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.

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

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.

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.

PLM-101 is an anticancer compound orally active against acute myeloid leukemia by targeting FLT3 and RET. It impedes RET function, promoting autophagic breakdown of FLT3, and suppresses the PI3K and Ras/ERK pathways, contributing to its anti-leukemic effects. The compound's antitumor efficacy is demonstrated in both a mouse MV4-11 flank xenograft model (doses of 3 and 10 mg/kg; po) and an allogeneic xenograft mouse model (dose of 40 mg/kg; po) [1].

Sorafenib N-oxide is an active metabolite of sorafenib , an inhibitor of Raf-1, B-RAF, and receptor tyrosine kinases. Sorafenib N-oxide inhibits FLT3 that contains the internal tandem duplication mutation (FLT3-ITD; Kd = 70 nM) and inhibits proliferation of MV4-11 acute myeloid leukemia (AML) cells expressing FLT3-ITD (IC50 = 25.8 nM). It is selective for AML cell lines containing FLT3-ITD over lines containing wild-type FLT3 (IC50s = 3.9-13.3 μM). Sorafenib N-oxide is also a linear-mixed inhibitor of the cytochrome P450 (CYP) isoform CYP3A4 (Ki = 15 μM in human liver microsomes).

BRD4-IN-4 is a selective BRD4 inhibitor with an IC50 value of 6.83 μM for BRD4.BRD4-IN-4 selectively inhibits the proliferation of the MV4-11 cell line and arrests the cells in G1 phase.BRD4-IN-4 can be used to study MLL leukemias.

HDAC/CD13-IN-1 (Compound 12) is an inhibitor of both HDAC and CD13, with IC50 values of 0.34 μM for hCD13, 0.53 μM for porcine CD13, and 0.03, 0.06, and 0.02 μM for HDAC1, HDAC2, and HDAC3, respectively. This compound effectively suppresses the proliferation of MV4-11, K562, Jeko-1, and HL60 cancer cells, with IC50 ranges between 0.25-2.04 μM, and also induces apoptosis in these cells. Furthermore, HDAC/CD13-IN-1 demonstrates capabilities in hindering metastasis and invasion [1].

CDK8-IN-7 (compound 12) is a potent and selective inhibitor of cyclin-dependent kinase 8 (CDK8) (Kd: 3.5 nM). CDK8-IN-7 has shown potential for AML-cancer research.

HDAC-IN-63 (Compound 63) is a dual FLT3/HDAC inhibitor with IC50 values of 0.844 nM for FLT3 and 30.0 nM for HDAC1. It effectively suppresses MV4-11 cell proliferation with an IC50 of 92 nM, induces apoptosis, and arrests the cell cycle in MV4-11 cells. This compound is applied in acute myeloid leukemia (AML) research [1].

CDK8-IN-6 (compound 9) is a potent inhibitor of cyclin-dependent kinase 8 (CDK8) (Kd: 13 nM), CDK8-IN-6 showed potential research value in AML cancers.

FLT3-IN-11 (compound 30) is an orally active, potent and selective inhibitor of FLT3 kinase, acting on wild-type FLT3 (IC50: 7.22 nM) and FLT3-D835Y (IC50: 4.95 nM). FLT3-IN-11 exhibited significant anti-AML effects with an IC50 value of 3.2 nM for MV4-11 cells.

FLT3-IN-12 is a selective, potent, orally active FLT3 kinase inhibitor that acts on FLT3-WT (IC50: 1.48 nM) and FLT3-D835Y (IC50: 2.87 nM). FLT3-IN-12 is more selective than c-KIT (>1000-fold). FLT3-IN-12 showed significant anti-AML effects, with an IC50 value of 0.75 nM for MV4-11 cells.

FLT3-IN-22 (compound 22f) is a potent inhibitor of FLT3, demonstrating IC50 values of 0.941 nM for FLT3 and 0.199 nM for the FLT3/D835Y mutant. This compound displays significant antiproliferative effects against MV4-11 cells and Ba/F3 cell lines expressing mutant FLT kinase variants, such as FLT-D835Y and FLT3-F691L [1].

MC2652 (compound 1a) is a potent LSD1 inhibitor that shows high inhibitory effects in leukaemia cells MV4-11 and NB4. MC2652 has antiproliferative activity against LNCaP cells of prostate cancer [1].

PAK4-IN-2 is an exceptionally effective inhibitor of PAK4, exhibiting an IC 50 value of 2.7 nM. This compound is capable of arresting MV4-11 cells at the G0/G1 phase and inducing cell apoptosis. It holds significant potential in cancer research [1].

CDK9-IN-19 is a selective and potent CDK9 inhibitor (IC50: 2.0 nM). CDK9-IN-19 exhibits good anti-proliferative activity in cancer cells, moderate pharmacokinetic properties and low hERG inhibition. CDK9-IN-19 significantly inhibited tumor growth in the MV4-11 xenograft mouse model. CDK9-IN-19 can be used in studies of acute myeloid leukemia (AML).

AES-350 is a potent and orally active HDAC6 inhibitor(IC50 and a Ki of 0.0244 μM and 0.035 μM, respectively). It is also against HDAC-3, -8, and -11 in an enzymatic activity assay with IC50 values of 0.187 μM, 0.245 μM, and >1μM, respectively. AES-350 tri

GSK3685032 is a non-covalent and selective DNMT1 inhibitor(IC50 = 36 nM). The inhibitory effect is time-independent and reversible. GSK3685032 induces loss of DNA methylation and transcriptional activation and inhibits cancer cell growth.

FLT3-IN-20 (compound 34f) is a potent FLT3 inhibitor, demonstrating IC50 values of 1 nM for FLT3-D835Y and 4 nM for FLT3-ITD. It exhibits anti-proliferative effects on FLT3-ITD-positive AML cell lines, with IC50s of 7 nM in MV4-11 and 9 nM in MOLM-13, as well as 4 nM in a MOLM-13 variant harboring the FLT3-ITD-D835Y mutation. FLT3-IN-20 is utilized in cancer research [1].

TCS 359 (FLT3 Inhibitor) is a potent FLT3 inhibitor with IC50 of 42 nM.

FY-56, a highly potent and selective inhibitor of LSD1/KDM1A with an IC50 value of 42 nM, demonstrates significant selectivity over MAO-A/B. This compound effectively induces differentiation in MOLM-13 and MV4-11 cells, showing promise for acute myeloid leukemia (AML) research [1].

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

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

PROTAC BRD4 Degrader-8 is a potent BRD4 inhibitor, with IC50s of 1.1 nM and 1.4 nM for BRD4 BD1 and BD2, respectively. PROTAC BRD4 Degrader-8 is capable of potently degrading the BRD4 protein in PC3 prostate cancer cells[1]. PROTAC BRD4 Degrader-8 (compound 8; 6 days) inhibits the proliferation of PC3 prostate cancer cells, with an IC50 of 28 nM[1].PROTAC BRD4 Degrader-8 (4 h) suppresses MYC gene transcript in MV4-11 AML cells, with an IC50 of 11 nM[1].PROTAC BRD4 Degrader-8 (4 h) potently degrades the BRD4 protein in PC3 prostate cancer cells, with an DC50 of 7.5 nM[1]. [1]. Dragovich PS, et, al. Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 2: Improvement of In Vitro Antiproliferation Activity and In Vivo Antitumor Efficacy. J Med Chem. 2021 Mar 11;64(5):2576-2607.