MOLM-13

UMB298 is a potent and selective CBP/P300 bromodomain inhibitor that inhibits BRD4 with an IC50 of 5193nM.

SGC0946 is a highly effective and specific DOT1L methyltransferase inhibitor (IC50: 0.3 nM); selectively kill mixed lineage leukemia cells.

Kevetrin hydrochloride (4-Isothioureidobutyronitrile hydrochloride) is a small molecule and activator of the tumor suppressor protein p53, with potential antineoplastic activity.

STM2457 is an inhibitor of the RNA methyltransferase METTL3 (IC50=16.9 nM) with selective and oral activity.STM2457 can be used in acute myeloid leukemia (AML) studies.

Atuveciclib (BAY 1143572) is a potent and highly selective PTEFb/CDK9 inhibitor with an IC50 value of 13 nm for CDK9/CycT1 and a selectivity ratio of 100 for CDK2, with highly bioavailable and orally available advantages.

Serdemetan (JNJ-26854165) is an orally bioavailable HDM2 antagonist with potential antineoplastic activity.

dBRD9 is a PROTAC. dBRD9 is a double-acting molecule, partially containing Bromodomain-containing protein 9 (BRD9), ligand that recruits the cereblon E3 ubiquitin ligase. Ligand that recruits the cereblon E3 ubiquitin ligase. dBRD9 can inhibit the degradation of BRD9 in MOLM-13 cells, and the IC50 is 104 nM.

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.

DHODH-IN-16 is an effective inhibitor of dihydroorotate dehydrogenase (DHODH, IC50 = 0.396 nM for human).

TDO-IN-1 is an orally active, potent, and selective inhibitor of tryptophan 2,3-dioxygenase (TDO), inhibiting indoleamine-2,3-dioxygenase, with antitumor activity that reverses local immune tolerance in tumor tissues.

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.

Zanubrutinib (BGB-3111) is an inhibitor of Bruton tyrosine kinase (BTK).

HSP70-IN-1 is a heat shock protein (HSP) inhibitor that suppresses the growth of Kasumi-1 cells with an IC50 of 2.3 μM.

BI-9321 trihydrochloride (BI9321 trihydrochloride) is a selective and potent NSD3-PWWP1 antagonist that downregulates Myc messenger RNA expression and reduces proliferation in MOLM-13 cells.

Alrizomadlin is an orally active MDM2 inhibitor. APG-115 shows significant dose-dependent inhibitory effects on TP53wt AML cell lines. The IC50 values ​​are 26.8 nM for MOLM-13 cells and 165.9 nM for MV-4-11 cells. , OCI-AML-3 cells 315.6 nM. Alrizomadlin blocks the interaction of MDM2 and p53 and induces cell cycle arrest and apoptosis in a p53-dependent manner.

Lenalidomide-C4-NH2 hydrochloride is a Cereblon ligand derived from Lenalidomide. It serves as a recruiting agent for the CRBN protein. The compound, known as PROTAC (Compound 24), can be formed by linking Lenalidomide-C4-NH2 hydrochloride to the ligand for the protein. It exhibits inhibitory effects with IC50s of 0.98 nM and 13.7 nM against the growth of RS4;11 and MOLM-13 acute leukemia cell lines, respectively[1].

YL-5092 is a YTHDC1 inhibitor (IC50=7.4 nM, KD=29.6 nM) that suppresses cancer cell proliferation, induces G0/G1 phase arrest and apoptosis, and can be used in studies of acute myeloid leukemia (AML).

Compound 25h, also known as FLT3/HDAC-IN-2, is a dual inhibitor of FLT3/HDAC. It exhibits antiproliferative activity against MOLM-13 cells and is used in the study of acute myeloid leukemia.

PROTAC METTL3 degrader 1 (Compound KH12) is a VHL-based degrader of METTL3, demonstrating a DC50 of 220 nM in MOLM-13 cells. This compound inhibits the METTL3/14 complex with an IC50 of 341 nM and exhibits antiproliferative activity against AML cells.

PRMT5-IN-45 (compound 36) is a potent and selective inhibitor of PRMT5, exhibiting an IC50 value of 3 nM. This compound effectively reduces the levels of symmetrical dimethylarginine (sDMA) and inhibits the proliferation of the MOLM-13 cell line by inducing apoptosis and causing cell cycle arrest.

Nampt-IN-15 (Example 3) is a Nampt inhibitor that exhibits cytotoxic effects on various cell lines, including BxPC-3, HepG2, L540cy, and MOLM-13. The respective IC50 values for these cell lines are 38.5 nM, 8 nM, 8.5 nM, and 7 nM.

FLT3-ITD-IN-2 (Compound A1) is an inhibitor of the FLT3-ITD kinase, exhibiting an IC50 of 2.12 nM. It effectively suppresses the proliferation of the FLT3-dependent human AML cell line MOLM-13, with an IC50 of 25.65 nM. FLT3-ITD-IN-2 demonstrates antitumor activity against acute myeloid leukemia.

Antituberculosis agent-13 (Compound 11) demonstrates antituberculosis activity, effectively inhibiting both wild-type and mutant strains of Mycobacterium tuberculosis, with an IC50 range of 4-62.5 nM. Additionally, Antituberculosis agent-13 exhibits anti-leukemia properties, inhibiting MOLM-13 with an IC50 of 3.8 μM.

FW-1 is a type I inhibitor of FLT3, with an IC50 of approximately 1 μM. It exhibits cytotoxic effects in FLT3-mutant AML cells, causes cell cycle arrest at the G0/G1 phase, and induces apoptosis in MV4-11 and MOLM-13 cells.