Tubulin inhibitor 8 is an inhibitor of tubulin and various cancer cell lines and inhibits tubulin polymerisation and K562 cell growth with an IC50 of 0.73 μM and 14 nM respectively.

SJB3-019A is a potent, potent and novel ubiquitin-specific protease 1 (USP1) inhibitor, which promotes ID1 degradation and cytotoxicity in K562 cells 5 times more than SJB2-043, with IC50 of 0.0781 μM. SJB3-019A inhibits cell proliferation and causes cell apoptosis.

Daunorubicin hydrochloride (Rubidomycin hydrochloride), an anthracycline aminoglycoside antineoplastic, inhibits DNA replication and repair and RNA and protein synthesis.

Spautin-1 is a novel autophagy inhibitor, IM inhibited the growth of K562 cells with IC50 of 1.03 μM. In contrast, co-treatment with Spautin-1 increased IM-induced inhibition of cell viability with IC50 of 0.45 μM.

Icaritin (Anhydroicaritin) has hormone regulation activity and cardiovascular function improvement activity. Icaritin has anticancer activity, can induce S phase arrest and apoptosis, inhibit ENKL cell proliferation. Icaritin has anti-multiple myeloma activity, mainly mediated by inhibiting IL-6/JAK2/STAT3 signaling. Icaritin at low concentration (4 or 8 μMol/L) can promote rat chondrocyte proliferation and inhibit cell apoptosis, while the effect of Icaritin on rat chondrocyte at high concentration was reversed.

1. Oroxylin A (Baicalein 6-methyl ether) has various anti-tumor effects including apoptosis, cell cycle arrest, drug-resistant reversion. 2. Oroxylin A possesses abilities of inhibiting the ATRA-induced IL-6 production via modulation of LAP/LIP/CHOP in leukemia cell lines, which could providing a therapeutic strategy for RAS. 3. Oroxylin A inhibits UCP2s triggers the MPTP opening, and promotes the apoptosis in CaCo-2 cells; uncoupling protein 2 plays a key role in mitochondrial apoptotic pathway. 4. Oroxylin A inhibits N1ICD translocating to the nucleus and binding to epithelial-mesenchymal transition-related transcription factor Snail, thus suppressing the invasion and migration of MCF-7 cells. 5. Oroxylin A improves the sensitivity of K562/ADM cells by increasing apoptosis in leukemic cells and decreasing the expression of CXCR4 and PI3K/Akt/NF-κB pathway, and probably served as a most promising agent for CML treatment.

Theasaponin E1 is a saponin derived from tea seeds, demonstrating antitumor potential in human tumor cell lines K562 and HL60. Additionally, it possesses quinone reductase (QR)-inducing activity, suggesting its efficacy as a chemopreventive agent in cancer [1].

Bonducellpin D may show inhibitory activities on the Para3 virus. It also exhibits moderate activity against four tested human cancer cell lines, HepG-2, K562, HeLa, and Du145.

Hygrolidin is a macrocyclic lactone originally isolated from S. hygroscopicus. It inhibits proliferation of a variety of cancer cell lines, including DLD-1 colon cancer, LNCaP prostate cancer, and K562 leukemia cells (IC50s = 2.9, 5.2, and 33 ng/ml, respectively). Hygrolidin induces the expression and levels of p21 in DLD-1 cells, but not WI-38 fibroblasts, and leads to cell accumulation in the G1 and S phases without inducing apoptosis. It has antiparasitic activity against T. cruzi, L. donovani, and T. b. brucei but also induces cytotoxicity in HepG2 cells (IC50s = 1.1, 72.5, 77, and 24.5 nM, respectively).

(+)-Norglaucine shows cytotoxic activity toward the tumor cell lines B16-F10 (mouse melanoma), HepG2 (human hepatocellular carcinoma), K562 (human chronic myelocytic leukemia) and HL-60 (human promyelocytic leukemia) and non-tumor peripheral blood mononuc

Reveromycin A is the major component of a complex of spiroketal antibiotics isolated from Streptomyces sp. It inhibits the mitogenic activity of epidermal growth factor in Balb/MK cells (IC50 = 0.7 μg/ml), displays antiproliferative activity against human KB and K562 tumor cell lines (IC50s = 1.9 and 1.6 μg/ml, respectively), and demonstrates antifungal activity against C. albicans (MIC = 2 μg/ml at pH 3). Reveromycin A also has been shown to inhibit bone resorption by inducing apoptosis in osteoclasts with an IC50 value of 0.7 μM.

2-Desoxy-4-epi-pulchellin has potent in vitro cytotoxicities against the K562, MCF-7, Hela, DU145, U937, H1975, SGC-7901, A549, MOLT-4, and HL60 cell lines with IC50 values ranging from 0.10 to 46.7uM, while it shows significant antiviral (H1N1 and H3N2) activities, it also displays significant antimycobacterial activity (IC50=7.6 uM).

AS-99 TFA is a first-in-class, potent and selective ASH1L histone methyltransferase inhibitor (IC50= 0.79 μM, Kd= 0.89 μM) with anti-leukemic activity. AS-99 TFA blocks cell proliferation, induces apoptosis and differentiation, downregulates MLL fusion target genes, and reduces the leukemia burden in vivo[1]. AS-99 TFA is tested against a panel of 20 histone methyltransferases, including NSD1, NSD2, NSD3, and SETD2. NO significant inhibition is observed at 50 μM of AS-99 TFA on any of the tested histone methyltransferases, indicating over 100-fold selectivity towards ASH1L[1].AS-99 TFA shows effect on the growth of the MLL leukemia cells (MV4;11, MOLM13, KOPN8, RS4;11) with the GI50 values ranging from 1.8 μM to 3.6 μM[1].AS-99 (1-8 μM; 7 days) TFA also induces apoptosis in the MLL leukemia cells, but not in the K562 cells, as assessed by the quantification of the Annexin V positive cells[1].AS-99 TFA suppresses MLL fusion driven transcriptional programs[1]. AS-99 (30 mg/kg; i.p.; q.d., treated for 14 consecutive days) TFA reduces leukemia burden in mice[1].AS-99 TFA is used for in vivo studies in mice, which reveals favorable exposure in plasma upon i.v. and i.p. administration (AUC = 9701 hr* ng/mL and 10,699 hr* ng/mL, respectively), suitable half-life (~5-6 h) and Cmax >10 μM[1]. [1]. David S. Rogawski, Jing Deng, Hao Li, Tomasz Cierpicki, Jolanta Grembecka, et al. Discovery of first-in-class inhibitors of ASH1L histone methyltransferase with anti-leukemic activity. Nat Commun. 2021 May 14;12(1):2792.

S-30-Hydroxygambogic acid, a polyprenylated xanthone epimer isolated from the gamboges of Garcinia hanburyi, exhibits cytotoxicity against Human Leukemia K562 cell lines with IC50 values of 4.49 μM for K562/R and 3.61 μM for K562/S. This compound is utilized in cancer research [1].

Tubulin inhibitor 6 (iHAP1) is an inhibitor of tubulin and a potent inhibitor of multiple cancer cell lines.

R-30-Hydroxygambogic acid, a polyprenylated xanthone epimer isolated from the gamboge of Garcinia hanburyi, exhibits cytotoxicity against human leukemia K562 cell lines, with IC50 values of 2.89 μM for the resistant strain (K562/R) and 1.27 μM for the sensitive strain (K562/S). This compound is utilized in cancer research [1].

Cisplatin-resistant cells-IN-1 (Compound 8) exhibits high cytotoxicity against Cisplatin-resistant cells and effectively diminishes metabolic activity at low nanomolar concentrations, with an IC50 ranging from 0.14 to 1.79 μM in various resistant cell lines, including A549/A549-R, K562/K562-R, and MCF-7/MCF-7TamR [1].

Danshenol A has strong aldose reductase (AR) inhibitory activity, has IC50 of 0.10 microM which is comparable to that of epalrestat in clinical use. Danshenol A also has antitumor activity in T-24, QGY, K562, Me180 and BIU87 cell lines, shows inhibited growth of K562 (IC50 = 0.53 μg/mL), T-24 (IC50 = 7.94 μg/mL), QGY (IC50 = 4.65 μg/mL) and Me180 (IC50 = 6.89 μg/mL) cell lines.

Ladanein is a phytochemicals inhibitor that is known to disrupt the interactions of core and other hepatitis C virus (HCV) proteins.Ladanein possesses free radicals DPPH and ABTS +.scavenging activity, it also displays moderate (20-40 microM) activities against K562, K562R (imatinib-resistant), and 697 human leukemia cell lines.

MET/PDGFRA-IN-1 (compound 8c) serves as an inhibitor of MET and PDGFRA proteins, displaying an IC50 of 36 μM against MET. It impedes MET phosphorylation, thereby promoting apoptosis, and curtails the proliferation of various MET-positive cell lines, with IC50 values of 15.3 μM for AsPc-1, 19.0 μM for EBC-1, 22.0 μM for MKN-45, 25.6 μM for Mia-Paca-2, 21.0 μM for HT-29, and 31.5 μM for K562 [1].

1. Kirenol (Kirel) has anti-oxidant, anti-inflammatory, anti-allergic, and anti-arthritic activities. 2. Kirenol is effective against gram-positive bacteria. 3. Kirenol possesses antitumor action on human chronic myeloid leukemia K562 cells in vitro. 4. Kirenol is capable of promoting osteoblast differentiation in MC3T3-E1 cells through activation of the BMP and Wnt/β-catenin signaling pathways. 5. Kirenol treatment reduces pro-inflammatory cytokine secretion, increases anti-inflammatory cytokine production, inhibits cell proliferation and induces apoptosis of CII-specific lymphocytes in vitro.

Tubulin polymerization-IN-9 is a potent inhibitor of tubulin (IC50: 1.82 μM). Tubulin polymerization-IN-9 arrests the cell cycle of K562 cells in G2/M phase and induces apoptosis and mitochondrial depolarization. Tubulin polymerization-IN-9 exhibits potent anti-vascular and anti-tumour effects.

MOZ-IN-3 (Compound 6j), a potent KAT6A (MOZ) acetyltransferase inhibitor with an IC50 of 30 nM, exhibits antitumor activity against multiple myeloid leukemia cell lines, including HL-60, U937, SKNO-1, and K562. This compound also demonstrates favorable metabolic stability and pharmacokinetics [1].

BCR-ABL-IN-4 is a BCR-ABLL inhibitor that exhibits anticancer activity.BCR-ABL-IN-4 has an inhibitory effect on cancer cell growth and is able to act on K562 cells (IC50: 0.67 nM) and BCR-ABL T315I-transfected Ba/F3 cells (IC50: 16 nM).

Cu(II)-Elesclomol is a complex formed by the anticancer agent Elesclomol and Cu(II), which selectively transports copper to mitochondria.Cu(II)-Elesclomol has anticancer activity, inhibits the growth of human leukemia K562 cells, and induces cell-cycle arrest, and is used in the study of leukemias.

Antiproliferative agent-30 (Compound 8g) demonstrates broad-spectrum antiproliferative activity, with IC50 values of 0.054 nM, 0.008 nM, and 0.144 nM against HCT-116, K562, and MV-4-11 cancer cell lines, respectively. It inhibits tubulin assembly as well as FLT3 and Abl1 kinases and exhibits vascular-disrupting capabilities. Additionally, it exerts an anticancer effect against acute myeloid leukemia (AML) with FLT3-ITD-TKD mutations [1].

GNF-2 is a highly selective non-ATP competitive inhibitor of Bcr-Abl.

7-oxo Staurosporine is an antibiotic originally isolated from S. platensis with diverse biological activites. It inhibits PKC, PKA, phosphorylase kinase, EGFR, and c-Src in vitro (IC50s = 9, 26, 5, 200, and 800 nM, respectively). 7-oxo Staurosporine induces cell cycle arrest in the G2/M phase in human leukemia K562 cells with a minimal effective dose (MED) of 30 ng/ml. It is cytotoxic to P388 mouse leukemia cells that are resistant and susceptible to doxorubicin . 7-oxo Staurosporine inhibits growth of the mycelial, but not yeast form of C. albicans, C. krusei, C. tropicalis, and C. lusitaniae (MICs = 3.1-25 μg/ml). It increases sphingomyelin synthesis in CHO-K1 cells when used at a concentration of 50 nM.

Hispidanin B shows significant cytotoxicities against tumor cell lines SGC7901, SMMC7721, and K562, with IC50 values of 10.7, 9.8, and 13.7 uM, respectively.

Eupahualin C shows significant activities against cell lines of human chronic myelogenous leukemia (K562) and human bone cancer (U2OS).

AS-99 is a first-in-class, potent and selective ASH1L histone methyltransferase inhibitor (IC50= 0.79 μM, Kd= 0.89 μM) with anti-leukemic activity. AS-99 blocks cell proliferation, induces apoptosis and differentiation, downregulates MLL fusion target genes, and reduces the leukemia burden in vivo[1]. AS-99 is tested against a panel of 20 histone methyltransferases, including NSD1, NSD2, NSD3, and SETD2. NO significant inhibition is observed at 50 μM of AS-99 on any of the tested histone methyltransferases, indicating over 100-fold selectivity towards ASH1L[1].AS-99 shows effect on the growth of the MLL leukemia cells (MV4;11, MOLM13, KOPN8, RS4;11) with the GI50 values ranging from 1.8 μM to 3.6 μM[1].AS-99 (1-8 μM; 7 days) also induces apoptosis in the MLL leukemia cells, but not in the K562 cells, as assessed by the quantification of the Annexin V positive cells[1].AS-99 suppresses MLL fusion driven transcriptional programs[1]. AS-99 (30 mg/kg; i.p.; q.d., treated for 14 consecutive days) reduces leukemia burden in mice[1].AS-99 is used for in vivo studies in mice, which reveals favorable exposure in plasma upon i.v. and i.p. administration (AUC = 9701 hr* ng/mL and 10,699 hr* ng/mL, respectively), suitable half-life (~5-6 h) and Cmax >10 μM[1]. [1]. David S. Rogawski, Jing Deng, Hao Li, Tomasz Cierpicki, Jolanta Grembecka, et al. Discovery of first-in-class inhibitors of ASH1L histone methyltransferase with anti-leukemic activity. Nat Commun. 2021 May 14;12(1):2792.

CML-IN-1, also known as compound 7 and compound 4, is a potent anticancer agent that demonstrates a strong induced-apoptosis effect in the human chronic myeloid leukemia (CML) cell line K562. It diminishes protein phosphorylation within the PI3K/Akt signaling pathway to exert its effects and suppresses cell proliferation through the inhibition of the MEK/ERK signaling pathway in colorectal cancer [1] [2].

JNK-IN-14 is a potent inhibitor of JNK with IC50 values of 1.81 nM for JNK1, 12.7 nM for JNK2, and 10.5 nM for JNK3. It induces early-stage apoptosis, arrests cell population at the G2/M phase, and moderately inhibits beclin-1 production in K562 leukemia cells, demonstrating greater inhibitory efficacy than SP600125. [1]

8-Chloroadenosine-5’-triphosphate (8-chloro ATP), a potent metabolite of the anticancer agent 8-chloro cyclic AMP (cAMP) and a nucleotide derivative, is produced through the biotransformation of 8-chloro cAMP into 8-chloroadenosine, followed by mono- and diphosphate intermediates. Accumulating for up to 12 hours after the administration of 8-chloro cAMP or 8-chloroadenosine, 8-chloro ATP inhibits cell growth, diminishes endogenous ATP levels, and reduces RNA synthesis without affecting DNA synthesis in multiple myeloma cells derived from patients. Moreover, it obstructs topoisomerase II-α-mediated relaxation of supercoiled pUC19 DNA at concentrations ranging from 1.5 to 8 mM and decreases topoisomerase II-α-enhanced ATP hydrolysis by 50% at a concentration of 1 mM in K562 human myelocytic leukemia cells.

Enmein shows significant inhibitory effect toward human tumor cell K562 with IC(50) values ranging from 3.2 microg/ml to 8.2 microg/ml

CAY10503 is a proapoptotic, antiproliferative compound that is able to arrest cell cycle progression in the G0-G1 phase. CAY10503 inhibits the growth of HL60, multidrug resistant HL60R, and K562 cells with IC50 values of 7.0, 23, and 20 μM, respectively. Accumulation of HL60 cells in G0-G1 occurred within eight hours following treatment with 50 μM CAY10503, whereas 10 μM CAY10503 required 96 hours for cell cycle arrest to appear. CAY10503 also induces differentiation of HL60 cells into the following positive cells: CD14 (monocytic marker) as well as CD11b and CD11c (granulocytic markers). Approximately 60% of HL60 cells exposed to 10 μM CAY10503 expressed these markers within 72 hours.

MPT0B206 is a novel tubulin polymerization inhibitor. MPT0B206 induced G2/M cell cycle arrest and the appearance of the mitotic marker MPM-2 in K562 and K562R cells, which is associated with the upregulation of cyclin B1 and the dephosphorylation of Cdc2.

Tubulin inhibitor 7 is an inhibitor of tubulin and a potent inhibitor of multiple cancer cell lines (tubulin polymerization (IC50: 0.52 μM), K562 cell growth (IC50: 11 nM)).

16-Hydroxycleroda-3,13-dien-15,16-olide, and prodigiosin are presented as candidates for autophagy inducers that can trigger cell death in a supplement or alternative medicine for cancer therapy. 16-Hydroxycleroda-3,13-dien-15,16-olide regulates the expre

Paris saponin VII (Dioscini) shows inhibitory effects on cell proliferation.

Scutebarbatine B shows weak cytotoxicity with IC50 values ranging from 35.11 to 42.73 μM against K562 cell lines and HL60 cell lines.

Pixantrone dimaleate (Pixantrone Maleate) (BBR 2778 dimaleate) is an experimental antineoplastic drug.

Scutebata E shows weak cytotoxicity with IC50 values ranging from 35.11 to 42.73 μM against K562 cell lines.

1. Crebanine iv 5mg/kg can eonvert BaCl_2-induced arrhythmia into sinus rhythm in rats, and can significantly increase the tolerant dose of aconitine to produce ventrieular fibrillation(VF) and cardiac arrest (CA) in rata. 2. Crebanine can also decrease t