Tubulin inhibitor 28 (compound 2g) is a potent tubulin inhibitor with an IC50 value of 1.2 µM. Tubulin inhibitor 28 shows anti-proliferative activity for MCF-7 cells[1].
KW-2478 is an inhibitor of Hsp90α, with an IC50 of 3.8 nM, and has antitumor activity against various human hematological tumor cells.
Mertansine (DM1) is a microtubulin inhibitor which binds at the tips of microtubules and suppresses the dynamicity of microtubules.. Mertansine is an antibody-conjugatable maytansinoid that was developed to overcome systemic toxicity associated with maytansine and to enhance tumor-specific delivery.
TC LPA5 4 is a LPA5 (GPR92)-specific non-lipid antagonist. TC LPA5 4 inhibits LPA-induced aggregation of isolated human platelet (LPA5-RH7777 cell line) with an IC50 of 800 nM. TC LPA5 4 displays selectivity for LPA5 over 80 other screened drug targets[1]. TC LPA5 4 inhibits cell proliferation and migration of thyroid cancer cells[2].
RIP1 kinase inhibitor 6 is a potent and selective RIP1 kinase inhibitor with an IC50 of < 100 nM in human R1P1 kinase assay. RIP1 kinase inhibitor 6 is extracted from patent WO2020103884, example 80[1].
Azido-PEG10-amine is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
CAY10677 (compound 15) is a potent ICMT inhibitor that inhibits cancer cell proliferation. CAY10677 has good PAMPA penetration[1].
Calythropsin is a cytotoxic chalcone, with weak effect on mitosis, and presumably also on tubulin polymerization[1].
Vismodegib (GDC-0449) is an orally active hedgehog pathway inhibitor with an IC50 of 3 nM. It also inhibits P-gp, ABCG2 with IC50 values of 3.0 μM and 1.4 μM, respectively.
Syk-IN-8 (compound 19q) is a Syk inhibitor, with antiproliferative activity against multiple hematological tumour cells. Syk-IN-8 inhibits PLCγ2 phosphorylation, can be used for research in blood cancers[1].
MS4077 is an anaplastic lymphoma kinase (ALK) PROTAC (degrader) with a Kd of 37 nM for binding affinity to ALK[1].
Fluorescein-thiourea-PEG6-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
PROTAC EGFR degrader 5 (Compound 10), a PROTAC EGFR degrader, potently degrades EGFRDel19 in HCC827 cells with the DC50 of 34.8 nM. PROTAC EGFR degrader 5 significantly induces the apoptosis of HCC827 cells and arrest the cells in G1 phase[1].
5-HT2B antagonist-1 is an orally active 5-HT2B receptor antagonist with an IC50 value of 33.4 nM. 5-HT2B antagonist-1 can be used in studies of diseases characterized by 5-HT2B receptor signaling, such as hepatocellular carcinoma, cardiovascular disease or gastrointestinal disease[1][2].
GZD856 is a novel PDGFRα/β inhibitor with IC50s of 68.6 and 136.6 nM, respectively. Anti-lung cancer activities[1].
5’-O-DMTr-3’-deoxyuridine 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].
Intoplicine is a DNA topoisomerase I and II inhibitor.
2’-O-Hexadecanyl 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].
RET-IN-19 (compound 59) is a potent RET inhibitor, with IC50 values of 6.8 and 13.51 nM against RET-wt and RET V804M, respectively. RET-IN-19 shows anticancer activity. RET-IN-19 can be used for non-small cell lung cancer (NSCLC) research[1].
BTK IN-1 is a potent BTK inhibitor, with an IC50 of <100 nM.
ICMT-IN-18 (compound 35) is an inhibitor of ICMT (IC50=0.066 μM)[1].
Uridine 13C is the 13C labeled Uridine[1].
p53-MDM2-IN-1 (Example 30) is an inhibitor of p53-MDM2/X protein interaction with an Ki value of 23.35 µM. p53-MDM2-IN-1 can be used for anti-tumor research[1].
Daunorubicin hydrochloride is a topoisomerase II inhibitor with potent antineoplastic activities.
JNJ-38877618 is a potent, highly selective, orally bioavailable Met kinase inhibitor with IC50s of 2 and 3 nM for wild type and mutant Met, respectively.
Efavirenz-d5 (DMP 266-d5) is the deuterium labeled Efavirenz. Efavirenz (DMP 266) is a potent inhibitor of the wild-type HIV-1 reverse transcriptase with a Ki of 2.93 nM and exhibits an IC95 of 1.5 nM for the inhibition of HIV-1 replicative spread in cell culture[1].
Androgen receptor antagonist 2 (example 12) is an androgen receptor antagonist. Androgen receptor antagonist 2 can be used for prostate cancer and male hair loss research[1].
Bcl-2-IN-11 (compound 6) is a potent and selective Bcl-2 activity inhibitor, with an IC50 of 0.9 nM. Bcl-2-IN-11 shows weak inhibition of Bcl-xl (IC50 > 1000 nM). Bcl-2-IN-11 can be used for the research of a variety of cancers caused by abnormal overexpression of Bcl-2 family proteins: especially malignant hematologic diseases of acute lymphoid leukemia, etc. Bcl-2-IN-11 can also avoid toxic side effects caused by Bcl-xl inhibition, such as thrombocytopenia[1].
Tigloylgomisin P, a lignin, has anti-HIV activity with an EC50 of 37 μM. Tigloylgomisin P has anticancer effect[1][2].