RUNX-IN-2 (Compound Conjugate 3) covalently binds to the RUNX-binding sequences, and inhibits the binding of RUNX proteins to their target sites. RUNX-IN-2 induces the p53-dependent apoptosis and inhibits cancer cell growth. RUNX-IN-2 inhibits tumor growth in PANC-1 xenograft mice. RUNX-IN-2 has high alkylation efficiency and specificity[1].
Oxythiamine, an antimetabolite and a vitamin B1 antagonist, is a well-known thiamine antagonist and inhibitor of transketolase.
RB-3, a PRC1 inhibitor, binds to RING1B-BMI1f, with a Kd of 2.8 μM[1].
ASTX660 is an orally bioavailable dual antagonist of cellular inhibitor of apoptosis protein (cIAP) and X-linked inhibitor of apoptosis protein (XIAP).
UM-164 is a highly potent inhibitor of c-Src with a Kd of 2.7 nM. UM-164 also potently inhibits p38α and p38β.
Iberin, a sulfoxide analogue of sulforaphane, is a naturally occurring member of isothiocyanate family. It inhibits cell survival with an IC50 of 2.3 μM in HL60 cell.
Aurora A inhibitor I is a potent and highly selective Aurora A inhibitor with with an IC50 of 3.4 nM.
Lapisteride (CS 891) is an orally active 5α-reductase inhibitor. Lapisteride can be used in cancer research[1].
hCAIX-IN-14 (compound 5a) is a potent inhibitor of human CA IX with a Ki value of 134.8 nM[1].
Sirt1/2-IN-2 (compound hsa55) is a dual inhibitor of SIRT1/2 with IC50s of 1.8 μM (SIRT1) and 2.4 μM (SIRT2), respsectivley. Sirt1/2-IN-2 completely blocks p53 deacetylation, and increase of p53 and α-tubulin acetylation. Sirt1/2-IN-2 induces apoptosis and shows anti-proliferation activity against human leukemia cell lines[1].
2’-Deoxy-2’-fluoro-N3-[(pyrid-4-yl)methyl]-beta-D-arabinouridine 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].
TC AQP1 1 (m-Phenylenediacrylic acid) is a potent AQP1 inhibitor. TC AQP1 1 inhibits AQP1-mediated water flux in oocytes, with an IC50 of 8 μM[1].
SC144 hydrochloride is the first-in-class orally active small-molecule gp130 inhibitor; inhibits cell growth in a panel of human ovarian cancer cell lines with IC50 values in a submicromolar range.IC50 value: < 1 uM (Cell assay) [1]Target: gp130 inhibitorSC144 shows greater potency in human ovarian cancer cell lines than in normal epithelial cells. SC144 binds gp130, induces gp130 phosphorylation (S782) and deglycosylation, abrogates Stat3 phosphorylation and nuclear translocation, and further inhibits the expression of downstream target genes. In addition, SC144 shows potent inhibition of gp130 ligand-triggered signaling. Oral administration of SC144 delays tumor growth in a mouse xenograft model of human ovarian cancer without significant toxicity to normal tissues.
Amino-PEG11-OH is non-cleavable 11 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
Isocucurbitacin D is an antitumor agent[1].
7,8-Dihydro-8-oxo-7-propargyl-3’-deoxy guanosine 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].
HSD17B13-IN-3 (compound 2) is a potent hydroxysteroid 17ß-dehydrogenase 13 (HSD17B13) inhibitor. HSD17B13-IN-3 does not have cell experimental activity[1].
Methyl chlorogenate is an antioxidant, and has radical scavenging activity. Methyl chlorogenate is an anti-inflammatory agent. Methyl chlorogenate also inhibits hepatocellular carcinoma (HCC) cell proliferation and metastasis[1][2].
Rac-Nedisertib (Rac-M3814) is a racemate of Nedisertib, a potent DNA-PK inhibitor, with an IC50 of <3 nM[1].
A novel potent, in vivo-active BCL6 inhibitor with IC50 of 0.1 uM in ELISA assays; exhibits good cellular BCL6BTB/ BCoR PPI inhibitory activity in the submicromolar range (M2H IC50=0.72 uM), showed a good pharmacokinetic profile, which is acceptable for both in vitro and in vivo studies.
SM-164 is a cell-permeable Smac mimetic compound. SM-164 binds to XIAP protein containing both the BIR2 and BIR3 domains with an IC50 value of 1.39 nM and functions as an extremely potent antagonist of XIAP.
USP7-IN-7 (compound 124) is a USP7 inhibitor with an IC50 value ＜10 nM. USP7-IN-7 shows cytotoxicity against p53-mutant cancer cell lines, p53 wild-type blood cancer and neuroblastoma cell lines with low nanomolar values. USP7-IN-7 can be used for cancer research[1].
EPZ004777 is a potent, selective DOT1L inhibitor with an IC50 of 0.4 nM.
AQ4 is a topoisomerase II inhibitor and DNA intercalator as a chemically stable cytotoxic agent in many human tumor lines[1].
Mapatumumab (HGS-ETR1) is a fully human IgG1 agonistic monoclonal antibody that targets tumor necrosis factor-related apoptosis-inducing ligand receptor 1 (TRAIL-R1). Mapatumumab can be used for the research of cancer[1].
Brivanib is an ATP-competitive inhibitor against VEGFR2 with IC50 of 25 nM, and has moderate potency against VEGFR-1 and FGFR-1, but >240-fold against PDGFR-β.
m-Carboxycinnamic acid bishydroxamide is a potent HDAC inhibitor, exhibiting ID50 values of 10 and 70 nM in vitro for HDAC1 and HDAC3, respectively[1]. m-Carboxycinnamic acid bishydroxamide also induces apoptosis and suppresses tumor growth[2].
CDK7/12-IN-1 is a selective CDK7/12 inhibitor with IC50s of 3 and 277 nM for CDK7 and CDK 12, respectively. CDK7 and CDK12 inhibition is an effective strategy to inhibit tumour growth[1].
Andrographiside is a labdane diterpenoid glucoside that can be isolated from the leaves of Andrographis paniculata Nees. Andrographiside has antihepatotoxic and antioxidative effects. Andrographiside shows protective effects on mice with hepatotoxicity induced by carbon tetrachloride or tert-butylhydroperoxide (tBHP)[1].
PI3Kγ inhibitor 7 (compound 2) is a potent and orally active PI3Kγ inhibitor with IC50 values of 4768, 878.1, 3.42, 355.2 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ, respectively. PI3Kγ inhibitor 7 shows antitumor activity[1].