acute lymphoblastic leukemia

L-Asparaginase (L-ASNase) (L-ASNase), a hydrolase that catalyzes the conversion of L-asparagine, used in acute lymphoblastic leukemia treatment.Asparaginase is an enzyme that is used as a medication. As a medication, L-asparaginase is used to treat acute lymphoblastic leukemia (ALL), acute myeloid leukemia (AML), and non-Hodgkin's lymphoma. It is given by injection into a vein, muscle, or under the skin.

Pheniramine maleate (Trimetose), an alkylamine derivative with antihistaminic and vasodilatory properties, binds to histamine H1 receptors, thereby inhibiting phospholipase A2 and production of the endothelium-derived relaxing factor, nitric oxide.

Revumenib (SNDX-5613) is a potent and selective oral inhibitor of menin-KMT2A interaction with Ki of 0.149 nM and IC50 between 10 and 20 nM, which can be used in the study of acute leukemia with MLL gene rearrangement.

(Rac)-SHIN2, a serine hydroxymethyltransferase (SHMT) inhibitor, enhances NOTCH1-driven in vivo survival of primary T-ALL in mice and is useful for studying T-cell acute lymphoblastic leukemia (T-ALL).

Pivanex (Pivalyloxymethyl butyrate) is an orally active HDAC inhibitor and an antimetastatic and antiangiogenic agent. Pivanex downregulates the Bcr-Abl protein and enhances apoptosis.

USP7-IN-4(USP7 inhibitor ALM4) is a non-competitive, potent and selective inhibitor of USP7 (ubiquitin-specific protease 7) with an IC50 = 6 nM, up-regulates p53 and p21, down-regulates MDM2, increases the level of ubiquitination of MDM2, and exhibits anti-proliferative activity in a variety of cancer cell lines, with an EC50 = 2.0 nM in RS4;11 (acute lymphoblastic leukemia cell line) .

CAD204520 functions as an inhibitor of SERCA (IC50 = 0.34 μM), specifically targeting mutations in the wild-type NOTCH1 protein associated with T-cell acute lymphoblastic leukemia (T-ALL) and mantle cell lymphoma (MCL).

Revumenib (also known as SNDX-5613) is an effective and selective Menin-MLL inhibitor. It is primarily used for the study of MLL-rearranged (MLL-r) acute leukemias, including acute lymphoblastic leukemia (ALL) and acute myeloid leukemia (AML).

AcBut-N-Ac-γ-Calicheamicin serves as a toxic molecule for ADCs, inducing cell cycle arrest and apoptosis (Apoptosis) by causing DNA double-strand breaks. Primarily utilized in the synthesis of antibody-drug conjugates (ADC), it holds promise for cancer research, particularly in studies related to acute lymphoblastic leukemia (ALL) and other hematological malignancies.

PKN3-IN-1 (compound 16) inhibits PKN3 (serine/threonine-protein kinase N3) and GAK (cyclin G-associated kinase) with an IC50 of 0.014 μM and a Ki of 0.0044 μM. PKN3-IN-1 is a potential tool compound for investigating the cell biology of PKN3 and its role in pancreatic and prostate cancers, as well as T-cell acute lymphoblastic leukemia.

Proteasome-IN-7 (Compound 6f) is a macrolactam-based epoxyketone proteasome inhibitor with an IC50 value of 37.92 nM against the 20S proteasome ChT-L subunit. It exhibits potent antiproliferative effects on multiple myeloma, acute lymphoblastic leukemia, and non-small cell lung cancer.

Metanilic acid, an anti-cancer drug, is used to treat several malignancies including choriocarcinoma and pediatric acute lymphoblastic leukemia.

4'-Ethynyl-2'-deoxycytidine is an anticancer nucleoside used in research on acute lymphoblastic leukemia and diffuse large B-cell lymphoma.

Lck-IN-3 (compound 7m) is an LCK inhibitor that targets acute lymphoblastic leukemia (ALL) by inhibiting LCK phosphorylation. Lck-IN-3 can induce cell cycle arrest at the G2/M phase, leading to apoptosis in ALL cells.

SJ45566 is an effective, orally active LCK PROTAC degrader with a DC50 value of 1.21 nM, suitable for research in acute T-cell lymphoblastic leukemia.

KI-TOX-A3 is a selective protein-protein interaction (PPI) inhibitor targeting the TOX protein, with an IC50 value of 0.51 μM for the TOX-KAT7 interaction. It promotes proteasomal degradation of TOX, restores KAT7-mediated H3K14 acetylation, reverses CD8+ T cell exhaustion, and inhibits proliferation of T-cell acute lymphoblastic leukemia (T-ALL) cells. KI-TOX-A3 holds potential for research in hematological malignancies, including T-ALL.

I3IN-002 is a small molecule inhibitor targeting the RNA-binding protein IGF2BP3, with an IC50 value of approximately 2 μM in SEM cells. It disrupts the interaction with m6A-modified mRNA, destabilizing target genes (such as CDK6, MYC, and BCL2), thereby inhibiting the growth of leukemia cells, inducing cell cycle arrest, and promoting apoptosis. I3IN-002 shows potential for research in B-cell acute lymphoblastic leukemia.

Lckdegrader-1 (Compound 17) is a molecular glue degrader that targets lymphocyte-specific protein tyrosine kinase (LCK) with a DC50 of 23.1 nM. It holds potential for research in T-cell acute lymphoblastic leukemia (T-ALL).

LCKdegrader-2 (Compound 17) is a Lck molecular glue degrader. It is applicable for research in cancers such as acute lymphoblastic leukemia (ALL).

FCN-338 (LOXO-338) is an orally active and selective Bcl-2 inhibitor, exhibiting an IC50 of 4.5 nM for the Bcl-2/BAK interaction. It effectively suppresses tumor growth in mouse models of follicular lymphoma (FL), acute myeloid leukemia (AML), and acute lymphoblastic leukemia (ALL) xenografts without causing significant weight loss. FCN-338 demonstrates broad-spectrum anticancer activity, making it suitable for treating FL, chronic lymphocytic leukemia (CLL)/small lymphocytic leukemia (SLL), AML, and ALL.

Menin-MLL inhibitor MI-2 dihydrochloride is a competitive and selective inhibitor of the Menin-MLL interaction, with an IC50 value of 446 nM and a Ki value of 158 nM. It reduces the expression of target genes such as HOXA9 and MEIS1, inhibits the proliferation of leukemic cells, and induces apoptosis and differentiation. Menin-MLL inhibitor MI-2 dihydrochloride shows potential for research in MLL-rearranged acute leukemias, such as acute myeloid leukemia and acute lymphoblastic leukemia.

SJ11646 is a Dasatinib-based LCK PROTAC degrader with a DC50 of 0.00838 pM. It exhibits potent cytotoxicity against LCK-activated T-cell acute lymphoblastic leukemia (T-ALL) cells and primary leukemia samples, significantly prolongs LCK signal inhibition, and induces apoptosis in T-ALL cells. SJ11646 binds with high affinity to 51 human kinases, particularly ABL1, KIT, and DDR1. In mouse models of T-ALL, SJ11646 demonstrates exceptional anti-leukemic efficacy.

ASX-173 is an orally active asparagine synthetase (ASNS) inhibitor with an IC50 of 0.113 μM and a Ki of 0.4 nM. It enhances the anticancer activity of L-Asparaginase (ASNase). When combined with ASNase, ASX-173 disrupts nucleotide synthesis and induces cell cycle arrest, apoptosis (apoptosis), and autophagy (autophagy) in leukemia cells. This combination also slows the growth of OCI-AML2 xenograft tumors. ASX-173 is applicable in research on acute lymphoblastic leukemia, acute myeloid leukemia, colorectal cancer, and other cancers.

Tubulin polymerization-IN-84 can inhibit the polymerization process of tubulin (Tubulin) by targeting the colchicine-binding pocket, with an IC50 value of 10.9 μM. Tubulin polymerization-IN-84 exhibits antiproliferative activity against four cell lines, namely Jurkat, B16-F10, HCT116 and MDA-MB-231, with corresponding IC50 values of 60 nM, 380 nM, 138 nM and 1.054 μM, respectively. In B16-F10 cells, Tubulin polymerization-IN-84 can induce G2/M phase cell cycle arrest and further trigger cell apoptosis. In addition, in the B16-F10 melanoma model, it can effectively inhibit the growth of tumor tissue; when combined with PD-L1 monoclonal antibody, it can also enhance the in vivo anti-tumor immune response, and can be used in the related research fields of T-cell acute lymphoblastic leukemia, melanoma, colon cancer and breast cancer.