Pulocimab is an anti-VEGFR2 monoclonal antibody (mAb). Pulocimab can be used for the research of cancers[1].
C646 is a selective and competitive histone acetyltransferase p300 inhibitor with Ki of 400 nM, and is less potent for other acetyltransferases.
MK2-IN-4 is a MAPKAPK2 (MK2) inhibitor with an IC50 value of 45 nM. MK2-IN-4 can be used in the research of cancer, inflammation, immunology[1].
Biorobin (Kaempferol 3-O-robinobioside), a flavonoid, significantly inhibits the human lymphocyte proliferation in vitro[1].
4-Iodo-SAHA (1k) is an orally active class I and class II histone deacetylase (HDAC) inhibitor with EC50s of 1.1, 0.95, 0.12, 0.24, 0.85 and 1.3 μM for Skbr3, HT29, U937, JA16 and HL60 cell lines, respectively. 4-Iodo-SAHA (1k) can be used for the research of cancer[1].
Aldoxorubicin (INNO-206) hydrochloride is an albumin-binding proagent of Doxorubicin (DNA topoisomerase II inhibitor), which is released from albumin under acidic conditions. Aldoxorubicin hydrochloride (INNO-206) has potent antitumor activities in various cancer cell lines and in murine tumor models.
Bufarenogin induces intrinsic apoptosis via Bax and ANT cooperation[1].
α-Hydroxyglutaric acid-d4 (disodium) is the deuterium labeled α-Hydroxyglutaric acid disodium[1]. α-Hydroxyglutaric acid (2-Hydroxyglutarate) disodium is an α-hydroxy acid form of glutaric acid. α-Hydroxyglutaric acid disodium is a competitive inhibitor of multiple α-ketoglutarate-dependent dioxygenases, including histone demethylases and the TET family of 5-methlycytosine (5mC) hydroxylases[2].
NAcM-OPT is an orally bioavailable cullin neddylation 1 (DCN1) inhibitor, which potently inhibits the DCN1-UBE2M interaction[1].
CU06-1004 (Sac-1004) is an orally active endothelial dysfunction blocker. CU06-1004 ameliorates endothelial dysfunction by inhibiting hyperpermeability and inflammation, and is potent in inhibiting vascular leakage and inflammation in various animal models, such as diabetic retinopathy, stroke, cancer, and inflammatory bowel disease. CU06-1004 ameliorates CDAA-induced mouse model of NASH. CU06-1004 also improves cardiac function[1][2][3].
Tilfrinib (compound 4f) is a potent and selective inhibitor of breast tumor kinase (Brk) with an IC50 of 3.15 nM, which displays anti-proliferative activity and acts as a promising antitumor agent[1].
Alpha-Naphthoflavone is a synthetic flavonoid, acts as a potent and competitive aromatase inhibitor with an IC50 and a Ki of 0.5 and 0.2 μM, respectively[1].
Bcl-2/Bcl-xl inhibitor 1 (compound 6) is a dual Bcl-2 and Bcl-xl inhibitor with anti-tumor activity, extracted from patent WO2018027097A1. Bcl-2/Bcl-xl inhibitor 1 exhibits IC50 values of 2 nM and 5.9 nM for Bcl-2 and Bcl-xl, respectively[1].
CCT244747 is a potent, orally bioavailable and highly selective CHK1 inhibitor, with an IC50 of 7.7 nM; CCT244747 also abrogates G2 checkpoint with an IC50 of 29 nM.
N6-Ethyl-2’-O-methyladenosine 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].
IL-17A modulator-2 is a IL-17A modulator, extracted from patent WO2021239743+A1, example 27. IL-17A modulator-2 inhibits the biological action of IL-17A with a pIC50 of 8.3. IL-17A modulator-2 can be used for the research of diseases or disorders associated with modulation of IL-17A activity including diseases with an immune component or autoimmune pathol, cancer and neurodegenerative disorders[1].
Topoisomerase I inhibitor 2 (ZML-8) is a highly selective inhibitor of DNA topoisomerase I (Top1). Topoisomerase I inhibitor 2 inhibits Top1 activity and results DNA damage. Topoisomerase I inhibitor 2 blocks G2/M phase and induces apoptosis, exhibits anti-tumor effect[1].
Obatoclax is an antagonist of the BCL-2 family proteins. It binds to BCL-2 with a Ki of 220 nM.
Efaproxiral-d6 (RSR13-d6) is the deuterium labeled Efaproxiral. Efaproxiral (RSR13) is a haemoglobin (Hb) synthetic allosteric modifier, decreases Hb-oxygen (O2) binding affinity and enhances oxygenation of hypoxic tumours during radiation therapy[1][2].
Carfilzomib-d8 is deuterium labeled Carfilzomib. Carfilzomib (PR-171) is an irreversible proteasome inhibitor with an IC50 of 5 nM in ANBL-6 and RPMI 8226 cells.
E3 ligase Ligand-Linker Conjugates 39 incorporates a cIAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. E3 ligase Ligand-Linker Conjugates 39 can be used to design PROTAC degrader[1].
FR901464 is a potent spliceosome inhibitor with prominent anti-tumor and anti-cancer effects[1].
Gentisuric acid, a metabolite of Aspirin (HY-14654), is a substrate of α-amidating monooxygenase (PAM). Gentisuric acid prevents DNA-damage by Mitomycin C (HY-13316)[1][2].
2’-O-Me-2-thio-U-3’-phos phoramidite 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].
CDK7-IN-5 is a CDK7 inhibitor with an IC50 value <100 nM. CDK7-IN-5 has anticancer effects. (WO2015154022A1 (Compound 104))[1].
2’,3’-Bis(O-t-butyldimethylsilyl)-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].
PC-766B is a macrolide antibiotic. PC-766B is active against Gram-positive bacteria, and some fungi and yeasts, but inactive against Gram-negative bacteria. PC-766B shows antitumor activity against murine tumor cells. PC-766B has weak inhibitory activity against Na+, K+-ATPase[1][2].
Onalespib (AT13387) is a potent inhibitor of Hsp90, with a Kd of 0.71 nM.
CL2 Linker is an ADC linker. CL2-SN-38 and CL2A-SN-38 are equivalent in drug substitution (~6), cell binding (Kd ~1.2 nM), cytotoxicity (IC50 ~2.2 nM), and serum stability in vitro (t1/2 ~20 hours)[1][2].