of ALK, with IC50s of 1.96 nM, 35.1 nM, and 61.3 nM for WT and mutated L1196M and G1269S-ALK. Envonalkib citrate can be used for the research of non-small cell lung cancer[1].
MC-PEG2-NH2 is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
RM-581, an aminosteroid derivative, has potent anticancer activity in different types of cancer, including high fatality pancreatic cancer[1].
GAC0003A4 is a novel LXR inverse agonist, functioning as LXR a degrader"
SCO-PEG2-NH2 is a cleavable ADC Linker containing 2 PEG units. SCO-PEG2-NH2 can be used as a copper-free click chemical reagent for catalyst-free click reactions.
Valecobulin (CKD516), a valine prodrug of (S516) and a vascular disrupting agent (VDA), is a potent beta-tubulin polymerization inhibitor with marked antitumor activity against murine and human solid tumors[1][2].
ERK5-IN-1 is a potent ERK5 inhibitor with an IC50 of 87±7 nM. ERK5-IN-1 also inhibits LRRK2[G2019S] with an IC50 of 26 nM.
2-Aminopurine-O-Ph-NHCO-C3-NHS ester (BG-GLA-NHS) is an amine-reactive building block. 2-Aminopurine-O-Ph-NHCO-C3-NHS ester can be used to modify viral capsids surface, and the synthesis of SNAP-tag substrates[1].
(1R,3S)-Compound E is the inactive isomer of Compound E (HY-14176), and can be used as an experimental control. Compound E is a γ-secretase inhibitor. Compound E bloks β-amyloid(40), β-amyloid(42), and Notch γ-secretase cleavage with IC50s of 0.24, 0.37, 0.32 nM, respectively.
Cryptomeridiol can be isolated from Phaulopsis imbricata. Cryptomeridiol has melanogenesis inhibitory activity in the α-MSH-stimulated B16 melanoma cells[1].
5-Fluorouracil is a potent antitumor agent that affects pyrimidine synthesis by inhibiting thymidylate synthetase thus depleting intracellular dTTP pools.
5-(Aminomethyl)-2′,3′-O-(1-methylethylidene)-2-thiouridine 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].
1-Dehydroxy-23-deoxojessic acid (compound 10) is a cycloartane-type triterpene. 1-Dehydroxy-23-deoxojessic acid exhibits cytotoxicity against murine colon 26-L5 carcinoma cells, with an EC50 of 62.38 μM[1].
GSK8573 (compound 23) is an inactive control compound for GSK2801. GSK8573 has binding activity to BRD9 with a Kd value of 1.04 μM and is inactive against BAZ2A/B and other bromodomain familiy[1].
Isoangustone A is an anticancer and anti-inflammatory agent. Isoangustone A induces cancer cells apoptosis and autophagic cell death[1][2][3].
5'-Amino-5'-deoxyadenosine (NH2dAdo; Nsc 238990) 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].