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Results for "

antiproliferative

" in MCE Product Catalog:

572

Inhibitors & Agonists

8

Peptides

1

Inhibitory Antibodies

92

Natural
Products

1

Recombinant Proteins

19

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas
  • HY-147776
    Antiproliferative agent-8

    MDM-2/p53 Cancer
    Antiproliferative agent-8 (Compound 5a) is an anti-cancer agent. Antiproliferative against-8 has antiproliferative activity. Antiproliferative agent-8 significantly increases the P53 levels.
  • HY-128224
    Antiproliferative agent-13

    Others Cancer
    Antiproliferative agent-13 (compound 16c) shows an antiproliferative activity against human A375 cells with an IC50 value of 32.7 nM. Antiproliferative agent-13 can be used for the research of cancer.
  • HY-146103
    Antiproliferative agent-7

    Apoptosis Reactive Oxygen Species Cancer
    Antiproliferative agent-7 (compound 8f) is a potent anti-proliferative agent. Antiproliferative agent-7 has antiproliferative activity against cancer cell lines MCF-7, MDA-MB-231, HCT-116 and FR-2 with IC50s of 3.5 μM, 15.54 μM, 30.43 μM and 34.8 μM, respectively. Antiproliferative agent-7 can increase ROS production and induce apoptosis.
  • HY-150968
    Antiproliferative agent-11

    Apoptosis Cancer
    Antiproliferative agent-11 (compound 7) is an antiproliferative and selective Ruthenium(II)-Tris-pyrazolylmethane complex. Antiproliferative agent-11 shows antiproliferative activity towards MCF-7, HeLa, 518A2, HCT116 and RD with IC50s of 6, 10, 6.8, 6.7 and 6 μM, respectively. Antiproliferative agent-11 can be used for the research of cancer.
  • HY-145866
    Antiproliferative agent-3

    Others Cancer
    Antiproliferative agent-3 (comp 4) shows the highest potency for MCF-7 cells (IC50 = 0.19 nM).
  • HY-146454
    Antiproliferative agent-6

    Others Cancer
    Antiproliferative agent-6 (compound 8a) is a potent antitumor agent. Antiproliferative agent-6 has antiproliferative activity against cancer cell lines HCT116, MCF-7, H460 and non-tumor aneuploid immortal keratinocyte HaCaT cells with GI50s of 0.5 μM, 2 μM, 0.7 μM and 3.5 μM, respectively.
  • HY-148265
    Antiproliferative agent-14

    Microtubule/Tubulin Cancer
    Antiproliferative agent-14 (compound 3b) a potent tubulin polymerization inhibitor, with an IC50 of 3.41 μM. Antiproliferative agent-14 has excellent antiproliferative activity. Antiproliferative agent-14 possess the ability to arrest cells at G2/M phases of the cell cycle.
  • HY-146354
    Antiproliferative agent-4

    Apoptosis Reactive Oxygen Species Cancer
    Antiproliferative agent-4 (compound 2y) has excellent anti-proliferative activity against certain cancer cell lines. Antiproliferative agent-4 reduces the mitochondrial membrane potential, and increases the apoptosis rate and the level of ROS on EC109. Antiproliferative agent-4 inhibits tumour growth in nude mice, with low toxicity.
  • HY-W278944
    Antiproliferative agent-15

    Others Cancer
    Antiproliferative agent-15 is an anticancer agent. Antiproliferative agent-15 shows antiproliferative activity against human colon (HCT116 and HCT15) and brain (LN-229 and GBM-10) cancer cell lines.
  • HY-146390
    Antiproliferative agent-5

    Autophagy Reactive Oxygen Species Cancer
    Antiproliferative agent-5 (compound 4o) can significantly and irreversibly inhibit proliferation of gastric cancer cells. Antiproliferative agent-5 causes the G2/M phase arrest, and induces ROS accumulation and activation of autophagy. Antiproliferative agent-5 can be used for researching anticancer.
  • HY-150966
    Antiproliferative agent-10

    Mitochondrial Metabolism
    Antiproliferative agent-10 (compound 8) is an anti-tumour ruthenium(II)-tris-pyrazolylmethane complex that inhibits the growth of cancer cells by inhibiting mitochondrial calcium uptake.
  • HY-150969
    Antiproliferative agent-12

    Mitochondrial Metabolism Cancer
    Antiproliferative agent-10 (compound 1) is an anti-tumour ruthenium(II)-tris-pyrazolylmethane complex that inhibits the growth of cancer cells by inhibiting mitochondrial calcium uptake.
  • HY-N8174
    Valeriandoid F

    NO Synthase Cancer Inflammation/Immunology
    Valeriandoid F is an iridoid, which potently inhibits NO production with an IC50 value of 0.88 μM. Valeriandoid F has anti-inflammatory and antiproliferative activities.
  • HY-123056
    EAD1

    Autophagy Apoptosis Cancer
    EAD1 is a potent autophagy inhibitor with antiproliferative activity in lung and pancreatic cancer cells. EAD1 also induces apoptosis.
  • HY-N7338
    Yadanziolide C

    Others Cancer
    Yadanziolide C is a quassinoid with antiproliferative and differentiation-inducing properties in promyelocytic HL-60 cells.
  • HY-146082
    (Z)-α-Cyanostilbene

    Others Cancer
    (Z)-α-Cyanostilbene (compound 8), a dicyano substituted acrylonitrile, shows selective antiproliferative activity against HeLa and HepG2 cells, with IC50s of 0.33 and 0.52 μM, respectively.
  • HY-148185
    T01-1

    Others Cancer
    T01-1 is an anticancer agent (camptothecin derivative) with good anti-proliferative activity.
  • HY-146184
    CCT373567

    Bcl-2 Family Cancer
    CCT373567 is a potent degrader of transcriptional repressor BCL6, with an IC50 of 2.9 nM. CCT373567 exhibits antiproliferative activity.
  • HY-150051
    IL-2-IN-1

    Interleukin Related Inflammation/Immunology
    IL-2-IN-1 is a potent IL-2 inhibitor with an IC50 value of 1978 nM. IL-2-IN-1 shows antiproliferative activities.
  • HY-111525
    Monactin

    Bacterial Antibiotic Infection
    Monactin is a mactrotetralide antibiotic and a non-selective ionophore for monovalent cations, including potassium, sodium, and lithium. Monactin is isolated from Streptomyces and has antiproliferative activity.
  • HY-122966
    Desmethylxanthohumol

    Apoptosis Cancer
    Desmethylxanthohumol is a prenylated hydroxychalcone isolated from hop cones (Humulus lupulus L.). Desmethylxanthohumol is a powerful apoptosis inducing agent. Desmethylxanthohumol has antiplasmodial, antiproliferative, and antioxidant bioactivities.
  • HY-115948
    Antitumor agent-46

    Others Cancer
    Antitumor agent-46 (Compound 2h) is an anti-tumor agent. Antitumor agent-46 demonstrates markedly higher antiproliferative activity on MCF-7 cells with an IC50 value of 2.08 µM.
  • HY-145865
    c-Met/MEK1/Flt-3-IN-1

    Apoptosis Cancer
    Antiproliferative against-3 (comp 33) shows a prominent activity against Hela (IC50 = 0.21 µM), A549 (IC50 = 0.39 µM), and MCF-7 (IC50 = 0.33 µM), respectively. Antiproliferative against-3 (comp 33) also dose dependently induces apoptosis by arresting A549 cells at G1 phase.
  • HY-145821
    Tubulin inhibitor 15

    Microtubule/Tubulin Cancer
    Tubulin inhibitor 15 is a potent tubulin inhibitor. Tubulin inhibitor 15 shows antiproliferative activity. Tubulin inhibitor 15 shows cytotoxicity in HepG2 cells.
  • HY-145822
    Tubulin inhibitor 16

    Microtubule/Tubulin Cancer
    Tubulin inhibitor 16 is a potent tubulin inhibitor. Tubulin inhibitor 16 shows antiproliferative activity. Tubulin inhibitor 16 shows cytotoxicity in HepG2 cells.
  • HY-122675
    ACG416B

    Others Cancer
    ACG416B (compound 18) is a potent inhibitor of ChoK (choline kinase) with an IC50 of 0.4 μM. ACG416B renders higher ChoK inhibitory and antiproliferative activities against the HT-29 human colon cancer cell.
  • HY-N3119
    Paeoniflorigenone

    Apoptosis Cancer
    Paeoniflorigenone, isolated as an active ingredient from the root of moutan cortex, induces apoptosis selectively in the cancer cell lines and exhibits antiproliferative effect.
  • HY-132175
    CK2 inhibitor 2

    Casein Kinase Cancer
    CK2 inhibitor 2 is a potent, selective and orally active inhibitor of CK2, with an IC50 of 0.66 nM. CK2 inhibitor 2 shows high selectivity for Clk2 (IC50=32.69 nM)/CK2. CK2 inhibitor 2 exhibits favorable antiproliferative and antitumor activity.
  • HY-139296
    PP2A Cancerous-IN-1

    Akt Cancer
    PP2A Cancerous-IN-1 is a strong and potent CIP2A (Cancerous inhibitor of PP2A) and p-Akt inhibitor. PP2A Cancerous-IN-1 shows the most potent antiproliferative activities.
  • HY-N0944
    (-)-Heraclenol

    Others Cancer
    (-)-Heraclenol is a derivative of furocoumarin isolated from Ducrosia anethifolia. (-)-Heraclenol shows antiproliferative and cytotoxic activities on cancer cell lines.
  • HY-N9454
    Garcinoic acid

    Others Cancer
    Garcinoic acid is the vitamin E analogue extracted from Garcinia Kola seeds. Garcinoic acid shows a marked antiproliferative effect on glioma C6 cancer cells.
  • HY-118384
    Sangivamycin

    NSC 65346; BA-90912

    PKC Nucleoside Antimetabolite/Analog Cancer
    Sangivamycin (NSC 65346), a nucleoside analog, is a potent inhibitor of protein kinase C (PKC) with an Ki of 10 μM. Sangivamycin has potent antiproliferative activity against a variety of human cancers.
  • HY-146616
    GLS1 Inhibitor-3

    Glutaminase Cancer
    GLS1 Inhibitor-3 (compound C147) is a potent GLS1 inhibitor with an IC50 of 27.98 nM. GLS1 Inhibitor-3 shows antiproliferative activity.
  • HY-149032
    Kobusine derivative-1

    Others Cancer
    Kobusine derivative-1 is a Kobusine derivative. Kobusine derivative-1 shows antiproliferative activities against cancer cells.
  • HY-146185
    CCT373566

    Bcl-2 Family Cancer
    CCT373566 is a potent and orally active degrader of transcriptional repressor BCL6, with an IC50 of 2.2 nM. CCT373566 shows strong antiproliferative efficacy in vitro and reduction in tumor growth in vivo.
  • HY-119502
    Camalexin

    Reactive Oxygen Species Fungal Bacterial Cancer Infection
    Camalexin is a phytoalexin isolated from Camelina sativa (Cruciferae) with antibacterial, antifungal, antiproliferative and anticancer activities. Camalexin can induce reactive oxygen species (ROS) production.
  • HY-144830
    6BrCaQ

    HSP Cancer
    6BrCaQ is a potent mitochondrial heat shock protein TRAP1 inhibitor, with antiproliferative activity. 6BrCaQ can be used in the synthesis of 6BrCaQ-TPP conjugates.
  • HY-101677
    cPrPMEDAP

    Drug Metabolite Infection
    cPrPMEDAP is an intermediate metabolite of GS-9219. cpr-PMEDAP functions as a prodrug of the guanine nucleotide analog PMEG and has antiproliferative activity. cPrPMEDAP is negatively charged at physiologic pH and has poor permeability into the skin.
  • HY-147896
    Tubulin polymerization-IN-29

    Microtubule/Tubulin Cancer
    Tubulin polymerization-IN-29 (compound 6g) is a potent tubulin polymerization inhibitor. Tubulin polymerization-IN-29 exhibits potent antiproliferative activity. Tubulin polymerization-IN-29 can induce HeLa cells arrest in G2/M phase.
  • HY-146096
    RMS3

    P-glycoprotein Apoptosis Cancer
    RMS3, a tetrandrine analogue, is a potent P-glycoprotein (P-gp) inhibitor. RMS3 has markedly antiproliferative and cytotoxic effects on cancer cells. RMS3 causes PARP cleavage, a marker for cells undergoing apoptosis. RMS3 has strong anticancer property.
  • HY-144444
    NSC381467

    EGFR Cancer
    NSC381467 is a potent and orally active inhibitor of EGFR tyrosine kinase (EGFR-TK). NSC381467 has strong antiproliferative activities. NSC381467 has the potential for the research of cancer diseases.
  • HY-144445
    NSC114126

    EGFR Cancer
    NSC114126 is a potent and orally active inhibitor of EGFR tyrosine kinase (EGFR-TK). NSC114126 has strong antiproliferative activities. NSC114126 has the potential for the research of cancer diseases.
  • HY-146030
    Anticancer agent 46

    Others Cancer
    Anticancer agent 46 (compound 2) is a potent anticancer agent. Anticancer agent 46 shows antiproliferative activity with an IC50 of 0.986 µM for MGC803 cells. Anticancer agent 46 has the potential for the research of gastric cancer.
  • HY-114646
    TMC-205

    Endogenous Metabolite Cancer
    TMC-205 is a natural fungal metabolite with antiproliferative activity against cancer cell lines. TMC-205 is a transcriptional up-regulator of SV40 promoter.
  • HY-121458
    Nemorosone

    Apoptosis Cancer
    Nemorosone is the main component of the floral resin of Clusia rosea. Nemorosone has an antiproliferative effect on cancer cells. Nemorosone induces apoptosis in HT-29 and LoVo cells.
  • HY-119694
    Rotenolone

    Others Cancer
    Rotenolone is an antiproliferative agent. Rotenolone shows antiproliferative activity against the ovarian cancer A2780, breast cancer BT-549, prostate cancer DU 145, NSCLC NCI-H460, and colon cancer HCC-2998 cell lines, with IC50s of 0.95, 1.6, 2.7, 2.0, and 2.9 μM, respectively.
  • HY-143463
    AC-386

    c-Met/HGFR Cancer
    AC-386 is a highly potent c-Met inhibitor with IC50 value of 7.42 nM. AC-386 has antiproliferative activities against certain cancer cell lines. AC-386 can be used for researching anti-cancer resistance.
  • HY-107856
    5-Fluorouridine

    DNA/RNA Synthesis Apoptosis Cancer
    5-Fluorouridine, a metabolite of 5-fluorouracil (HY-90006), is a potent ribozyme self-cleavage inhibitor. 5-Fluorouridine incorporates into both total and poly A RNA and has antiproliferative activity. 5-Fluorouridine induces apoptosis.
  • HY-144810
    CDK2-IN-8

    CDK Cancer
    CDK2-IN-8 is a potent CDK2 inhibitor with an IC50 of 1.74 µM. CDK2-IN-8 shows antiproliferative activity. CDK2-IN-8 has the potential for the research of melanoma.
  • HY-132173
    GL0388

    Bcl-2 Family Cancer
    GL0388 is a Bax activator that results in Bax insertion into mitochondrial membrane. GL0388 shows antiproliferative activities against various cancer cells, with IC50s of 0.299-1.57 μM. GL0388 activates Bax and induce Bax-mediated apoptosis. GL0388 suppresses breast cancer xenograft tumor growth in vivo.
  • HY-144807
    Carbonic anhydrase inhibitor 9

    Carbonic Anhydrase Cancer
    Carbonic anhydrase inhibitor 9 is a potent carbonic anhydrase (CA) inhibitor with Kis of 56.4 and 56.9 nM for hCA II and IX, respectively. Antiproliferative activity.
  • HY-143385
    Cdc7-IN-12

    CDK Cancer
    Cdc7-IN-12 (compound 1) is a potent CDC7 inhibitor with an IC50 of <1 nM. Cdc7-IN-12 shows antiproliferative activities with IC50 of 100-1000 nM in COLO205 cells. Cdc7-IN-12 has the potential for the research of cancer.
  • HY-145261
    hDHODH-IN-8

    Lactate Dehydrogenase Inflammation/Immunology
    hDHODH-IN-8 is a potent inhibitor of human dihydroorotate dehydrogenase (hDHODH) with an IC50 of 16 nM. hDHODH-IN-8 has potent antiproliferative activity and excellent aqueous solubility. hDHODH-IN-8 has the potential for the research of tumor disease, especially lymphoma.
  • HY-143432
    Cdc7-IN-18

    CDK Cancer
    Cdc7-IN-18 (compound 1-2) is a potent CDC7 inhibitor with an IC50 of 1.29 nM for Cdc7/DBF4 enzyme. Cdc7-IN-18 shows antiproliferative activities with IC50 of 53.62 nM in COLO205 cells.
  • HY-151168
    3-Chlorogentisyl alcohol

    Bacterial Cancer Inflammation/Immunology
    3-Chlorogentisyl alcohol is a potent E. coli β-glucuronidase inhibitor with an IC50 value of 0.74 µM, an Ki value of 0.58 µM. 3-Chlorogentisyl alcohol shows antiproliferative activity. 3-Chlorogentisyl alcohol has the potential for the research of anti-cancer and anti-inflammatory therapies.
  • HY-151169
    MDM2/4-p53-IN-1

    MDM-2/p53 Cancer
    MDM2/4-p53-IN-1 is a potent MDM2-p53 and MDM4-p53 inhibitor with IC50 values of 35.9, 57.4 nM, respectively. MDM2/4-p53-IN-1 shows antiproliferative activity.
  • HY-150082
    CP681301

    CDK Cancer
    CP681301 is a potent CDK5 inhibitor. CP681301 shows antiproliferative activity. CP681301 decreases the expression of CD133, OLIG2, SOX2, KI67, pCDK5 protein level in GSCs (Glioma stem cells). CP681301 reduces self-renewal in mouse glioma xenografts. CP681301 shows anti-tumor activity in Drosophila.
  • HY-136521
    AZ13824374

    Epigenetic Reader Domain Cancer
    AZ13824374 is a highly potent and selective ATAD2 bromodomain inhibitor which shows cellular target engagement and antiproliferative activity in a range of breast cancer models. AZ13824374 inhibits ATAD2 with pIC50s of 8.2 and 6.2 in ATAD2 FRET assay and ATAD2 NanoBRET assay, respectively.
  • HY-N10354
    27-Methyl withaferin A

    Apoptosis Cancer
    27-Methyl withaferin A (comppund 26) is an apoptosis inducer with anticancer effects. 27-Methyl withaferin A shows antiproliferative effects against HeLa, A-549 and MCF-7 human tumor cell lines with IC50 values of 3.2 μM, 4.2 μM and 1.4 μM, respectively.
  • HY-N2584A
    Isoxanthohumol

    HSV Cancer Infection
    Isoxanthohumol is a prenylflavonoid from hops and beer. Isoxanthohumol exhibits an antiproliferative activity against several human cancer cell lines. Isoxanthohumol inhibits the development of lung metastatic foci in tumor-challenged animals. Isoxanthohumol shows an antiviral activity towards herpes viruses (HSV1 and HSV2) and bovine viral diarrhea virus (BVDV).
  • HY-N0005S
    Curcumin-d6

    Diferuloylmethane-d6; Natural Yellow 3-d6; Turmeric yellow-d6

    Keap1-Nrf2 Ferroptosis Autophagy Histone Acetyltransferase Epigenetic Reader Domain Mitophagy Influenza Virus Infection Metabolic Disease Inflammation/Immunology
    Curcumin D6 (Diferuloylmethane D6) is a deuterium labeled Curcumin (Turmeric yellow). Curcumin (Turmeric yellow) is a natural phenolic compound with diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin is an inhibitor of p300 histone acetylatransferase (HATs) and also shows inhibitory effects on NF-κB and MAPKs.
  • HY-146358
    Anticancer agent 49

    Microtubule/Tubulin Cancer
    Anticancer agent 49 (compound 69) is a broad spectrum anticancer agent. Anticancer agent 49 inhibits tubulin polymerization. Anticancer agent 49 shows antiproliferative activity. Anticancer agent 49 has the potential for the research of solid and hematological tumors.
  • HY-143270
    PROTAC BRD9-binding moiety 5

    Ligands for Target Protein for PROTAC Epigenetic Reader Domain Cancer
    PROTAC BRD9-binding moiety 5 is a selective BRD9 binder with an IC50 value of 4.20 μM, can be used for the synthesis of PROTACs. PROTAC BRD9-binding moiety 5 has antiproliferative activity against cancer cells.
  • HY-146465
    Anticancer agent 60

    Microtubule/Tubulin Cancer
    Anticancer agent 60 (compound 3h) has antiproliferative activity against human HepG2 cells (IC50 = 4.13 μM) and presents antitumor efficacy in a human HepG2 xenograft mouse model.
  • HY-151166
    β-Glucuronidase-IN-2

    Bacterial Cancer
    β-Glucuronidase-IN-2 is a potent E. coli β-glucuronidase inhibitor with an IC50 value of 0.24 µM, an Ki value of 1.09 µM. β-Glucuronidase-IN-2 shows antiproliferative activity. β-Glucuronidase-IN-2 has the potential for the research of anti-cancer and anti-inflammatory therapies.
  • HY-129337
    Reveromycin A

    Antibiotic Fungal Apoptosis Cancer Infection
    Reveromycin A, a benzoquinoid antibiotic isolated from the genus Streptomyces, is a selective inhibitor of protein synthesis in eukaryotic cells. Reveromycin A inhibits bone resorption by inducing apoptosis specifically in osteoclasts. Reveromycin A has antiproliferative activity against tumor cell lines and antifungal activity.
  • HY-148281
    TMX-2164

    Bcl-2 Family Cancer
    TMX-2164 is a potent, irreversible B-cell lymphoma 6 (BCL6) inhibitor with an IC50 value of 152 nM. TMX-2164 displays sustained target engagement and antiproliferative activity in cells.
  • HY-N10351
    27-O-(tert-Butyldimethylsilyl)withaferin A

    Apoptosis Cancer
    27-O-(tert-Butyldimethylsilyl)withaferin A (compound 9a), a natural withanolide, is an apoptosis inducer. 27-O-(tert-Butyldimethylsilyl)withaferin A shows antiproliferative activity against HeLa, A-549 and MCF-7 human cancer cell lines, and against normal Vero cells.
  • HY-131961
    Triciferol

    VD/VDR HDAC Cancer
    Triciferol functions as a multiple ligand with combined VDR agonist and HDAC antagonist activities. Triciferol binds directly to the VDR (IC50=87 nM), and functions as an agonist with 1,25D-like potency on several 1,25D target genes. Triciferol induces marked tubulin hyperacetylation, and augments histone acetylation. Antiproliferative and cytotoxic activities.
  • HY-147839
    Topoisomerase II inhibitor 10

    Topoisomerase Apoptosis Cancer
    Topoisomerase II inhibitor 10 (compound 32a) is a potent topoisomerase II inhibitor with an IC50 value of 7.45 μM. Topoisomerase II inhibitor 10 causes cell cycle arrest at G2-M phase and induces apoptosis of HepG-2 cells. Topoisomerase II inhibitor 10 has excellent anti-proliferative activities against HepG-2, MCF-7, and HCT-116 cells.
  • HY-143253
    Estrogen receptor antagonist 7

    Estrogen Receptor/ERR Cancer
    Estrogen receptor antagonist 7 (compound 13) is a potent estrogen receptors (ER) antagonist. Estrogen receptor antagonist 7 has antiproliferative activity against breast and ovarian cancer cells. Anticancer and anti-uterotrophic activities.
  • HY-151618
    Antitumor agent-79

    Apoptosis Cancer
    Antitumor agent-79 shows good antiproliferative activities against hepatocellular carcinoma and breast cancer cells with IC50 values of 0.7-7.9 μM. Antitumor agent-79 induces cancer cells apoptosis and shows in vivo antitumor effects. Antitumor agent-79 can be used for the research of cancer.
  • HY-149035
    PAA4

    Others Cancer
    PAA4 is a methide carbon-centered polynuclear Au(I) clusters. PAA4 shows antiproliferative activity. PAA4 increases the expression of pH2AX in a time dependent manner. PAA4 shows anti-tumor effect in orthotopic bladder cancer mouse model.
  • HY-145314
    TC113

    Integrin Cancer
    TC113 is a c(RGDyK)-Based conjugate of Gemcitabine (GEM). TC113 could be internalized by A549 cells through integrin αvβ3. TC113 shows potent antiproliferative properties against WM266.4 and A549 cells.
  • HY-18336
    GlyH-101

    CFTR Cardiovascular Disease
    GlyH-101 is a potent CFTR inhibitor. GlyH-101 also is a potent and reversible inhibitor of the VSORC conductance. GlyH-101 shows antiproliferative activity. GlyH-101 inhibits CFTR-like current and VSORC current.
  • HY-N10355
    27-TBDMS-4-Dehydrowithaferin A

    Apoptosis Cancer
    27-TBDMS-4-Dehydrowithaferin A, a withaferin A derivative, exhibits potent antiproliferative effects on the tumor cells.27-TBDMS-4-Dehydrowithaferin A induces tumor cells apoptosis. 27-TBDMS-4-Dehydrowithaferin A is a anticancer agent.
  • HY-N8432
    Dipyrithione

    Apoptosis Bacterial Fungal Cancer Infection Inflammation/Immunology
    Dipyrithione is a potent antimicrobial agent. Dipyrithione shows antifungal activity and antiproliferative activity. Dipyrithione induces apoptosis and cycle arrest at G1 phase. Dipyrithione shows anti-inflammatory activity in vivo. Dipyrithione shows anti-tumor activity. Dipyrithione has the potential for the research of dermatophytosis.
  • HY-146988
    hCAIX/XII-IN-1

    Carbonic Anhydrase Apoptosis Cancer
    hCAIX/XII-IN-1 is a potent CAIX/XII inhibitor with the KI values of 0.48 µM and 0.83 µM for CAIX and CAXII, respectively. hCAIX/XII-IN-1 shows antiproliferative activity in vitro. hCAIX/XII-IN-1 induces apoptosis in MCF-7 cells.
  • HY-146083
    (Z)-p-cyano-α-Cyanostilbene

    Others Cancer
    (Z)-p-cyano-α-Cyanostilbene (compound 11), a phenantrene derivative, has antiproliferative activity. (Z)-p-cyano-α-Cyanostilbene shows significant selectivity against HeLa (IC50=0.21 µM) and HepG2 (IC50=0.230 µM) cells without cytotoxic against normal skin fibroblasts (IC50>100 µM).
  • HY-144724
    HSP90-IN-10

    HSP Apoptosis Cancer
    HSP90-IN-10 (Compound 16s) is a potent inhibitor of HSP90. HSP90-IN-10 exhibits high antiproliferative potency against HCC1954 breast cancer cells with the IC50 value of 6 µM. HSP90-IN-10 does not inhibit the growth of normal epithelial cells. HSP90-IN-10 also induces apoptosis.
  • HY-118834
    Teleocidin A1

    Lyngbyatoxin A

    PKC Cancer
    Teleocidin A1 (Lyngbyatoxin A), a highly toxic skin irritant, is a potent activator of protein kinase C (PKC). Teleocidin A1 shows antiproliferative activity against HeLa cancer cells (IC50=9.2 nM).
  • HY-N7654
    (-)-Epipodophyllotoxin

    Apoptosis Cancer
    (-)-Epipodophyllotoxin (2) is an antiproliferative agent against cancer cells isolated from American mayapple Podophyllum peltatum, with GI50s of 0.36 and 0.24 μM in HeLa cells and MCF-7 cells, respectively. (-)-Epipodophyllotoxin can inhibit mitotic spindle assembly in vitro.
  • HY-15228
    RX-3117

    TV-1360; fluorocyclopentenylcytosine

    Nucleoside Antimetabolite/Analog Apoptosis Cancer
    RX-3117 (TV-1360) is a potent and orally active anticancer and antimetaboliteagent. RX-3117 inhibits DNA methyltransferase 1 (DNMT1). RX-3117 shows antiproliferative and anti-tumour activity. RX-3117 induces cell cycle arrest at S phase and apoptosis.
  • HY-144720
    BRG1-IN-1

    Others Cancer
    BRG1-IN-1 (Compound 11d) is a potent inhibitor of BRG1. BRG1-IN-1 shows better efficacy than PFI-3 in sensitizing GBM cells to the antiproliferative and cell death inducing effects of Temozolomide in vitro. BRG1-IN-1 enhances the inhibitor effect of Temozolomide on the growth of subcutaneous GBM tumors.
  • HY-147322
    YAP/TAZ inhibitor-2

    YAP Cancer
    YAP/TAZ inhibitor-2 is a potent and orally active TEAD-YAP/TAZ inhibitor with an EC50 value of 3 nM. YAP/TAZ inhibitor-2 shows anti-proliferative activity. YAP/TAZ inhibitor-2 shows antitumor activity.
  • HY-148278
    BI-0474

    Ras Cancer
    BI-0474 is a potent KRAS G12C inhibitor with an IC50 value of 7.0 nM for the GDP-KRAS::SOS1 protein-protein interaction. BI-0474 exhibits good anti-proliferative activity against NCI-H358 cells carrying the G12C mutation. BI-0474 also shows good anti-tumour activity in non-small cell lung cancer xenograft models.
  • HY-144451
    TRK-IN-12

    Trk Receptor Cancer
    TRK-IN-12 (Compound 9e) is a potent inhibitor of TRK (TRK G595R IC50 = 13.1 nM). TRK-IN-12 is a macrocyclic derivative compound. TRK-IN-12 shows significant antiproliferative activity in the Ba/F3-LMNA-NTRK1 cell line (IC50 = 0.080 μM). TRK-IN-12 has shown a better inhibitory effect (IC50 = 0.646 μM) than control drug LOXO-101 in Ba/F3-LMNA-NTRK1-G595R cell line.
  • HY-146357
    Anticancer agent 48

    Microtubule/Tubulin Cancer
    Anticancer agent 48 (compound 48) is a broad spectrum anticancer agent. Anticancer agent 48 inhibits tubulin polymerization. Anticancer agent 48 shows antiproliferative activity. Anticancer agent 48 shows antitumor activity in vivo. Anticancer agent 48 has the potential for the research of solid and hematological tumors.
  • HY-146230
    VEGFR-2-IN-26

    VEGFR Cancer
    VEGFR-2-IN-26 (compound 5h) is a highly potent VEGFR-2 inhibitor with an IC50 value of 15.5 nM. VEGFR-2-IN-26 has good antiproliferative activity against the leukemic, non-small lung, CNS, ovarian, renal, prostate and breast cancer cells.
  • HY-146063
    Anticancer agent 54

    Apoptosis Cancer
    Anticancer agent 54 is a potent anticancer agent. Anticancer agent 54 shows antiproliferative activity. Anticancer agent 54 induces apoptosis and cell cycle arrest at G0/G1 phases. Anticancer agent 54 shows anticancer activity depends on DNA intercalation and ROS generation.
  • HY-146254
    hCAIX-IN-12

    Carbonic Anhydrase Apoptosis Reactive Oxygen Species Cancer
    hCAIX-IN-12 is a potent hCAIX inhibitor with IC50 values of 0.74, 10.78 µM for CAIX and CAII, respectively. hCAIX-IN-12 shows antiproliferative effect and induces apoptosis. hCAIX-IN-12 increases ROS production. hCAIX-IN-12 has the potential for the research of colorectal cancer (CRC) .
  • HY-120400
    KDM5-C70

    Histone Demethylase Cancer
    KDM5-C70 is an ethyl ester derivative of KDM5-C49 and a potent, cell-permeable and pan-KDM5 histone demethylase inhibitor. KDM5-C70 has an antiproliferative effect in myeloma cells, leading to genome-wide elevation of H3K4me3 levels.
  • HY-132135
    (1E)-CFI-400437 dihydrochloride

    Polo-like Kinase (PLK) Cancer
    (1E)-CFI-400437 dihydrochloride is a potent PLK4 (IC50= 0.6 nM) inhibitor and selective against other members of the PLK family (>10 μM). (1E)-CFI-400437 dihydrochloride inhibits Aurora A, Aurora B, KDR and FLT-3 with IC50s of 0.37, 0.21, 0.48, and 0.18 μM, respectively. Antiproliferative activity.
  • HY-P2282
    APTSTAT3-9R

    STAT Cancer
    APTSTAT3-9R, a specific STAT3-binding peptide, inhibits STAT3 activation and downstream signaling by specifically blocking STAT3 phosphorylation. APTSTAT3-9R exerts antiproliferative effects and antitumor activity.
  • HY-146565
    DNA-PK-IN-8

    DNA-PK Cancer
    DNA-PK-IN-8 is a highly potent, selective and orally active DNA-dependent protein kinase (DNA-PK) inhibitor with an IC50 value of 0.8 nM. DNA-PK-IN-8 exhibits synergistic antiproliferative activity against a series of cancer cell lines and significantly suppresses HL-60 tumor growth, when using in combination with Doxorubicin.
  • HY-147825
    EGFR/BRAFV600E-IN-1

    EGFR Raf Apoptosis Cancer
    EGFR/BRAFV600E-IN-1 (Compound 23) is a potent EGFR and BRAF V600E dual inhibitor with IC50s of 0.08 and 0.15 µM, respectively. EGFR/BRAFV600E-IN-1 induces apoptosis and cell cycle arrest in both pre-G1 and G2/M phases. EGFR/BRAFV600E-IN-1 exhibits antiproliferative activity againist A-549, MCF-7, Panc-1, HT-29 with IC50s of 1.2, 0.79, 1.3, and 1.23 µM, respectively.
  • HY-115885
    XP5

    HDAC Cancer Inflammation/Immunology
    XP5 is a potent, orally active HDAC6 inhibitor with an IC50 of 31 nM. XP5 displays high antiproliferative activity against various cancer cell lines including the HDACi-resistant YCC3/7 gastric cancer cells (IC50=0.16-2.31 μM). XP5 enhances antitumor immunity when combined with a PD-L1 inhibitor in melanoma.
  • HY-144307
    Aurora A/PKC-IN-1

    Aurora Kinase PKC Cancer
    Aurora A/PKC-IN-1 (Compound 2e) is a potent dual inhibitor of Aurora A (AurA) and PKC (α, β1, β2, and θ) kinases with IC50s of 6.9 nM and 16.9 nM for AurA and PKCα, respectively. Aurora A/PKC-IN-1 has antiproliferative activity in breast cancer cells and antimetastatic activity.
  • HY-146884
    MET kinase-IN-3

    c-Met/HGFR VEGFR Cancer
    MET kinase-IN-3 (compound 8) is an orally active and potent MET inhibitor, with an IC50 of 9.8 nM. MET kinase-IN-3 shows good and broad-spectrum antiproliferative activity against cancer cell lines.
  • HY-146020
    Topoisomerase IIα-IN-1

    Topoisomerase Cancer
    Topoisomerase IIα-IN-1 (compound 2) is a potent DNA-binding ligands and topoisomerase IIα inhibitor. Topoisomerase IIα-IN-1 exhibits high antiproliferative activity against human cancer cell lines.
  • HY-79135
    Pasireotide ditrifluoroacetate

    SOM230 ditrifluoroacetate; Pasireotide TFA salt

    Somatostatin Receptor Endocrinology Cancer
    Pasireotide (SOM230) ditrifluoroacetate, a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide ditrifluoroacetate exhibits antisecretory, antiproliferative, and proapoptotic activity.
  • HY-139039
    BSJ-4-116

    PROTACs CDK Cancer
    BSJ-4-116 is a PROTAC connected by ligands for Cereblon and CDK. BSJ-4-116 is a highly potent and selective CDK12 degrader (PROTAC) with an IC50 of 6 nM. BSJ-4-116 downregulates DDR genes through a premature termination of transcription, primarily through increasing poly(adenylation). BSJ-4-116 exhibits potent antiproliferative effects, alone and in combination with the poly(ADP-ribose) polymerase inhibitor Olaparib (HY-10162).
  • HY-16381B
    Pasireotide (diaspartate)

    SOM230 (diaspartate)

    Somatostatin Receptor Cancer Neurological Disease
    Pasireotide (SOM230) diaspartate, a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide diaspartate exhibits antisecretory, antiproliferative, and proapoptotic activity.
  • HY-108768
    Pasireotide pamoate

    SOM230 pamoate

    Somatostatin Receptor Cancer Endocrinology
    Pasireotide (SOM230) pamoate, a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide pamoate exhibits antisecretory, antiproliferative, and proapoptotic activity.
  • HY-146097
    RMS5

    P-glycoprotein Apoptosis Cancer
    RMS5, a tetrandrine analogue, is a potent P-glycoprotein (P-gp) inhibitor. RMS5 has markedly antiproliferative and cytotoxic effects on cancer cells. RMS5 slightly diminishes the expression of the anti-apoptotic Bcl-2 family proteins Bcl-XL and Mcl-1. RMS3 causes PARP cleavage, a marker for cells undergoing apoptosis. RMS5 has strong anticancer property.
  • HY-13591
    Piclidenoson

    IB-MECA; CF-101

    Adenosine Receptor Apoptosis Cancer Inflammation/Immunology
    Piclidenoson (IB-MECA) is a first-in-class, orally active and selective A3 adenosine receptor (A3AR) agonist. Piclidenoson exhibits antiproliferative effect and induces apoptosis in different cancer cell types like melanoma, leukemia. Piclidenoson can be used for the research of autoimmune inflammatory diseases and COVID-19.
  • HY-150684
    GXH-II-052

    Epigenetic Reader Domain Cancer
    GXH-II-052 is a potent bivalent bromodomain and extraterminal domain (BET) inhibitor. GXH-II-052 shows binding potential for BRD4-1, BRD4-2, BRD4-T, BRDT-1, BRDT-2, BRDT-T with Kd values of 28, 9.1, 4.8, 0.6, 8.4, 2.6 nM, respectively. GXH-II-052 shows antiproliferative activity. GXH-II-052 decreases the expression of c-Myc.
  • HY-143462
    c-Met/HDAC-IN-2

    HDAC c-Met/HGFR Apoptosis Cancer
    c-Met/HDAC-IN-2 is a highly potent c-Met and HDAC dual inhibitor with IC50s of 18.49 nM and 5.40 nM for HDAC1 and c-Met, respectively. c-Met/HDAC-IN-2 has antiproliferative activities against certain cancer cell lines. c-Met/HDAC-IN-2 can cause G2/M-phase arrest and induce apoptosis in HCT-116. c-Met/HDAC-IN-2 can be used for researching anti-cancer resistance.
  • HY-N3451
    Isothymusin

    Lipoxygenase Cancer
    Isothymusin is a potent anti-oxidant agent. Isothymusin shows radical scavenging activities. Isothymusin shows anti-proliferative activities in cancer cell lines. Isothymusin inhibited the enzymes associated with the promotion stage of cancer, including cycloxygenase- 2 and lipoxygenase-5.
  • HY-144811
    CDK2-IN-9

    CDK Apoptosis Cancer
    CDK2-IN-9 is a potent CDK2 inhibitor with an IC50 of 0.63 µM. CDK2-IN-9 shows antiproliferative activity. CDK2-IN-9 induces apoptosis and cell cycle arrest at S and G2/M phase. CDK2-IN-9 has the potential for the research of melanoma.
  • HY-79136
    Pasireotide L-aspartate salt

    SOM230 L-aspartate

    Somatostatin Receptor Cancer Endocrinology
    Pasireotide (SOM230) L-aspartate salt, a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide L-aspartate salt exhibits antisecretory, antiproliferative, and proapoptotic activity.
  • HY-150565
    P-gp inhibitor 5

    P-glycoprotein Cancer
    P-gp inhibitor 5 is a potent P-glycoprotein (P-gp) inhibitor. P-gp inhibitor 5 has antiproliferative activity against certain cancer cell lines. P-gp inhibitor 5 is effective in reversing the multidrug resistance (MDR) phenotype in ABCB1/Flp-In TM-293 and KBvin cells by restoring their sensitivity to Vincristine (HY-N0488A) and Paclitaxel (HY-B0015).
  • HY-122727
    STL127705

    DNA-PK Apoptosis Cancer
    STL127705 (Compound L) is a potent Ku 70/80 heterodimer protein inhibitor with an IC50 of 3.5 μM. STL127705 interferes the binding of Ku70/80 to DNA and by inhibits the activation of the DNA-PKCS kinase. STL127705 shows antiproliferative and anticancer activity. STL127705 induces apoptosis.
  • HY-150797
    QA-68

    QA-68-ZU81

    Epigenetic Reader Domain Cancer Inflammation/Immunology
    QA-68 (QA-68-ZU81) is a potent bromodomain-containing protein 9 (BRD9) degrader. QA-68 can inhibit cell cycle progression and cell colony formation. QA-68 has antiproliferative activity against acute myeloid leukemia (AML) cell lines.
  • HY-129476
    L-Canaline

    Parasite Endogenous Metabolite Cancer Infection
    L-Canaline is a nonprotein amino acid stored in many leguminous plants. L-Canaline is a cytotoxic metabolite catalyzed by L-canavanine and its arginase. L-Canaline is a potent and irreversible inhibitor of ornithine aminotransferase. L-Canaline inhibits the growth of the malaria parasite Plasmodium falciparum with an IC50 of 297 nM. L-Canaline has anticancer and antiproliferative effects.
  • HY-150683
    NC-III-49-1

    Epigenetic Reader Domain Cancer
    NC-III-49-1 is a potent bivalent bromodomain and extraterminal domain (BET) inhibitor. NC-III-49-1 shows binding potential for BRD4-1, BRD4-2, BRD4-T, BRDT-1, BRDT-2, BRDT-T with Kd values of 0.095, 0.32, 0.29, 0.089, 5.5, 0.058 nM, respectively. NC-III-49-1 shows antiproliferative activity. NC-III-49-1 decreases the expression of c-Myc.
  • HY-122639
    ZINC05007751

    Others Cancer
    ZINC05007751 is a potent NIMA-related kinase NEK6 inhibitor with an IC50 of 3.4 μM. ZINC05007751 shows antiproliferative activity against a panel of human cancer cell lines, and displays a synergistic effect with Cisplatin and Paclitaxel in a BRCA2 mutated ovarian cancer cell line. ZINC05007751 is very selective against NEK1 and NEK6 with no significant activity was observed against NEK2, NEK7, and NEK9.
  • HY-146672
    ITK inhibitor 6

    Itk Cancer
    ITK inhibitor 6 (compound 43) is a potent and selective ITK inhibitor with IC50s of 4 nM, 133 nM, 320 nM, 2360 nM, 155 nM for ITK, BTK, JAK3, EGFR, LCK, respectively. ITK inhibitor 6 inhibits phosphorylation of PLCγ1 and ERK1/2. ITK inhibitor 6 shows antiproliferative activities.
  • HY-W011404
    Tributyrin

    Glyceryl tributyrate

    Apoptosis Metabolic Disease
    Tributyrin (Glyceryl tributyrate), a neutral short-chain fatty acid triglyceride, is a stable and rapidly absorbed prodrug of Butyric Acid. Tributyrin diffuses through biological membranes and is metabolized by intracellular lipases, releasing effective butyrate directly into the cell in vivo. Tributyrin has potent antiproliferative, proapoptotic and differentiation-inducing effects.
  • HY-18979
    Lactimidomycin

    Influenza Virus Cancer Infection
    Lactimidomycin is a glutarimide-containing compound isolated from Streptomyces. Lactimidomycin is a potent inhibitor of eukaryotic translation elongation. Lactimidomycin has a potent antiproliferative effect on tumor cell lines and selectively inhibit protein translation. Lactimidomycin inhibits protein synthesis with an IC50 value of 37.82 nM. Lactimidomycin is also a potent and non-toxic inhibitor of dengue virus 2 and other RNA viruses. Anticancer and antiviral activities.
  • HY-147419
    Vulolisib

    PI3K Cancer
    Vulolisib is a potent and orally active phosphatidylinositol 3-kinase (PI3K) inhibitor, with IC50 values of 0.2 nM, 168 nM, 90 nM and 49 nM for PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ, respectively. Antiproliferative and antineoplastic activity.
  • HY-102078
    ZINC69391

    Ras Apoptosis Cancer
    ZINC69391, a specific Rac1 inhibitor, interferes with Rac1-GEF interaction by masking Trp56 residue on Rac1 surface. ZINC69391 interferes with the interaction of Rac1 with Dock180 and reduces Rac1-GTP levels. ZINC69391 induces apoptosis, and shows antiproliferative and antimetastatic effects.
  • HY-146325
    HSP90-IN-11

    HSP Cancer
    HSP90-IN-11 (Compound 12c) is a potent inhibitor of HSP90. HSP90-IN-11 displays potent HSP90α inhibition comparable to AUY-922 (Luminespib). HSP90-IN-11 shows significant antiproliferative activity in CRC and NSCLC cells in a double digit nM range. HSP90-IN-11 leads to rapid degradation of client proteins EGFR and Akt in NSCLC cells. HSP90-IN-11 induces significant accumulation of a sub-G1 phase population.
  • HY-115944
    BTK-IN-9

    Btk Apoptosis Cancer Inflammation/Immunology
    BTK-IN-9 is a reversible BTK inhibitors with potent antiproliferative activity in mantle cell lymphoma. BTK-IN-9 specifically disturbs mitochondrial membrane potential and increases reactive oxygen species level in Z138 cells. BTK-IN-9 also induces cell apoptosis in Z138 cells.
  • HY-145406
    IHCH-3064

    Adenosine Receptor HDAC Cancer Inflammation/Immunology
    IHCH-3064 is a dual-acting compounds targeting Adenosine A2A Receptor and HDAC. IHCH-3064 exhibits potent binding to A2AR (Ki=2.2 nM) and selective inhibition of HDAC1 (IC50=80.2 nM), with good antiproliferative activity against tumor cell lines in vitro. IHCH-3064 is a tumor immunotherapeutic agent.
  • HY-124113
    4'-Bromo-resveratrol

    4′‐BR

    Sirtuin Apoptosis Cancer
    4'-Bromo-resveratrol is a potent and dual inhibitor Sirtuin-1 and Sirtuin-3. 4'-Bromo-resveratrol inhibits melanoma cell growth through mitochondrial metabolic reprogramming. 4'-Bromo-resveratrol imparts antiproliferative effects in melanoma cells through a metabolic reprogramming and affecting the cell cycle and apoptosis signaling.
  • HY-10252
    NVP-ADW742

    ADW742; GSK 552602A; ADW

    IGF-1R Insulin Receptor Apoptosis Cancer Endocrinology
    NVP-ADW742 (ADW742) is an orally active, selective IGF-1R tyrosine kinase inhibitor with an IC50 of 0.17 μM. NVP-ADW742 inhibits insulin receptor (InsR) with an IC50 of 2.8 μM. NVP-ADW742 induces pleiotropic antiproliferative/proapoptotic biologic sequelae in tumor cells.
  • HY-N0998
    1,7-Bis(4-hydroxyphenyl)-hepta-4E,6E-dien-3-one

    Others Cancer
    1,7-Bis(4-hydroxyphenyl)-hepta-4E,6E-dien-3-one (compound 6) shows antiproliferative activity with ED50s of 57.7, 78.8 µM for 26-L5 and HT-1080 cells, respectively. 1,7-Bis(4-hydroxyphenyl)-hepta-4E,6E-dien-3-one inhibits melanogenesis in B16 melanoma 4A5 cells. 1,7-Bis(4-hydroxyphenyl)-hepta-4E,6E-dien-3-one has the potential for the research of skin disorders.
  • HY-16381A
    Pasireotide acetate

    SOM230 acetate

    Somatostatin Receptor Cancer Endocrinology
    Pasireotide (SOM230) acetate, a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide acetate can suppress GH, IGF-I and ACTH secretion, indicating potential efficacy in acromegaly and Cushing's disease. Pasireotide acetate also exhibits antisecretory, antiproliferative, and proapoptotic activity.
  • HY-150562
    CDK9-IN-19

    CDK Cancer
    CDK9-IN-19 is a highly potent and selective CDK9 inhibitor with an IC50 value of 2.0 nM. CDK9-IN-19 has excellent cellular antiproliferative activity, moderate pharmacokinetic property and low hERG inhibition. CDK9-IN-19 significantly induces tumour growth inhibition in an MV4-11 xenograft mice model. CDK9-IN-19 can be used for researching acute myeloid leukaemia (AML).
  • HY-16381
    Pasireotide

    SOM230

    Somatostatin Receptor Cancer Endocrinology
    Pasireotide (SOM230), a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide can suppress GH, IGF-I and ACTH secretion, indicating potential efficacy in acromegaly and Cushing's disease. Pasireotide also exhibits antisecretory, antiproliferative, and proapoptotic activity.
  • HY-126052
    Gnetol

    COX Tyrosinase HDAC Cancer Metabolic Disease
    Gnetol is a phenolic compound isolated from the root of Gnetum ula Brongn. Gnetol potently inhibits COX-1 (IC50 of 0.78 μM) and HDAC. Gnetol is a potent tyrosinase inhibitor with an IC50 of 4.5 μM for murine tyrosinase and suppresses melanin biosynthesis. Gnetol has antioxidant, antiproliferative, anticancer and hepatoprotective activity. Gnetol also possesses concentration-dependent α-Amylase, α-glucosidase, and adipogenesis activities.
  • HY-150543
    Steroid sulfatase-IN-3

    Others Cancer
    Steroid sulfatase-IN-3 (compound 1q) is a potent STS (Steroid sulfatase) inhibitor, with an IC50 of 25.8 nM. Steroid sulfatase-IN-3 shows antiproliferative activity against T-47D estrogen-dependent breast cancer cells, with an IC50 of 1.04 µM.
  • HY-146316
    Topoisomerase II inhibitor 6

    Topoisomerase Cancer
    Topoisomerase II inhibitor 6 (Compound 5), a tryptanthrin derivative, is a potent and selective inhibitor of topoisomerase II. Topoisomerase II inhibitor 6 exhibits antiproliferative activity on different tumor cell lines. Topoisomerase II inhibitor 6 blocks the cell cycle of CCRF-CEM in the G2 phase and induces DNA DSB. Topoisomerase II inhibitor 6 has the potential for the research of cancer diseases.
  • HY-N10264
    Avrainvillamide

    (+)-Avrainvillamide; CJ-17,665

    Antibiotic Cancer Infection
    Avrainvillamide ((+)-Avrainvillamide) is a naturally occurring alkaloid with antiproliferative effects, binds to the nuclear chaperone nucleophosmin, a proposed oncogenic protein that is overexpressed in many different human tumors. Avrainvillamide affects cell biology both by directly binding NPM1 and Crm1 as well as by inhibiting the association of these proteins with certain native cellular partners. Avrainvillamide, an antibiotic, inhibits growth of multi-drug resistant Staphylococcus aureus, Streptococcus pyogenes, and Enterococcus faecalis, with MICs of 12.5, 12.5 and 25 μg/ml, respectively.
  • HY-143246
    EGFR kinase inhibitor 1

    EGFR Apoptosis Cancer
    EGFR kinase inhibitor 1 is a potent EGFR inhibitor with IC50s of 37, 1.7, >300 nM for WT, l885R/T790M, L858R/T790M/C797S, respectively. EGFR kinase inhibitor 1 induces apoptosis and cell cycle arrest at G0/G1-phase. EGFR kinase inhibitor 1 inhibits the cell motility. EGFR kinase inhibitor 1 shows antiproliferative and anti-tumor activity.
  • HY-103387
    DuP-697

    COX Apoptosis Cancer Inflammation/Immunology
    DuP-697 is a member of the vicinal diaryl heterocycles and a potent, irreversible, selective and orally active COX-2 inhibitor (IC50 of 10 nM and 800 nM for human COX-2 and COX-1, respectively). DuP-697 exerts antiproliferative (IC50 of 42.8 nM), antiangiogenic and apoptotic effects on HT29 colorectal cancer cells. DuP-697 inhibits prostaglandin synthesis and has anti-inflammatory, anticancer and antipyretic effects.
  • HY-146021
    Topoisomerase IIα-IN-2

    Topoisomerase Cancer
    Topoisomerase IIα-IN-2 (compound 5) is a potent DNA-binding ligands and topoisomerase IIα inhibitor. Topoisomerase IIα-IN-2 exhibits high antiproliferative activity against human cancer cell lines. Topoisomerase IIα-IN-2 significantly induces DNA damage and arrests cancer cells at G2/M phase.
  • HY-144637
    Autophagy inducer 2

    Apoptosis Autophagy Cancer
    Autophagy inducer 2 (Compound 11i) is a potent autophagy inducer. Autophagy inducer 2 exhibits apparent antiproliferative activity against the MCF-7 cell line with an IC50 value of 1.31 μM and remarkably inhibits the colony formation of the MCF-7 cells. Autophagy inducer 2 arrests the MCF-7 cells in the G2/M phase by regulating the cell-cycle-related proteins Cdk-1 and Cyclin B1. Autophagy inducer 2 has the potential for the research of breast cancer.
  • HY-N9093
    (3R,5R)-3,5-Diacetoxy-1-(3,4-dihydroxyphenyl)-7-(4-hydroxyphenyl)heptane

    Others Cancer Inflammation/Immunology
    (3R,5R)-3,5-Diacetoxy-1-(3,4-dihydroxyphenyl)-7-(4-hydroxyphenyl)heptane, a diarylheptanoid from the rhizomes of Curcuma kwangsiensis, possesses a variety of biological and pharmacological activities including antioxidant, antihepa totoxic, anti-inflammatory, antiproliferative, antiemetic, and antitumor activities.
  • HY-14993
    SCH79797

    Protease Activated Receptor (PAR) Apoptosis Cardiovascular Disease
    SCH79797 is a highly potent, selective nonpeptide protease activated receptor 1 (PAR1) antagonist. SCH79797 inhibits binding of a high-affinity thrombin receptor-activating peptide to PAR1 with an IC50 of 70 nM and a Ki of 35 nM. SCH79797 inhibits thrombin-induced platelet aggregation with an IC50 of 3 μM. SCH79797 has antiproliferative and pro-apoptotic effects, and limits myocardial ischemia/reperfusion injury in rat hearts. SCH79797 also potently prevents PAR1 activation in vascular smooth muscle cells, endothelial cells, and astrocytes.
  • HY-139996
    Pomalidomide-C5-Dovitinib

    PROTACs Ligands for E3 Ligase Cancer
    Pomalidomide-C5-Dovitinib (compound 2) is a PROTAC containing Pomalidomide, Dovitinib and connected with CRBN. Pomalidomide-C5-Dovitinib shows enhanced antiproliferative effects against FLT3-ITD+ AML cells. Pomalidomide-C5-Dovitinib induces the degradation of the FLT3-ITD and KIT proteins in a ubiquitin-proteasome-dependent manner and completely blocks their downstream signaling pathway. Pomalidomide-C5-Dovitinib has the potential for the research of FLT3-ITD + acute myeloid leukemia.
  • HY-14994
    SCH79797 dihydrochloride

    Protease Activated Receptor (PAR) Apoptosis Cardiovascular Disease
    SCH79797 dihydrochloride is a highly potent, selective nonpeptide protease activated receptor 1 (PAR1) antagonist. SCH79797 dihydrochloride inhibits binding of a high-affinity thrombin receptor-activating peptide to PAR1 with an IC50 of 70 nM and a Ki of 35 nM. SCH79797 dihydrochloride inhibits thrombin-induced platelet aggregation with an IC50 of 3 μM. SCH79797 dihydrochloride has antiproliferative and pro-apoptotic effects, and limits myocardial ischemia/reperfusion injury in rat hearts. SCH79797 dihydrochloride also potently prevents PAR1 activation in vascular smooth muscle cells, endothelial cells, and astrocytes.
  • HY-146617
    GLS1 Inhibitor-4

    Glutaminase Apoptosis Cancer
    GLS1 Inhibitor-4 (compound 41e) is a potent GLS1 inhibitor with an IC50 of 11.86 nM. GLS1 Inhibitor-4 shows antiproliferative activity, good metabolic stability, robust GLS1 binding affinity. GLS1 Inhibitor-4 blocks the glutamine metabolism and induce the production of ROS. GLS1 Inhibitor-4 induces apoptosis and shows antitumor activity.
  • HY-N10067
    Micromonosporamide A

    Others Cancer
    Micromonosporamide A exhibits glutamine-dependent antiproliferative activity.
  • HY-150688
    JAK3-IN-13

    JNK Cancer
    JAK3-IN-13 is a potent, selective and orally active JAK3 inhibitor with IC50 values of 4728, 2039, 8, 365 nM for NK1, JNK2, JNK3, Tyk2, respectively. JAK3-IN-13 shows antiproliferative activity. JAK3-IN-13 induces cell cycle arrest at G0/G1 phase. JAK3-IN-13 shows antitumor activity.
  • HY-139990
    CSF1R-IN-3

    c-Fms Cancer
    CSF1R-IN-3 (compound 21) is a potent and orally active CSF-1R inhibitor (IC50=2.1 nM). CSF1R-IN-3 is a potent antiproliferative activity against colorectal cancer cells. CSF1R-IN-3 inhibits the progression of colorectal cancer by suppressing the migration of macrophages, reprograming M2-like macrophages to the M1 phenotype, and enhancing the antitumor immunity.
  • HY-146682
    KS100

    Aldehyde Dehydrogenase (ALDH) Apoptosis Cancer
    KS100 is a potent ALDH inhibitor with IC50s of 230, 1542, 193 nM for ALDH1A1, ALDH2, and ALDH3A1, respectively. KS100 shows antiproliferative and anticancer effects with low low toxic. KS100 significantly increases ROS activity, lipid peroxidation and toxic aldehyde accumulation. KS10600 induces apoptosis and cell cycle arrest at the G2/M phase.
  • HY-146307
    TrxR-IN-3

    Others Cancer
    TrxR-IN-3 (Compound 2c) is a potent inhibitor of TrxR. TrxR-IN-3 exhibits potent antiproliferative activities against five human cancer cell lines, especially against breast tumor cells. TrxR-IN-3 increases ROS levels and resulted in marked apoptosis by regulating apoptosis-related proteins expressed in the breast cancer cells. TrxR-IN-3 also triggers the formation of autophagosomes and autolysosomes by promoting the expression of LC3-II and Beclin-1 and diminishing the expression of LC3-I and p62 proteins.
  • HY-146683
    KS106

    Aldehyde Dehydrogenase (ALDH) Apoptosis Cancer
    KS106 is a potent ALDH inhibitor with IC50s of 334, 2137, 360 nM for ALDH1A1, ALDH2, and ALDH3A1, respectively. KS106 shows antiproliferative and anticancer effects with low low toxic.KS106 significantly increases ROS activity, lipid peroxidation and toxic aldehyde accumulation. KS106 induces apoptosis and cell cycle arrest at the G2/M phase.
  • HY-146276
    CDK/HDAC-IN-2

    HDAC CDK Apoptosis Cancer
    CDK/HDAC-IN-2 is a potent HDAC/CDK dual inhibitor with IC50 of 6.4, 0.25, 45, >1000, 8.63, 0.30, >1000 nM for HDAC1, HDAC2, HDAC3, HDAC6,8, CDK1, CDK2, CDK4,6,7, respectively. CDK/HDAC-IN-2 shows excellent antiproliferative activities. CDK/HDAC-IN-2 induces apoptosis and cell cycle arrest at G2/M phase. CDK/HDAC-IN-2 shows potent antitumor efficacy.
  • HY-N10152
    Malonylginsenoside Rc

    Others Cancer
    Malonylginsenoside Rc is a natural active compound with anti-proliferative activity.
  • HY-U00345
    CHK-IN-1

    Checkpoint Kinase (Chk) Cancer
    CHK-IN-1 is an inhibitor of CHK1 and CHK2, with anti-proliferative activities.
  • HY-N0181
    Ergosterol

    Ergosterin; Provitamin D; Provitamin D2

    Endogenous Metabolite Inflammation/Immunology
    Ergosterol is the primary sterol found in fungi, with antioxidative, anti-proliferative, and anti-inflammatory effects.
  • HY-16114
    BNC105

    Microtubule/Tubulin Cancer
    BNC105 is a tubulin polymerization inhibitor with potent antiproliferative and tumor vascular disrupting properties.
  • HY-146749
    FLT3/TrKA-IN-1

    FLT3 Trk Receptor Apoptosis Cancer
    FLT3/TrKA-IN-1 is a potent FLT3/TrKA dual kinase inhibitor with the IC50s of 43.8 nM, 97.2 nM, 92.5 nM and 23.6 nM for FLT3, FLT3-ITD, FLT3-TKD and TrKA, respectively. FLT3/TrKA-IN-1 induces cell cycle arrest at the G0/G1 phase as well as apoptosis and shows antiproliferative activity in vitro. FLT3/TrKA-IN-1 has the potential for the research of Acute myeloid leukemia (AML).
  • HY-N4313
    Eriosematin

    Apoptosis Metabolic Disease
    Eriosematin is a compound from the roots of Flemingia philippinensis with antiproliferative activity and apoptosis-inducing property.
  • HY-N10503
    Norartocarpetin

    Tyrosinase Ras Raf MAPKAPK2 (MK2) Apoptosis Cancer
    Norartocarpetin is a tyrosinase inhibitor. Norartocarpetin has strong tyrosinase inhibitory activity with an IC50 value of 0.47 μM. Norartocarpetin as an antibrowning agent can be used for the research of food systems. Norartocarpetin also has a significant anticancer activity in lung carcinoma cells (NCI-H460) with an IC50 value of 22 μM. Norartocarpetin has antiproliferative effects are mediated via targeting Ras/Raf/MAPK signalling pathway, mitochondrial mediated apoptosis, S-phase cell cycle arrest and suppression of cell migration and invasion in human lung carcinoma cells.
  • HY-143658
    SH498

    Autophagy Cancer
    SH498, a novel Bmi-1-mediated antitumor agent, shows potent antiproliferative activity.
  • HY-19909
    NRC-2694

    EGFR Cancer
    NRC-2694 is an epidermal growth factor receptor (EGFR) antagonist with anti-cancer and anti-proliferative properties.
  • HY-139189
    DHODH-IN-16

    Dihydroorotate Dehydrogenase DNA/RNA Synthesis Cancer
    DHODH-IN-16 is a potent dihydroorotate dehydrogenase (DHODH) inhibitor with an IC50 of 0.396 nM for human DHODH.
  • HY-N0202
    Atractylenolide II

    Asterolide

    Apoptosis Cancer
    Atractylenolide II is a sesquiterpene compound isolated from the dried rhizome of Atractylodes macrocephala (Baizhu in Chinese); anti-proliferative activity.
  • HY-N1497
    Plumbagin

    2-Methyljuglone

    Others Cancer
    Plumbagin (2-Methyljuglone) is a naphthoquinone isolated from Plumbago zeylanica, exhibits anticancer and antiproliferative activities.
  • HY-N0180
    18β-Glycyrrhetinic acid

    Endogenous Metabolite Cancer Inflammation/Immunology
    18β-Glycyrrhetinic acid is the major bioactive component of Glycyrrhiza uralensis and possesses anti-ulcerative, anti-inflammatory and antiproliferative properties.
  • HY-N0743
    Senkyunolide A

    Others Cancer
    Senkyunolide A, isolated from Ligusticum chuanxiong Hort, has cytoprotective and antiproliferative activities. Anti-tumor activity.
  • HY-B0421S
    Mycophenolic acid-d3

    Mycophenolate-d3

    Endogenous Metabolite Antibiotic Fungal Apoptosis Bacterial Others Others
    Mycophenolic acid D3 (Mycophenolate D3) is deuterium labeled Mycophenolic acid, which is an an immunosuppresant drug and has potent anti-proliferative activity.
  • HY-N0009
    Geniposide

    Amyloid-β Influenza Virus Neurological Disease
    Geniposide is an iridoid glucoside extracted from Gardenia jasminoidesEllis fruits; exhibits a varity of biological activities such as anti-diabetic, antioxidative, antiproliferative and neuroprotective activities.
  • HY-N6735
    Apicidin

    OSI 2040

    HDAC Parasite Cancer Infection
    Apicidin (OSI 2040) is a fungal metabolite, acts as a histone deacetylase (HDAC) inhibitor, with antiparasitic activity and a broad spectrum antiproliferative activity.
  • HY-14808
    Adarotene

    ST1926

    Apoptosis Cancer
    Adarotene is an effective apoptosis inducer, which surprisingly produces DNA damage and exhibites a potent antiproliferative activity on a large panel of human tumor cells.
  • HY-146506
    isoCA-4

    Microtubule/Tubulin Cancer
    isoCA-4, a Combretastatin A4 derivative, is a tubulin polymerization inhibitor. isoCA-4 has anti-proliferative activities.
  • HY-139103
    Thailanstatin C

    DNA/RNA Synthesis Cancer
    Thailanstatin C is a pre-mRNA splicing inhibitor (IC50= 6.84 μM) and antiproliferative agent from Burkholderia thailandensis MSMB43.
  • HY-N7809
    Pelargonidin 3-galactoside chloride

    Others Cancer
    Pelargonidin 3-galactoside chloride is a major anthocyanin with anticancer effects. Pelargonidin 3-galactoside chloride inhibits α-glucosidase.
  • HY-N6871
    Abietic acid

    Bacterial Cancer Infection Metabolic Disease Inflammation/Immunology
    Abietic acid, a diterpene isolated from Colophony, possesses antiproliferative, antibacterial, and anti-obesity properties. Abietic acid inhibits lipoxygenase activity for allergy treatment.
  • HY-151394
    Tubulin polymerization-IN-33

    Microtubule/Tubulin Cancer
    Tubulin polymerization-IN-33 is an inhibitor of [1,2]oxazoloisoindoles tubulin polymerization, exhibits high antiproliferative activity against the NCI panel.
  • HY-115713
    Heme Oxygenase-1-IN-2

    Reactive Oxygen Species Cancer
    Heme Oxygenase-1-IN-2 is a novel heme oxygenase-1 inhibitor (IC50 = 0.95 μM) with potent in vitro antiproliferative activity.
  • HY-116896
    LY117018

    Estrogen Receptor/ERR Cancer
    LY117018, a Raloxifene analog, is a selective estrogen receptor modulator. LY117018 exerts antiproliferative effects on breast cancer cell lines.
  • HY-W013332
    3-Deazaadenosine

    HIV Infection Inflammation/Immunology
    3-Deazaadenosine is an inhibitor of S-adenosylhomocysteine hydrolase, with a Ki of 3.9 µM; 3-Deazaadenosine has anti-inflammatory, anti-proliferative and anti-HIV activity.
  • HY-W013332A
    3-Deazaadenosine hydrochloride

    HIV Infection Inflammation/Immunology
    3-Deazaadenosine (hydrochloride) is an inhibitor of S-adenosylhomocysteine hydrolase, with a Ki of 3.9 µM; 3-Deazaadenosine has anti-inflammatory, anti-proliferative and anti-HIV activity.
  • HY-14807
    Tosedostat

    CHR-2797

    Aminopeptidase Cancer
    Tosedostat (CHR-2797) is an orally active aminopeptidase inhibitor. CHR-2797 exerts antiproliferative effects against a range of tumor cell lines.
  • HY-N7611
    7-Prenyloxyaromadendrin

    Others Cancer
    7-Prenyloxyaromadendrin is a flavonoid from Pterocaulon alopecuroides with antitumor activity. 7-Prenyloxyaromadendrin shows good antiproliferative activity in tumor cell lines.
  • HY-100757
    CPUY074020

    Histone Methyltransferase Cancer
    CPUY074020 is a potent and oral bioavailable inhibitor of histone methyltransferase G9a, with an IC50 of 2.18 μM. CPUY074020 possesses anti-proliferative activity.
  • HY-107470
    Antitumor agent-21

    Others Cancer Inflammation/Immunology
    Antitumor agent-21 is an aryl-quinolin derivative, with potential anticancer, anti-inflammatory, anti-proliferative, anti-hormonal effects and inhibition of vasculogenic mimicry .
  • HY-15995
    Tubulysin A

    TubA

    Microtubule/Tubulin ADC Cytotoxin Apoptosis Cancer
    Tubulysin A(TubA) is a myxobacterial product that can function as an antiangiogenic agent in many in vitro assays; anti-microtubule, anti-mitotic, an apoptosis inducer, anticancer, anti-angiogenic, and antiproliferative.
  • HY-N10393
    Vibsanin A

    PKC HSP Cancer
    Vibsanin A, a protein kinase C (PKC) activator, exhibits anti-proliferative activity against human cancer cell lines. Vibsanin A is also a HSP90 inhibitor.
  • HY-15605
    Encorafenib

    LGX818

    Raf Cancer
    Encorafenib (LGX818) is a highly potent BRAF inhibitor with selective anti-proliferative and apoptotic activity in cells expressing BRAF V600E (EC50=4 nM).
  • HY-146889
    ATX inhibitor 16

    Others Cancer
    ATX inhibitor 16 is a potent ATX inhibitor with an IC50 of 0.0021 µM. ATX inhibitor 16 shows excellent anti-proliferative activities in breast cancer cells.
  • HY-N6621
    Hippeastrine

    Topoisomerase Cancer
    Hippeastrine, an active alkaloid, exhibits a good dose-dependent inhibitory effect against topoisomerase I (Top I) with an IC50 at 7.25 μg/mL. Antiproliferative and anticancer activities.
  • HY-136328
    EZM0414 TFA

    SETD2-IN-1 TFA

    Histone Methyltransferase Cancer
    EZM0414 TFA is a potent, selective and orally active inhibitor of SETD2 which is a human histone methyltransferase. EZM0414 TFA has anti-proliferative effects.
  • HY-146890
    ATX inhibitor 17

    Others Cancer
    ATX inhibitor 17 is a potent ATX inhibitor with an IC50 of 0.019 µM. ATX inhibitor 17 shows excellent anti-proliferative activities in breast cancer cells.
  • HY-117737A
    RRD-251

    Raf Apoptosis Cancer
    RRD-251 is an inhibitor of retinoblastoma tumor suppressor protein (Rb)-Raf-1 interaction, with potent anti-proliferative, anti-angiogenic and anti-tumor activities.
  • HY-W000427
    Ethyl Orsellinate

    Bacterial Cancer Infection
    Ethyl orsellinate is a lichen metabolite and a derivative of lecanoric acid with antiproliferative and antitumour activities. Ethyl Orsellinate is against A. salina for the cytotoxic activity with an LC50 of 495 μM.
  • HY-N2198
    Podocarpusflavone A

    Topoisomerase Apoptosis Cancer
    Podocarpusflavone A is a DNA topoisomerase I inhibitor. Podocarpusflavone A has moderated anti-proliferative activity and induces cell apoptosis in MCF-7. Podocarpusflavone A is developing anti-tumor drugs.
  • HY-N3980
    Guaiol

    Champacol; Guaiac alcohol

    Autophagy Cancer Infection
    Guaiol is a sesquiterpene alcohol that has been found in several traditional Chinese medicinal plants and has antiproliferative, pro-autophagic, insect repellent, and insecticidal biological activities.
  • HY-P2228
    Chlamydocin

    HDAC Apoptosis Cancer
    Chlamydocin, a fungal metabolite, is a highly potent HDAC inhibitor, with an IC50 of 1.3 nM. Chlamydocin exhibits potent antiproliferative and anticancer activities. Chlamydocin induces apoptosis by activating caspase-3.
  • HY-W013032A
    Oxamic acid sodium

    Sodium oxamate

    Lactate Dehydrogenase Apoptosis Cancer
    Oxamic acid (oxamate) sodium salt is a lactate dehydrogenase-A (LDH-A) inhibitor. Oxamic acid sodium salt shows anti-tumor activity, and anti-proliferative activity against cancer cells, and can induce apoptosis.
  • HY-100599
    Urolithin A

    Drug Metabolite Reactive Oxygen Species DNA/RNA Synthesis Autophagy Apoptosis Endogenous Metabolite Cancer
    Urolithin A, a gut-microbial metabolite of ellagic acid, exerts anti-inflammatory, antiproliferative, and antioxidant properties. Urolithin A induces autophagy and apoptosis, suppresses cell cycle progression, and inhibits DNA synthesis.
  • HY-107203
    Propentofylline

    HWA 285

    Phosphodiesterase (PDE) Inflammation/Immunology Neurological Disease
    Propentofylline is a xanthine-derivative that inhibits adenosine uptake and blocks phosphodiesterase activity. Propentofylline has neuroprotective, antiproliferative, and anti-inflammatory effects that improve cognition and dementia severity in patients with Alzheimer's disease or vascular dementia.
  • HY-N6074
    Soyasapogenol B

    Autophagy Apoptosis Cancer
    Soyasapogenol B, an ingredient of soybean, exerts anti-proliferative, anti-metastatic activities. Soyasapogenol B triggers endoplasmic reticulum stress, which mediates apoptosis and autophagy in colorectal cancer.
  • HY-N1205
    Spathulenol

    Others Cancer
    Spathulenol is isolated from Aristolochia yunnanensis, and has antioxidant, anti-inflammatory, antiproliferative and antimycobacterial activities. Spathulenol shows a high antioxidant activity with an IC50 of 85.60 μg/mL in the DPPH system[1].
  • HY-15717
    Kobe2602

    Ras Cancer
    Kobe2602 is a Ras-Raf interaction inhibitor. Kobe2602 inhibits the binding of H-Ras·GTP to c-Raf-1 RBD with a Ki of 149 μM. Kobe2602 has antitumor activity.
  • HY-143250
    Tubulin inhibitor 12

    Microtubule/Tubulin Cancer
    Tubulin inhibitor 12 (Hit 9) is a novel tubulin inhibitor (IC50=25.3 μM). Tubulin inhibitor 12 shows anti-tumor activity and anti-proliferative activity.
  • HY-N4208
    Taccalonolide AJ

    Microtubule/Tubulin Cancer
    Taccalonolide AJ is a semi-synthesis compound with cellular microtubule stabilizing activity. Taccalonolide AJ exhibits high potency antiproliferative activity against cancer cells, with an IC50 of 4.2 nM for HeLa cells.
  • HY-147318
    PBENZ-DBRMD

    Apoptosis Cancer
    PBENZ-DBRMD is a potent iodothyronine deiodinase type 3 (DIO3) inhibitor. PBENZ-DBRMD has anti-proliferative activity and induces apoaptosis. PBENZ-DBRMD can be used for cancer research.
  • HY-32735
    Triptolide

    PG490

    NF-κB Apoptosis Cancer
    Triptolide is a diterpenoid triepoxide extracted from the root of Tripterygium wilfordii with immunosuppressive, anti-inflammatory, antiproliferative and antitumour effects. Triptolide is a NF-κB activation inhibitor.
  • HY-N10392
    (S)-Erypoegin K

    Apoptosis Cancer
    (S)-Erypoegin K is a potent anticancer agent. (S)-Erypoegin K shows potent anti-proliferative activity against HL-60 cells. (S)-Erypoegin K induces apoptosis.
  • HY-N0815
    Resibufogenin

    Bufogenin; Recibufogenin

    Others Cancer
    Resibufogenin, a component of huachansu, has been shown to exhibit the anti-proliferative effect against cancer cells, and this may be attributed to the degradation of cyclin D1 caused by the activation of GSK-3β.
  • HY-146214
    CDK4/6-IN-13

    CDK Cancer
    As a cdk4/6 inhibitor. Compounds 10B and 10C showed low nanomolar activity, ideal antiproliferative activity, excellent metabolic properties and acceptable pharmacokinetics on cdk4/6.
  • HY-13626
    Spisulosine

    ES-285

    PKC Cancer
    Spisulosine (ES-285) is an antiproliferative (antitumoral) compound of marine origin. Spisulosine inhibits the growth of the prostate PC-3 and LNCaP cells through intracellular ceramide accumulation and PKCζ activation.
  • HY-100004
    Fumarate hydratase-IN-1

    Mitochondrial Metabolism Cancer
    Fumarate hydratase-IN-1 (compound 2) is a cell-permeable fumarate hydratase inhibitor. Fumarate hydratase-IN-1 has antiproliferative activity against several cancer cell lines with a mean IC50 of 2.2 μM.
  • HY-N0578
    Apigenin 7-glucoside

    Apigenin-7-O-β-D-glucopyranoside; Cosmosiin; Apigetrin

    Reactive Oxygen Species Cancer
    Apigenin-7-glucoside (Apigenin-7-O-β-D-glucopyranoside) exhibits significant anti-proliferative and antioxidant activity and scavenges reactive oxygen species (ROS).
  • HY-147887
    Tubulin inhibitor 28

    Microtubule/Tubulin Cancer
    Tubulin inhibitor 28 (compound 2g) is a potent tubulin inhibitor with an IC50 value of 1.2 µM. Tubulin inhibitor 28 shows anti-proliferative activity for MCF-7 cells.
  • HY-146255
    Apoptosis inducer 10

    Apoptosis Cancer
    Apoptosis inducer 10 is a potent apoptosis inducer. Apoptosis inducer 10 shows antiproliferative effect. Apoptosis inducer 10 induces apoptosis in HeLa cancer cells via a mitochondria-dependent endogenous pathway.
  • HY-N1060
    Yatein

    HSV Apoptosis Cancer Infection
    Yatein is a lignan isolated from A. chilensis, with antiproliferative activity. Yatein suppresses herpes simplex virus type 1 (HSV-1 ) replication by interruption the immediate-early gene expression.
  • HY-148109
    FAK-IN-7

    FAK Cancer
    FAK-IN-7 (compound 5r) is a FAK inhibitor (IC50=11.72 µM). FAK-IN-7 has good anti-proliferative activity and can be used in cancer research.
  • HY-12424
    Zotarolimus

    ABT-578; A 179578

    Others Cancer Cardiovascular Disease
    Zotarolimus (ABT-578) is a derivative of rapamycin (HY-10219), with anti-proliferative activity. Zotarolimus is an immunosuppressant. Zotarolimus is developed specifically for local delivery from stents for the prevention of coronary artery restenosis.
  • HY-N7085
    Citropten

    5,7-Dimethoxycoumarin; Limettin

    Others Cancer
    Citropten (5,7-Dimethoxycoumarin) is a coumarin isolated from bergamot oil. Citropten (5,7-Dimethoxycoumarin) has an antiproliferative activity against A2058 human melanoma cell line.
  • HY-N3845
    Ergosterol peroxide

    Bacterial Cancer Inflammation/Immunology
    Ergosterol peroxide is a steroid derivative and can be isolated from a variety of fungi, yeast, lichens or sponges. Ergosterol peroxide has anti-tumour, proapoptotic, anti-inflammatory, anti-mycobacterial, and anti-proliferative activities.
  • HY-148110
    FAK-IN-8

    FAK Cancer
    FAK-IN-8 (compound 5h) is a FAK inhibitor (IC50=5.32 µM). FAK-IN-8 has good anti-proliferative activity and can be used in cancer research.
  • HY-B1115A
    Buspirone

    5-HT Receptor Reactive Oxygen Species Cancer Neurological Disease
    Buspirone is an orally active 5-HT1A receptor agonist. Buspirone is a potent anticancer agent. Buspirone shows antiproliferative activity. Buspirone can be used for anxiety, depression and cancer research.
  • HY-N3005
    Britannin

    Apoptosis Autophagy Cancer Inflammation/Immunology
    Britannin, isolated from Inula aucheriana, is a sesquiterpene lactone. Britannin induces apoptosis and autophagy by activating AMPK regulated by ROS in liver cancer cells. Britannin has anti-proliferative and anti-inflammatory activities.
  • HY-114323
    PROTAC FLT-3 degrader 1

    PROTACs FLT3 Apoptosis Cancer
    PROTAC FLT-3 degrader 1 is a von Hippel-Lindau-based PROTAC FLT-3 internal tandem duplication (ITD) degrader with an IC50 0.6 nM. Anti-proliferative activity; apoptosis induction.
  • HY-B0421S1
    Mycophenolic acid 13C,D3

    Mycophenolate 13C,D3

    Fungal Bacterial Endogenous Metabolite Apoptosis Antibiotic Inflammation/Immunology
    Mycophenolic acid 13C,D3 (Mycophenolate 13C,D3) is deuterium labeled Mycophenolic acid 13C. Mycophenolic acid is an an immunosuppresant drug and has potent anti-proliferative activity.
  • HY-116015
    Dihomo-γ-Linolenic acid methyl ester

    Endogenous Metabolite Inflammation/Immunology
    Dihomo-γ-Linolenic acid is an n-6 polyunsaturated fatty acid that is mainly metabolized to an anti-inflammatory eicosanoid, prostaglandin (PG) E1, via the cyclooxygenase (COX) pathway. Anti-inflammatory and anti-proliferative effects.
  • HY-15187
    Filanesib

    ARRY-520

    Kinesin Apoptosis Cancer
    Filanesib (ARRY-520) is a selective and noncompetitive kinesin spindle protein (KSP) inhibitor, with an IC50 of 6 nM for human KSP. Filanesib induces cell death by apoptosis in vitro. Filanesib has potent anti-proliferative activity.
  • HY-110244
    Tilfrinib

    Others Cancer
    Tilfrinib (compound 4f) is a potent and selective Brk/PTK6 inhibitor with an IC50 value of 3.15 nM for Brk. Tilfrinib shows good anti-proliferative activity and has potential of anti-tumour.
  • HY-B1394
    Khellin

    EGFR Cancer Cardiovascular Disease
    Khellin is a furochromone that can be isolated from Ammi visnuga L.. Khellin is an EGFR inhibitor with an IC50 of 0.15 µM. Khelline has anti-proliferative activity in vitro. Khellin has antispasmodic and coronary vasodilator effects.
  • HY-15587
    L82

    DNA/RNA Synthesis Cancer
    L82 is a selective and uncompetitive DNA ligase 1 (DNA Lig1) inhibitor (hLig1 IC50=12 μM). L82 shows anti-proliferative activity to breast cancer cells.
  • HY-N0180S
    18β-Glycyrrhetinic acid-d3

    Endogenous Metabolite Cancer Inflammation/Immunology
    18β-Glycyrrhetinic acid-d3 is deuterium labeled 18β-Glycyrrhetinic acid. 18β-Glycyrrhetinic acid is the major bioactive component of Glycyrrhizae Radix and possesses anti-ulcerative, anti-inflammatory and antiproliferative properties.
  • HY-13626S
    Spisulosine-d3

    PKC Cancer
    Spisulosine-d3 is deuterium labeled Spisulosine. Spisulosine (ES-285) is an antiproliferative (antitumoral) compound of marine origin. Spisulosine inhibits the growth of the prostate PC-3 and LNCaP cells through intracellular ceramide accumulation and PKC
  • HY-151191
    LSD1-IN-22

    Histone Demethylase Cancer
    LSD1-IN-22 is a potent Lysine-specific demethylase 1 (LSD1) inhibitor with a Ki value of 98 nM. LSD1-IN-22 has anti-proliferative activity against certain cancer cells.
  • HY-122844
    BI-853520

    IN-10018

    FAK Cancer
    BI 853520 (IN-10018) is an orally active and potent focal adhesion kinase (FAK) inhibitor (recombinant FAK IC50=1 nM). BI 853520 shows anti-proliferative activity against cancer cells.
  • HY-N7640
    Deoxylimonin

    Others Cancer Inflammation/Immunology
    Desoxylimonin is an orally active triterpenoid compound found from grapefruit seed. Desoxylimonin shows anti-proliferative activities to breast cancer cells. Desoxylimonin derivatives shows better anticancer, analgesic and anti-inflammatory activity than the lead compound.
  • HY-146197
    Apoptotic agent-1

    Apoptosis Cancer
    Apoptotic agent-1 (Compound 8a) is an apoptotic agent with high antiproliferative activity against cancer cells and low cytotoxic effect. Apoptotic agent-1 induces over-expression of Fas receptor and Cyto C genes.
  • HY-146250
    Antitumor agent-71

    Microtubule/Tubulin Cancer
    Antitumor Agent-71 is an antiproliferative activity antitumor agent and against tumor cell lines with IC50 values ranging from 3.98-15.70 μM. Antitumor Agent-71 is an antitumor agent that can inhibit tubulin polymerization.
  • HY-150693
    Estrogen receptor β antagonist 2

    Estrogen Receptor/ERR Cancer
    Estrogen receptor β antagonist 2 is a potent and selective estrogen receptor β (ERβ) antagonist with IC50s of 109.10, 0.63 µM for Erα and Erβ, respectively.
  • HY-122402
    Umirolimus

    Bacterial Inflammation/Immunology
    Umirolimus, a macrocyclic triene lactone Rapamycin derivative, is powerful immunosuppressant and anti-inflammatory agent. Umirolimus has highly lipophilicity and can be used drug-eluting stent (DES) applications.
  • HY-N2254
    (-)-Oxypeucedanin hydrate

    (-)-Prangol

    Others Cancer
    (-)-Oxypeucedanin hydrate ((-)-Prangol) is a derivative of furocoumarin isolated from Ducrosia anethifolia.
  • HY-139108
    DCH36_06

    Histone Acetyltransferase Apoptosis Cancer
    DCH36_06 is a potent and selective p300/CBP inhibitor with IC50s of 0.6 μM and 3.2 μM for p300 and CBP, respectively. DCH36_06 mediated p300/CBP inhibition leading to hypoacetylation on H3K18 in leukemic cells. Anti-tumor activity.
  • HY-32344
    Inecalcitol

    TX 522

    VD/VDR Apoptosis Cancer
    Inecalcitol (TX 522), a unique vitamin D3 analog, is an orally active vitamin D receptor (VDR) agonist with a Kd of 0.53 nM. Inecalcitol can induce cell apoptosis and has potent anticancer activities.
  • HY-N7225
    Yuanhuacine

    Gnidilatidin

    Others Cancer
    Yuanhuacine (Gnidilatidin), a daphnane diterpenoid from the flowers of Daphne genkwa with extensive anti-tumor activity. Yuanhuacine is a DNA-damaging agent with orally active.
  • HY-13737
    R1530

    VEGFR FGFR Apoptosis Cancer
    R1530 is a highly potent, orally active, dual-acting mitosis/angiogenesis inhibitor, with anti-tumor and anti-angiogenic activities. R1530 is a multikinase inhibitor which binds to 31 kinases with Kd values of <500 nM. R1530 inhibits VGFR2 and FGFR1 with IC50 of 10 nM and 28 nM, respectively. R1530 triggers apoptosis (mitotic catastrophe) or senescence.
  • HY-N2959
    Brevilin A

    JAK STAT Apoptosis Autophagy Cancer
    Brevilin A is an orally active STAT3/JAK inhibitor (STAT3 IC50= 10.6 µM). Brevilin A shows anti-tumor activity, anti-proliferative activity to cancer cells, and can induce apoptosis and autophagy.
  • HY-15187B
    Filanesib TFA

    ARRY-520 TFA

    Kinesin Cancer
    Filanesib TFA (ARRY-520 TFA) is a selective kinesin spindle protein (KSP) inhibitor, with an IC50 of 6 nM for human KSP. Filanesib TFA induces cell death by apoptosis in vitro. Filanesib TFA has potent anti-proliferative activity.
  • HY-112316
    BAY1238097

    Epigenetic Reader Domain Cancer
    BAY1238097 is a potent and selective inhibitor of BET binding to histones and has strong anti-proliferative activity in different AML (acute myeloid leukemia) and MM (multiple myeloma) models through down-regulation of c-Myc levels and its downstream transcriptome (IC50 <100 nM).
  • HY-150730
    FAK-IN-6

    FAK Cancer
    FAK-IN-6 is a potent FAK inhibitor with an IC50 value of 1.415 nM. FAK-IN-6 has anti-proliferative activity against certain cancer cell lines. FAK-IN-6 can be used for researching pancreatic cancer.
  • HY-150567
    SMO-IN-3

    Smo Hedgehog Cancer
    SMO-IN-3 (compound 12a) is a potent smoothened (SMO) inhibitor with an IC50 value of 34.09 nM for hedgehog (Hh) signaling pathway. SMO-IN-3 has antiproliferative activity against human medulloblastoma cell line Daoy. Anticancer activity.
  • HY-16984
    GNE-4997

    Itk Inflammation/Immunology
    GNE-4997 is a potent and selective interleukin-2-inducible T-cell kinase (ITK) inhibitor with a Ki of 0.09 nM, and the correlation between the basicity of solubilizing elements in GNE-4997 and off-target antiproliferative effects reduces cytotoxicity.
  • HY-146754
    MMP2-IN-1

    MMP Apoptosis Cancer
    MMP2-IN-1 is a moderate potenet MMP2 inhibitor with IC50 of 6.8 µM. MMP2-IN-1 exhibits remarkable antiproliferative activity in certain cancer cells by arresting the cell cycle and inducing apoptosis.
  • HY-17037
    Pirenzepine dihydrochloride

    LS 519; Pirenzepin dihydrochloride; Gastrozepin dihydrochloride

    mAChR Cancer Metabolic Disease
    Pirenzepine (LS 519) dihydrochloride is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist. Pirenzepine dihydrochloride reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine dihydrochloride shows anti-proliferative activity to cancer cells.
  • HY-118091A
    Bexlosteride

    LY300502

    Others Cancer
    Bexlosteride (LY300502) is a benzoquinolinone human type I 5α-reductase inhibitor. Bexlosteride shows metabolic inhibitory, antiproliferative, and antisecretory effects in LNCaP human prostatic adenocarcinoma cell cultures. Bexlosteride can be used for the research of prostatic cancer.
  • HY-149033
    Kobusine derivative-2

    Others Cancer
    Kobusine derivative-2, a kobusine derivative, has antiproliferative activity against cancer cells. Kobusine derivative-2 can induce the arrest of MDA-MB-231 cells in the sub-G1 phase. Anticancer activity.
  • HY-N7015
    Zerumbone

    HSV Infection
    Zerumbone is a monocyclic sesquiterpene compound isolated from the rhizomes of Zingiber zerumbet Smith. Zerumbone potently inhibits the activation of Epstein-Barr virus with an IC50 of 0.14 mM. Zerumbone has anti-cancer, antioxidant, anti-inflammatory and anti-proliferative activity.
  • HY-150564
    SMO-IN-2

    Smo Hedgehog Cancer
    SMO-IN-2 (compound 1) is a potent smoothened (SMO) inhibitor with an IC50 value of 123.4 nM for hedgehog (Hh) signaling pathway. SMO-IN-2 has antiproliferative activity against human medulloblastoma cell line Daoy. Anticancer activity.
  • HY-144755
    MC2652

    Histone Demethylase Cancer
    MC2652 (compound 1a) is a potent LSD1 inhibitor. MC2652 displays high inhibiting effects in MV4-11 and NB4 leukaemia cells. MC2652 shows antiproliferative activity against prostate cancer LNCaP cells.
  • HY-144898
    SB-216

    Microtubule/Tubulin Cancer
    SB-216 is a potent tubulin polymerization inhibitor. SB-216 shows strong antiproliferative potency in a panel of human cancer cell lines, including melanoma, lung cancer, and breast cancer.  SB-216 can be used for cancer research.
  • HY-147928
    Apoptotic agent-2

    Apoptosis Caspase Bcl-2 Family Cancer
    Apoptotic agent-2 (compound 14b) induces apoptosis by down-regulation of Bcl-2 and up-regulation of Bax and caspase-3. Apoptotic agent-2 exhibits anti-proliferative activities and can be used for cancer research.
  • HY-128359
    ACBI1

    PROTACs Epigenetic Reader Domain Apoptosis Cancer
    ACBI1 is a potent and cooperative SMARCA2, SMARCA4 and PBRM1 degrader with DC50s of 6, 11 and 32 nM, respectively. ACBI1 is a PROTAC degrader. ACBI1 shows anti-proliferative activity. ACBI1 induces apoptosis.
  • HY-128602
    c-Kit-IN-2

    c-Kit Cancer
    c-Kit-IN-2 is a c-KIT inhibitor with an IC50 of 82 nM, shows superior antiproliferative activities against all the three GIST cell lines, GIST882, GIST430, and GIST48, with GI50s of 3, 1, and 2 nM, respectively.
  • HY-147570
    ATR-IN-18

    ATM/ATR Cancer
    ATR-IN-18 (compound 2) is an orally active and potent ATR kinase inhibitor, with an IC50 of 0.69 nM. ATR-IN-18 shows antiproliferative activity in LoVo cells, with an IC50 of 37.34 nM. ATR-IN-18 has anti-tumor activity.
  • HY-146209
    Tubulin polymerization-IN-13

    Microtubule/Tubulin Apoptosis Cancer
    Tubulin polymerization-IN-13 (Compound 4f) is a tubulin polymerization inhibitor (IC50=0.37 μM). Tubulin polymerization-IN-13 shows anti-proliferative activity against cancer cells, induces apoptosis and potential antivascular activity.
  • HY-120607
    Chevalone C

    Parasite Cancer Infection
    Chevalone C, a meroterpenoid fungal metabolite, shows antimalarial activity with IC50 value of 25.00 μg/mL. Chevalone C has anti-proliferative activity on colon HCT116, liver HepG2 and melanoma A375 cancer cell lines.
  • HY-17037A
    Pirenzepine

    LS 519 free base; Pirenzepin; Gastrozepin

    mAChR Cancer Metabolic Disease
    Pirenzepine (LS 519 free base) is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist. Pirenzepine reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine shows anti-proliferative activity to cancer cells.
  • HY-136611
    ω-Hydroxy-DEET

    Drug Metabolite Infection
    ω-Hydroxy-DEET is a major metabolite of insect repellent N-N-diethyl-meta-toluamide (DEET). ω-Hydroxy-DEET has anti-proliferative effects. DEET is a spatial repellent and an irritant that commonly used to prevent contact with mosquitoes.
  • HY-100775
    Fezagepras sodium

    Setogepram sodium; PBI-4050 sodium

    Free Fatty Acid Receptor GPR84 Metabolic Disease Inflammation/Immunology
    Fezagepras (Setogepram) sodium acts as an orally active agonist for GPR40 and as an antagonist or inverse agonist for GPR84. Fezagepras sodium decreases renal, liver and pancreatic fibrosis. Fezagepras sodium exerts anti-fibrotic, anti-inflammatory and anti-proliferative actions.
  • HY-100775A
    Fezagepras

    Setogepram; PBI-4050

    Free Fatty Acid Receptor GPR84 Metabolic Disease Inflammation/Immunology
    Fezagepras (Setogepram) acts as an orally active agonist for GPR40 and as an antagonist or inverse agonist for GPR84. Fezagepras decreases renal, liver and pancreatic fibrosis. Fezagepras exerts anti-fibrotic, anti-inflammatory and anti-proliferative actions.
  • HY-143280
    Topoisomerase II inhibitor 4

    Topoisomerase Cancer
    Topoisomerase II inhibitor 4 (compound E17) is a potent Topoisomerase II inhibitor. Topoisomerase II inhibitor 4 triggers G2/M cell cycle arrest and shows anti-tumor activity with strong cytotoxic and anti-proliferative effect.
  • HY-115928
    M24

    Bcl-2 Family Cancer
    M24 is a Mcl-1 selective inhibitor. M24 exhibits good binding affinity against Mcl-1 with Ki value of 0.33 μM. M24 exhibits good anti-proliferative activity and induce apoptosis in HepG2 cells.
  • HY-123159
    AKI603

    Aurora Kinase Cancer
    AKI603 is an inhibitor of Aurora kinase A (AurA), with an IC50 of 12.3 nM. AKI603 is developed to overcome resistance mediated by BCR-ABL-T315I mutation. AKI603 exhibits strong anti-proliferative activity in leukemic cells.
  • HY-146188
    Topoisomerase II inhibitor 8

    Topoisomerase Cancer
    Topoisomerase II inhibitor 8 (compound 22) is a potent topoisomerase II inhibitor, with an IC50 of 0.52 μM. Topoisomerase II inhibitor 8 exhibits good anti-proliferative activities and can arrest the cell cycle at G2/M phase.
  • HY-151203
    PKG1α activator 3

    Others Cardiovascular Disease
    PKG1α activator 3 is a PKG1α activator (EC50 basal/partial=13/0.52 μM). PKG1α activator 3 shows anti-proliferative effects to smooth muscle cell, and can be used in cardiovascular disease research.
  • HY-N1066
    Xanthohumol D

    Others Cancer
    Xanthohumol D, isolated from hops, is an inhibitor of quinone reductase-2 (QR-2) with the IC50 value of 110 μM, and binds to the active site of QR-2. Xanthohumol D shows antiproliferative activity on human cancer cell lines in vitro.
  • HY-N0448
    10-Gingerol

    Others Cancer Inflammation/Immunology
    10-Gingerol is a major pungent constituent in the ginger oleoresin from fresh rhizome, with anti-inflammatory, antioxidant and anti-proliferative activities. 10-Gingerol inhibits the proliferation of MDA-MB-231 tumor cell line with an IC50 of 12.1 μM.
  • HY-14807S
    Tosedostat-d5

    Aminopeptidase Cancer
    Tosedostat-d5 (CHR-2797-d5) is the deuterium labeled Tosedostat. Tosedostat (CHR-2797) is an orally active aminopeptidase inhibitor. CHR-2797 exerts antiproliferative effects against a range of tumor cell lines.
  • HY-147741
    DPPY

    JAK Btk EGFR Cancer Inflammation/Immunology
    DPPY (compound 6) is a potent PTK inhibitor with IC50 values of <10, <10, <10 nM for EGFR, BTK, JAK3, respectively. DPPY shows anti-proliferative activity against B-cell lymphoma cells. DPPY has the potential for the research of idiopathic pulmonary fibrosis (IPF).
  • HY-N2920
    β-Amyrenonol

    11-Oxo-β-amyrin

    Cytochrome P450 Cancer Inflammation/Immunology
    β-Amyrenonol (11-Oxo-β-amyrin), an oleanolic-type triterpenoid in licorice roots, is a precursor of Glycyrrhetinic acid. β-Amyrenonol has anti-proliferative and anti-inflammatory activities, and β-Amyrenonol could function as the skeleton for the synthesis of many triterpenoids.
  • HY-128587
    Mevociclib

    SY-1365

    CDK Cancer
    Mevociclib (SY-1365) is a potent and first-in-class selective CDK7 inhibitor, with a Ki of 17.4 nM. Mevociclib exhibits anti-proliferative and apoptotic effects in solid tumor cell lines. Mevociclib possesses anti-tumor activity in hematological and multiple aggressive solid tumors.
  • HY-126141
    JAK/HDAC-IN-1

    JAK HDAC Cancer
    JAK/HDAC-IN-1 is a potent JAK2/HDAC dual inhibitor, exhibits antiproliferative and proapoptotic activities in several hematological cell lines. JAK/HDAC-IN-1 shows IC50s of 4 and 2 nM for JAK2 and HDAC, respectively.
  • HY-147803
    TrxR-IN-5

    Reactive Oxygen Species Cancer
    TrxR-IN-5 (compound 4f) is a potent TrxR (thioredoxin reductase) inhibitor, with an IC50 of 0.16 μM. TrxR-IN-5 increases the levels of ROS, thus leading to potent antiproliferative effects. TrxR-IN-5 exhibits prominent anticacer and anti-metastasis effects.
  • HY-N7072
    Grape seed extract

    Apoptosis Cancer Metabolic Disease Inflammation/Immunology
    Grape seed extract is a natural product, with anti-inflammatory and anti-proliferative effects. Grape seed extract shows inhibitory activity on the fat-metabolizing enzymes pancreatic lipase and lipoprotein lipase. Grape seed extract induces apoptotic in human colorectal cancer cells.
  • HY-B0199
    Mycophenolate Mofetil

    RS 61443; TM-MMF

    Drug Metabolite Apoptosis Endogenous Metabolite Bacterial Cancer
    Mycophenolate mofetil (RS 61443) is the morpholinoethylester prodrug of Mycophenolic acid. Mycophenolate mofetil inhibits de novo purine synthesis via the inhibition of inosine monophosphate dehydrogenase (IMPDH). Mycophenolate mofetil shows selective lymphocyte antiproliferative effects involve both T and B cells, preventing antibody formation.
  • HY-111538
    MAGL-IN-1

    MAGL Cancer
    MAGL-IN-1 is a potent, selective, reversible and competitive inhibitor of MAGL, with an IC50 of 80 nM. MAGL-IN-1 exhibits anti-proliferative effects against human breast, colorectal, and ovarian cancer cells. MAGL-IN-1 blocks MAGL in cell-based as well as in vivo assays.
  • HY-101667
    LTURM34

    DNA-PK Cancer
    LTURM34 is a specific DNA-PK inhibitor (IC50=34 nM). LTURM34 exhibits 170-fold selectivity for DNA-PK over PI3K. LTURM34 shows potent antiproliferative activity in a wide range of tumor cell lines.
  • HY-N0181A
    Lumisterol

    9β,10α-Ergosterol

    Endogenous Metabolite Metabolic Disease
    Lumisterol (9β,10α-Ergosterol), a steroid compound, is the (9β,10α)-stereoisomer of Ergosterol (HY-N0181). Lumisterol is a photoprotective agent against UVB-induced DNA damage and anti-proliferative activities.
  • HY-15456
    NVP-BVU972

    c-Met/HGFR Cancer
    NVP-BVU972 is an selective and potent Met inhibitor, with an IC50 of 14 nM. NVP-BVU972 also exhibits good anti-proliferative activity against Met with drug-resistant mutations and inhibits phosphorylation. NVP-BVU972 can be used in study of cancer.
  • HY-146227
    DNA topoisomerase II inhibitor 1

    Topoisomerase Apoptosis Cancer
    DNA topoisomerase II inhibitor 1 (compound 8ed) is a potent DNA topoisomerase II inhibitor. DNA topoisomerase II inhibitor 1 shows anti-proliferative activity. DNA topoisomerase II inhibitor 1 induces apoptosis and cell cycle arrest at sub G1 phase.
  • HY-N3523
    3-O-Beta-D-Glucopyranosylplatycodigenin

    Others Cancer
    3-O-Beta-D-Glucopyranosylplatycodigenin is an oleanane-type triterpenoid isolated from roots of Platycodon grandiflorum. 3-O-Beta-D-Glucopyranosylplatycodigenin exhibits anti-proliferative activities against HSC-T6 cell line with an IC50 of 13.36 μM.
  • HY-147929
    Apoptotic agent-3

    Apoptosis Caspase Bcl-2 Family Cancer
    Apoptotic agent-3 (compound 15f) promotes apoptosis through the potential mitochondria-mediated Bcl-2/Bax pathway and activation of the Caspase 3 pathway. Apoptotic agent-3 exhibits anti-proliferative activities and can be used for cancer research.
  • HY-N6797
    Meleagrin

    Bacterial c-Met/HGFR Antibiotic Cancer Infection
    Meleagrin is a roquefortine C-derived alkaloid produced by fungi of the genus Penicillium and has antimicrobial and anti-proliferative activities. Meleagrin is a class of FabI inhibitor. Meleagrin is a lead c-Met inhibitory entity useful for the control of c-Met-dependent metastatic and invasive breast malignancies.
  • HY-147726
    Microtubule inhibitor 5

    Microtubule/Tubulin Cancer
    Microtubule inhibitor 5 (compound 17f) is a potent microtubule inhibitor. Microtubule inhibitor 5 shows cytotoxicity with an IC50 value of 154.5 nM for NCI-H460 cells. Microtubule inhibitor 5 shows good cell permeability.
  • HY-147941
    MS9427

    PROTACs EGFR Cancer
    MS9427 is a potent PROTAC EGFR degrader with Kds of 7.1 nM and 4.3 nM for EGFR WT and EGFR L858R, respectively. MS9427 effectively induces degradation of mutant EGFRs through both the ubiquitin/proteasome system (UPS) and autophagy/lysosome pathways. MS9427 potently inhibits the proliferation of NSCLC cells. MS9427 can be used for researching anticancer.
  • HY-124007
    4-Iodo-SAHA

    ISAHA

    HDAC Cancer
    4-Iodo-SAHA (1k) is an orally active class I and class II histone deacetylase (HDAC) inhibitor with EC50s of 1.1, 0.95, 0.12, 0.24, 0.85 and 1.3 μM for Skbr3, HT29, U937, JA16 and HL60 cell lines, respectively. 4-Iodo-SAHA (1k) can be used for the research of cancer.
  • HY-151382
    CK2-IN-3

    Casein Kinase Cancer
    CK2-IN-3 is a selective and potent CK2 inhibitor (Kd: 12 nM), with IC50 values of 1.51 μM (CK2α) and 7.64 μM (CK2α’). CK2-IN-3 can be used in the research of cancers.
  • HY-132197
    CBP/p300-IN-12

    Epigenetic Reader Domain Histone Acetyltransferase Cancer
    CBP/p300-IN-12 is a potent and selective covalent histone acetyltransferases p300 (IC50 of 166 nM) and CBP inhibitor. CBP/p300-IN-12 decreases the levels of H3K27Ac of PC-3 cells (EC50 of 37 nM). CBP/p300-IN-12 forms a covalent adduct with C1450.
  • HY-147942
    MS9449

    PROTACs EGFR Cancer
    MS9449 is a potent PROTAC EGFR degrader with Kds of 17 nM and 10 nM for EGFR WT and EGFR L858R, respectively. MS9449 effectively induces degradation of mutant EGFRs through both the ubiquitin/proteasome system (UPS) and autophagy/lysosome pathways. MS9449 potently inhibits the proliferation of NSCLC cells. MS9449 can be used for researching anticancer.
  • HY-147935
    NTQ1062

    Akt Cancer
    NTQ1062 is a potent and orally active Akt inhibitor with IC50s of 0.4 nM, 6.3 nM and 0.1 nM for Akt1, Akt2 and Akt3, respectively. NTQ1062 induces cell apoptosis and arrests the cell cycle at G0/G1 phase. NTQ1062 exhibits antiproliferation activity against various cancer cells. NTQ1062 exhibits potent antitumor efficacy in LNCap xenograft mouse model.
  • HY-143389
    Cdc7-IN-14

    CDK Cancer
    Cdc7-IN-14 (compound 82) is a potent CDC7 inhibitor with an IC50 of <1 nM. Cdc7-IN-14 has the potential for the research of cancer.
  • HY-143387
    Cdc7-IN-13

    CDK Cancer
    Cdc7-IN-13 (compound 84) is a potent CDC7 inhibitor with an IC50 of <1 nM. Cdc7-IN-13 has the potential for the research of cancer.
  • HY-146114
    Antitumor agent-67

    Others Cancer
    Antitumor agent-67 (compound 3) is a potent antitumor agent. Antitumor agent-67 has highly selective toxicity to cancer cells and lower damage to normal cells. Antitumor agent-67 can be activated by NQO1 and effectively liberate podophyllotoxin and kill tumor cells. Antitumor agent-67 significantly suppresses cancer growth in HepG2 xenograft models without obvious toxicity.
  • HY-115937
    c-Met-IN-9

    c-Met/HGFR Apoptosis Cancer
    c-Met-IN-9, a 4-phenoxypyridine derivative, is a c-Met kinas inhibitor with an IC50 of 12 nM. c-Met-IN-9 induces cells apoptosis, and has antitumor activities.
  • HY-147030
    PARP1-IN-8

    PARP Cancer
    PARP1-IN-8 (compound 11c) is a potent and BBB-penetrated PARP1 inhibitor, with an IC50 of 97 nM. PARP1-IN-8 shows significantly potent anti-proliferative activity against Human lung adenocarcinoma epithelial cell line A549.
  • HY-N6005
    Methyl caffeate

    Bacterial Cancer Infection
    Methyl caffeate, an antimicrobial agent, shows moderate antimicrobial and prominent antimycobacterial activities. Methyl caffeate also exhibits α-glucosidase inhibition activity, oxidative stress inhibiting activity, anti-platelet activity, antiproliferative activity in cervix adenocarcinoma and anticancer activity in lung and leukmia cell lines.
  • HY-P99218
    Robatumumab

    Sch 717454; 19D12

    IGF-1R Cancer
    Robatumumab (Sch 717454) is an anti-human IGF-1R (insulin-like growth factor receptor-1) antibody. Robatumumab shows anti-tumor activity and anti-proliferative activity to cancer cells. Robatumumab can be used in osteosarcoma and Ewing sarcoma research.
  • HY-122594
    BNS-22

    Topoisomerase Cancer
    BNS-22 is a DNA topoisomerase II (TOP2) catalytic inhibitor with the IC50 values of 2.8 μM and 0.42 μM for human TOP2α and TOP2β, respectively. BNS-22 induces abnormal division and has anti-proliferative activity.
  • HY-16196
    ENMD-1198

    IRC-110160

    Microtubule/Tubulin HIF/HIF Prolyl-Hydroxylase STAT Cancer
    ENMD-1198 (IRC-110160), an orally active microtubule destabilizing agent, is a 2-methoxyestradiol analogue with antiproliferative and antiangiogenic activity. ENMD-1198 is suitable for inhibiting HIF-1alpha and STAT3 in human HCC cells and leads to reduced tumor growth and vascularization.
  • HY-151480
    HP590

    STAT Apoptosis Cancer
    HP590 is an orally active, novel and potent STAT3 inhibitor (STAT3 luciferase activity: IC50=27.8 nM; ATP inhibition: IC50=24.7 nM). HP590 shows anti-proliferative activity to gastric cancer cells and induces apoptosis.
  • HY-146368
    PROTAC VEGFR-2 degrader-1

    PROTACs VEGFR Cancer
    PROTAC VEGFR-2 degrader-1(PROTAC-1), a PROTAC VEGFR-2 degrader, exhibits little VEGFR-2 inhibition (IC50> 1 μM) and anti-proliferative activity against EA.hy926 cells (IC50> 100 μM).
  • HY-145438
    Antitumor agent-38

    Others Cancer
    Antitumor agent-38 is a potent antitumor agents. Antitumor agent-38 shows antiproliferative activity for cancer cells. Antitumor agent-38 induces cell cycle arrest at the late S and G2/M phase without interfering with microtubule formation or cell morphology[1].
  • HY-137977
    DMU-212

    ERK Apoptosis Cancer
    DMU-212 is a methylated derivative of Resveratrol (HY-16561), with antimitotic, anti-proliferative, antioxidant and apoptosis promoting activities. DMU-212 induces mitotic arrest via induction of apoptosis and activation of ERK1/2 protein. DMU-212 has orally active.
  • HY-147888
    Tubulin inhibitor 29

    Microtubule/Tubulin Cancer
    Tubulin inhibitor 29 (compound 3c) is a potent tubulin inhibitor with an IC50 value of 1.2 µM. Tubulin inhibitor 29 shows antiproliferative effects with an IC50 value of 7.5 µM for MCF-7 cells. Tubulin inhibitor 29 inhibits tubulin assembly and bounds in the colchicine site.
  • HY-B0356B
    Ciprofloxacin hydrochloride monohydrate

    Bay-09867 hydrochloride monohydrate

    Topoisomerase Apoptosis Antibiotic Bacterial Mitochondrial Metabolism Reactive Oxygen Species Infection Cancer
    Ciprofloxacin (Bay-09867) hydrochloride monohydrate is a potent, orally active topoisomerase IV inhibitor. Ciprofloxacin hydrochloride monohydrate induces mitochondrial DNA and nuclear DNA damage and lead to mitochondrial dysfunction, ROS production. Ciprofloxacin hydrochloride monohydrate has anti-proliferative activity and induces apoptosis. Ciprofloxacin hydrochloride monohydrate is a fluoroquinolone antibiotic, exhibiting potent antibacterial activity.
  • HY-100933
    MY-5445

    Phosphodiesterase (PDE) Cancer Inflammation/Immunology Cardiovascular Disease
    MY-5445 is a specific inhibitor of the cyclic GMP phosphodiesterase, phosphodiesterase type 5 (PDE5), with a Ki of 1.3 μM. MY-5445 inhibits human platelet aggregation. MY-5445 is a selective modulator of ATP-binding cassette (ABC) transporter ABCG2, with anti-proliferative effect.
  • HY-144288
    BLK-IN-2

    Btk Cancer
    BLK-IN-2 (compound 25) is a potent and selective irreversible inhibitor of B-Lymphoid tyrosine kinase (BLK), with an IC50 of 5.9 nM. BLK-IN-2 also inhibits BTK (IC50=202.0 nM). BLK-IN-2 shows potent antiproliferative activities against several lymphoma cells.
  • HY-101870B
    Uzansertib phosphate

    INCB053914 phosphate

    Pim Cancer
    Uzansertib (INCB053914) phosphate is an orally active, ATP-competitive pan-PIM kinase inhibitor with IC50s of 0.24 nM, 30 nM, 0.12 nM for PIM1, PIM2, PIM3, respectively. Uzansertib phosphate has broad anti-proliferative activity against a variety of hematologic tumor cell lines.
  • HY-143458
    FAK PROTAC B5

    FAK PROTACs Cancer
    FAK PROTAC B5 (Compound B5) is a FAK PROTAC degrader with an IC50 value of 14.9 nM. FAK PROTAC B5 presents strong FAK degradation activity, antiproliferative activity, outstanding plasma stability and moderate membrane permeability. FAK PROTAC B5 inhibits cell migration and invasion.
  • HY-115994
    Carbonic anhydrase inhibitor 10

    Carbonic Anhydrase Cancer
    Carbonic anhydrase inhibitor 10 is a potent hCA IX inhibitor with a Ki value of 6.2 nM. Carbonic anhydrase inhibitor 10 exhibits anti-proliferative activity against MCF-7 cancer cell line with an IC50 of 11.9 μM. Carbonic anhydrase inhibitor 10 can be used for cancer research.
  • HY-147290
    NSC 694623

    Histone Acetyltransferase Cancer
    NSC 694623 is a potent histone acetyltransferase (HAT) inhibitor with an IC50 value of 15.9 μM for recombinant HAT p300/CBP-associated factor (PCAF). NSC 694623 has antiproliferative activity against certain cancer cells. NSC 694623 can be used for researching anticancer.
  • HY-101870
    Uzansertib

    INCB053914

    Pim Cancer
    Uzansertib (INCB053914) is an orally active, ATP-competitive pan-PIM kinase inhibitor with IC50s of 0.24 nM, 30 nM, 0.12 nM for PIM1, PIM2, PIM3, respectively. Uzansertib has broad anti-proliferative activity against a variety of hematologic tumor cell lines.
  • HY-144304
    PROTAC EGFR degrader 2

    PROTACs EGFR Cancer
    PROTAC EGFR degrader 2 is a potent PROTAC EGFR degrader. PROTAC EGFR degrader 2 exhibits excellent antiproliferative activity with IC50 of 4.0 nM and good EGFR degradation activity with DC50 of 36.51 nM. PROTAC EGFR degrader 2 can be used for the synthesis of nitroreductase (NTR)-responsive PROTAC.
  • HY-107551
    GLI antagonist-1

    Gli Cancer
    GLI antagonist-1 is a potent GLI antagonist with an IC50 value of 1.1 µM. GLI antagonist-1 shows anti-proliferative activity. GLI antagonist-1 decreases the GLI1 mRNA expression. GLI antagonist-1 inhibits colony formation in a dose-dependent manner.
  • HY-N6776
    Penitrem A

    Potassium Channel Cancer Neurological Disease
    Penitrem A is an indole diterpene neurotoxic alkaloid produced by Penicillium, acts as a selective BK channel antagonist with antiproliferative and anti-invasive activities against multiple malignancies. Penitrem A increases the spontaneous release of endogenous glutamate, gamma-aminobutyric acid (GABA) and aspartate from cerebrocortical synaptosomes, and induces tremorgenic syndromes in animals.
  • HY-107203S
    Propentofylline-d6

    HWA 285-d6

    Phosphodiesterase (PDE) Inflammation/Immunology Neurological Disease
    Propentofylline-d6 (HWA 285-d6) is the deuterium labeled Propentofylline. Propentofylline is a xanthine-derivative that inhibits adenosine uptake and blocks phosphodiesterase activity. Propentofylline has neuroprotective, antiproliferative, and anti-inflammatory effects that improve cognition and dementia severity in patients with Alzheimer's disease or vascular dementia.
  • HY-150611
    EGFR-IN-70

    EGFR Cancer
    EGFR-IN-70 (compound 18j) is a potent EGFR inhibitor with IC50 values of 23.6 and 307.5 nM for EGFR LR/TM/CS and EGFR WT, respectively. EGFR-IN-70 has anti-proliferative activity and suppresses phosphorylation of the EGFR. EGFR-IN-70 can be used for cancer research.
  • HY-151576
    PRMT5:MEP50 PPI

    Others Cancer
    PRMT5:MEP50 PPI is a novel PRMT5:MEP50 protein-protein interaction (PRMT5:MEP50 PPI) inhibitor, shows anti-tumor activity and anti-proliferative activity of lung and prostate cancer cells.
  • HY-32735S
    Triptolide-d3

    PG490-d3

    NF-κB Apoptosis Cancer
    Triptolide-d3 (PG490-d3) is the deuterium labeled Triptolide. Triptolide is a diterpenoid triepoxide extracted from the root of Tripterygium wilfordii with immunosuppressive, anti-inflammatory, antiproliferative and antitumour effects. Triptolide is a NF-κB activation inhibitor.
  • HY-13491
    GNF-5837

    Trk Receptor Cancer
    GNF-5837 is a potent, selective, and orally bioavailable pan-tropomyosin receptor kinase (TRK) inhibitor which display antiproliferative effects in cellular Ba/F3 assays ( IC50 values of 7 nM, 9 nM and 11 nM for cells containing the fusion proteins Tel-TrkC, Tel-TrkB and Tel-TrkA, respectively) .
  • HY-146093
    Antitumor agent-62

    Apoptosis Cancer
    Antitumor agent-62 (Compound 47) is a NO-releasing antitumor agent. Antitumor agent-62 shows antiproliferative activity against four cancer cell lines. Antitumor agent-62 activates mitochondrial apoptosis pathway and arrests cell cycle at G2/M phase.
  • HY-A0143
    Dihomo-γ-linolenic acid

    all-cis-8,11,14-Eicosatrienoic acid

    Endogenous Metabolite Cancer Inflammation/Immunology Cardiovascular Disease
    Dihomo-γ-linolenic acid (all-cis-8,11,14-Eicosatrienoic acid) is a 20-carbon ω-6 fatty acid, with anti-inflammatory and anti-proliferative activities. Dihomo-γ-linolenic acid attenuates atherosclerosis in the apolipoprotein E deficient mouse model system.
  • HY-147703
    Aurora kinase inhibitor-9

    Aurora Kinase Cancer
    Aurora kinase inhibitor-9 (compound 9d) is a potent AURKA/B dual aurora kinase inhibitor with IC50s of 0.093, 0.09 µM for Aurora A, Aurora B, respectively. Aurora kinase inhibitor-9 shows broad spectrum anti-proliferative activity.
  • HY-14543
    Sertindole

    Lu 23-174

    5-HT Receptor Dopamine Receptor Adrenergic Receptor Autophagy Neurological Disease Cancer
    Sertindole (Lu 23-174) is an orally active 5-HT2A, 5-HT2C, dopamine D2, and αl-adrenergic receptors antagonist. Sertindole shows antipsychotic activity and anti-proliferative activity to multiple cancer cells.
  • HY-146040
    Anticancer agent 47

    Apoptosis Cancer
    Anticancer agent 47 (compound 4j) is a potent anticancer agent. Anticancer agent 47 shows antiproliferative activities. Anticancer agent 47 induces apoptosis and cell cycle arrest at G0/G1 phase. Anticancer agent 47 shows shows antitumor activities in vivo.
  • HY-N4286
    4-Methyldaphnetin

    Apoptosis Cancer
    4-Methyldaphnetin is a precursor in the synthesis of derivatives of 4-methyl coumarin. 4-Methyldaphnetin has potent, selective anti-proliferative and apoptosis-inducing effects on several cancer cell lines. 4-Methyldaphnetin possesses radical scavenging property and strongly inhibits membrane lipid peroxidation.
  • HY-146389
    Anticancer agent 50

    MDM-2/p53 P-glycoprotein Cancer
    Anticancer agent 50 (compound 6) is a potent ABCB1 efflux pump modulator. Anticancer agent 50 shows cytotoxic effects and antiproliferative effects. Anticancer agent 50 decreases the expression of cyclin D1 and induces p53 expression. Anticancer agent 50 has the potential for the research of T-lymphoma.
  • HY-B0356
    Ciprofloxacin

    Bay-09867

    Topoisomerase Apoptosis Antibiotic Bacterial Mitochondrial Metabolism Reactive Oxygen Species Cancer Infection
    Ciprofloxacin (Bay-09867) is a potent, orally active topoisomerase IV inhibitor. Ciprofloxacin induces mitochondrial DNA and nuclear DNA damage and lead to mitochondrial dysfunction, ROS production. Ciprofloxacin has anti-proliferative activity and induces apoptosis. Ciprofloxacin is a fluoroquinolone antibiotic, exhibiting potent antibacterial activity.
  • HY-146369
    PROTAC VEGFR-2 degrader-2

    PROTACs VEGFR Cancer
    PROTAC VEGFR-2 degrader-2(PROTAC-4), a PROTAC VEGFR-2 degrader, exhibits little VEGFR-2 inhibition (IC50> 1 μM) and anti-proliferative activity against EA.hy926 cells (IC50> 100μM).
  • HY-N10158
    1,7-Bis(4-hydroxyphenyl)-3-hydroxy-1,3-heptadien-5-one

    Others Cancer
    1,7-Bis(4-hydroxyphenyl)-3-hydroxy-1,3-heptadien-5-one (compound 39), a diarylheptanoid, exhibits antiproliferative activity towards human HT-1080 fibrosarcoma and murine colon 26-L5 carcinoma cells.
  • HY-150595
    HDAC6-IN-10

    HDAC Microtubule/Tubulin Cancer
    HDAC6-IN-10 is a highly selective HDAC6 inhibitor with the IC50 of 0.73 nM. HDAC6-IN-10 has 144~10941-fold selectivity over other HDAC isoforms. HDAC6-IN-10 shows anti-proliferative activities against multiple myeloma cells.
  • HY-B1816
    Zaprinast

    M&B 22948

    Phosphodiesterase (PDE) GPR35 Neurological Disease Cardiovascular Disease Endocrinology
    Zaprinast (M&B 22948) is an inhibitor of cGMP-selective Phosphodiesterases(PDEs). Zaprinast is a G protein-coupled receptor (GPR) 35 agonist which activates rat GPR35 strongly and activates human GPR35 moderately. Zaprinast reduces vessel remodeling through antiproliferative and proapoptotic effects.
  • HY-123024
    Cefatrizine

    BL-S-640; SK&F 60771

    Apoptosis Bacterial Antibiotic Cancer Infection
    Cefatrizine (BL-S-640) is an orally active and broad-spectrum cephalosporin antibiotic. Cefatrizine is also a eEF2K inhibitor, with anti-proliferative activity in human breast cancer cells, which could induce ER stress, leading to cell death. Cefatrizine can be used in studies of cancer and bacterial infection.
  • HY-147298
    Plogosertib

    CYC140

    Polo-like Kinase (PLK) Cancer
    Plogosertib (CYC140) is a selective, potent, and orally active ATP-competitive PLK1 inhibitor (IC50: 3 nM). Plogosertib is an anti-cancer agent with anti-proliferative activity. Plogosertib can be used in the research of several tumors, including esophageal, gastric, leukemia, non–small cell lung cancer, ovarian, and squamous cell cancers.
  • HY-150576
    c-Met-IN-13

    c-Met/HGFR Cancer
    c-Met-IN-13 is a potent c-Met inhibitor with an IC50 value of 2.43 nM. c-Met-IN-13 shows excellent cytotoxicity for cancer cells. c-Met-IN-13 shows antiproliferative activity in a concentration- and time- dependent manner. c-Met-IN-13 has the potential for the research of cancer.
  • HY-112316A
    (R)-BAY1238097

    Epigenetic Reader Domain Cancer
    (R)-BAY1238097 is the R-isomer with lower activity of BAY1238097. BAY1238097 is a potent and selective inhibitor of BET binding to histones and has strong anti-proliferative activity in different AML (acute myeloid leukemia) and MM (multiple myeloma) models through down-regulation of c-Myc levels and its downstream transcriptome.
  • HY-W027968
    Coumarin-3-carboxylic Acid

    2-Oxochromene-3-carboxylic acid

    Others Cancer
    Coumarin-3-carboxylic acid (2- Oxochromene-3-carboxylic acid) is an important initial compound for the synthesis of coumarins which are well known natural products for their diverse biological activities. Lanthanide complexes of Coumarin-3-carboxylic acid exhibit antiproliferative activity towards K-562 cell line.
  • HY-147897
    Apoptosis inducer 9

    Apoptosis
    Apoptosis inducer 9 induces apoptosis with IC50 value of 4.21 μM. Apoptosis inducer 9 induces apoptosis through the mitochondrial pathway and enhance the expression of Cl-caspase-3, Cl-caspase-9 and Cl-PARP. Apoptosis inducer 9 can be used the potential to develop new anti-proliferative agents.
  • HY-144793
    Deac-SS-Biotin

    Others Cancer
    Deac-SS-Biotin is a potent antitumor agent. Deac-SS-Biotin uptakes into the cells through biotin-mediated internalization. Deac-SS-Biotin combined with DTT (Glutathione mimetic) can effectively inhibit microtubule assembly and displays greater antitumor activity.
  • HY-137092
    IACS-13909

    SHP2 Phosphatase Cancer
    IACS-13909 is a selective, potent and orally active SHP2 allosteric inhibitor with an IC50 of 15.7 nM and a Kd of 32 nM. IACS-13909 is more selective for SHP2 than other phosphatases (including SHP1). IACS-13909 has antitumor activities and suppresses MAPK pathway signaling in receptor tyrosine kinases (RTK)-dependent cancers.
  • HY-149029
    TH-6

    HDAC Apoptosis Reactive Oxygen Species Cancer
    TH-6 is a potent HDAC inhibitor with IC50s of 0.115, 0.135, 0.242, 0.138, 2.120 µM for HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, respectively. TH-6 inhibits cell migration and invasion. TH-6 induces apoptosis and cell cycle arrest at G2/M phase. TH-6 shows anti-tumor activity.
  • HY-N6722
    Swainsonine

    Tridolgosir

    Apoptosis Antibiotic Cancer Infection
    Swainsonine (Tridolgosir) is an natural indolizidine alkaloid, a potent and reversible α-mannosidase inhibitor. Swainsonine induces apoptosis and cell cycle arrest at G2/M phase. Swainsonine shows anti-tumor activity.
  • HY-147824
    Tubulin polymerization-IN-22

    Microtubule/Tubulin Apoptosis Cancer
    Tubulin polymerization-IN-22 is a tubulin polymerization inhibitor with an IC50 of 8.1 μM. Tubulin polymerization-IN-22 arrests cell cycle at G2/M phase and induces apoptosis.
  • HY-114162A
    VTP50469 fumarate

    Epigenetic Reader Domain Apoptosis Cancer
    VTP50469 fumarate is a potent, highly selective and orally active Menin-MLL interaction inhibitor with a Ki of 104 pM. VTP50469 fumarate has potently anti-leukemia activity.
  • HY-151563
    OTUB1/USP8-IN-1

    Deubiquitinase Cancer
    OTUB1/USP8-IN-1 is a potent dual OTUB1/USP8 inhibitor with IC50 values of 0.17 and 0.28 nM for OTUB1 and USP8, respectively. OTUB1/USP8-IN-1 can be used in research of cancer.
  • HY-114162
    VTP50469

    Epigenetic Reader Domain Apoptosis Cancer
    VTP50469 is a potent, highly selective and orally active Menin-MLL interaction inhibitor with a Ki of 104 pM. VTP50469 has potently anti-leukemia activity.
  • HY-146735
    MNK1/2-IN-6

    MNK Apoptosis Cancer
    MNK1/2-IN-6 is a potent and selective MNK1/2 inhibitor with IC50s of 2.3 nM and 3.4 nM for MNK1 and MNK2, respectively. MNK1/2-IN-6 induces apoptosis in a concentration-dependent manner.
  • HY-B1793
    Tetraethylammonium chloride

    Potassium Channel Cancer Neurological Disease
    Tetraethylammonium chloride is a non-selective potassium channel blocker. Tetraethylammonium chloride is a good substrate for organic cation transporter (OCTN1). Tetraethylammonium chloride antitumor properties.
  • HY-144450
    PI3K-IN-29

    PI3K Akt Cancer
    PI3K-IN-29 is a potent PI3K inhibitor. PI3K-IN-29 displays good inhibition potencies against U87MG, HeLa and HL60 cells with IC50 values of 0.264, 2.04 and 1.14 µM, respectively. PI3K-IN-29 inhibits PI3K/Akt pathway by inhibiting phosphorylation of Akt that is catalyzed by PI3K.
  • HY-131065
    MET kinase-IN-2

    c-Met/HGFR Cancer
    MET kinase-IN-2 is a potent, selective, orally bioavailable MET kinase inhibitor with an IC50 of 7.4 nM. MET kinase-IN-2 has antitumor activity.
  • HY-117884
    (Rac)-CCT 250863

    Apoptosis Cancer
    (Rac)-CCT 250863 (compound rac-21) is a selective and reversible NEK 2 inhibitor with an IC50 of 0.073 µM. (Rac)-CCT 250863 shows good effects of inducing cell cycle arrest and also can antiproliferative in cells (Pomalidomide sensitive/resistant). (Rac)-CCT 250863 induces apoptosis when combines with Pomalidomide.
  • HY-144369
    Proteasome-IN-4

    Proteasome Cancer
    Proteasome-IN-4 is an excellent and non-covalent proteasome inhibitor (IC50=8.39 nM). Proteasome-IN-4 has potent antiproliferative activities against RPMI-8226, MM-1S and MV-4-11 cell lines. Proteasome-IN-4 can be used for cancer research.
  • HY-10082A
    (E)-3-AP

    (E)-PAN-811; (E)-NSC# 663249; (E)-OCX191

    DNA/RNA Synthesis Cancer
    (E)-3-AP is the E configuration of 3-AP. 3-AP is a potent ribonucleotide reductase inhibitor. 3-AP shows anti-proliferative activity. 3-AP shows anticancer activity in L1210 leukemia model. 3-AP inhibits RR activity and DNA synthesis.
  • HY-137756
    JAK2-IN-6

    JAK Cancer
    JAK2-IN-6, a multiple-substituted aminothiazole derivative, is a potent and selective JAK2 inhibitor with an IC50 of 22.86 μg/mL. JAK2-IN-6 shows no activity against JAK1 and JAK3. JAK2-IN-6 has anti-proliferative effect against cancer cells.
  • HY-B1452
    Licofelone

    ML-3000

    COX Lipoxygenase Apoptosis Cancer Inflammation/Immunology
    Licofelone (ML-3000) is a dual COX/5-lipoxygenase (5-LOX) inhibitor (IC50=0.21/0.18 μM, respectively) for the treatment of osteoarthritis. Licofelone exerts anti-inflammatory and anti-proliferative effects. Licofelone induces apoptosis, and decreases the production of proinflammatory leukotrienes and prostaglandins.
  • HY-147966
    HDAC-IN-43

    HDAC PI3K mTOR Cancer
    HDAC-IN-43 is a potent HDAC 1/3/6 inhibitor with IC50 values of 82, 45, and 24 nM, respectively. HDAC-IN-43 is a weak PI3K/mTOR inhibitors with IC50 values of 3.6 and 3.7 μM, respectively. HDAC-IN-43 shows broad anti-proliferative activity .
  • HY-N0108
    Physcion

    Parietin; Rheochrysidin

    Bacterial Cancer Infection Inflammation/Immunology
    Physcion (Parietin) is an anthraquinone isolated from traditional Chinese medicine Radix et Rhizoma Rhei, acts as an inhibitor of 6-phosphogluconate dehydrogenase, with an IC50 and a Kd of 38.5 μM and 26.0 μM, respectively. Physcion (Parietin) exhibits laxative, hepatoprotective, anti-inflammatory, anti-microbial, anti-proliferative and anti-tumor effects.
  • HY-150694
    HDAC6-IN-11

    HDAC Cancer
    HDAC6-IN-11 (Compound 9) is a selective HDAC6 inhibitor with the IC50 value of 20.7 nM. HDAC6-IN-11 has more than 300-fold selectivity over HDAC other isoforms. HDAC6-IN-11 shows anti-proliferative activities against cancer cells.
  • HY-147414
    Vamotinib

    PF-114

    Bcr-Abl Cancer
    Vamotinib (PF-114) is a potent, selective and orally active tyrosine kinase inhibitor. Vamotinib inhibits the autophosphorylation of BCR/ABL and BCR/ABL-T315I. Vamotinib induces apoptosis. Vamotinib shows anti-proliferative and anti-tumor activity. Vamotinib has the potential for the research of resistant philadelphia chromosome-positive (Ph+) leukemia.
  • HY-142945
    KRAS G12C inhibitor 43

    Ras Cancer
    KRAS G12C inhibitor 43 (compound 59) is a potent KRAS G12C inhibitor. KRAS G12C inhibitor 43 shows antimigration and anti-proliferative activity with IC50s of 0.001-1 µM, >1 µM, >1 µM for H358, A549, HCC cells ,respectively.
  • HY-146467
    Anticancer agent 62

    Others Cancer
    Anticancer agent 62 (compound 4c) is a potent anticancer agent. Anticancer agent 62 shows antiproliferative activity in HepG2, Bel-7402 and MCF-7 cancer cells, with IC50 values of 0.019, 0.060 and 0.016 μM, respectively. Anticancer agent 62 shows effective tumor growth inhibition.
  • HY-100683
    A12B4C3

    Phosphatase Cancer
    A12B4C3 is a potent human polynucleotide kinase/phosphatase (hPNKP) inhibitor with an IC50 value of 0.06 μM. A12B4C3 has antiproliferative activity against cancer cells. A12B4C3 can also enhance the radiosensitivity of certain cancer cells.
  • HY-15605S
    Encorafenib-13C,d3

    LGX818-13C,d3

    Raf Cancer
    Encorafenib-13C,d3 (LGX818-13C,d3) is the 13C- and deuterium labeled Encorafenib. Encorafenib (LGX818) is a highly potent BRAF inhibitor with selective anti-proliferative and apoptotic activity in cells expressing BRAF V600E (EC50=4 nM).
  • HY-128588
    STAT3-IN-3

    STAT Apoptosis Cancer
    STAT3-IN-3 is a potent and selective inhibitor of signal transducer and activator of transcription 3 (STAT3), with anti-proliferative activity. STAT3-IN-3 induces apoptosis in breast cancer cells. STAT3-IN-3 acts as a promising mitochondria-targeting STAT3 inhibitor for cancer research.
  • HY-W040298
    Ciprofloxacin lactate

    Bay-09867 lactate

    Topoisomerase Apoptosis Antibiotic Bacterial Mitochondrial Metabolism Reactive Oxygen Species Cancer Infection
    Ciprofloxacin (Bay-09867) lactate is a potent, orally active topoisomerase IV inhibitor. Ciprofloxacin lactate induces mitochondrial DNA and nuclear DNA damage and lead to mitochondrial dysfunction, ROS production. Ciprofloxacin lactate has anti-proliferative activity and induces apoptosis. Ciprofloxacin lactate is a fluoroquinolone antibiotic, exhibiting potent antibacterial activity.
  • HY-145857
    GRP78-IN-1

    HSP Apoptosis Cancer
    GRP78-IN-1 exhibits several interactions with GRP78 residues with binding energy of -8.07 kcal/mol. GRP78-IN-1 shows the potent cytotoxic, anti-proliferative in cancer cells. GRP78-IN-1 exhibits promising apoptosis in breast cancer cells and wound healing properties.
  • HY-B0356A
    Ciprofloxacin monohydrochloride

    Bay-09867 monohydrochloride

    Topoisomerase Apoptosis Antibiotic Bacterial Mitochondrial Metabolism Reactive Oxygen Species Infection Cancer
    Ciprofloxacin (Bay-09867) monohydrochloride is a potent, orally active topoisomerase IV inhibitor. Ciprofloxacin monohydrochloride induces mitochondrial DNA and nuclear DNA damage and lead to mitochondrial dysfunction, ROS production. Ciprofloxacin monohydrochloride has anti-proliferative activity and induces apoptosis. Ciprofloxacin monohydrochloride is a fluoroquinolone antibiotic, exhibiting potent antibacterial activity.
  • HY-111551
    FT113

    Fatty Acid Synthase (FASN) Cancer
    FT113 is a potent and orally active fatty acid synthase (FASN) inhibitor, with an IC50 of 213 nM for full-length recombinant human FASN enzyme. In cell-based assay, FT113 blocks FASN activity in BT474 cells (IC50, 90 nM). FT113 shows anti-proliferative activity, and exhibits anti-cancer activity both in vitro and in vivo.
  • HY-124822
    COH-SR4

    AMPK Cancer Metabolic Disease
    COH-SR4 is an AMPK activator. COH-SR4 shows potent anti-proliferative activities against leukemia, melanoma, breast and lung cancers. COH-SR4 inhibits adipocyte differentiation via AMPK activation. COH-SR4 can be used for the research of obesity and related metabolic disorders.
  • HY-145426
    MPT0B390

    HDAC Cancer
    MPT0B390 is an arylsulfonamide-based derivative with potent HDAC inhibitory ability. MPT0B390, TIMP3 inducer, inhibits tumor growth, metastasis and angiogenesis. MPT0B390 shows antiproliferative activity against human colon cancer cell line HCT116 with the GI50 of 0.03 μM.
  • HY-147906
    Anticancer agent 71

    Apoptosis PARP Cancer
    Anticancer agent 71 (Compound 4b) is a potent anticancer agent and induces apoptosis. Anticancer agent 71 arrests cell cycle at G2/M phase and induces apoptosis through upregulating Bax, Ikb-α and cleaved PARP and downregulating Bcl-2 expression levels. Anticancer agent 71 shows antiproliferative activity.
  • HY-150615
    SphK1-IN-2

    SphK Apoptosis Cancer
    SphK1-IN-2 is a potent, selective SphK1 inhibitor with IC50 values of 19.81 nM and >10 μM for SphK1 and SphK2, respectively. SphK1-IN-2 exhibits anti-proliferative activities and induces cell cycle arrest and apoptosis. SphK1-IN-2 can be used for cancer research.
  • HY-134601
    KH-3

    Histone Demethylase Cancer
    KH-3 is a potent RNA-binding protein Hu antigen R (HuR) inhibitor with an IC50 value of 0.35 μM. KH-3 has anti-proliferative activity. KH-3 suppresses breast cancer cell invasion as well as delays the initiation of lung colonies by disrupting HuR-FOXQ1 mRNA interaction.
  • HY-147742
    Thi-DPPY

    JAK Inflammation/Immunology
    Thi-DPPY (compound 8e) is a potent and orally active JAK3 inhibitor with IC50 values of 62.4, 1.38 nM for BTK, JAK, respectively. Thi-DPPY shows anti-proliferative activity against HBE cells. Thi-DPPY shows anti-inflammatory activity in vivo. Thi-DPPY has the potential for the research of idiopathic pulmonary fibrosis (IPF).
  • HY-146466
    Anticancer agent 61

    Others Cancer
    Anticancer agent 61 (compound 3v) is an orally active and potent anticancer agent. Anticancer agent 61 shows antiproliferative activity in HepG2, Bel-7402 and MCF-7 cancer cells, with IC50 values of 1.12, 1.97 and 1.08 μM, respectively. Anticancer agent 61 shows effective tumor growth inhibition.
  • HY-50767C
    Palbociclib hydrochloride

    PD-0332991 hydrochloride

    CDK Cancer
    Palbociclib (PD 0332991) hydrochloride is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib hydrochloride has potent anti-proliferative activity and induces cell cycle arrest in cancer cells. Palbociclib hydrochloride can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma.
  • HY-103193
    NKH477

    Colforsin dapropate hydrochloride

    Adenylate Cyclase Cardiovascular Disease
    NKH477 (Colforsin dapropate hydrochloride) directly activates the catalytic unit of adenylate cyclase and increases intracellular cAMP. NKH477 is a forskolin derivative that improves cardiac failure mainly through its beneficial effects on diastolic cardiac function. NKH477 exerts an antiproliferative effect in vivo with an altered cytokine profile to inhibit the acute rejection of rat orthotopic lung allografts.
  • HY-B0199S
    Mycophenolate Mofetil-d4

    Drug Metabolite Apoptosis Endogenous Metabolite Cancer
    Mycophenolate Mofetil-d4 is the deuterium labeled Mycophenolate Mofetil. Mycophenolate mofetil (RS 61443) is the morpholinoethylester prodrug of Mycophenolic acid. Mycophenolate mofetil inhibits de novo purine synthesis via the inhibition of inosine monophosphate dehydrogenase (IMPDH). Mycophenolate mofetil shows selective lymphocyte antiproliferative effects involve both T and B cells, preventing antibody formation.
  • HY-147892
    HDAC-IN-42

    HDAC Apoptosis Cancer
    HDAC-IN-42 (compound 14f) is a potent and selective HDAC inhibitor with IC50 values of 0.19 and 4.98 µM for HDAC1 and HDAC6, respectively. HDAC-IN-42 shows anticancer and anti-proliferative activity. HDAC-IN-42 induces apoptosis and cell cycle arrest at G2/M phase.
  • HY-50767B
    Palbociclib dihydrochloride

    PD-0332991 dihydrochloride

    CDK Cancer
    Palbociclib (PD 0332991) dihydrochloride is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib dihydrochloride has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma.
  • HY-144831
    6BrCaQ-C10-TPP

    HSP Cancer
    6BrCaQ-C10-TPP is a potent mitochondrial heat shock protein TRAP1 inhibitor, with antiproliferative activity in various human cancer cells (IC50=0.008-0.30 μM). 6BrCaQ-C10-TPP can also induces mitochondrial membrane disturbance.
  • HY-150791
    FLDP-5

    Reactive Oxygen Species DNA/RNA Synthesis Cancer
    FLDP-5 is a blood-brain barrier (BBB) penetrant curcuminoid analogues. FLDP-5 can induce production of ROS (Reactive Oxygen Species), DNA damage and cell cycle S phase arrest. FLDP-5 exhibits highly potent tumour-suppressive effects with anti-proliferative and anti-migratory activities on LN-18 cells.
  • HY-50767
    Palbociclib

    PD 0332991

    CDK Cancer
    Palbociclib (PD 0332991) is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma.
  • HY-147734
    Calpain Inhibitor-2

    Others Cancer
    Calpain inhibitors are lipophilic and show moderate to good antiproliferative activity in vitro compared with melanoma cell lines (a-375 and b-16f1) and PC-3 prostate cancer cells. In addition, a member of this group (compound 3) expressed 2 μ M concentration inhibited the invasion of DU-145 cells by 80%.
  • HY-150590
    20S Proteasome-IN-2

    Proteasome Cancer
    20S Proteasome-IN-2 is a human 20S proteasome inhibitor. 20S Proteasome-IN-2 shows high selectivity to its β5 subunit with the IC50 of 0.18 μM. 20S Proteasome-IN-2 displays anti-proliferative effect in vitro and in vivo, and arrests cell cycle at G2/M.
  • HY-B0391A
    Naftopidil dihydrochloride

    KT-611 dihydrochloride; BM-15275 dihydrochloride

    Adrenergic Receptor Cancer
    Naftopidil dihydrochloride (KT-611 dihydrochloride) is a selective alpha1-adrenoceptor antagonist, with Kis of 3.7 nM, 20 nM and 1.2 nM for the cloned human α1a-, α1b- and α1d-adrenoceptor subtypes, respectively. Naftopidil dihydrochloride has antiproliferative effects. Naftopidil dihydrochloride can be used for the research of prostate hyperplasia.
  • HY-144732
    TRK/ALK-IN-1

    Trk Receptor Anaplastic lymphoma kinase (ALK) Cancer
    TRK/ALK-IN-1 (compound 21) is a potent and dual inhibitor of TRK and ALK. TRK/ALK-IN-1 in the enzymatic assays is in good accordance with anti-proliferative activity with IC50 values of 2.2, 9.3 and 38 nM towards TRKA, ALK WT and ALK L1196M, respectively. TRK/ALK-IN-1 has the potential for the research of cancer diseases.
  • HY-115980
    Anticancer agent 39

    Apoptosis Cancer
    Anticancer agent 39 (compound B12), a fluorescent derivative of Jiyuan Oridonin A (JOA), induces the collapse of mitochondrial membrane potential (MMP)and thus induced apoptosis.Anticancer agent 39 inhibits cell cloning and migration.Anticancer agent 39 exhibits promising anti-proliferative activity against HGC-27 cells with IC50 value of 0.39 μM.
  • HY-15856B
    Flupentixol dihydrochloride

    Flupenthixol dihydrochloride

    Dopamine Receptor PI3K Apoptosis Cancer Neurological Disease
    Flupentixol is an orally active D1/D2 dopamine receptor antagonist and new PI3K inhibitor (PI3Kα IC50=127 nM). Flupentixol shows anti-proliferative activity to cancer cells and induces apoptosis. Flupentixol can also be used in schizophrenia, anxiolytic and depressive research.
  • HY-150566
    BCR-ABL-IN-5

    Bcr-Abl Cancer
    BCR-ABL-IN-5 (compound II) is a Bcr-Abl kinase (Breakpoint cluster region-Abelson) inhibitor. BCR-ABL-IN-5 inhibits Bcr-Abl WT and Bcr-Abl T3151 with the IC50 value of 0.014 μM and 0.45 μM, respectively. BCR-ABL-IN-5 has some anti-proliferative activity against leukemic cells.
  • HY-115672
    KS15

    Others Cancer
    KS15 is an inhibitor of the interactions between cryptochromes (CRYs: CRY1 and CRY2) and the CLOCK:BMAL1 heterodimer. KS15 impairs the feedback actions of CRYs on E-box-dependent transcription (EC50=4.9 μM) by CLOCK:BMAL1 heterodimer, an indispensable transcriptional regulator of the mammalian circadian clock. Anti-proliferative activity.
  • HY-B0391B
    Naftopidil hydrochloride

    KT-611 hydrochloride; BM-15275 hydrochloride

    Adrenergic Receptor Cancer
    Naftopidil hydrochloride (KT-611 hydrochloride) is a selective alpha1-adrenoceptor antagonist, with Kis of 3.7 nM, 20 nM and 1.2 nM for the cloned human α1a-, α1b- and α1d-adrenoceptor subtypes, respectively. Naftopidil hydrochloride has antiproliferative effects. Naftopidil hydrochloride can be used for the research of prostate hyperplasia.
  • HY-B0736
    Sertaconazole

    FI7056 free base

    Fungal Autophagy Apoptosis p38 MAPK Microtubule/Tubulin Cancer Infection Inflammation/Immunology
    Sertaconazole (FI7056 free base) is a broad-spectrum topical antifungal agent, exhibits anti-inflammatory activity via activation of a p38-COX-2-PGE2 pathway. Sertaconazole is also a microtubule inhibitor, shows antiproliferative effect, induces apoptosis and autophagy, and can also inhibit the migration of cells.
  • HY-B0391
    Naftopidil

    KT-611; BM-15275

    Adrenergic Receptor Cardiovascular Disease Endocrinology
    Naftopidil (KT-611) is is a selective alpha1-adrenoceptor antagonist, with Kis of 3.7 nM, 20 nM and 1.2 nM for the cloned human α1a-, α1b- and α1d-adrenoceptor subtypes, respectively. Naftopidil has antiproliferative effects. Naftopidil can be used for the research of prostate hyperplasia.
  • HY-N6844
    8,​9-​Epoxy-​3-​isobutyryloxy-​10-​(2-​methylbutanoyl)​thymol

    Others Cancer
    8,9-Epoxy-3-isobutyryloxy-10-(2-methylbutanoyl)thymol is a chemical composition of essential oils from Telekia speciosa. 8,9-Epoxy-3-isobutyryloxy-10-(2-methylbutanoyl)thymol also shows marked antipro-liferative activity against human cancer cell lines in vitro.
  • HY-147793
    FGFR4-IN-12

    FGFR Cancer
    FGFR4-IN-12 (Compound A34) is a potent inhibitor of FGFR4. FGFR4-IN-12 exhibits improved FGFR4 inhibitory capability and selectivity and excellent anti-proliferative activities against FGFR4-dependent HCC cell lines. FGFR4-IN-12 has the potential for the research of cancer diseases.
  • HY-15856A
    Flupentixol

    Flupenthixol

    Dopamine Receptor PI3K Apoptosis Neurological Disease
    Flupentixol is an orally active D1/D2 dopamine receptor antagonist and new PI3K inhibitor (PI3Kα IC50=127 nM). Flupentixol shows anti-proliferative activity to cancer cells and induces apoptosis. Flupentixol can also be used in schizophrenia, anxiolytic and depressive research.
  • HY-B0736A
    Sertaconazole nitrate

    FI7056

    Fungal Autophagy Apoptosis p38 MAPK Microtubule/Tubulin Infection
    Sertaconazole nitrate (FI7056) is a broad-spectrum topical antifungal agent, exhibits anti-inflammatory activity via activation of a p38-COX-2-PGE2 pathway. Sertaconazole nitrate is also a microtubule inhibitor, shows antiproliferative effect, induces apoptosis and autophagy, and can also inhibit the migration of cells.
  • HY-B0360
    Rebamipide

    OPC12759; Proamipide

    COX Cancer Inflammation/Immunology
    Rebamipide (OPC12759) is an orally active gastroprotective agent that enhances the production of endogenous PGs (especially intragastric PGE2) by inducing COX-2 expression, thereby protecting the gastric mucosa from injury. Rebamipide exerts anti-proliferative activity against gastric cancer cells. Rebamipide can be used in studies of mucosal protection, gastroduodenal ulcer, gastritis and gastric cancer.
  • HY-147027
    PARP-1-IN-2

    PARP Caspase Apoptosis Cancer
    PARP-1-IN-2 (compound 11g) is a potent and BBB-penetrated PARP1 inhibitor, with an IC50 of 149 nM. PARP1-IN-2 shows significantly potent anti-proliferative activity against Human lung adenocarcinoma epithelial cell line A549. PARP1-IN-2 can induce A549 cells apoptosis.
  • HY-50767A
    Palbociclib monohydrochloride

    PD 0332991 monohydrochloride

    CDK Cancer
    Palbociclib (PD 0332991) monohydrochloride is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib monohydrochloride has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma.
  • HY-A0065
    Palbociclib isethionate

    PD 0332991 isethionate

    CDK Cancer
    Palbociclib (PD 0332991) isethionate is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib isethionate has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma.
  • HY-129589
    Thailanstatin A

    ADC Cytotoxin Cancer
    Thailanstatin A is an ultra-potent inhibitor of eukaryotic RNA splicing (IC50=650 nM). Thailanstatin A exerts effects via non-covalent binding to the SF3b subunit of the U2 snRNA subcomplex of the spliceosome and shows low-nM to sub-nM IC50s against multiple cancer cell lines. Thailanstatin A, a payload for ADCs, is conjugated to the lysines on trastuzumab yielding “linker-less” ADC.
  • HY-107096
    CH-0793076

    TP3076

    Topoisomerase Cancer
    CH-0793076 (TP3076), a hexacyclic camptothecin analog, is active drug and major metabolite of TP300. CH-0793076 inhibits DNA topoisomerase I with an IC50 of 2.3 μM. CH-0793076 is efficacious against cells expressing BCRP (breast cancer resistance protein).
  • HY-N1039A
    Manool

    Others Cancer
    Manool is a diterpene from Salvia officinalis. Manool induces selective cytotoxicity in cancer cells. Manool arrests the cancer cells at the G(2)/M phase of the cell cycle.
  • HY-13821
    Epoxomicin

    BU-4061T

    Proteasome Apoptosis Cancer Inflammation/Immunology
    Epoxomicin (BU-4061T) is an epoxyketone-containing natural product and a potent, selective and irreversible proteasome inhibitor. Epoxomicin covalently binds to the LMP7, X, MECL1, and Z catalytic subunits of the proteasome and potently inhibits primarily the chymotrypsin-like activity. Epoxomicin can cross the blood-brain barrier. Epoxomicin has strongly antitumor and anti-inflammatory activity.
  • HY-139361
    Sulfopin

    PIN1-3

    Others Cancer
    Sulfopin (PIN1-3) is a highly selective covalent inhibitor of Pin1 with an apparent Ki of 17 nM. Sulfopin blocks Myc-driven tumors in vivo. The peptidyl-prolyl isomerase, Pin1, is exploited in cancer to activate oncogenes and inactivate tumor suppressors.
  • HY-19544
    JAK3-IN-1

    JAK Cancer
    JAK3-IN-1 is a potent, selective and orally active JAK3 inhibitor with an IC50 of 4.8 nM. JAK3-IN-1 shows over 180-fold more selective for JAK3 than JAK1 (IC50 of 896 nM) and JAK2 (IC50 of 1050 nM).
  • HY-145264
    OARV-771

    Epigenetic Reader Domain PROTACs Cancer
    OARV-771 is a VHL-based BET degrader (PROTAC) with improved cell permeability. OARV-771 shows DC50s of 6, 1, and 4 nM for Brd4, Brd2 and Brd3, respectively.
  • HY-15346
    Copanlisib

    BAY 80-6946

    PI3K Apoptosis Cancer
    Copanlisib (BAY 80-6946) is a potent, selective and ATP-competitive pan-class I PI3K inhibitor, with IC50s of 0.5 nM, 0.7 nM, 3.7 nM and 6.4 nM for PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ, respectively. Copanlisib has more than 2,000-fold selectivity against other lipid and protein kinases, except for mTOR. Copanlisib has superior antitumor activity.
  • HY-149036
    PAA5

    Ferroptosis Endogenous Metabolite Reactive Oxygen Species Cancer
    PAA5 is a methide carbon-centered polynuclear Au(I) cluster. PAA5 can release Au(I) causing Pro-oxidant response and accelerated ferroptosis. PAA5 increases the expression of pH2AX in a time-dependent manner. PAA5 has anticancer activity.
  • HY-137478A
    KB-0742 dihydrochloride

    CDK Cancer
    KB-0742 dihydrochloride is a potent, selective and orally active CDK9 inhibitor with an IC50 of 6 nM for CDK9/cyclin T1. KB-0742 dihydrochloride is selective for CDK9/cyclin T1 with >50-fold selectivity over other CDK kinases. KB-0742 dihydrochloride has potent anti-tumor activity.
  • HY-147725
    Microtubule inhibitor 4

    Microtubule/Tubulin Cancer
    Microtubule inhibitor 4 (compound 2) is a potent microtubule inhibitor. Microtubule inhibitor 4 shows cytotoxicity with IC50s of 4.0, 3.2, 2.1 nM for NCI-H460, BxPC-3, HT-29 cells, respectively. Microtubule inhibitor 4 shows the inhibition of tubulin polymerization.
  • HY-15346A
    Copanlisib dihydrochloride

    BAY 80-6946 dihydrochloride

    PI3K Apoptosis Cancer
    Copanlisib dihydrochloride (BAY 80-6946 dihydrochloride) is a potent, selective and ATP-competitive pan-class I PI3K inhibitor, with IC50s of 0.5 nM, 0.7 nM, 3.7 nM and 6.4 nM for PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ, respectively. Copanlisib dihydrochloride has more than 2,000-fold selectivity against other lipid and protein kinases, except for mTOR. Copanlisib dihydrochloride has superior antitumor activity.
  • HY-19792
    Mertansine

    DM1; Maytansinoid DM1

    Microtubule/Tubulin ADC Cytotoxin Cancer
    Mertansine (DM1) is a microtubulin inhibitor and is an antibody-conjugatable maytansinoid that is developed to overcome systemic toxicity associated with maytansine and to enhance tumor-specific delivery. Mertansine can be attached to a monoclonal antibody with a linker to create an antibody-drug conjugate (ADC).
  • HY-107096B
    CH-0793076 TFA

    TP3076 TFA

    Topoisomerase Cancer
    CH-0793076 (TP3076) TFA, a hexacyclic camptothecin analog, is active drug and major metabolite of TP300. CH-0793076 TFA inhibits DNA topoisomerase I with an IC50 of 2.3 μM. CH-0793076 TFA is efficacious against cells expressing BCRP (breast cancer resistance protein).
  • HY-N4114
    Picrocrocin

    Apoptosis Cancer
    Picrocrocin, an apocarotenoid found in Saffron. Picrocrocin shows anticancer effect. Picrocrocin exhibits growth inhibitory effects against SKMEL-2 human malignant melanoma cells.
  • HY-144661
    KRAS G12D inhibitor 14

    Ras Apoptosis Cancer
    KRAS G12D inhibitor 14 is a potent KRAS G12D inhibitor with a KD of 33 nM for binding to KRAS G12D protein. KRAS G12D inhibitor 14 decreases the active form of KRAS G12D (KRAS G12D-GTP) but not KRAS G13D.
  • HY-150695
    hCAIX/XII-IN-5

    Carbonic Anhydrase Apoptosis Cancer
    hCAIX/XII-IN-5 (Coumarin 9a) a carbonic anhydrase (CA) inhibitor, and exhibits excellent hCA IX/XII selectivity (Ki=93.9 and 85.7 nM, respectively) over hCA I and hCA II. hCAIX/XII-IN-5 shows anti-proliferative activities to cancer cells. hCAIX/XII-IN-5 can delay cell cycle and induce apoptosis.
  • HY-13065
    Isobavachalcone

    Corylifolinin; Isobacachalcone

    Akt Reactive Oxygen Species Apoptosis Autophagy Cancer
    Isobavachalcone (Corylifolinin) is derived from Psoralea corylifolia Linn. and is a potent inhibitor of Akt signaling pathway, which induces apoptosis in human cancer cells (Inhibits OVCAR-8 cell growth with an IC50 value of 7.92 μM). Isobavachalcone also induces Reactive Oxyen Species (ROS) generation in OVCAR-8 cells and has exhibit cancer anti-promotive and anti-proliferative activity.
  • HY-N0181AS
    Lumisterol-d3

    9β,10α-Ergosterol-d3

    Endogenous Metabolite Metabolic Disease
    Lumisterol-d3 (9β,10α-Ergosterol-d3) is the deuterium labeled Lumisterol. Lumisterol (9β,10α-Ergosterol), a steroid compound, is the (9β,10α)-stereoisomer of Ergosterol. Lumisterol is a photoprotective agent against UVB-induced DNA damage and anti-proliferative activities.
  • HY-147731
    HDAC6-IN-9

    HDAC Cancer
    HDAC6-IN-9 (compound 12c) is a potent and selective HDAC6 inhibitor with IC50 values of 11.8, 15.2, 4.2, 139.6, 21.3 nM for HDAC1,HDAC3, HDAC6, HDAC8, HDAC10, respectively. HDAC6-IN-9 shows anti-proliferative activities.
  • HY-121333
    Dinactin

    Antibiotic Wnt β-catenin Cancer Neurological Disease Infection
    Dinactin, an antibiotic ionophore produced by Streptomyces species, as an effective small molecule targeting Wnt/β-catenin signaling pathway in cancer cells. Dinactin shows marked inhibition of HCT-116 cell growth with an IC50 of 1.1 µM. Dinactin shows anti-proliferative activity against the cancer cells in apoptosis-independent manner. Dinactin is also an effective agent for the research of neuropathic pain.
  • HY-115924
    CDK1-IN-1

    CDK Cancer
    CDK1-IN-7 is a potent CDK1 inhibitor (CDK1/CycB IC50=161.2 nM) with potential antiproliferative activity and selectivity for cancer tissues. CDK1-IN-7 induces apoptosis in p53 dependent manner through the intrinsic apoptotic pathway. CDK1-IN-7 is a potential targeted antitumor agent.
  • HY-146061
    KRAS G12C inhibitor 48

    Ras Cancer
    KRAS G12C inhibitor 48 (compound 6e) is a potent KRAS G12C inhibitor with an IC50 of 639.91 nM. KRAS G12C inhibitor 48 (0-50 µM) shows anti-proliferative activity with IC50s of 0.796, 6.33, 16.14 µM for H358, H23, A549 cells, respectively.
  • HY-146287
    Zn(BQTC)

    DNA/RNA Synthesis Apoptosis Cancer
    Zn(BQTC) is a highly potent mitochondrial DNA (mtDNA) and nuclear DNA (nDNA) inhibitor. Zn(BQTC) causes severe damage to the mtDNA and nDNA, sequentially disruptes mitochondrial and nuclear functions. Zn(BQTC) promotes the DNA damage-induced apoptotic signaling pathway. Zn(BQTC) has selectively antiproliferative activity against A549R cells. Zn(BQTC) can be used for researching anticancer.
  • HY-150654
    WDR5-IN-5

    Histone Methyltransferase Cancer
    WDR5-IN-5 is an orally active and selective inhibitor of WIN site of WD repeat domain 5 (WDR5). WDR5-IN-5 exhibits anti-proliferative activity towards cancer cells and good pharmacokinetics profile in mice. WDR5-IN-5 shows high affinity to WDR5 and the binding affinity Ki value <0.02 nM.
  • HY-N0181AS1
    Lumisterol-d5

    9β,10α-Ergosterol-d5

    Endogenous Metabolite Metabolic Disease
    Lumisterol-d5 (9β,10α-Ergosterol-d5) is the deuterium labeled Lumisterol. Lumisterol (9β,10α-Ergosterol), a steroid compound, is the (9β,10α)-stereoisomer of Ergosterol. Lumisterol is a photoprotective agent against UVB-induced DNA damage and anti-proliferative activities.
  • HY-147575
    Axl-IN-8

    TAM Receptor c-Met/HGFR Cancer
    Axl-IN-8 (NO.1) is a potent AXL inhibitor, with an IC50 of <1 nM. Axl-IN-8 also inhibits c-MET, with an IC50 of 1-10 nM. Axl-IN-8 shows anti-proliferative activity against BaF3/TEL-AXL, MKN45, and EBC-1 cells, with IC50 values of <10, 226.6 and 120.3 nM, respectively.
  • HY-50767D
    Palbociclib orotate

    PD 0332991 orotate

    CDK Cancer
    Palbociclib (PD 0332991) orotate is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib orotate has potent anti-proliferative activity and induces cell cycle arrest in cancer cells. Palbociclib orotate can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma.
  • HY-150765
    PARP1-IN-12

    PARP Apoptosis Cancer
    PARP1-IN-12 is a potent PARP1 inhibitor with an IC50 of 2.99 nM. PARP1-IN-12 exhibits antiproliferative activity, can induce cell apoptosis and cause cycle arrest at G2/M phase. PARP1-IN-12 also can induce DNA double strand breaks (DSBs) in BRCA-deficient cells.
  • HY-131031
    KCC-07

    DNA Alkylator/Crosslinker Cancer
    KCC-07 is a potent, selective and brain-penetrant MBD2 (methyl-CpG-binding domain protein 2) inhibitor. KCC-07 prevents binding of MBD2 to methylated DNA and activates brain specific angiogenesis inhibitor 1 (BAI1) inducing anti-proliferative BAI1/p53/p21 signaling. Anticancer activity.
  • HY-100900
    ML364

    Deubiquitinase Cancer
    ML364 is a selective ubiquitin specific peptidase 2 (USP2) inhibitor (IC50=1.1 μM) with anti-proliferative activity, which direct binds to USP2 (Kd=5.2 μM), induces an increase in cellular cyclin D1 degradation and causes cell cycle arrest. ML364 increases the levels of mitochondrial ROS and decreases in the intracellular content of ATP.
  • HY-151110
    PROTAC CDK12/13 Degrader-1

    CDK Cancer
    PROTAC CDK12/13 Degrader-1 (7f) is a highly selective cell cycle protein-dependent kinase CDK12/CDK13 dual degrader with the DC50 values of 2.2 nM and 2.1 nM, respectively. PROTAC CDK12/13 Degrader-1 has anti-proliferative activity and can be used in breast cancer research.
  • HY-B0965A
    Thioridazine

    Dopamine Receptor Apoptosis 5-HT Receptor Autophagy Bacterial Neurological Disease
    Thioridazine, an antagonist of the dopamine receptor D2 family proteins, exhibits potent anti-psychotic and anti-anxiety activities. Thioridazine is also a potent inhibitor of PI3K-Akt-mTOR signaling pathways with anti-angiogenic effect. Thioridazine shows antiproliferative and apoptosis induction effects in various types of cancer cells, with specificity on targeting cancer stem cells (CSCs).
  • HY-146283
    LSD1-IN-18

    Histone Demethylase Cancer
    LSD1-IN-18 (compound 7) is a potent, non-covalent and selective LSD1 inhibitor, with Ki of 0.156 μM and KD of 0.075 μM, respectively. LSD1-IN-18 shows antiproliferative activity in THP-1 leukemia cells and MDA-MB-231 breast cancer cells, with IC50 (72 h) of 0.16 and 0.21 μM, respectively.
  • HY-N6064
    Polygalacin D

    Apoptosis IAP Cancer
    Polygalacin D (PGD) is a bioactive compound isolated from Platycodon grandiflorum with anticancer and anti-proliferative properties. PGD suppresses the expression of the IAP family of proteins including survivin, cIAP-1 and cIAP-2 and blocks the PI3K/Akt pathway by inhibiting the phosphorylation of GSK3β, Akt and the expression of PI3K. Polygalacin D induces apoptosis
  • HY-147949
    SKLB0565

    Microtubule/Tubulin Apoptosis Cancer
    SKLB0565 is a potent tubulin inhibitor. SKLB0565 shows significant anti-proliferative activity against CRC (colorectal carcinoma) cell lines, with IC50 values ranging from 0.012 μM to 0.081 μM. SKLB0565 causes G2/M phase arrest and mitochondria-mediated intrinsic apoptosis. SKLB0565 inhibits cell migration and disrupted the tube formation of HUVECs.
  • HY-N2453
    Convallatoxin

    PPAR NF-κB P-glycoprotein Cancer Inflammation/Immunology
    Convallatoxin is a cardiac glycoside isolated from Adonis amurensis Regel et Radde. Convallatoxin ameliorates colitic inflammation via activation of PPARγ and suppression of NF-κB. Convallatoxin is a P-glycoprotein (P-gp) substrate and recognized Val982 as an important amino acid involved in its transport. Convallatoxin is an enhancer of ligand-induced MOR endocytosis with high potency and efficacy. Anti-inflammatory and anti-proliferative properties.
  • HY-146284
    LSD1-IN-19

    Histone Demethylase Cancer
    LSD1-IN-19 (compound 29) is a potent, non-covalent and selective LSD1 inhibitor, with Ki of 0.108 μM and KD of 0.068 μM, respectively. LSD1-IN-19 shows antiproliferative activity in THP-1 leukemia cells and MDA-MB-231 breast cancer cells, with IC50 (72 h) of 0.17 and 0.40 μM, respectively.
  • HY-111552
    PIM1-IN-1

    Pim Cancer
    PIM1-IN-1 is a potent and highly selective PIM1/3 inhibitor, with IC50s of 7, 5530 and 70 nM for PIM1, PIM2, and PIM3, respectively, inhibits the phosphorylation of BAD, a downstream target of PIM, with an EC50 of 262 nM. PIM1-IN-1 shows no obvious effect on FLT3 or hERG binding. Antiproliferative and anti-cancer activity.
  • HY-151606
    Akt3 degrader 1

    Akt Cancer
    Akt3 degrader 1 (compound 12l) is a selective Akt3 degrader that overcomes Osimertinib (HY-15772)-induced resistance in H1975OR NSCLC cells. Akt3 degrader 1 also has anti-proliferative activity and significantly inhibits tumour growth in mice. Akt3 degrader 1 can be used in the study of drug-resistant non-small cell lung cancer.
  • HY-15221
    Methylstat

    Apoptosis Histone Demethylase MDM-2/p53 Cancer Cardiovascular Disease
    Methylstat is a potent histone demethylases inhibitor. Methylstat shows anti-proliferative activity with low cytotoxicity. Methylstat induces apoptosis and cell cycle arrest at G0/G1 phase. Methylstat increases the expression of p53 and p21 protein levels. Methylstat inhibits angiogenesis induced by various cytokines. Methylstat can be used as a chemical probe for addressing its role in angiogenesis.
  • HY-118858
    UCPH-102

    Others Cancer Neurological Disease
    UCPH-102 is a highly selective EAAT1 inhibitor with an IC50 of 0.43 µM. UCPH-102 exhibits a specific anti-proliferative effect on T-ALL cells. UCPH-102 also shows good blood-brain permeability, which can be used in studies of amyotrophic lateral sclerosis, Alzheimer’s disease, chronic pain and obsessive compulsive disorder.
  • HY-144709
    FLT3/ITD-IN-1

    FLT3 Cancer
    FLT3/ITD-IN-1 (Compound 1) is a potent FLT3 internal tandem duplications (FLT3-ITD) inhibitor with IC50 values of 38.2 nM and 144.1 nM against FLT3 and FLT3-ITD, respectively. FLT3/ITD-IN-1 displays excellent antiproliferative activities against acute myeloid leukemia cell lines.
  • HY-113505
    Delta-12-Prostaglandin J2

    Δ12-PGJ2

    Endogenous Metabolite Apoptosis Cancer
    Delta-12-Prostaglandin J2 (Δ12-PGJ2) is a cyclopentenone prostaglandin (PG) with anti-proliferative effect on various tumor cell growth. Delta-12-Prostaglandin J2, a naturally occurring dehydration product of prostaglandin D2, is able to induce apoptosis in HeLa cells via caspase activation.
  • HY-B0965
    Thioridazine hydrochloride

    Dopamine Receptor Apoptosis 5-HT Receptor Autophagy Bacterial Cancer Infection Neurological Disease
    Thioridazine hydrochloride, an orally active antagonist of the dopamine receptor D2 family proteins, exhibits potent anti-psychotic and anti-anxiety activities. Thioridazine hydrochloride is also a potent inhibitor of PI3K-Akt-mTOR signaling pathways with anti-angiogenic effect. Thioridazine hydrochloride shows antiproliferative and apoptosis induction effects in various types of cancer cells, with specificity on targeting cancer stem cells (CSCs).
  • HY-N2787
    8-​Prenylnaringenin

    Apoptosis Cancer
    8-prenylnaringenin is a prenylflavonoid isolated from hop cones Humulus lupulus, with cytotoxicity. 8-prenylnaringenin has anti-proliferative activity against HCT-116 colon cancer cells via induction of intrinsic and extrinsic pathway-mediated apoptosis. 8-Prenylnaringenin also promotes recovery from immobilization-induced disuse muscle atrophy through activation of the Akt phosphorylation pathway in mice .
  • HY-144691
    PP-C8

    PROTACs CDK Cancer
    PP-C8 is a potent and selective PROTAC CDK12-Cyclin K degrader. PP-C8 induces CDK12-Cyclin K degradation with DC50s of 416 and 412 nM for CDK12 and Cyclin K, respectively. PP-C8 demonstrates profound synergistic antiproliferative effects with PARP inhibitor in triple-negative breast cancer (TNBC).
  • HY-143400
    HSP70-IN-3

    HSP Hedgehog Cancer
    HSP70-IN-3 is a potent HSP70 inhibitor (IC50s of 1.1 and 1.9 μM in ASZ001 and C3H10T1/2, respectively). HSP70-IN-3 has anti-Hh (Hedgehog signaling) activity and anti-proliferative activity and reduces expression of the oncogenic transcription factor GLI1.
  • HY-112083
    BAY-3827

    AMPK Cancer
    BAY-3827 is a potent and selective AMPK inhibitor with IC50 values of 1.4 nM at low (10 µM ATP concentration) and 15 nM at high (2 mM ATP concentration). BAY-3827 shows over 500-fold selectivity for most of the 331 kinases. BAY-3827 prevents phosphorylation of acetyl-CoA carboxylase 1 and shows strongest anti-proliferative activity in androgen-dependent prostate cancer cell lines.
  • HY-145655
    CDK7-IN-11

    CDK Cancer
    CDK7-IN-11 is an orally active CDK7 inhibitor. CDK7-IN-11 exhibits high CDK7 inhibitory activity with IC50 value of 4.2 nM. CDK7-IN-11 can be effectively used for the research of diseases associated with CDK7.
  • HY-N7523
    Neoxanthin

    DNA/RNA Synthesis Apoptosis Cancer
    Neoxanthin is a major xanthophyll carotenoid and a precursor of the plant hormone abscisic acid in dark green leafy vegetables. Neoxanthin is a potent antioxidant and light-harvesting pigment. Neoxanthin induces apoptosis and has anticancer actions.
  • HY-W077242
    1,4-Anthraquinone

    DNA/RNA Synthesis Cancer
    1,4-Anthraquinone is a potent anticancer agent. 1,4-Anthraquinone blocks nucleoside transport, inhibits macromolecule synthesis, induces DNA fragmentation, and decreases the growth and viability of cancer cells. 1,4-Anthraquinone can be used to research anti-leukemia.
  • HY-15482
    D-64131

    Microtubule/Tubulin Cancer
    D-64131 is an orally active tubulin inhibitor, with an IC50 of 0.53 μM for tubulin polymerization. D-64131 has antimitotic activity. D-64131 can be used for cancer research.
  • HY-148088
    M1069

    Adenosine Receptor Cancer
    M1069 is a selective and orall active, dual A2A/A2B adenosine receptor antagonist with a selectivity of >100 fold against the A1 and A3 receptors. M1069 counteracts immune-suppressive mechanisms of adenosine, and exhibits anti-tumor activity.
  • HY-108511A
    PB28

    Sigma Receptor Apoptosis SARS-CoV Cancer Infection
    PB28 is a cyclohexylpiperazine derivative and a high affinity and selective sigma 2 (σ2) receptor agonist with a Ki of 0.68 nM. PB28 is also a σ1 antagonist with a Ki of 0.38 nM. PB28 is less affinity for other receptors. PB28 inhibits electrically evoked twitch in guinea pig bladder and ileum with EC50 values of 2.62 μM and 3.96 μM, respectively. PB28 can modulate SARS-CoV-2-human protein-protein interaction. PB28 induces caspase-independent apoptosis and has antitumor activity.
  • HY-108511
    PB28 dihydrochloride

    Sigma Receptor Apoptosis SARS-CoV Cancer Infection
    PB28 dihydrochloride, a cyclohexylpiperazine derivative, is a high affinity and selective sigma 2 (σ2) receptor agonist with a Ki of 0.68 nM. PB28 dihydrochloride is also a σ1 antagonist with a Ki of 0.38 nM. PB28 dihydrochloride is less affinity for other receptors. PB28 dihydrochloride inhibits electrically evoked twitch in guinea pig bladder and ileum with EC50 values of 2.62 μM and 3.96 μM, respectively. PB28 dihydrochloride can modulate SARS-CoV-2-human protein-protein interaction. PB28 dihydrochloride induces caspase-independent apoptosis and has antitumor activity.
  • HY-115999
    Carbonic anhydrase inhibitor 12

    Carbonic Anhydrase Cancer
    Carbonic anhydrase inhibitor 12 is a potent CA II inhibitor, also has inhibitory activity in CA I (Kis of 1.72 and 271 nM in CA II and CA I, respectively). Carbonic anhydrase inhibitor 12 has potent anticancer activity against different cancer cell lines.
  • HY-150597
    HDAC-IN-46

    HDAC Apoptosis Cancer
    HDAC-IN-46 (compound 12c) is a potent HDAC inhibitor with an IC50 value of 0.21 μM and 0.021 μM for HDAC1 and HDAC6, respectively. HDAC-IN-46 upregulates p-p38, and downregulates Bcl-xL and cyclin D1 in MDA-MB-231 cells. HDAC-IN-46 induces significant G2 phase arrest and apoptosis. HDAC-IN-46 can be used for researching triple-negative breast cancer (TNBC).
  • HY-146750
    HDAC-IN-37

    HDAC Apoptosis Cancer
    HDAC-IN-37 is a potent HDAC inhibitor with IC50s of 0.0551 μM, 1.24 μM, 0.948 μM and 34.2 μM for HDAC1, HDAC3, HDAC8 and HDAC6, respectively. HDAC-IN-37 induces histone acetylation in a slow-off manner. HDAC-IN-37 prevents cell transition from G1 phase to S phase and induces early cell apoptosis.
  • HY-144299
    Tubulin polymerization-IN-5

    Microtubule/Tubulin Apoptosis Cancer
    Tubulin polymerization-IN-5 (compound 20q) is a potent tubulin inhibitor with potential anticancer activities. Tubulin polymerization-IN-5 can arrest ESCC cells at G2/M phase and cause cells apoptosis.
  • HY-136657
    SC-43

    Phosphatase STAT Apoptosis Cancer
    SC-43, a Sorafenib derivative, is a potent and orally active SHP-1 (PTPN6) agonist. SC-43 inhibits the phosphorylation of STAT3 and induces cell apoptosis. SC-43 has anti-fibrotic and anticancer effects.
  • HY-146277
    CBP/p300-IN-19

    Histone Acetyltransferase Cancer
    CBP/p300-IN-19 is a potent p300/CBP HAT inhibitor with IC50s of 1.4, 2.2, >100, >100 µM for p300-HAT, CBP-HAT, PCAF, Myst3, respectively. CBP/p300-IN-19 shows antitumor activity.
  • HY-146277A
    CBP/p300-IN-19 hydrochloride

    Histone Acetyltransferase Cancer
    CBP/p300-IN-19 hydrochloride is a potent and selective p300/CBP HAT inhibitor with IC50s of 1.4, 2.2, >100, >100 µM for p300-HAT, CBP-HAT, PCAF, Myst3, respectively. CBP/p300-IN-19 hydrochloride shows antitumor activity.
  • HY-B0391S1
    Naftopidil-d5

    KT-611-d5; BM-15275-d5

    Adrenergic Receptor Cardiovascular Disease Endocrinology
    Naftopidil-d5 is deuterium labeled Naftopidil. Naftopidil (KT-611) is is a selective alpha1-adrenoceptor antagonist, with Kis of 3.7 nM, 20 nM and 1.2 nM for the cloned human α1a-, α1b- and α1d-adrenoceptor subtypes, respectively. Naftopidil has antiproliferative effects. Naftopidil can be used for the research of prostate hyperplasia.
  • HY-147831
    EIF2α activator 1

    Eukaryotic Initiation Factor (eIF) Cancer
    EIF2α activator 1 (Compound 40) is an activator of eukaryotic initiation factor 2 alpha (eIF2α) phosphorylation. EIF2α activator 1 increases the expression level of eIF2α downstream proteins, ATF and CHOP. EIF2α activator 1 exhibits antiproliferative activity againist K562 and PBMC cells with IC50s of 4.00 and 19.3 μM, respectively.
  • HY-18684
    SIBA

    5'-Isobutylthioadenosine; 5'-Deoxy-5'-isobutylthioadenosine

    Nucleoside Antimetabolite/Analog HSV Parasite Cancer Infection Metabolic Disease
    SIBA (5'-Isobutylthioadenosine) is a transmethylation inhibitor (SAH (HY-19528) analogue), with potent anti-proliferative activity. SIBA reversibly inhibits the production of HSV-1 by blocking methylation, specifically by blocking the 5' end-capping of viral mRNA. SIBA also inhibits the growth of tumour cells in vitro and metastatic spread in vivo. SIBA can be used in cancer, HSV-1 infection and anti-malaria studies.
  • HY-112724
    Ivarmacitinib

    SHR0302

    JAK Apoptosis Cancer Inflammation/Immunology
    Ivarmacitinib (SHR0302) is a potent and orally active all members of the JAK family inhibitor, particularly JAK1. The selectivity of Ivarmacitinib for JAK1 is >10-fold for JAK2, 77-fold for JAK3, 420-fold for Tyk2. Ivarmacitinib inhibits JAK1-STAT3 phosphorylation and induces the apoptosis of hepatic stellate cells. Ivarmacitinib has anti-proliferative and anti-inflammatory effects.
  • HY-13846
    BM-1074

    Bcl-2 Family Apoptosis Cancer
    BM-1074 is a potent and specific Bcl-2/Bcl-xL inhibitor with Ki values of < 1 nM and IC50 values of 1.8 nM and 6.9 nM for Bcl-2 and Bcl-xL, respectively. BM-1074 induces apoptosis, and exhibits antiproliferative activity against four small-cell lung cancer cell lines (H146, H1963, H187 and H1417) with IC50 values of 1-2 nM.
  • HY-10209A
    Masitinib mesylate

    AB-1010 mesylate

    c-Kit PDGFR Src FGFR Apoptosis Cancer
    Masitinib mesylate (AB-1010 mesylate) is a potent, orally bioavailable, and selective inhibitor of c-Kit (IC50=200 nM for human recombinant c-Kit). It also inhibits PDGFRα/β (IC50s=540/800 nM), Lyn (IC50= 510 nM for LynB), Lck, and, to a lesser extent, FGFR3 and FAK. Masitinib mesylate (AB-1010 mesylate) has anti-proliferative, pro-apoptotic activity and low toxicity.
  • HY-120599
    Sabizabulin

    VERU-111; ABI-231

    Microtubule/Tubulin Apoptosis HPV Cancer
    VERU-111 (ABI-231) is a potent and orally active α and β tubulin inhibitor, which displays strong antiproliferative activity, with an average IC50 of 5.2 nM against panels of melanoma and prostate cancer cell lines. VERU-111 (ABI-231) suppresses tumor growth and metastatic phenotypes of cervical cancer cells via targeting HPV E6 and E7, and has potential for the treatment of prostate cancer.
  • HY-B0413
    Fenbendazole

    Parasite HIF/HIF Prolyl-Hydroxylase Microtubule/Tubulin Antibiotic Infection
    Fenbendazole is an orally active benzimidazole anthelmintic agent, with a broad antiparasitic range. Fenbendazole is a microtubule destabilizing agent and acts on helminthes primarily by binding to tubulin and disrupting the tubulin microtubule equilibrium. Fenbendazole stabilizes the transcriptional activator HIF-1α. Fenbendazole possesses an efficient anti-proliferative activity and induces apoptosis. Fenbendazole causes cell-cycle arrest and mitotic cell death, and has antitumor activity in mice xenografted with wild-type p53.
  • HY-147832
    EIF2α activator 2

    Eukaryotic Initiation Factor (eIF) Cancer
    EIF2α activator 2 (Compound 1) is an activator of eukaryotic initiation factor 2 alpha (eIF2α) phosphorylation. EIF2α activator 2 exhibits high potency in SRB cell proliferation assays (IC50=0.46 μM). EIF2α activator 2 exhibits antiproliferative activity againist K562 and PBMC cells with IC50s of 4.79 and 10.52 μM, respectively.
  • HY-B1452S
    Licofelone-d4

    COX Lipoxygenase Apoptosis Cancer Inflammation/Immunology
    Licofelone-d4 (ML-3000-d4) is the deuterium labeled Licofelone. Licofelone (ML-3000) is a dual COX/5-lipoxygenase (5-LOX) inhibitor (IC50=0.21/0.18 μM, respectively) for the treatment of osteoarthritis. Licofelone exerts anti-inflammatory and anti-proliferative effects. Licofelone induces apoptosis, and decreases the production of proinflammatory leukotrienes and prostaglandins.
  • HY-146792
    PLK1-IN-4

    Polo-like Kinase (PLK) Cancer
    PLK1-IN-4 is a potent and selective PLK1 inhibitor with IC50 < 0.508 nM. PLK1-IN-4 has broad antiproliferative activity against a variety of cancer cell lines. PLK1-IN-4 induces mitotic arrest at the G2/M phase checkpoint, leading to cancer cell apoptosis. PLK1-IN-4 can be used for researching hepatocellular carcinoma.
  • HY-146285
    LSD1-IN-20

    Histone Demethylase Histone Methyltransferase Cancer
    LSD1-IN-20 (compound 1) is a potent dual non-covalent LSD1/G9a inhibitor, with Ki values of 0.44 and 0.68 μM, respectively. LSD1-IN-20 shows antiproliferative activity in THP-1 leukemia cells and MDA-MB-231 breast cancer cells, with IC50 (72 h) of 0.51 and 1.60 μM, respectively.
  • HY-115463
    EB-3D

    AMPK Apoptosis Cancer
    EB-3D is a potent and selective choline kinase α (ChoKα) inhibitor, with an IC50 of 1 μM for ChoKα1. EB-3D exerts effects on ChoKα expression, AMPK activation, apoptosis, endoplasmic reticulum stress and lipid metabolism. EB-3D exhibits a potent antiproliferative activity in a panel of T-leukemia cell lines. Anti-cancer activity.
  • HY-10209
    Masitinib

    AB1010

    c-Kit PDGFR Src FGFR FAK Apoptosis Cancer
    Masitinib (AB1010) is a potent, orally bioavailable, and selective inhibitor of c-Kit (IC50=200 nM for human recombinant c-Kit). It also inhibits PDGFRα/β (IC50s=540/800 nM), Lyn (IC50= 510 nM for LynB), Lck, and, to a lesser extent, FGFR3 and FAK. Masitinib (AB1010) has anti-proliferative, pro-apoptotic activity and low toxicity.
  • HY-W011266
    JNJ-10198409

    PDGFR Cancer
    JNJ-10198409 is a relatively selective, orally active, and ATP competitive PDGF-RTK (platelet-derived growth factor receptor tyrosine kinase) inhibitor (IC50=2 nM). It is a dual-mechanism, antiangiogenic, and tumor cell antiproliferative agent. JNJ-10198409 has good activity against PDGFR-β kinase (IC50=4.2 nM) and PDGFR-α kinase (IC50=45 nM).
  • HY-N0005
    Curcumin

    Diferuloylmethane; Natural Yellow 3; Turmeric yellow

    Histone Acetyltransferase Epigenetic Reader Domain Keap1-Nrf2 Autophagy Mitophagy Influenza Virus Ferroptosis Cancer
    Curcumin (Diferuloylmethane), a natural phenolic compound, is a p300/CREB-binding protein-specific inhibitor of acetyltransferase, represses the acetylation of histone/nonhistone proteins and histone acetyltransferase-dependent chromatin transcription. Curcumin shows inhibitory effects on NF-κB and MAPKs, and has diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin induces stabilization of Nrf2 protein through Keap1 cysteine modification.
  • HY-122214
    AC-73

    Autophagy Cancer
    AC-73 is a first specific, orally active inhibitor of cluster of differentiation 147 (CD147), which specifically disrupts CD147 dimerization, thereby mainly suppressing the CD147/ERK1/2/STAT3/MMP-2 pathways. AC-73 inhibits the motility and invasion of hepatocellular carcinoma cells. AC-73 is also an anti-proliferative drug and an inducer of autophagy in leukemic cells.
  • HY-N2983
    Cajanin

    Others Others
    Cajanin is a potent and orally active anti-melanogenic agent. Cajanin shows antiproliferative activity in MNT1 Cells. Cajanin efficiently decreases the melanin content. Cajanin down-regulates the mRNA and protein expression levels of MITF, tyrosinase, TRP-1 and Dct (TRP-2). Cajanin induces cell cycle arrest at G2/M and S phase. Cajanin stimulates osteoblast proliferation. Cajanin has the potential for the research of human hyperpigmented disorders and menopausal osteoporosis.
  • HY-124653
    HSP27 inhibitor J2

    J2

    HSP Cancer
    HSP27 inhibitor J2 (J2) is a HSP27 inhibitor, which significantly induces abnormal HSP27 dimer formation and inhibits a production of HSP27 giant polymers, thereby having an effect of inhibiting a chaperone function of the HSP27 and reducing a cell protection function thereof. HSP27 inhibitor J2 (J2) remarkably enhances the antiproliferative activity of 17-AAG and sensitizes cisplatin-induced lung cancer cell growth inhibition.
  • HY-B0988
    Deferoxamine mesylate

    Desferrioxamine B mesylate; DFOM

    Autophagy HIF/HIF Prolyl-Hydroxylase Reactive Oxygen Species Apoptosis Akt Cancer Infection Metabolic Disease Inflammation/Immunology Neurological Disease
    Deferoxamine mesylate (Deferoxamine B mesylate) is an iron chelator (binds to Fe(III) and many other metal cations), is widely used to reduce iron accumulation and deposition in tissues. Deferoxamine mesylate upregulates HIF-1α levels with good antioxidant activity. Deferoxamine mesylate also shows anti-proliferative activity, can induce apoptosis and autophagy in cancer cells. Deferoxamine mesylate can be used in studies of diabetes, neurodegenerative diseases as well as anti-cancer and anti-COVID-19.
  • HY-B1625
    Deferoxamine

    Deferoxamine B; Deferriferrioxamine B; Deferrioxamine

    HIF/HIF Prolyl-Hydroxylase Reactive Oxygen Species Apoptosis Akt Autophagy Cancer Infection Metabolic Disease Inflammation/Immunology Neurological Disease
    Deferoxamine (Deferoxamine B) is an iron chelator (binds to Fe(III) and many other metal cations), is widely used to reduce iron accumulation and deposition in tissues. Deferoxamine upregulates HIF-1α levels with good antioxidant activity. Deferoxamine also shows anti-proliferative activity, can induce apoptosis and autophagy in cancer cells. Deferoxamine can be used in studies of diabetes, neurodegenerative diseases as well as anti-cancer and anti-COVID-19.
  • HY-146210
    EGFR-IN-50

    EGFR Cancer
    EGFR-IN-50 (Compound 9h) is a potent EGFR inhibitor against L858R resistance mutation (TEL-EGFR-L858R-BaF3: GI50=8 nM, TEL-EGFR-T790M-L858R-BaF3: GI50=6.03 μM). EGFR-IN-50 shows anti-proliferative activity to cancer cells.
  • HY-19617A
    EGFR-IN-1 hydrochloride

    EGFR Cancer
    EGFR-IN-1 hydrochloride is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 hydrochloride potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 hydrochloride displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity.
  • HY-133121
    WDR5-IN-1

    Histone Methyltransferase Apoptosis Cancer
    WDR5-IN-1 is a potent and selective WD repeat domain 5 (WDR5) inhibitor, with a Kd of <0.02 nM. WDR5-IN-1 inhibits MLL1 histone methyltransferase (HMT) activity with an IC50 of 2.2 nM. WDR5-IN-1 diminishes MYC recruitment at WDR5-displaced genes and exhibits potent anti-proliferative effects in CHP-134 (neuroblastoma) and Ramos (Burkitt’s lymphoma) lines.
  • HY-101144
    RSM-932A

    TCD-717

    Others Cancer
    RSM-932A (TCD-717) is a specific ChoKα inhibitor with IC50s of 1 and 33 μM for human recombinant ChoKα and ChoKβ enzymes, respectively. RSM-932A acts as the “first in humans” compound targeting ChoKα. RSM-932A is potent in vitro anti-proliferative and in vivo anti-tumoral activity against human xenografts in mice, showing high efficacy with low toxicity profiles.
  • HY-B0391S
    Naftopidil-d3

    KT-611-d3; BM-15275-d3

    Adrenergic Receptor Cardiovascular Disease Endocrinology
    Naftopidil-d3 (KT-611-d3) is the deuterium labeled Naftopidil. Naftopidil (KT-611) is is a selective alpha1-adrenoceptor antagonist, with Kis of 3.7 nM, 20 nM and 1.2 nM for the cloned human α1a-, α1b- and α1d-adrenoceptor subtypes, respectively. Naftopidil has antiproliferative effects. Naftopidil can be used for the research of prostate hyperplasia.
  • HY-B0965AS
    Thioridazine-d3 hydrochloride

    Dopamine Receptor Apoptosis 5-HT Receptor Autophagy Bacterial Neurological Disease
    Thioridazine-d3 hydrochloride is the deuterium labeled Thioridazine. Thioridazine, an antagonist of the dopamine receptor D2 family proteins, exhibits potent anti-psychotic and anti-anxiety activities. Thioridazine is also a potent inhibitor of PI3K-Akt-mTOR signaling pathways with anti-angiogenic effect. Thioridazine shows antiproliferative and apoptosis induction effects in various types of cancer cells, with specificity on targeting cancer stem cells (CSCs).
  • HY-145669
    DIF-3

    CDK GSK-3 Cancer
    DIF-3 reduces the expression levels of cyclin D1 and c-Myc by facilitating their degradation via activation of GSK-3β. DIF-3 inhibits Wnt/β-catenin signaling pathway-related proteins in DLD-1 cells. DIF-3 exerts a strong antiproliferative effect on the human cervical cancer cell line HeLa by inducing cyclin D1 degradation and inhibiting cyclin D1 mRNA expression.
  • HY-147860
    EGFR-IN-61

    EGFR Cancer
    EGFR-IN-61 (compound 22a) is a potent EGFR kinase inhibitor, with IC50 values of 42 nM (L858R/T790 M), 137 nM (L858R/T790 M/C797S), and 743 nM (WT), respectively. EGFR-IN-61 shows antiproliferative activity against A549 and H1975 cell lines, with IC50 values of 2.14 and 1.82 μM, respectively.
  • HY-144819
    Bcl-2-IN-8

    Apoptosis Bcl-2 Family Cancer
    Bcl-2-IN-8 is a potent anticancer agent. Bcl-2-IN-8 shows anti-proliferative activity against both drug-sensitive and drug-resistant cancer cells. Bcl-2-IN-8 induce apoptosis and cell cycle arrest at G1 phase. Bcl-2-IN-8 inhibits cell migration in a dose-dependent manner. Bcl-2-IN-8 has the potential for the research of triple negrative breast cancer.
  • HY-N7255
    Cycloartenol

    p38 MAPK Apoptosis Cancer
    Cycloartenol, a phytosterol compound, is one of the key precusor substances for biosynthesis of numerous sterol compounds. Cycloartenol inhibits the migration of glioma cells and suppresses the phosphorylation of the p38 MAP kinase. Cycloartenol has a variety of pharmacological activities such as anti-inflammatory, anti-tumor, antioxidant, antibiosis and anti-alzheimer's disease. Cycloartenol also plays an important role in the process of plant growth and development.
  • HY-126856
    HC-Toxin

    HDAC Apoptosis Cancer
    HC-Toxin, a cyclic tetrapeptide, is a potent HDAC inhibitor with an IC50 of 30 nM. HC-Toxin induces tumor cell apoptosis and has anticancer effects.
  • HY-117843
    Ppc-1

    Mitochondrial Metabolism Interleukin Related Bacterial Infection Metabolic Disease Inflammation/Immunology
    Ppc-1 is a mitochondrial uncoupler. Ppc-1 enhances mitochondrial oxygen consumption without adverse effects on ATP production. Ppc-1 is a cell-permeate interleukin-2 (IL-2) inhibitor. Ppc-1 inhibits the Gram-negative periodontopathogen Porphyromonas gingivalis. Ppc-1 has anti-obesity, antibacterial and anti-inflammatory activities.
  • HY-114489B
    Haemanthamine hydrochloride

    Apoptosis Influenza Virus Parasite Cancer Infection Neurological Disease
    Haemanthamine hydrochloride is a crinine-type alkaloid isolated from the Amaryllidaceae plants with potent anticancer activity. Haemanthamine hydrochloride targets ribosomal that inhibits protein biosynthesis during the elongation stage of translation. Haemanthamine hydrochloride has pro-apoptotic, antioxidant, antiviral, antimalarial and anticonvulsant activities.
  • HY-143900
    BTK-IN-7

    Btk Apoptosis Cancer Inflammation/Immunology
    BTK-IN-7 is a potent and selective inhibitor of BTK (IC50=4.0 nM). BTK-IN-7 has high selectivity in both enzymatic (ITK >250-fold, EGFR >2500-fold) and cellular levels(ITK >227-fold, EGFR 27-fold). BTK-IN-7 also has potent antitumor activity.
  • HY-114489A
    Haemanthamine

    Apoptosis Influenza Virus Parasite Cancer Infection Neurological Disease
    Haemanthamine is a crinine-type alkaloid isolated from the Amaryllidaceae plants with potent anticancer activity. Haemanthamine targets ribosomal that inhibits protein biosynthesis during the elongation stage of translation. Haemanthamine has pro-apoptotic, antioxidant, antiviral, antimalarial and anticonvulsant activities.
  • HY-149031
    DHODH-IN-22

    Dihydroorotate Dehydrogenase Cancer
    DHODH-IN-22 is a potent, selective and orally active dihydroorotate dehydrogenase (DHODH) inhibitor with an IC50 value of 0.3 nM. DHODH-IN-22 can be used for researching acute myelogenous leukemia (AML).
  • HY-147754
    JAK3/BTK-IN-6

    Btk JAK Inflammation/Immunology
    JAK3/BTK-IN-6 (compound 14h) is a potent BTK and JAK3 dual inhibitor, with IC50 values of 0.6 and 0.4 nM, respectively. JAK3/BTK-IN-6 shows good metabolic stability in human liver microsome. JAK3/BTK-IN-6 can be used for hematological and immune diseases research.
  • HY-117203A
    CDK12-IN-E9

    CDK Cancer
    CDK12-IN-E9 is a potent and selective covalent CDK12 inhibitor and a non-covalent CDK9 inhibitor, while avoiding ABC transporter-mediated efflux. CDK12-IN-E9 has weak binding ability to CDK7/CyclinH complex with an IC50> 1 μM.
  • HY-151443
    HDAC-IN-47

    HDAC Cancer
    HDAC-IN-47 is an orally active inhibitor of histone deacetylase (HDAC), with IC50s of 19.75 nM (HDAC1), 5.63 nM (HDAC2), 40.27 nM (HDAC3), 57.8 nM (HDAC2), 302.73 nM (HDAC8), respectively. HDAC-IN-47 inhibits autophagy and induces apoptosis via the Bax/Bcl-2 and caspase-3 pathways. HDAC-IN-47 arrests cell cycle at G2/M phase, and shows anti-tumor efficacy in vivo.
  • HY-B0965S
    Thioridazine-d3 2-Sulfone

    Dopamine Receptor Apoptosis 5-HT Receptor Autophagy Bacterial Cancer Infection Neurological Disease
    Thioridazine-d3 2-Sulfone is the deuterium labeled Thioridazine hydrochloride. Thioridazine hydrochloride, an orally active antagonist of the dopamine receptor D2 family proteins, exhibits potent anti-psychotic and anti-anxiety activities. Thioridazine hydrochloride is also a potent inhibitor of PI3K-Akt-mTOR signaling pathways with anti-angiogenic effect. Thioridazine hydrochloride shows antiproliferative and apoptosis induction effects in various types of cancer cells, with specificity on targeting cancer stem cells (CSCs).
  • HY-144711
    FLT3/ITD-IN-3

    FLT3 Cancer
    FLT3/ITD-IN-3 (Compound 19) is a potent FLT3 internal tandem duplications (FLT3-ITD) inhibitor with IC50 values of 0.3, 0.4 and 0.9 nM against FLT3 D835Y, FLT3 and FLT3-ITD, respectively. FLT3/ITD-IN-3 potently inhibits the phosphorylation of FLT3 and displays excellent antiproliferative activities against acute myeloid leukemia cell lines.
  • HY-113952
    Actinonin

    (-)-Actinonin

    Aminopeptidase Bacterial MMP Apoptosis Antibiotic Cancer Infection
    Actinonin ((-)-Actinonin) is a naturally occurring antibacterial agent produced by Actinomyces. Actinonin inhibits aminopeptidase M, aminopeptidase N and leucine aminopeptidase. Actinonin is a potent reversible peptide deformylase (PDF) inhibitor with a Ki of 0.28 nM. Actinonin also inhibits MMP-1, MMP-3, MMP-8, MMP-9, and hmeprin α with Ki values of 300 nM, 1,700 nM, 190 nM, 330 nM, and 20 nM, respectively. Actinonin is an apoptosis inducer. Actinonin has antiproliferative and antitumor activities.
  • HY-144710
    FLT3/ITD-IN-2

    FLT3 Cancer
    FLT3/ITD-IN-2 (Compound 17) is a potent FLT3 internal tandem duplications (FLT3-ITD) inhibitor with IC50 values of 0.3, 0.4 and 1.0 nM against FLT3 D835Y, FLT3 and FLT3-ITD, respectively. FLT3/ITD-IN-2 potently inhibits the phosphorylation of FLT3 and displays excellent antiproliferative activities against acute myeloid leukemia cell lines.
  • HY-A0143S
    Dihomo-γ-linolenic acid-d6

    all-cis-8,11,14-Eicosatrienoic acid-d6

    Endogenous Metabolite Cancer Inflammation/Immunology Cardiovascular Disease
    Dihomo-γ-linolenic acid-d6 (all-cis-8,11,14-Eicosatrienoic acid-d6) is the deuterium labeled Dihomo-γ-linolenic acid. Dihomo-γ-linolenic acid (all-cis-8,11,14-Eicosatrienoic acid) is a 20-carbon ω-6 fatty acid, with anti-inflammatory and anti-proliferative activities. Dihomo-γ-linolenic acid attenuates atherosclerosis in the apolipoprotein E deficient mouse model system.
  • HY-151477
    SARS-CoV-2-IN-32

    SARS-CoV Cancer Infection
    SARS-CoV-2-IN-32 (compound 3g) is a COVID-19 inhibitor. SARS-CoV-2-IN-32 shows anti-proliferative activity against cancer cells. SARS-CoV-2-IN-32 exhibits comparatively high binding affinity (-8.8 Kcal/mole) to COVID-19 main protease (M pro) (PDB ID: 6LU7). SARS-CoV-2-IN-32 can be used in studies of cancer and COVID-19.
  • HY-151359
    Hsp90-IN-16

    Apoptosis HSP Cancer
    Hsp90-IN-16 (compound 16s) is an HSP90 inhibitor with high selectivity and potency against HER2-positive cancer cells. Hsp90-IN-16 exhibits high anti-proliferative capacity against HCC1954 breast cancer cells with an IC50 of 6 μM. Hsp90-IN-16 induces apoptosis by inhibiting HSP90 "client" proteins, including a key oncogenic receptor, HER2/neu.
  • HY-113831
    CLK1/2-IN-3

    CDK SRPK Cancer
    LK1/2-IN-3 (compound 3) is a potent and selective CLK1 and CLK2 inhibitor with IC50 values of 1.1, 2.1, 130, 260, 260 nM for CLK1, CLK2, SRPK1, SRPK2, SRPK3, respectively. CLK1/2-IN-3 shows anti-proliferative activity. CLK1/2-IN-3 reduces the levels of endogenous phosphorylated SR proteins and increases the expression of S6K mRNAs.
  • HY-143317
    XY153

    Epigenetic Reader Domain Cancer
    XY153 (compound 8l) is a BD2-selective BET inhibitor and selectively binds to BRD4 BD2. XY153 binds to BRD4 BD2, BRD3 BD2 and BRD2 BD2 with IC50s of 0.79, 5.31 and 5.09 nM, respectively. XY153 shows potent antiproliferative activity against multiple tumor cell lines. XY153 can be used for the research of acute myeloid leukemia (AML) and cancer.
  • HY-19617B
    EGFR-IN-1 TFA

    EGFR Cancer
    EGFR-IN-1 TFA is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 TFA potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 TFA displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity.
  • HY-146494
    Androgen receptor antagonist 5

    Androgen Receptor Cancer
    Androgen receptor antagonist 5 (compound 42f) is a potent androgen receptor (AR) antagonist with an IC50 value of 6.17 μM. Androgen receptor antagonist 5 can effectively impair AR nuclear translocation, reducing the levels of nuclear AR, and disrupts AR-mediated gene regulation. Androgen receptor antagonist 5 has antiproliferative activity against LNCaP and exhibits antitumor activity in LNCaP xenograft tumor mice model. Androgen receptor antagonist 5 can be used for researching prostate cancer.
  • HY-19617
    EGFR-IN-1

    EGFR Cancer
    EGFR-IN-1 (compound 24) is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity.
  • HY-120275
    CYD-2-11

    Bcl-2 Family Apoptosis Cancer
    CYD-2-11 is a selective Bax agonist with a Ki value of 34.1 nM. CYD-2-11 induces cell apoptosis and shows antiproliferative activity to breast cancer MDA-MB-231 and MCF-7 cell lines with IC50 values of 3.22 and 3.81 μM, respectively. CYD-2-11 suppresses tumor growth in MDA-MB-231 tumor models. CYD-2-11 can be used for the research of breast and lung cancer.
  • HY-115904
    FLT3/CDK4-IN-1

    CDK FLT3 Cancer
    FLT3/CDK4-IN-1 is a potent, high selective and orally active FLT3/CDK4 dual inhibitor (IC50=11 and 7 nM for FLT3 and CDK4, respectively). FLT3/CDK4-IN-1 has antiproliferative activities against certain cancer cells. FLT3/CDK4-IN-1 has good antitumor effect in vivo.
  • HY-151478
    SARS-CoV-2-IN-33

    SARS-CoV Cancer Infection
    SARS-CoV-2-IN-33 (compound 3m) is a COVID-19 inhibitor. SARS-CoV-2-IN-33 shows anti-proliferative activity against cancer cells. SARS-CoV-2-IN-33 exhibits comparatively good binding affinity (-8.0 Kcal/mole) to COVID-19 main protease (M pro) (PDB ID: 6LU7). SARS-CoV-2-IN-33 can be used in studies of cancer and COVID-19.
  • HY-146440
    LSD1/ER-IN-1

    Histone Demethylase Estrogen Receptor/ERR Apoptosis Cancer
    LSD1/ER-IN-1 (compound 11g) is a potent ER and LSD1 inhibitor, with an IC50 of 1.55 μM (LSD1). LSD1/ER-IN-1 has high affinity selectivity for ERα protein, with α/β ratio of 7.11. LSD1/ER-IN-1 shows good antiproliferative activity against MCF-7 breast cancer cells, with an IC50 of 8.79 μM.
  • HY-16018A
    Ilorasertib hydrochloride

    ABT-348 hydrochloride

    Aurora Kinase PDGFR VEGFR Cancer
    Ilorasertib (ABT-348) hydrochloride is a potent, orally active and ATP-competitive aurora inhibitor with IC50s of116, 5, 1 nM for aurora A, aurora B, aurora C, respectively. Ilorasertib hydrochloride also is a potent VEGF, PDGF inhibitor. Ilorasertib hydrochloride has the potential for the research of acute myeloid leukemia (AML) and myelodysplastic syndrome (MDS).
  • HY-130612
    PROTAC BRD2/BRD4 degrader-1

    Epigenetic Reader Domain PROTACs Cancer
    PROTAC BRD2/BRD4 degrader-1 (compound 15) is a potent and selective BET protein BRD4 and BRD2 degrader, connected by ligands for Cereblon and BET. PROTAC BRD2/BRD4 degrader-1 rapidly induces reversible, long-lasting, and unexpectedly selective removal of BRD4 and BRD2 over BRD3. It effectively inhibits solid tumors with low cytotoxic effect. PROTAC BRD2/BRD4 degrader-1 is composed of the BET inhibitor, a linker, and the ligand thalidomide for cereblon (CRBN)/cullin 4A.
  • HY-112345
    PD-089828

    FGFR PDGFR EGFR Src Cancer
    PD-089828 is an ATP competitive inhibitor of FGFR-1, PDGFR-β and EGFR (IC50s=0.15, 1.76, and 5.47 µM, respectively) and a noncompetitive inhibitor of c-Src tyrosine kinase (IC50=0.18 µM). PD-089828 also inhibits MAPK with an IC50 of 7.1 µM. PD-089828 inhibits PDGF-, EGF- and bFGF-mediated tyrosine kinase receptor autophosphorylation in vitro. PD-089828 has a long-lasting cellular activity.
  • HY-13603
    Crolibulin

    EPC2407

    Microtubule/Tubulin Apoptosis Cancer
    Crolibulin (EPC2407) is a tubulin polymerization inhibitor, with potent apoptosis induction and cell growth inhibition. Crolibulin has anti-tumor activity. Crolibulin also has cardiovascular toxicity and neurotoxicity.
  • HY-112130
    AGI-24512

    Methionine Adenosyltransferase (MAT) Cancer
    AGI-24512 is a potent methionine adenosyltransferase 2α (MAT2A) inhibitor, with an IC50 of 8 nM. AGI-24512 triggers DNA damage response. AGI-24512 can block proliferation of MTAP-deleted cancer cells in vitro. AGI-24512 can be used for researching anticancer.
  • HY-12248A
    Telaglenastat hydrochloride

    CB-839 hydrochloride

    Glutaminase Autophagy Cancer
    Telaglenastat (CB-839) hydrochloride is a first-in-class, selective, reversible and orally active glutaminase 1 (GLS1) inhibitor. Telaglenastat hydrochloride selectively inhibits GLS1 splice variants KGA (kidney-type glutaminase) and GAC (glutaminase C) compared to GLS2. The IC50s are 23 nM and 28 nM for endogenous glutaminase in mouse kidney and brain, respectively. Telaglenastat hydrochloride inudces autophagy and has antitumor activity.
  • HY-12248
    Telaglenastat

    CB-839

    Glutaminase Autophagy Cancer
    Telaglenastat (CB-839) is a first-in-class, selective, reversible and orally active glutaminase 1 (GLS1) inhibitor. Telaglenastat selectively inhibits GLS1 splice variants KGA (kidney-type glutaminase) and GAC (glutaminase C) compared to GLS2. The IC50s are 23 nM and 28 nM for endogenous glutaminase in mouse kidney and brain, respectively. Telaglenastat inuduces autophagy and has antitumor activity.
  • HY-16018
    Ilorasertib

    ABT-348

    Aurora Kinase VEGFR PDGFR Cancer
    Ilorasertib (ABT-348) is a potent, orally active and ATP-competitive aurora inhibitor with IC50s of116, 5, 1 nM for aurora A, aurora B, aurora C, respectively. Ilorasertib also is a potent VEGF, PDGF inhibitor. Ilorasertib has the potential for the research of acute myeloid leukemia (AML) and myelodysplastic syndrome (MDS).
  • HY-N1930
    (-)-Hinesol

    Hinesol

    Apoptosis Cancer
    (-)-Hinesol (Hinesol) is a potent anticancer agent. (-)-Hinesol induces apoptosis and cell cycle arrest at G0/G1 phase. (-)-Hinesol downregulates MEK/ERK pathway and NF-κB pathway and mediates theexpression of cyclin D1, Bax and Bcl-2. (-)-Hinesol has the potential for the research of non–small cell lung cancer.
  • HY-146411
    microRNA-21-IN-1

    MicroRNA Apoptosis Cancer
    microRNA-21-IN-1 (compound 7A) is an efficient microRNA inhibitor. microRNA-21-IN-1 has antiproliferative activity against Hela and HCT-116 cells with IC50s of 5.5 μM and 2.8 μM respectively, as well as promotes apoptosis of Hela cells. microRNA-21-IN-1 upregulates the expression of microRNA-21 downstream functional targets (PTEN, EGR1 and SLIT2). microRNA-21-IN-1 can be used for researching anticancer.
  • HY-N1445
    Isoquercetin

    Quercetin 3-glucoside

    NF-κB NO Synthase Inflammation/Immunology Cancer
    Isoquercetin (Quercetin 3-glucoside) is a naturally occurring polyphenol that has antioxidant, anti-proliferative, and anti-inflammatory properties. Isoquercetin alleviates ethanol-induced hepatotoxicity, oxidative stress, and inflammatory responses via the Nrf2/ARE antioxidant signaling pathway. Isoquercetin regulates the expression of nitric oxide synthase 2 (NO2) via modulating the nuclear factor-κB (NF-κB) transcription regulation system. Isoquercetin has high bioavailability and low toxicity, is a promising candidate agent to prevent birth defects in diabetic pregnancies.
  • HY-150603
    STAT3-IN-13

    STAT Apoptosis Bcl-2 Family Cancer
    STAT3-IN-13 (compound 6f) is a potent STAT3 inhibitor. STAT3-IN-13 has anti-proliferative effects and binds to the STAT3 SH2 domain with a KD of 0.46 μM. STAT3-IN-13 inhibits the phosphorylation of STAT3 Y705 and downstream target gene expression. STAT3-IN-13 induces apoptosis in vitro and suppresses the growth and metastasis of tumor in vivo. STAT3-IN-13 can be used for cancer research.
  • HY-136123
    Tubulin inhibitor 8

    Microtubule/Tubulin Cancer
    Tubulin inhibitor 8 (Compound 33b) is a tubulin inhibitor and a potent inhibitor of multiple cancer cell lines. Tubulin inhibitor 8 inhibits tubulin polymerization with an IC50 of 0.73 μM. Tubulin inhibitor 8 inhibits K562 cell growth with an IC50 of 14 nM.
  • HY-136122
    Tubulin inhibitor 7

    Microtubule/Tubulin Cancer
    Tubulin inhibitor 7 (Compound 33c) is a tubulin inhibitor and a potent inhibitor of multiple cancer cell lines. Tubulin inhibitor 7 inhibits tubulin polymerization with an IC50 of 0.52 μM. Tubulin inhibitor 7 inhibits K562 cell growth with an IC50 of 11 nM.
  • HY-10181B
    Dasatinib monohydrate

    BMS-354825 monohydrate

    Bcr-Abl Src Autophagy Apoptosis Cancer
    Dasatinib (BMS-354825) monohydrate is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib monohydrate inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively. Dasatinib monohydrate also induces apoptosis and autophagy.
  • HY-151453
    Topoisomerase IIα-IN-4

    Topoisomerase Apoptosis Cancer
    Topoisomerase IIα-IN-4 (F2) is a non-intercalative ATP-competitive human DNA topoisomerase II inhibitor with an IC50 value of 3.8 and 10.1 μM for TopoIIα and TopoIIβ, respectively. Topoisomerase IIα-IN-4 shows potent potency in apoptosis induction and cell cycle arrest in HepG2 cells. Topoisomerase IIα-IN-4 exhibits strong antitumor activities against human cancer cell lines, it can be used for the research of cancer.
  • HY-32340
    Lexacalcitol

    KH1060

    VD/VDR Cancer Inflammation/Immunology
    Lexacalcitol (KH1060), a vitamin D analog, is a potent regulator of cell growth and immune responses. Lexacalcitol can be used for the research of graft rejection, psoriasis, cancer and auto-immune diseases.
  • HY-144315
    Snail/HDAC-IN-1

    HDAC Cancer
    Snail/HDAC-IN-1 is a potent Snail/HDAC dual target inhibitor. Snail/HDAC-IN-1 displays potent inhibitory activity against HDAC1 with an IC50 of 0.405 μM and potent inhibition against Snail with a Kd of 0.18 μM. Snail/HDAC-IN-1 increases histone H4 acetylation in HCT-116 cells and decreases the expression of Snail protein to induce cell apoptosis.
  • HY-150752
    BTK-IN-15

    Btk Pyroptosis Cancer
    BTK-IN-15 is a potent Bruton's tyrosine kinase (BTK) inhibitor with high oral absorption. BTK-IN-15 inhibits BTK with an IC50 value of 0.7 nM. BTK-IN-15 displays excellent kinase selectivity, antitumor activity, and induces apoptosis.
  • HY-10181A
    Dasatinib hydrochloride

    BMS-354825 hydrochloride

    Bcr-Abl Src Autophagy Apoptosis Cancer
    Dasatinib (BMS-354825) hydrochloride is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib hydrochloride inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively. Dasatinib hydrochloride also induces apoptosis and autophagy.
  • HY-147947
    Tubulin polymerization-IN-30

    Microtubule/Tubulin Cancer
    Tubulin polymerization-IN-30 (compound 6e) is a potent Tubulin polymerization inhibitor. Tubulin polymerization-IN-30 is a colchicine binding site inhibitor. Tubulin polymerization-IN-30 can disrupt intracellular microtubule organization, arrest cell cycle at the G2/M phase. Tubulin polymerization-IN-30 exhibits the high potency against the cancer cell lines including SGC-7901, A549 and HeLa, with IC50 values of 2.16, 2.21, and 0.403 μM.
  • HY-10181
    Dasatinib

    BMS-354825

    Bcr-Abl Src Autophagy Apoptosis Cancer
    Dasatinib (BMS-354825) is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively. Dasatinib also induces apoptosis and autophagy.
  • HY-136121
    Tubulin inhibitor 6

    Microtubule/Tubulin Cancer
    Tubulin inhibitor 6 (Compound 14b) is a tubulin inhibitor and a potent inhibitor of multiple cancer cell lines. Tubulin inhibitor 6 inhibits tubulin polymerization with an IC50 of 0.87 μM. Tubulin inhibitor 6 inhibits K562 cell growth with an IC50 of 840 nM.
  • HY-144693
    MEK/PI3K-IN-2

    MEK PI3K PERK Cancer
    MEK/PI3K-IN-2 (compound 6s) is a potent MEK/PI3K inhibitor, with IC50 values of 352 nM (MEK1), 107 nM (PI3Kα), and 137 nM (PI3Kδ), respectively. MEK/PI3K-IN-2 suppresses pAKT and pERK1/2 levels. MEK/PI3K-IN-2 shows anti-proliferative activity against tumor cell lines.
  • HY-119944
    JND3229

    EGFR Cancer
    JND3229 is a reversible EGFR C797S inhibitor with IC50 values of 5.8, 6.8 and 30.5 nM for EGFR L858R/T790M/C797S, EGFR WT and EGFR L858R/T790M, respectively. JND3229 has good anti-proliferative activity and can effectively inhibit tumour growth in vivo. JND3229 can be used in cancer research, especially in non-small cell carcinoma.
  • HY-144692
    MEK/PI3K-IN-1

    MEK PI3K PERK Cancer
    MEK/PI3K-IN-1 (compound 6r) is a potent MEK/PI3K inhibitor, with IC50 values of 124 nM (MEK1), 130 nM (PI3Kα), and 236 nM (PI3Kδ), respectively. MEK/PI3K-IN-1 suppresses pAKT and pERK1/2 levels. MEK/PI3K-IN-1 shows anti-proliferative activity against tumor cell lines.
  • HY-151436
    ZLMT-12

    CDK Cholinesterase (ChE) Apoptosis Cancer
    ZLMT-12 (compound 35), tacrine derivatives, is a potent, orally active CDK2/9 inhibitor with IC50 values of 0.002 and 0.011 μM for CDK9 and CDK2, respectively. ZLMT-12 has a weak inhibitory effect on AChE (IC50=19.023 μM) and BChE (IC50=2.768 μM). ZLMT-12 has low toxicity and antiproliferative activity. ZLMT-12 induces apoptosis and arrests the cell cycle in the S phase and G2/M phase.
  • HY-145289
    Antitumor agent-37

    Apoptosis Cancer
    Antitumor agent-37 possesses potent anti-proliferative and anti-metastasis activities. Antitumor agent-37 induces serious DNA damage and further leads to high expression of γ-H2AX and p53. Antitumor agent-37 promotes apoptosis of tumor cells through mitochondrial apoptotic pathway Bcl-2/Bax/caspase3. Antitumor agent-37 significantly improves immune response through restraining the expression of PD-L1 to increase CD3+ and CD8+ T infiltrating cells in tumor tissues.
  • HY-150618
    PI3Kα-IN-9

    PI3K Apoptosis Cancer
    PI3Kα-IN-9 (compound 27) is a selective, long-acting and oral active PI3Kα inhibitor with IC50 values of 4.4, 128, 146 and 153 nM for PI3Kα, PI3Kγ, PI3Kδ and PI3Kβ, respectively. PI3Kα-IN-9 has antiproliferative activity and induces apoptosis. PI3Kα-IN-9 can be used for cancer research.
  • HY-126247
    BI-2852

    Ras Cancer
    BI-2852 is a KRAS inhibitor for the switch I/II pocket (SI/II-pocket) by structure-based drug design with nanomolar affinity. BI-2852 is mechanistically distinct from covalent KRAS G12C inhibitor (binds to switch II pocket) and binds ten-fold more strongly to active KRAS G12D versus KRAS wt (740 nM vs 7.5 μM). BI-2852 blocks GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in KRAS mutant cells.
  • HY-145288
    Antitumor agent-36

    Apoptosis Cancer
    Antitumor agent-36 possesses potent anti-proliferative and anti-metastasis activities. Antitumor agent-36 induces serious DNA damage and further leads to high expression of γ-H2AX and p53. Antitumor agent-36 promotes apoptosis of tumor cells through mitochondrial apoptotic pathway Bcl-2/Bax/caspase3. Antitumor agent-36 significantly improves immune response through restraining the expression of PD-L1 to increase CD3+ and CD8+ T infiltrating cells in tumor tissues.
  • HY-100555
    CH5138303

    HSP Cancer Infection
    CH5138303 is a potent and orally active Hsp90 inhibitor. CH5138303 shows high binding affinity for N-terminal Hsp90α, with Kd of 0.52 nM. CH5138303 shows potent anti-proliferative activity against human cancer cell lines (HCT116 and NCI-N87), with IC50 values of 0.098 and 0.066 μM, respectively. CH5138303 shows high oral bioavailability in mice (F=44.0%). CH5138303 shows potent antitumor efficacy in a human NCI-N87 gastric cancer xenograft model.
  • HY-150613
    PARP1/BRD4-IN-2

    Epigenetic Reader Domain PARP Apoptosis Cancer
    PARP1/BRD4-IN-2 is a potent and selective PARP1 and BRD4 inhibitor with IC50 values of 197 nM and 238 nM, respectively. PARP1/BRD4-IN-2 inhibits DNA damage repair, arrests G0/G1 transition and induces apoptosis. PARP1/BRD4-IN-2 has anti-tumor activity in MDA-MB-468 xenograft mouse model. PARP1/BRD4-IN-2 can be used for researching triple-negative breast cancer (TNBC).
  • HY-19322
    PIM447

    LGH447

    Pim Apoptosis Cancer
    PIM447 (LGH447) is a potent, orally available, and selective pan-PIM kinase inhibitor, with Ki values of 6, 18, and 9 pM for PIM1, PIM2, and PIM3, respectively. PIM447 displays dual antimyeloma and bone-protective effects. PIM447 induces apoptosis.
  • HY-P3624
    Cenderitide

    Guanylate Cyclase Cardiovascular Disease
    Cenderitide is a potent agonist of particulate guanylyl cyclase receptor (pGC). Cenderitide is a natriuretic peptide (NP) composed of C-type natriuretic peptide (CNP) fused to the C-terminus of Dendroaspis natriuretic peptide (DNP). Cenderitide activates both pGC-A and pGC-B, activates the second messenger cGMP, suppresses aldosterone, and preserves GFR without reducing blood pressure. Cenderitide can be used for heart failure research.
  • HY-146980
    GLUT4-IN-2

    Apoptosis GLUT Cancer
    GLUT4-IN-2 is a potent and selective GLUT4 inhibitor with IC50s of 11.4 µM and 6.8 µM for GLUT1 and GLUT4, respectively. GLUT4-IN-2 induces cell apoptosis and cell cycle arrest at G0/G1phase. GLUT4-IN-2 shows potent antitumor activity.
  • HY-101522
    CHMFL-EGFR-202

    EGFR BMX Kinase Btk MEK Cancer
    CHMFL-EGFR-202 is a potent, irreversible inhibitor of epidermal growth factor receptor (EGFR) mutant kinase, with IC50s of 5.3 nM and 8.3 nM for drug-resistant mutant EGFR T790M and WT EGFR kinases, respectively. CHMFL-EGFR-202 exhibits ∼10-fold selectivity for EGFR L858R/T790M against the EGFR wild-type in cells. CHMFL-EGFR-202 adopts a covalent “DFG-in-C-helix-out” inactive binding conformation with EGFR, with strong antiproliferative effects against EGFR mutant-driven nonsmall-cell lung cancer (NSCLC) cell lines.
  • HY-147862
    EGFR-IN-62

    EGFR Apoptosis Cancer
    EGFR-IN-62 (compound 9h) is a potent and reversible EGFR kinase inhibitor, with IC50 values of 10 nM (L858R/T790 M), 29 nM (WT), and 242 nM (L858R/T790 M/C797S), respectively. EGFR-IN-62 shows antiproliferative activity against A549 and H1975 cell lines, with IC50 values of 2.53 and 1.56 μM, respectively. EGFR-IN-62 induces dose-dependent apoptosis process, G1/G0-phase arrestation, and the inhibition of motility on A549 and/or H1975 cell lines.
  • HY-145836
    FGFR4-IN-8

    FGFR Cancer
    FGFR4-IN-8 (Compound 7v) is an ATP-competitive, highly selective covalent inhibitor of wild-type and gatekeeper mutant FGFR4. FGFR4-IN-8 exhibits excellent potency against FGFR4, FGFR4 V550L, FGFR4 V550M and FGFR4 C552S with IC50s of 0.5, 0.25, 1.6, 931 nM, respectively. FGFR4-IN-8 exhibits potent antiproliferative activity against Hep3B hepatocellular carcinoma cells with the IC50 value of 29 nM. FGFR4-IN-8 demonstrates modest in vivo antitumor efficacy in nude mice bearing the Huh-7 xenograft model.
  • HY-112296
    T025

    CDK Apoptosis DYRK Cancer
    T025 is an orally active and highly potent inhibitor of Cdc2-like kinase (CLKs), with Kd values of 4.8, 0.096, 6.5, 0.61, 0.074, 1.5 and 32 nM for CLK1, CLK2, CLK3, CLK4, DYRK1A, DYRK1B and DYRK2, respectively. T025 induces caspase-3/7-mediated cell apoptosis. T025 reduces CLK-dependent phosphorylation. T025 exerts anti-proliferative activities in both hematological and solid cancer cell lines (IC50 values: 30-300 nM). T025 has an anti-tumor efficiency, mainly for MYC-driven disease research.
  • HY-144725
    HDAC1/6-IN-1

    HDAC Apoptosis Cancer
    HDAC1/6-IN-1 (compound D7) is a potent multitarget inhibitor of GLP, HDAC6 and HDAC1, with IC50 values of 1.3, 13, and 89 nM, respectively. HDAC1/6-IN-1 can inhibit the methylation and deacetylation of H3K9 on protein level. HDAC1/6-IN-1 induces cancer cell apoptosis, G0/G1 cell cycle arrest, and blocks migration and invasion.
  • HY-151375
    CDK9/10/GSK3β-IN-1

    Others Cancer
    CDK9/10/GSK3β-IN-1 (compound 13c) is a kinase inhibitor (Flavopiridol (HY-10005) analogue) that effectively inhibits HsGSK3β (IC50=59 nM), HsCDK9/CyclinT (IC50=64 nM), HsCDK5/p25 (IC50=1.093 µM) and HsCDK2/CyclinA (IC50=1.725 µM). CDK9/10/GSK3β-IN-1 has anti-cancer cellular activity comparable to or higher than that of Flavopiridol. CDK9/10/GSK3β-IN-1 shows high anti-proliferative activity in vitro against up to seven cancer cell lines.
  • HY-122578
    P53R3

    MDM-2/p53 Cancer
    P53R3 is a potent p53 reactivator and restores sequence-specific DNA binding of p53 hot spot mutants, including p53 R175H, p53 R248W and p53 R273H. P53R3 induces p53-dependent antiproliferative effects with much higher specificity than PRIMA-1. P53R3 enhances the recruitment of wild-type p53 and p53 M237I to several target gene promoters. P53R3 strongly enhances the mRNA, total protein and cell surface expression of the death receptor death receptor 5 (DR5). P53R3 is used for cancer research.
  • HY-P3808
    [D-Pro2,D-Trp7,9] Substance P

    Inflammation/Immunology
    [D-Pro2,D-Trp7,9] Substance P, a Substance P (HY-P0201) analogue, is a weak agonist and a potent, specific, competitive Substance P antagonist.
  • HY-112608
    CHMFL-PI3KD-317

    PI3K Cancer
    CHMFL-PI3KD-317 is a highly potent, selective and orally active PI3Kδ inhibitor, with an IC50 of 6 nM, and exhibits over 10-1500 fold selectivity over other class I, II and III PIKK family isoforms, such as PI3Kα (IC50, 62.6 nM), PI3Kβ (IC50, 284 nM), PI3Kγ (IC50, 202.7 nM), PIK3C2A (IC50, >10000 nM), PIK3C2B (IC50, 882.3 nM), VPS34 (IC50, 1801.7 nM), PI4KIIIA (IC50, 574.1 nM) and PI4KIIIB (IC50, 300.2 nM). CHMFL-PI3KD-317 inhibits PI3Kδ-mediated Akt T308 phosphorylation in Raji cells, with an EC50 of 4.3 nM. CHMFL-PI3KD-317 has antiproliferative effects on cancer cells.
  • HY-148369
    U7D-1

    PROTACs Deubiquitinase Apoptosis MDM-2/p53 Cancer
    U7D-1 is a first-in-class potent and selective USP7 (ubiquitin-specific protease 7) PROTAC degrader, with a DC50 of 33 nM in RS4;11 cells. U7D-1 shows anticancer activity. U7D-1 induces apoptosis in Jeko-1 cells.