mm.1s

Fludarabine (Fludarabinum) is a fluorinated purine analog, an inhibitor of nucleic acid synthesis and an inhibitor of STAT1 activation. Fludarabine has antitumor activity and can be used for the treatment of leukemia and lymphoma.

Lenalidomide (CC-5013) is an immunomodulator with oral activity. Lenalidomide is a ligand for the ubiquitin E3 ligase cereblon (CRBN), which selectively ubiquitinates and degrades two lymphoid transcription factors, IKZF1 and IKZF3, via the CRBN-CRL4 ubiquitin ligase, and is commonly used in the synthesis of PROTAC products.

AVN-944 (VX-944)(VX-944) is a selective, noncompetitive inhibitor of human IMPDH with Ki of 6-10 nM for IMPDH1 IMPDH2.

8-Chloroadenosine (NSC-354258) is a 5' AMP-activated protein kinase agonist potentially for the treatment of chronic lymphocytic leukemia. 8-chloroadenosine activity is associated with inhibition of the mTOR pathway.8-Chloroadenosine (NSC-354258) is a nucleoside analog; metabolized in vivo to 8-Chloro-ATP. Incorporates into RNA during transcription and inhibits RNA synthesis. Exhibits cytotoxicity in MM.1S, RPMI-8226, and U266 cancer cell lines; induces G2 M cell cycle arrest and mitotic catastrophe in A549 and H1299 cells. 8-Chloroadenosine (NSC-354258) has been shown to deplete ATP and inhibit tumor growth in hematological malignancies as well as in lung and breast cancer cell lines.

USP7-IN-16 (Compound 61) is a selective inhibitor of USP7, with IC50 values of 5.5 nM in the FLINT assay and 2.1 nM in MM.1S cells. This compound exhibits antitumor activity in mice and holds potential for research in the field of oncology.

CST 530 is a monovalent IAP antagonist. It induces cIAP1 and cIAP2 autodegradation in MM.1S cells (cIAP1 degradation at 0.1 μM and cIAP2 degradation at 1 μM after 16 hours). CST 530 reduces cell viability in multiple cancer cell lines including SUDHL6, MOLM13, and HEL (IC50 values ​​of 170 nM, 420 nM, and 450 nM, respectively).

FF2039 (compound 1j) is a PROTAC degrader specifically targeting HDAC1, HDAC6, and various subtypes of class I, IIa, and IIb HDACs. It induces cell cycle arrest and apoptosis, showing significant antiproliferative activity against both hematological and solid tumor cell lines. The IC50 values for FF2039 against HDAC1, HDAC2, HDAC4, and HDAC6 are 1.03, 2.15, 12.4, and 0.053 μM, respectively. FF2039 exhibits antiproliferative effects on solid tumors such as MM.1S, MDA-MB-231, and U-87MG, with EC50 values of 2.8, 28, and 30 μM, respectively.

Abz-Ala-Pro-Glu-Glu-Ile-Met-Arg-Arg-Gln-EDDnp is a fluorescence-quenched peptide substrate for human neutrophil elastase (kcat/Km = 531 mM-1s-1). Enzymatic peptide hydrolysis disrupts the Abz:EDDnp donor-acceptor pair allowing fluorescence measurement of Abz (ex = 320 nm; em = 420 nm).

Abz-Val-Ala-Asp-Nva-Arg-Asp-Arg-Gln-EDDnp is a fluorescence-quenched peptide substrate for human proteinase 3 (kcat/Km = 1,570 mM-1s-1). Enzymatic peptide hydrolysis disrupts the Abz:EDDnp donor-acceptor pair allowing fluorescence measurement of Abz (ex = 320 nm; em = 420 nm).

TMX-4100 is a potent degrader of phosphodiesterase 6D (PDE6D), exhibiting high degradation selectivity towards PDE6D with DC50 values below 200 nM in MOLT4, Jurkat, and MM.1S cells. This compound holds significant potential for research pertaining to multiple myeloma.

TMX-4116, a casein kinase 1α (CK1α) degrader, preferentially degrades CK1α in MOLT4, Jurkat, and MM.1S cells, exhibiting degradation concentration 50s (DC50s) below 200 nM. TMX-4116 is utilized in the research of multiple myeloma [1].

XPO1-IN-1 is an orally active XPO1 inhibitor capable of acting on MM.1S cells (IC50: 24 nM). XPO1-IN-1 effectively induces cell cycle arrest and apoptosis. XPO1-IN-1 exhibits good metabolic stability and pharmacokinetic properties. XPO1-IN-1 can be used to study multiple myeloma.

PC-046 is a potent tubulin-binding agent, which was originally identified for development based on selective activity in deleted in pancreas cancer locus 4 (DPC4 SMAD4) deficient tumors. PC-046 has growth inhibitory activity in a variety of tumor types in vitro, and efficacy in SCID mice was shown in human tumor xenografts of MV-4-11 acute myeloid leukemia, MM.1S multiple myeloma, and DU-145 prostate cancer. Pharmacokinetic studies demonstrated relatively high oral bioavailability (71 %) with distribution to both plasma and bone marrow. No myelosuppression was seen in non-tumor bearing SCID mice given a single dose just under the acute lethal dose. The COMPARE algorithm in the NCI-60 cell line panel demonstrated that PC-046 closely correlated to other known tubulin destabilizing agents (correlation coefficients ≈0.7 for vincristine and vinblastine). Mechanism of action studies showed cell cycle arrest in metaphase and inhibition of tubulin polymerization. Overall, these studi......

Proteasome-IN-4, a non-covalent proteasome inhibitor (IC 50 = 8.39 nM), exhibits potent antiproliferative effects on RPMI-8226, MM-1S, and MV-4-11 cell lines, making it valuable for cancer research.

PROTAC pan-IAP degrader-1 (Compound 9) is a pan- IAP degrader PROTAC . PROTAC pan-IAP degrader-1 degrades XIAP , cIAP1 and cIAP2 with DC 50 s of 0.7, 2.4, and 6.2 nM in MM.1S cells, respectively [1] .

HDAC6-IN-18 (Compound 4), an irreversible and selective HDAC6 isoform inhibitor, exhibits potent anti-multiple myeloma effects. It demonstrates HDAC6 inhibitory activity with IC50 values of 0.17, 0.7, and 0.42 μM in RPMI8266, U266, and MM.1S cells, respectively [1].

UNC8153 TFA is a selective and potent NSD2 protein degrader with anticancer activity.UNC8153 TFA induces NSD2 degradation in MM.1S multiple myeloma cells and inhibits the proliferation of MM.1S cells.

LSD1 HDAC6-IN-2 (JBI-802) is an orally effective inhibitor targeting LSD1, HDAC6, and MAO-A, demonstrating IC50 values of 5 nM, 11 nM, and 5 nM, respectively. This compound effectively suppresses the growth of multiple myeloma cells, including MM.1S, MM.1R, and RPMI-8226. Additionally, LSD1 HDAC6-IN-2 is utilized for researching acute myeloid leukemia and lymphoma.