h929

Iberdomide (CC-220) is a modulator of cereblon( IC50 value of 60 nM in a competitive TR-FRET assay).

CDK9-IN-2 is a specific CDK9 inhibitor with an IC50 of 5 nM in the A2058 skin cell line (72 hours) and 7 nM in the H929 multiple myeloma cell line (72 hours).

rac-CCT-250863 HCl is a selective and reversible inhibitor of NEK 2. rac-CCT-250863 HCl induces cell cycle arrest and has good anti-proliferative activity against cancer cells. rac-CCT-250863 HCl can be used in combination with Pomalidomide to induce apoptosis and can be used in combined anti-cancer studies.

Mcl-1 inhibitor19 (compound 26) binds to Mcl-1 with a Ki of 86 pM and inhibits the growth of H929 cells with a GI50 of 43 nM.

PROTAC SMARCA2-degrader-36 (compound 38) is an SMARCA2 degrader that achieves a 99% degradation rate at 100 nM in H929 cells. It possesses antiproliferative activity and is used in cancer research.

PROTAC CARM1/IKZF3 degrader-1 (Compound 074) inhibits CARM1, reducing the methylation level of its substrate BAF155. This PROTAC degrader works by degrading IKZF 1/3 via a CRBN-dependent mechanism. It suppresses MYC protein expression, thereby inhibiting the proliferation of various multiple myeloma cells. Additionally, PROTAC CARM1/IKZF3 degrader-1 can induce apoptosis in H929 cells and overcomes resistance to immunomodulatory drugs (IMiDs, such as pomalidomide). It is applicable for cancer and immunology research. (Pink: ligand for target protein CARM1/IKZF3 ligand 1; Active form of target protein ligand: EZM 2302; Black: linker; Blue: ligand for E3 ligase Cereblon Thalidomide 4-fluoride)

TAK1-IN-5 (Compound 26) is an inhibitor of transforming growth factor-β activated kinase (TAK1) with an IC50 value of 55 nM. It effectively suppresses the growth of MPC-11 and H929 cells, with a GI50 below 30 nM. TAK1-IN-5 is a useful tool for research in multiple myeloma.

GQN-B37-Me is an MCL-1 inhibitor that can induce caspase-dependent apoptosis. It exhibits significant cytotoxicity in H929 (IC50= 3.71 μM) and MV-4-11 (IC50= 5.57 μM) cell lines. GQN-B37-Me is useful for leukemia research.

KZR-261 is a Sec61 inhibitor that directly binds to the Sec61 channel, effectively impeding the synthesis of certain Sec61 client proteins. It exhibits broad anti-tumor activity, particularly against colorectal, pancreatic, and prostate cancers, activating the endoplasmic reticulum stress response while showing minimal adverse effects on normal cells. KZR-261 significantly induces apoptosis in H929 cells and effectively suppresses tumor growth in various xenograft mouse models, demonstrating good tolerability.

MGD-22 is a molecular glue and orally active degrader of IKZF1/2/3, with DC50 values of 8.33 nM, 9.91 nM, and 5.74 nM, respectively. It exhibits strong anti-proliferative activity against various hematological cancer cells and induces cell apoptosis (apoptosis). MGD-22 demonstrates significant anti-tumor efficacy in mice with NCI-H929 or WSU-DLCL-2 xenografts. This compound is useful for researching blood cancers, including multiple myeloma (MM), acute myeloid leukemia (AML), and diffuse large B-cell lymphoma (DLBCL).

Mcl-1-IN-17 (Compound 25) is an orally active inhibitor of myeloid cell leukemia 1 protein (Mcl-1), with a Ki of less than 0.08 nM. It exhibits significant antiproliferative activity with GI50 values of 39 nM in H929 cells and 105 nM in A427 cells, and it inhibits apoptosis. This compound is suitable for research in hematological and solid tumors.

Gusacitinib, also known as ASN-002 and EN-3351, is a potent dual inhibitor of SYK/JAK kinases. ASN002 showed strong antitumor activity in both hematological and solid tumor xenograft models. ASN002 strongly suppressed the SYK and JAK family kinase signaling pathways as measured in pLAT and pSTAT assays, respectively. When profiled in a panel of 178 cell lines, ASN002 showed strong anti-proliferative activity in many lymphoid/leukemia cell lines, including SU-DHL-6, SU-DHL-4, OCI-LY10, H929 and Pfeiffer.

A-1208746 is an inhibitor of MCL-1 with a Ki value of 0.454 nM. This compound effectively activates caspase-3/-7, induces apoptosis in H929 cells, and reduces mitochondrial membrane potential. Additionally, A-1208746 synergizes with Navitoclax, making it applicable in cancer research.

GBR-1342 is a human bispecific antibody targeting CD38 and CD3. It inhibits the activity of cancer cell lines Daudi, RAJI, RPMI8226, IM-9, and NCI-H929, and is applicable to multiple myeloma research.