mv4–11

DC-S239 (DC-S239) is a selective inhibitor of histone methyltransferase SETD7 (IC50 = 4.59 μM) with anticancer activity.

AES-350 is a potent and orally active HDAC6 inhibitor (IC50 and Ki of 0.0244 μM and 0.035 μM, respectively), also exhibiting activity against HDAC-3, -8, and -11 in an enzymatic assay with IC50 values of 0.187 μM, 0.245 μM, and >1 μM, respectively. AES-350 triggers apoptosis in AML cells through HDAC inhibition and can be used for acute myeloid leukemia (AML) research.

Alisertib (MLN 8237) is a specific Aurora A inhibitor (IC50: 1.2 nM). The selectivity of Alisertib(MLN 8237) is >200-fold higher for Aurora A than Aurora B.

CDK8-IN-12 is a selective, potent and orally active inhibitor of CDK8 (Ki: 14 nM) and is an anti-cancer agent. CDK8-IN-12 inhibits GSK-3α, GSK-3β and PCK-θ with Ki of 13 nM, 4 nM and 109 nM respectively. CDK8-IN-12 showed anti-proliferative activity against MV4-11 cells.

GNE-049 is a highly selective and potent inhibitor designed to target the CREB-binding protein (CBP) with high affinity, exhibiting an IC50 of 1.1 nM for the suppression of BRET and BRD4 activity, which consequently blocks prostate cancer cell proliferation in both in vitro and in vivo models.

Adavosertib (MK-1775) is a small molecule inhibitor of the checkpoint kinase WEE1 (IC50: 5.2 nM). It hinders the G2 DNA damage checkpoint.

DDO-2728 is a selective pyrazolo[1,5-a]pyrimidine-based ALKBH5 inhibitor with an IC50 of 2.97 μM. It increases the levels of N6-methyladenosine (m6A) modifications in acute myeloid leukemia (AML) cells and exhibits antiproliferative activity in these cells. DDO-2728 also demonstrates anti-tumor efficacy in the MV4-11 xenograft model.

SKLB4771 (FLT3-IN-1) is a novel potent and selective Flt3 inhibitor.

SHP099 is an oral, highly selective, allosteric SHP2 (PTPN11) inhibitor with an IC₅₀ of 70 nM. SHP099 inhibits tumor cell proliferation and survival by stabilizing the autoinhibitory conformation of SHP2 and blocking RAS-ERK signaling. SHP099 inhibits the growth of cancer cells, such as MV4-11 and TF-1 cells (IC₅₀ = 0.32 and 1.73 μM). SHP099 can be used in tumor research.

M-808 is a potent and efficacious covalent inhibitor, targeting the interaction between Menin and MLL. It demonstrates a high binding affinity with an IC50 value of 2.6 nM.

BPR1J-097, a new-type small molecule FLT-3 inhibitor(IC50=11±7 nM), is with great anti-tumor activities in vivo.

Compound 12k (THP-1/MV-4-11 against-1) is a 5-substituted thiazolyl urea anticancer agent with significant inhibitory efficacy against THP-1/MV-4-11 cancer cells, demonstrating IC50 values of 29 nM and 98 nM, respectively.

VAS 3947 is a specific inhibitor of NADPH oxidase (NOX).VAS 3947 has a potent anti-platelet effect, inducing apoptosis through UPR activation, mainly due to protein aggregation and misfolding, independent of anti-NOX activity.

Prexasertib (LY2606368) is a selective checkpoint kinase 1 (CHK1) inhibitor (Ki 0.9 nM, IC50<1 nM). Prexasertib causes double-stranded DNA breaks and replication mutations, leading to apoptosis. Prexasertib has antitumor activity.

Entospletinib (GS-9973) is a Syk inhibitor (IC50=7.7 nM) with selective, oral activity. Entospletinib has potential value in the treatment of a variety of hematological malignancies and immune-related diseases.

MS-177 is a PROTAC EZH2 degrader that promotes cholangiocarcinoma growth through the EZH2-mediated WNT7B/β-catenin pathway.MS-177 inhibits the growth of leukemia cells, induces apoptosis, and cell cycle arrest.MS-177 induces degradation of the classical EZH2-PRC2 and the non-classical EZH2-cMyc complexes and activates the immune-responsive genes in MM cells.

Gilteritinib hemifumarate (ASP2215 hemifumarate) is a potent ATP-competitive dual FLT3 (IC50: 0.29 nM) and AXL (IC50: 0.73 nM) inhibitor for the treatment of relapsed or refractory FLT3 mutant AML.

SJ995973 is a highly potent bromodomain and extraterminal (BET) protein degrader and a BET PROTAC with potential anticancer activity.

GSK3685032 is a time-independent, non-covalent, selective, and reversible DNMT1 inhibitor with an IC₅₀ of 0.036 μM. GSK3685032 induces loss of DNA methylation, transcriptional activation, and inhibition of cancer cell growth, and can be used in cancer therapy research.

Senexin C is a novel orally active and specific CDK8/19 inhibitor with potential anticancer activity.Senexin C is more metabolically stable and potent than Senexin B. Senexin C inhibits the growth of MV4-11 leukaemia cells.

DB818 dihydrochloride is the dihydrochloride salt form of DB818. It acts as an inhibitor of Homeobox A9 (HOXA9). By reducing the formation of the HOXA9-DNA complex, DB818 dihydrochloride inhibits the growth of AML cell lines OCI/AML3, MV4-11, and THP-1 and induces cell apoptosis (apoptosis).

Dot1L-IN-8 (Compound 15) is an effective Dot1L inhibitor. It suppresses the viability of HL-60, K562, MV4-11, HH, and KG-1 cells, with IC50 values of 0.45, 1.03, 0.68, 1.66, and 1.12 μM, respectively.

Homer is a specific probe targeting WDR5. In MV4-11 cells, Homer induces the degradation of WDR5 protein with a DC50 of 53 nM. At a concentration of 1 µM, Homer reduces WDR5 protein levels in MV4-11 cells without affecting its mRNA expression.

MI-1063 is a DMD-2 inhibitor that prevents the MDM2-p53 interaction and activates p53's tumor-suppressing abilities. It inhibits the growth of cancer cells RS4-11 and MV4-11, with IC50 values of 179 nM and 93 nM, respectively. MI-1063 serves as a target protein ligand for the synthesis of the PROTAC degrader [MD-265].