2. Search Result
Search Result
Results for "

antitumor

" in MCE Product Catalog:

879

Inhibitors & Agonists

3

Screening Libraries

2

Dye Reagents

21

Peptides

3

Inhibitory Antibodies

256

Natural
Products

9

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas
  • HY-15961
    Antitumor agent-3

    		Others Cancer
    Antitumor agent-3 is a potent compound which comprises a new imidazopyridine having excellent antitumor activity as an active ingredient.
  • HY-128934
    Antitumor agent-2

    		Others Cancer Inflammation/Immunology
    Antitumor agent-2 is sourced from patent CN102250203, compound 6a-r, has antitumor action and anti-inflammatory action.
  • HY-141478
    Antitumor agent-28

    		ATM/ATR Cancer
    Antitumor agent-28 selectively inhibits ataxia telangiectasia mutated (ATM) kinase. Antitumor agent-28 prevents ATM mediated disease and has potent anti-cancer activity.
  • HY-U00414
    Antitumor agent-4

    		Others Cancer
    Antitumor agent-4, a butenylphenyl phosphate derivative, is a drug for mammary cancer and anovulatory sterility.
  • HY-128776
    Antitumor agent-19

    		Others Cancer
    Antitumor agent-19 is an antitomor agent targeting tumor-associated macrophages (TAMs) to serve as an effective TAMs modulator. The EC50 values of Antitumor agent-19 in the RAW 264.7 cells and the BMDM cells are 17.18 μM and 18.87 μM, respectively.
  • 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-136342
    Antitumor agent-23

    		Others Cancer
    Antitumor agent-23 is a potent anti-cancer agent with GI50s of 38, 48, 5, 27, 80, and 28 nM for lymphoma cell line GRANTA-519, KARPAS-422, KARPAS-299, RAMOS, DAUDI, and RAJI, respectively. Antitumoral activity.
  • HY-105237
    Eesperamicin A1

    		Antibiotic DNA/RNA Synthesis Cancer
    Esperamicin A1, as an extremely potent antitumor antibiotic, is isolated from cultures of Actinomadura verrucosospora. Esperamicin A1 can be used for the research of antitumor.
  • HY-115677
    ILK-IN-3

    		Integrin Cancer
    ILK-IN-3 is an integrin linked kinase inhibitor with antitumor activity.
  • HY-N7994
    Hellebrigenol

    		Others Cancer
    Hellebrigenol is a metabolite of bufadienolides with antitumor activity.
  • HY-N7685
    Podophyllol

    		Others Cancer
    Podophyllol, a derivative of podophyllotoxin esters, has antitumor activity.
  • HY-N0827
    Perillene

    		Bacterial Cancer Infection
    Perillene is a component of the essential oil, has antibacterial and antitumor effects.
  • HY-N7595
    Microhelenin C

    		Others Cancer
    Microhelenin C is a sesquiterpene lactone that can be isolated from Helenium microcephalum, with antitumor activity.
  • HY-17565A
    Bleomycin hydrochloride

    		DNA/RNA Synthesis Antibiotic Cancer
    Bleomycin hydrochloride is a DNA synthesis inhibitor. Bleomycin hydrochloride is a DNA damaging agent. Bleomycin hydrochloride is an antitumor antibiotic.
  • HY-111999A
    E7766 diammonium salt

    		STING Cancer
    E7766 diammonium salt is a macrocycle-bridged STING agonist with a Kd of 40 nM. E7766 diammonium salt shows potent pan-genotypic and antitumor activities.
  • HY-111999B
    E7766 disodium

    		STING Cancer
    E7766 disodium is a macrocycle-bridged STING agonist with a Kd of 40 nM. E7766 disodium shows potent pan-genotypic and antitumor activities.
  • HY-N3741
    Didrovaltrate

    Didrovaltratum

    		 Others Cancer
    Didrovaltrate (Didrovaltratum), isolated from the roots of Valeriana wallichii D.C, is a cytotoxic and antitumor agent.
  • HY-N8533
    Sodium Camptothecin

    		DNA/RNA Synthesis Cancer Infection
    Sodium Camptothecin is a plant alkaloid, with antitumor activity. Sodium Camptothecin is a reversible inhibitor of RNA synthesis. Sodium Camptothecin is an effective inhibitor of adenovirus replication. Sodium Camptothecin inhibits DNA synthesis and causes breaks in intracellular preformed viral DNA.
  • HY-16059
    Arglabin

    (+)-Arglabin

    		 NOD-like Receptor (NLR) Farnesyl Transferase Autophagy Cancer Inflammation/Immunology
    Arglabin ((+)-Arglabin), a natural product isolated from Artemisia glabella, is a NLRP3 inflammasome inhibitor. Arglabin shows anti-inflammatory and antitumor activities. The antitumor activity of Arglabin proceeds through its inhibition of farnesyl transferase which leads to the activation of RAS proto-oncogene.
  • HY-116786
    11-Hydroxycanthin-6-one

    		Others Cancer
    11-Hydroxycanthin-6-one, a canthin-6-one alkaloid, is an antitumor agent which shows potent cytotoxic activity.
  • HY-132001
    Ziftomenib

    		Epigenetic Reader Domain Cancer
    Ziftomenib is a menin-MLL interaction inhibitor with antitumor activities (WO2017161028A1, compound 151).
  • HY-N2909
    Aurantiamide

    		Others Inflammation/Immunology
    Aurantiamide is an orally active constituent of Portulaca oleracea L and has various biological activities, including antioxidant, antiplatelet, anti-inflammatory, and antitumor activities.
  • HY-136327
    Phenylacetic acid mustard

    		DNA Alkylator/Crosslinker Cancer
    Phenylacetic acid mustard is the major metabolite of the cancer chemotherapeutic agent Chlorambucil (HY-13593). Chlorambucil is an alkylating agent with antitumor activity.
  • HY-133571A
    Aminohexylgeldanamycin hydrochloride

    AHGDM hydrochloride

    		 HSP ADC Cytotoxin Cancer
    Aminohexylgeldanamycin (AHGDM) hydrochloride, a Geldanamycin derivative, is a potent HSP90 inhibitor. Aminohexylgeldanamycin hydrochloride shows antiangiogenic and antitumor activities.
  • HY-130115
    IACS-8803

    		STING Cancer
    IACS-8803 is a highly potent cyclic dinucleotide STING agonist with robust systemic antitumor efficacy.
  • HY-133571
    Aminohexylgeldanamycin

    AHGDM

    		 HSP ADC Cytotoxin Cancer
    Aminohexylgeldanamycin (AHGDM), a Geldanamycin derivative, is a potent HSP90 inhibitor. Aminohexylgeldanamycin shows antiangiogenic and antitumor activities.
  • HY-130115A
    IACS-8803 disodium

    		STING Cancer
    IACS-8803 disodium is a highly potent cyclic dinucleotide STING agonist. IACS-8803 disodium has a robust systemic antitumor efficacy.
  • HY-B0063
    Gimatecan

    ST1481

    		 Topoisomerase Cancer
    Gimatecan (ST1481) is a potent topoisomerase I inhibitor. Gimatecan is an orally bioavailable camptothecin analogue with antitumor activity.
  • HY-101647
    Intoplicine

    RP 60475

    		 Topoisomerase Cancer
    Intoplicine (RP 60475), an antitumor derivative in the 7H-benzo[e]pyrido[4,3-b]indole series, is a DNA topoisomerase I and II inhibitor. Intoplicine strongly binds DNA (KA = 2 x 10 5 /M) and thereby increases the length of linear DNA.
  • HY-101647A
    Intoplicine dimesylate

    RP 60475 dimesylate

    		 Topoisomerase Cancer
    Intoplicine (RP 60475) dimesylate, an antitumor derivative in the 7H-benzo[e]pyrido[4,3-b]indole series, is a DNA topoisomerase I and II inhibitor. Intoplicine dimesylate strongly binds DNA (KA = 2 x 10 5 /M) and thereby increases the length of linear DNA.
  • HY-W048303
    L-Azatyrosine

    		Antibiotic Cancer Infection
    L-Azatyrosine is an antitumor antibiotic isolated from Streptomyces chibaensis. L-Azatyrosine can restore normal phenotypic behavior to transformed cells bearing oncogenic Ras genes.
  • HY-138645A
    5-Iminodaunorubicin hydrochloride

    		DNA/RNA Synthesis Cancer
    5-Iminodaunorubicin hydrochloride is a quinone-modified anthracycline that retains antitumor activity. 5-Iminodaunorubicin hydrochloride produces protein-concealed DNA strand breaks in cancer cells.
  • HY-138645
    5-Iminodaunorubicin

    		DNA/RNA Synthesis Cancer
    5-Iminodaunorubicin is a quinone-modified anthracycline that retains antitumor activity. 5-Iminodaunorubicin produces protein-concealed DNA strand breaks in cancer cells.
  • HY-15579S
    D8-MMAF

    Monomethylauristatin F D8

    		 Microtubule/Tubulin ADC Cytotoxin Cancer
    D8-MMAF hydrochloride is a deuterated form of MMAF hydrochloride. MMAF Hydrochloride, a potent tubulin polymerization inhibitor, is used as a antitumor agent and a cytotoxic component of antibody-drug conjugates (ADCs).
  • HY-131345
    PI3Kα-IN-4

    		PI3K Cancer
    PI3Kα-IN-4 is a potent, selective and orally active inhibitor of PI3Kα, with an IC50 of 1.8 nM. PI3Kα-IN-4 has antitumor activity.
  • HY-126804
    Safracin B

    		Antibiotic Cancer Infection
    Safracin B, a tetrahydroisoquinoline (THIQ) alkaloid, is a naturally occurring antibiotic from Pseudomonas fluorescens. Safracin B exhibits broad spectrum antimicrobial and strong antitumor activities.
  • HY-136293
    Mechercharmycin A

    		Apoptosis Cancer
    Mechercharmycin A is a cytotoxic substance isolated from marine-derived Thermoactinomyces sp. YM3-251. Mechercharmycin A exhibits relatively strong antitumor activity.
  • HY-12019
    SGX-523

    		c-Met/HGFR Cancer
    SGX523 is a exquisitely selective and ATP-competitive MET inhibitor. SGX523 potently inhibits MET with an IC50 of 4 nM and is >1,000-fold selective versus other protein kinases. Antitumor activity.
  • HY-N0936
    Coixol

    6-Methoxy-2-benzoxazolinone; 6-MBOA

    		 Bacterial Cancer Infection
    Coixol (6-Methoxy-2-benzoxazolinone;6-MBOA) is a polyphenol extracted from coix (Coix lachryma-jobi L.var.ma-yuen Stapf) with antimicrobial and antitumor activities.
  • HY-10204
    OSI-930

    		c-Kit VEGFR c-Fms Apoptosis Cancer
    OSI-930 is an orally selective inhibitor of Kit, KDR and CSF-1R (c-Fms) with IC50s of 80 nM, 9 nM and 15 nM, respectively. OSI-930 also moderately inhibits Flt-1, c-Raf, Lck and low activity against PDGFRα/β, Flt-3 and Abl. OSI-930 has antitumor activity.
  • HY-123291
    SM-276001

    		Toll-like Receptor (TLR) IFNAR Cancer Inflammation/Immunology
    SM-276001 is a potent selective TLR7 agonist that can induce antitumor immune responses. SM-276001 is an orally active interferon (IFN) inducer.
  • HY-136718
    CLEFMA

    		Apoptosis Cancer
    CLEFMA is a curcuminoid with antitumor activity. CLEFMA inhibits tumor growth is associated with NF-κB-regulated anti-inflammatory and anti-metastatic effects.
  • 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-136294
    Cryptophycin 1

    Cryptophycin A

    		 Microtubule/Tubulin Apoptosis Cancer
    Cryptophycin 1 is a potent cytotoxic antimicrotubule agent which is isolated from Nostoc sp. Cryptophycin 1 can induce cells apoptosis, and exhibits antitumor activity and exceptional antiproliferative potency.
  • HY-126534A
    LSN3106729 hydrochloride

    		CDK Ligand for Target Protein for PROTAC Cancer
    LSN3106729 hydrochloride, the metabolite of Abemaciclib (HY-16297A), is a CDK inhibitor with antitumor activity. LSN3106729 hydrochloride and a CRBN ligand have been used to design PROTAC CDK4/6 degrader.
  • HY-126534
    LSN3106729

    		CDK Ligand for Target Protein for PROTAC Cancer
    LSN3106729, the metabolite of Abemaciclib (HY-16297A), is a CDK inhibitor with antitumor activity. LSN3106729 and a CRBN ligand have been used to design PROTAC CDK4/6 degrader.
  • HY-133117
    BAY-985

    		IKK Cancer
    BAY-985 is a highly potent, orally active and selective ATP-competitive dual inhibitor of TBK1 and IKKε with IC50s of 2/30 and 2 nM for TBK1 (low/high ATP) and IKKε, respectively. Antitumor efficacy.
  • HY-138799
    KA2507

    		HDAC Cancer
    KA2507 is a potent and selective HDAC6 inhibitor, with an IC50 of 2.5 nM. KA2507 shows antitumor activities and immune modulatory effects in preclinical models.
  • HY-N9460
    Sibiromycin

    		DNA Alkylator/Crosslinker Antibiotic Cancer
    Sibiromycin is a naturally produced glycosylated pyrrolobenzodiazepines (PBDs). Sibiromycin is also a potent antitumor antibiotic that binds covalently to DNA in the minor groove at the NH2 of guanine.
  • 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-13598
    Valecobulin

    CKD-516

    		 Microtubule/Tubulin Cancer
    Valecobulin (CKD516) is a valine prodrug of (S516) and a vascular disrupting agent (VDA). Valecobulin is a potent β-tubulin polymerization inhibitor with marked antitumor activity against murine and human solid tumors.
  • HY-101162
    SGD-1910

    		Drug-Linker Conjugates for ADC Cancer
    SGD-1910 is a drug-linker conjugate for ADC by using the antitumor antibiotic, pyrrolobenzodiazepine (PBD, a cytotoxic DNA crosslinking), linked via the cleavable linker MC-Val-Ala.
  • HY-14429
    (-)-Irofulven

    MGI 114; 6-Hydroxymethylacylfulvene; NSC 683863

    		 DNA Alkylator/Crosslinker Apoptosis Cancer
    (-)-Irofulven (MGI 114), an Illudin S analog, is a DNA alkylating agent. (-)-Irofulven inhibits the replication of DNA, induces tumor cells apoptosis, and has potent antitumor activity.
  • HY-138799A
    KA2507 monohydrochloride

    		HDAC Cancer Inflammation/Immunology
    KA2507 hydrochloride is a potent and highly selective inhibitor of HDAC6 (IC50=2.5 nM) with no significant toxicities. KA2507 hydrochloride shows antitumor efficacy and immune modulatory effects.
  • HY-N9351
    Cleistanthin B

    Diphyllin O-glucoside

    		 SARS-CoV Cancer Infection Metabolic Disease Cardiovascular Disease
    Cleistanthin B (Diphyllin O-glucoside) is an orally active arylnaphthalene lignan lactone glycoside. Cleistanthin B exhibits anti-SARS-CoV-2 effects in Vero cells, with EC50 of 6.51 µM. Cleistanthin B also exhibits antitumor, diuretic and antihypertensive effects in vivo.
  • HY-13598A
    Valecobulin hydrochloride

    CKD-516 hydrochloride

    		 Microtubule/Tubulin Cancer
    Valecobulin hydrochloride (CKD-516 hydrochloride) is a valine prodrug of S516 (HY-130233) and a vascular disrupting agent (VDA). Valecobulin hydrochloride is a potent β-tubulin polymerization inhibitor with marked antitumor activity against murine and human solid tumors.
  • HY-15866
    FR901465

    		Others Cancer
    FR901465 is a potent anti-cancer and anti-tumor agent. FR901465 can be used for cancer research.
  • HY-120448
    QTX125

    		HDAC Apoptosis Cancer
    QTX125 is a potent and highly selective HDAC6 inhibitor. QTX125 exhibits excellent selectivity over other HDACs. QTX125 has antitumor effects.
  • HY-139279
    TPX-0131

    		ALK Cancer
    TPX-0131 is a potent, selective, CNS-penetrant and orally active inhibitor of wild-type ALK (IC50 of 1.4 nM) and ALK-resistant mutation, e.g. G1202R (IC50 of 0.3 nM), L1196M (IC50 of 0.3 nM). TPX-0131 has strong antitumor activities.
  • HY-N0114A
    (±)-Evodiamine

    		Topoisomerase Apoptosis Cancer Inflammation/Immunology Cardiovascular Disease
    (±)-Evodiamine, a quinazolinocarboline alkaloid, is a Top1 inhibitor. Evodiamine exhibits anti-inflammatory, antiobesity, and antitumor effects. (±)-Evodiamine inhibits the proliferation of a wide variety of tumor cells by inducing their apoptosis.
  • HY-119016A
    SK1-​I hydrochloride

    BML-258 hydrochloride

    		 SphK Cancer
    SK1-I hydrochloride (BML-258 hydrochloride), an analog of sphingosine, is an isozyme-specific competitive SPHK1 inhibitor with a Ki value of 10 µM. SK1-I hydrochloride shows no activity at SPHK1 PKCα, PKCδ, PKA, AKT1, ERK1, EGFR, CDK2, IKKβ or CamK2β. SK1-I hydrochloride enhances autophagy and has antitumor activity.
  • HY-119016
    SK1-I

    BML-258

    		 SphK Cancer
    SK1-I (BML-258), an analog of sphingosine, is an isozyme-specific competitive SPHK1 inhibitor with a Ki value of 10 µM. SK1-I shows no activity at SPHK1 PKCα, PKCδ, PKA, AKT1, ERK1, EGFR, CDK2, IKKβ or CamK2β. SK1-I enhances autophagy and has antitumor activity.
  • HY-103682A
    PF-06726304 acetate

    		Histone Methyltransferase Cancer
    PF-06726304 acetate is a potent and selective EZH2 inhibitor. PF-06726304 acetate inhibits wild-type and Y641N mutant EZH2 with Kis of 0.7 and 3.0 nM, respectively. PF-06726304 acetate displays robust antitumor growth activity.
  • HY-103682
    PF-06726304

    		Histone Methyltransferase Cancer
    PF-06726304 is a potent and selective EZH2 inhibitor. PF-06726304 inhibits wild-type and Y641N mutant EZH2 with Kis of 0.7 and 3.0 nM, respectively. PF-06726304 displays robust antitumor growth activity.
  • HY-N0878
    Bufotalin

    		Apoptosis Reactive Oxygen Species Cancer
    Bufotalin is a steroid lactone isolated from Venenum Bufonis with potently antitumor activities. Bufotalin induces cancer cell apoptosis and also induces endoplasmic reticulum (ER) stress activation.
  • HY-100846
    JQEZ5

    		Histone Methyltransferase Cancer
    JQEZ5 is a potent and selective EZH2 lysine methyltransferase inhibitor. JQEZ5 SAM-competitive inhibition of polycomb repressive complex 2 (PRC2) with an IC50 of 80 nM. JQEZ5 has anti-tumor effects.
  • HY-120882
    BM-1197

    		Bcl-2 Family Cancer
    BM-1197 is a potent and selective inhibitor of dual Bcl-2/Bcl-xL, with IC50s of 3.5 nM and 5.2 nM for Bcl-2 and Bcl-xL, respectively. BM-1197 exhibits antitumor effects both in vitro and in vivo.
  • HY-16200
    Ethynylcytidine

    ECyD; TAS-106; 3'-C-Ethynylcytidine

    		 DNA/RNA Synthesis Nucleoside Antimetabolite/Analog Cancer
    Ethynylcytidine (ECyD), a nucleoside analog and a potent inhibitor of RNA synthesis, inhibits RNA polymerases I, II and II. Ethynylcytidine has robust antitumor activity in a wide range of models of cancer.
  • HY-111899
    7-Ethoxyrosmanol

    		Others Cancer
    7-Ethoxyrosmanol is a phenolic diterpene that is isolated from Salvia chamelaeagnea. 7-Ethoxyrosmanol has antioxidant activity in vitro and antitumor effects on neuroblastoma cells.
  • HY-131349
    CCR4 antagonist 3

    		CCR Cancer
    CCR4 antagonist 3 is an orally active, potent and selective CCR4 antagonist. CCR4 antagonist 3, featuring a novel piperidinyl-azetidine motif, has IC50s of 22 nM and 50 nM in the calcium flux and CTX assay. CCR4 antagonist 3 has antitumor activity.
  • HY-131349A
    CCR4 antagonist 3 hydrochloride

    		CCR Cancer Metabolic Disease
    CCR4 antagonist 3 hydrochloride is an orally active, potent and selective CCR4 antagonist. CCR4 antagonist 3, featuring a novel piperidinyl-azetidine motif, has IC50s of 22 nM and 50 nM in the calcium flux and CTX assay. CCR4 antagonist 3 has antitumor activity.
  • HY-113649
    AKB-6899

    		HIF/HIF Prolyl-Hydroxylase Cancer
    AKB-6899, a prolyl hydroxylase domain 3 (PHD3) inhibitor, is a selective HIF-2α stabilizer. AKB-6899 also increases soluble form of the VEGF receptor (sVEGFR-1) production from GM-CSF-treated macrophages, and has antitumor and antiangiogenic effects.
  • HY-133141
    DI-87

    		Others Cancer
    DI-87 is an orally active and selective deoxycytidine kinase (dCK) inhibitor with an EC50 of 10.2 nM. DI-87 has antitumor activity and is used in combination therapy against tumors expressing dCK.
  • 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 Kds of <500 nM. R1530 inhibits VGFR2 and FGFR1 with IC50s of 10 nM and 28 nM, respectively.
  • HY-103266
    TC-A 2317 hydrochloride

    		Aurora Kinase Cancer
    TC-A 2317 hydrochloride is an orally active Aurora A kinase inhibitor (Ki=1.2 nM). TC-A 2317 hydrochloride exhibits excellent selectivity to Aurora B kinase (Ki=101 nM) and other 60 kinases, good cell permeability and good PK profile. Antitumor activity.
  • HY-136499
    DI-82

    		Others Cancer
    DI-82 is a potent deoxycytidine kinase (dCK) inhibitor with an IC50 app of 27.8 nM and Ki app of 9.2 nM. DI-82 has antitumor activity.
  • HY-137377
    TAS-119

    		Aurora Kinase Cancer
    TAS-119 is a potent, selective and orally active Aurora A inhibitor with an IC50 of 1.0 nM. TAS-119 shows high selectivity for Aurora A over other protein kinases, including Aurora B (IC50 of 95 nM). TAS-119 has potent antitumor activites.
  • HY-15337
    Hesperidin

    Hesperetin 7-rutinoside

    		 Apoptosis Autophagy Reactive Oxygen Species Endogenous Metabolite Cancer
    Hesperidin (Hesperetin 7-rutinoside), a flavanone glycoside, is isolated from citrus fruits. Hesperidin has numerous biological properties, such as decreasing inflammatory mediators and exerting significant antioxidant effects. Hesperidin also exhibits antitumor and antiallergic activities.
  • HY-N0035
    Arctigenin

    (-)-Arctigenin

    		 MMP Influenza Virus Autophagy Apoptosis Cancer Infection Metabolic Disease Inflammation/Immunology Neurological Disease
    Arctigenin ((-)-Arctigenin), a biologically active lignan, can be used as an antitumor agent. Arctigenin exhibits potent antioxidant, anti-inflammatory and antiviral (influenza A virus) activities. Arctigenin can be used for the research of metabolic disorders, and central nervous system dysfunctions.
  • HY-129441
    Metoprine

    BW 197U

    		 Histone Methyltransferase Antifolate Cancer Neurological Disease
    Metoprine (BW 197U) is a potent histamine N-methyltransferase (HMT) inhibitor. Metoprine, a diaminopyrimidine derivative, can cross the blood-brain barrier and increase brain histamine levels by inhibiting HMT. Metoprine is an antifolate and antitumor agent.
  • HY-134673A
    UZH1a

    		Apoptosis Cancer
    UZH1a is a potent and selective METTL3 inhibitor, with an IC50 of 280 nM. UZH1a can be used for epitranscriptomic modulation of cellular processes. UZH1a has antitumor activity. UZH1a also can be used as a chemical probe for studying METTL3.
  • HY-131972
    PF-06843195

    		PI3K Cancer
    PF-06843195 is a highly selective PI3Kα inhibitor with an IC50 of 18 nM in Rat1 fibroblasts. The Kis of PF-06843195 for PI3Kα and PI3Kδ in biochemical kinase assay are less than 0.018 nM and 0.28 nM, respectively. PF-06843195 has great suppression of the PI3K/mTOR signaling pathway and durable antitumor efficacy.
  • HY-10032
    PF 477736

    PF 00477736

    		 Checkpoint Kinase (Chk) VEGFR Src c-Fms Aurora Kinase FGFR FLT3 RET CDK Cancer
    PF 477736 (PF 00477736) is a potent, selective and ATP-competitive inhibitor of Chk1, with a Ki of 0.49 nM, it is also a Chk2 inhibitor, with a Ki of 47 nM. PF 477736 shows <100-fold selectivity for Chk1 over VEGFR2, Fms, Yes, Aurora-A, FGFR3, Flt3, and Ret (IC50=8 (Ki), 10, 14, 23, 23, 25, and 39 nM, respectively). PF 477736 can enhance Gemcitabine antitumor activity in vitro and in vivo.
  • HY-124944
    APS6-45

    		Ras Cancer
    APS6-45 is an orally active tumor-calibrated inhibitor (TCI). APS6-45 inhibits RAS/MAPK signaling and exhibits antitumor activity.
  • HY-123979
    ζ-Stat

    NSC37044

    		 PKC Apoptosis Cancer
    ζ-Stat (NSC37044) is a specific and atypical PKC-ζ inhibitor, with an IC50 of 5 μM. ζ-Stat can reduce melanoma cell lines proliferation and induce apoptosis, and has antitumor activity in vitro.
  • HY-12457
    Rachelmycin

    CC-1065; NSC 298223

    		 Antibiotic Cancer Infection
    Rachelmycin (CC-1065; NSC 298223) is a potent naturally antibiotic isolated from Streptomyces zelensis. Rachelmycin binds non-covalently and covalently (N-3 adenine adduct) in the minor groove of B-form DNA. Rachelmycin has exceptionally potent antitumor activity.
  • HY-N7449
    Neamine

    		Bacterial Cancer Infection Neurological Disease Cardiovascular Disease
    Neamine, a degradation product of Neomycin, is a broad-spectrum aminoglycoside antibiotic. Neamine is an anti-angiogenesis agent targeting angiogenin. Neamine has potent antibacterial, antitumor and neuroprotective activities.
  • HY-101117
    EED226

    		Histone Methyltransferase Cancer
    EED226 is a polycomb repressive complex 2 (PRC2) inhibitor, which binds to the K27me3-pocket on embryonic ectoderm development (EED) and shows strong antitumor activity in xenograft mice model. EED226 is a potent, selective, and orally bioavailable EED inhibitor. EED226 inhibits PRC2 with an IC50 of 23.4 nM when the H3K27me0 peptide is used as a substrate in the in vitro enzymatic assays.
  • HY-141514
    MSA-2 dimer

    		STING Cancer Inflammation/Immunology
    MSA-2 dimer is a selective, orally active non-nucleotide STING agonist (Kd=145 μM) with long-term antitumor and immunogenic activity. MSA-2 dimer is bound to STING as a non-covalent dimer exhibiting higher permeability than cyclic dinucleotide.
  • HY-19825
    Rebeccamycin

    		Topoisomerase ADC Cytotoxin Cancer
    Rebeccamycin, an antitumor antibiotic, inhibits DNA topoisomerase I. Rebeccamycin appears to exert its primary antineoplastic effect by poisoning topoisomerase I and has negligible effect on protein kinase C and topoisomerase II.
  • HY-N7271
    Solanidine

    		Others Cancer
    Solanidine is a cholestane alkaloid isolated from several potato species including Solanum demissum, Solanum acaule, and Solanum tuberosum. Solanidine can inhibit proliferation and exhibit obvious antitumor effect.
  • HY-N7504
    Isopsoralenoside

    		Bacterial Cancer Infection Metabolic Disease
    Isopsoralenoside is a benzofuran glycoside from Psoralea corylifolia. Isopsoralenoside can be quickly metabolized to Psoralen (HY-N0053) in digestive tract contents. Isopsoralenoside show estrogen-like activity, osteoblastic proliferation accelerating activity, antitumor effects and antibacterial activity.
  • HY-100748
    CXD101

    		HDAC Cancer
    CXD101 is a potent, selective and orally active class I HDAC inhibitor with IC50s of 63 nM, 570 nM and 550 nM for HDAC1, HDAC2 and HDAC3, respectively. CXD101 has no activity against HDAC class II. CXD101 has antitumor activity.
  • HY-W013164
    SC-58125

    		COX Cancer Inflammation/Immunology
    SC-58125 is a potent and selective inhibitor of cyclooxygenase 2 (COX-2), with an IC50 of 0.04 μM. SC-58125 exhibits antitumor activity in vitro and in vivo. SC-58125 also can inhibit edema at the inflammatory site and has analgesic effect.
  • HY-N9488
    Girinimbine

    Girinimbin

    		 Apoptosis Bacterial Parasite Cancer Infection Inflammation/Immunology
    Girinimbine (Girinimbin) is a carbazole alkaloid with a variety of biological effects. Girinimbine can induce apoptosis, and has antitrypanosomal, antiplatelet activity, antibacterial activity, anti-inflammatory, antioxidant and antitumor activities.
  • HY-10517A
    (Z)-Orantinib

    (Z)-SU6668; (Z)-TSU-68

    		 VEGFR PDGFR FGFR Cancer
    (Z)-Orantinib ((Z)-SU6668) is a potent, selective, orally active and ATP competitive inhibitor of Flk‐1/KDR, PDGFRβ, and FGFR1, with IC50s of 2.1, 0.008, and 1.2 µM, respectively. (Z)-Orantinib is a potent antiangiogenic and antitumor agent that induces regression of established tumors.
  • HY-101030
    MBM-17

    		Apoptosis Cancer
    MBM-17 is a potent NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 3 nM. It effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis. MBM-55 shows antitumor activities, and no obvious toxicity to mice.
  • HY-123979A
    ζ-Stat trisodium

    NSC37044 trisodium

    		 PKC Apoptosis Cancer
    ζ-Stat trisodium (NSC37044 trisodium) is a specific and atypical PKC-ζ inhibitor, with an IC50 of 5 μM. ζ-Stat trisodium can reduce melanoma cell lines proliferation and induce apoptosis, and has antitumor activity in vitro.
  • HY-N7765
    Oenothein B

    		HCV Bacterial Apoptosis Fungal Cancer Infection Inflammation/Immunology
    Oenothein B is a dimeric macrocyclic ellagitannin and has widely pharmacological activities, including antioxidant, anti-inflammatory, antifungal, anti-HCV, and antitumor properties. Oenothein B is a potent and specific inhibitor of poly(ADP-ribose) glycohydrolase.
  • HY-112151A
    EG01377 dihydrochloride

    		Complement System Cancer
    EG01377 dihydrochloride is a potent, bioavailable and selective inhibitor of neuropilin-1 (NRP1), with a Kd of 1.32 μM, and IC50s of 609 nM for both NRP1-a1 and NRP1-b1. EG01377 dihydrochloride has antiangiogenic, antimigratory, and antitumor effects.
  • HY-112151
    EG01377

    		Complement System Cancer
    EG01377 is a potent, bioavailable and selective inhibitor of neuropilin-1 (NRP1), with a Kd of 1.32 μM, and IC50s of both 609 nM for NRP1-a1 and NRP1-b1. EG01377 has antiangiogenic, antimigratory, and antitumor effects.
  • HY-139348
    PFI-90

    		Histone Demethylase Cancer
    PFI-90 is a selective inhibitor of histone demethylase (KDM3B) that inhibits PAX3-FOXO1 action. PFI-90 induces apoptosis and myogenic differentiation, resulting in the cell death increased. PFI-90 has the potential for the antitumor activity. (patent WO2021101929A1).
  • HY-115349
    Neamine tetrahydrochloride

    		Bacterial Cancer Infection Neurological Disease
    Neamine tetrahydrochloride, a degradation product of Neomycin, is a broad-spectrum aminoglycoside antibiotic. Neamine tetrahydrochloride is an anti-angiogenesis agent targeting angiogenin. Neamine tetrahydrochloride has potent antibacterial, antitumor and neuroprotective activities.
  • HY-103257
    CHM-1

    NSC656158

    		 Microtubule/Tubulin Cancer
    CHM-1, a microtubule-destabilizing agent, inhibits tubulin polymerization. CHM-1 is a potent and selective antimitotic antitumor activity against human hepatocellular carcinoma. CHM-1 induces growth inhibition and apoptosis via G2-M phase arrest in human hepatocellular carcinoma cells by activation of Cdc2 kinase activity.
  • HY-U00279
    Nitracrine

    		DNA/RNA Synthesis Cancer
    Nitracrine inhibits RNA synthesis and covalently, reversibly binds to DNA but also forms covalent adducts with DNA in vivo. Nitracrine, a 1-nitroacridine derivative, is a potent hypoxia-selective agent in vitro and antitumor drug. Nitracrine has cytotoxicity towards most cells.
  • HY-129040A
    Iobenguane sulfate

    MIBG sulfate

    		 Others Cancer
    Iobenguane sulfate (MIBG sulfate) is an analogue of the neurotransmitter norepinephrine with antitumor activity. Radioiodinated Iobenguane sulfate is clinically used as a tumor-targeted radiopharmaceutical in the diagnosis and treatment of adrenergic tumors. Iobenguane sulfate is a high-affinity substrate for cholera toxin that interferes with cellular mono(ADP-ribosylation).
  • HY-N7591
    Millepachine

    		Apoptosis Cancer
    Millepachine is a bioactive natural chalcone from Chinese herbal medicine Millettia pachycarpa Benth, exhibits strong antitumor effects against numerous human cancer cells both in vitro and in vivo.
  • HY-D0162
    Malachite green oxalate

    		IKK NF-κB Apoptosis Cancer
    Malachite green oxalate is a triphenylmethane dye which can be used to detect the release of phosphate in enzymatic reactions. Malachite green oxalate is also a potent and selective inhibitor of IKBKE, and inhibits its downstream targets such as IκBα, p65 and IRF3. Malachite green oxalate exhibits antitumor activity in vitro and in vivo.
  • HY-119339
    SX-682

    		CXCR Cancer Inflammation/Immunology Endocrinology
    SX-682 is an orally bioavailable, potent allosteric inhibitor of CXCR1 and CXCR2. SX-682 can block tumor myeloid-derived suppressor cells (MDSCs) recruitment and enhance T cell activation and antitumor immunity.
  • HY-132233
    DDO-2093

    		Histone Methyltransferase Cancer
    DDO-2093 is a potent MLL1-WDR5 protein-protein interaction inhibitor (IC50=8.6 nM; Kd=11.6 nM) with antitumor activity. DDO-2093 selectively inhibits the catalytic activity of MLL complex.
  • HY-126562
    Piperlonguminine

    		Bacterial Fungal Cancer Infection Inflammation/Immunology Neurological Disease Cardiovascular Disease
    Piperlonguminine is an alkaloid amide isolated from the Piper species. Piperlonguminine shows various biological properties, including anti-inflammatory, antitumor, neuroprotective, anti-platelet, anti-melanogenic, antifungal and antibacterial activities.
  • HY-B2144A
    Chitosan (MW 150000)

    Deacetylated chitin (MW 150000); Poly(D-glucosamine) (MW 150000)

    		 Bacterial Fungal Cancer Infection
    Chitosan (MW 150000) (Deacetylated chitin (MW 150000)) is a polycationic linear polysaccharide derived from chitin with the molecular weight of 150000. Chitosan is an versatile biomaterial because of its non-toxicity, low allergenicity, biocompatibility and biodegradability. Chitosan also has antitumor, antibacterial, antifungal, and antioxidant activities.
  • HY-B2144B
    Chitosan (MW 30000)

    Deacetylated chitin (MW 30000); Poly(D-glucosamine) (MW 30000)

    		 Bacterial Fungal Cancer Infection
    Chitosan (MW 30000) (Deacetylated chitin (MW 30000)) is a polycationic linear polysaccharide derived from chitin with the molecular weight of 30000. Chitosan is an versatile biomaterial because of its non-toxicity, low allergenicity, biocompatibility and biodegradability. Chitosan also has antitumor, antibacterial, antifungal, and antioxidant activities.
  • HY-101489A
    GZD856 formic

    		PDGFR Bcr-Abl Apoptosis Cancer
    GZD856 formic is a potent and orally active PDGFRα/β inhibitor, with IC50s of 68.6 and 136.6 nM, respectively. GZD856 formic is also a Bcr-Abl T315I inhibitor, with IC50s of 19.9 and 15.4 nM for native Bcr-Abl and the T315I mutant. GZD856 formic has antitumor activity.
  • HY-101489
    GZD856

    		PDGFR Bcr-Abl Apoptosis Cancer
    GZD856 formic is a potent and orally active PDGFRα/β inhibitor, with IC50s of 68.6 and 136.6 nM, respectively. GZD856 formic is also a Bcr-Abl T315I inhibitor, with IC50s of 19.9 and 15.4 nM for native Bcr-Abl and the T315I mutant. GZD856 formic has antitumor activity.
  • HY-19829
    Sandramycin

    		ADC Cytotoxin Bacterial Antibiotic Cancer Infection
    Sandramycin ia a cyclic depsipeptide antibiotic isolated from cultured broth of a Nocardioides sp. Sandramycin is also a DNA intercalator that potently binds DNA and is an ADC cytotoxin. Sandramycin is active against Gram-positive bacteria and has potent antitumor activity.
  • HY-106662
    Chloroquinoxaline sulfonamide

    Chloroquinoxaline; NSC-339004

    		 Topoisomerase Parasite Cancer Infection
    Chloroquinoxaline sulfonamide (Chloroquinoxaline), a structural analogue of sulfaquinoxaline, is a topoisomerase II alpha/beta poison. Chloroquinoxaline sulfonamide is used to control coccidiosis in poultry, rabbit, sheep, and cattle. Antitumor activity.
  • HY-50751
    Linifanib

    ABT-869; AL-39324

    		 PDGFR VEGFR FLT3 c-Fms c-Kit Autophagy Apoptosis Cancer
    Linifanib (ABT-869) is a potent and orally active multi-target inhibitor of VEGFR and PDGFR family with IC50s of 4, 3, 66, and 4 nM for KDR, FLT1, PDGFRβ, and FLT3, respectively. Linifanib shows prominent antitumor activity. Linifanib has much less activity against unrelated RTKs, soluble tyrosine kinases, or serine/threonine kinases. Linifanib is a specific miR-10b inhibitor that blocks miR-10b biogenesis.
  • HY-112090
    ABBV-744

    		Epigenetic Reader Domain HIV Cancer Infection Inflammation/Immunology
    ABBV-744 is a first-in-class, orally active and selective inhibitor of the BDII domain of BET family proteins with IC50 values range from 4 to 18 nM for BRD2, BRD3, BRD4 and BRDT. ABBV-744 is primarily metabolized by CYP3A4 with drug-like properties enable the investigation of its antitumor efficacy and tolerability.
  • HY-10446
    Pralatrexate

    		Antifolate Apoptosis Cancer
    Pralatrexate is an antifolate and is a potent dihydrofolate reductasean (DHFR) inhibitor with a Ki of 13.4 pM. Pralatrexate is a substrate for folylpolyglutamate synthetase with improved cellular uptake and retention. Pralatrexate has antitumor activities and has the potential for relapsed/refractory T-cell lymphoma treatment.
  • HY-10080
    Teglarinad chloride

    GMX1777; EB-1627

    		 NAMPT Cancer
    Teglarinad chloride (GMX1777) is a prodrug of GMX1778 (a nicotinamide phosphoribosyl transferase inhibitor). Teglarinad chloride exhibits antitumor activity in mice can be attributed to inhibition of NAMPT. Teglarinad chloride also enhances radiation efficacy, mediated by interference with DNA repair and antiangiogenesis.
  • HY-101030A
    MBM-17S

    		Apoptosis Cancer
    MBM-17S is a potent NIMA-related kinase 2 (Nek2) inhibitor, with an IC50 of 3 nM. MBM-17S effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis. MBM-17S shows antitumor activities, and no obvious toxicity to mice.
  • HY-12803
    Fulvene-5

    		NADPH Oxidase Reactive Oxygen Species Cancer
    Fulvene-5 is a potent NADPH oxidase 4 (NOX4) inhibitor with antioxidant properties. Fulvene-5 is a reactive oxygen species (ROS) modifying agent and a potent radioprotector. Fulvene-5 has antitumor activity.
  • HY-13563
    Batabulin

    T138067

    		 Microtubule/Tubulin Apoptosis Cancer
    Batabulin (T138067) is an antitumor agent, which binds covalently and selectively to a subset of the β-tubulin isotypes, thereby disrupting microtubule polymerization. Batabulin affects cell morphology and leads to cell-cycle arrest ultimately induces apoptotic cell death.
  • HY-13563A
    Batabulin sodium

    T138067 sodium

    		 Microtubule/Tubulin Apoptosis Cancer
    Batabulin sodium (T138067 sodium) is an antitumor agent, which binds covalently and selectively to a subset of the β-tubulin isotypes, thereby disrupting microtubule polymerization. Batabulin sodium affects cell morphology and leads to cell-cycle arrest ultimately induces apoptotic cell death.
  • HY-134673
    UZH1

    		Apoptosis Cancer
    UZH1 is a racemate of UZH1a and UZH1b. UZH1a is a potent and selective METTL3 inhibitor, with an IC50 of 280 nM. UZH1b (IC50=28 µM) is essentially inactive. UZH1 can be used for epitranscriptomic modulation of cellular processes. UZH1 has antitumor activity. UZH1 also can be used as a chemical probe for studying METTL3.
  • HY-B0723S
    Ospemifene D4

    FC-1271a D4

    		 Estrogen Receptor/ERR Cancer
    Ospemifene D4 (FC-1271a D4) is a deuterium labeled Ospemifene. Ospemifene is a selective and orally active estrogen receptor modulator for the prevention of osteoporosis with IC50 values of 827 nM and 1633 nM for estrogen receptor α (ERα) and ERβ, respectively. Ospemifene has bone-sparing, antitumor, and cholesterol-lowering effects.
  • HY-N6036
    Ganoderic acid F

    		Others Cancer
    Ganoderic acid F is a ganoderic acid. Ganoderic acid F exhibits antitumor and antimetastatic activities through inhibition of angiogenesis and alteration of proteins involving cell proliferation and/or cell death, carcinogenesis, oxidative stress, calcium signaling, and endoplasmic reticulum stress.
  • HY-19356A
    Didesmethylrocaglamide

    		Eukaryotic Initiation Factor (eIF) Apoptosis Cancer
    Didesmethylrocaglamide, a derivative of Rocaglamide, is a potent eukaryotic initiation factor 4A (eIF4A) inhibitor. Didesmethylrocaglamide has potent growth-inhibitory activity with an IC50 of 5 nM. Didesmethylrocaglamide suppresses multiple growth-promoting signaling pathways and induces apoptosis in tumor cells. Antitumor activity.
  • HY-135299
    CH6953755

    		Src Cancer
    CH6953755 is a potent, orally active and selective YES1 kinase (a member of the SRC family) inhibitor with an IC50 of 1.8 nM. CH6953755 inhibits YES1 kinase, leading to antitumor activity against YES1 Gene -amplified cancers in vitro and in vivo.
  • HY-100450
    BML-111

    		Angiotensin-converting Enzyme (ACE) Cancer Inflammation/Immunology Cardiovascular Disease
    BML-111, a lipoxin A4 analog, is a lipoxin A4 receptor agonist. BML-111 represses the activity of angiotensin converting enzyme (ACE) and increases the activity of angiotensinconverting enzyme 2 (ACE2). BML-111 has antiangiogenic, antitumor and anti-inflammatory properties.
  • HY-100912
    W-7 hydrochloride

    		CaMK Phosphodiesterase (PDE) Myosin Apoptosis Cancer
    W-7 hydrochloride is a selective calmodulin antagonist. W-7 hydrochloride inhibits the Ca 2+-calmodulin-dependent phosphodiesterase and myosin light chain kinase with IC50 values of 28 μM and 51 µM, respectively. W-7 hydrochloride induces apoptosis and has antitumor activity.
  • HY-B0421
    Mycophenolic acid

    Mycophenolate

    		 Apoptosis Bacterial Fungal Endogenous Metabolite Antibiotic Cancer Infection Inflammation/Immunology
    Mycophenolic acid is a potent uncompetitive inosine monophosphate dehydrogenase (IMPDH) inhibitor with an EC50 of 0.24 µM. Mycophenolic acid demonstrates antiviral effects against a wide range of RNA viruses including influenza. Mycophenolic acid is an immunosuppressive agent. Antiangiogenic and antitumor effects.
  • HY-P1791
    Lactoferrin (17-41)

    Lactoferricin B; Lfcin B

    		 Bacterial Fungal Apoptosis Cancer Infection
    Lactoferrin 17-41 (Lactoferricin B), a peptide corresponding to residues 17-41 of bovine lactoferrin, has antimicrobial activity against a wide range of microorganisms, including Gram-positive and Gramnegative bacteria, viruses, protozoa, and fungi. Lactoferrin 17-41 has antitumor activities.
  • HY-P1791B
    Lactoferrin (17-41) (acetate)

    Lactoferricin B acetate; Lfcin B acetate

    		 Bacterial Fungal Apoptosis Cancer Infection
    Lactoferrin 17-41 (Lactoferricin B) acetate, a peptide corresponding to residues 17-41 of bovine lactoferrin, has antimicrobial activity against a wide range of microorganisms, including Gram-positive and Gramnegative bacteria, viruses, protozoa, and fungi. Lactoferrin 17-41 acetate has antitumor activities.
  • HY-131454
    SR-717

    		STING Cancer Inflammation/Immunology
    SR-717 is a non-nucleotide STING agonist with EC50s of 2.1 μM and 2.2 μM in ISG-THP1 (WT) and ISG-THP1 cGAS KO (cGAS KO) cell lines, respectively. SR-717 is a stable cyclic guanosine monophosphate-adenosine monophosphate (cGAMP) mimetic. Antitumor activity.
  • HY-19745
    BMS-202

    		PD-1/PD-L1 Apoptosis Cancer
    BMS-202 is a potent and nonpeptidic PD-1/PD-L1 complex inhibitor with an IC50 of 18 nM and a KD of 8 μM. BMS-202 binds to PD-L1 and blocks human PD-1/PD-L1 interaction. BMS-202 has antitumor activity.
  • HY-16399
    Pladienolide B

    		Apoptosis Cancer
    Pladienolide B is a potent cancer cell growth inhibitor that targets the SF3B1 subunit of the spliceosome. Pladienolide B exerts antitumor activities mediated through the inhibition of pre-mRNA splicing. Pladienolide B induces apoptosis.
  • HY-100507
    Avadomide

    CC 122

    		 E1/E2/E3 Enzyme Apoptosis Cancer Inflammation/Immunology
    Avadomide (CC 122) is an orally active cereblon modulator. Avadomide modulates cereblon E3 ligase activity and induces apoptosis of diffuse large B-cell lymphoma (DLBCL) cell lines. Avadomide exhibits potent antitumor and immunomodulatory activities.
  • HY-15779
    K145

    		SphK Apoptosis Cancer
    K145 is a selective, substrate-competitive and orally active SphK2 inhibitor with an IC50 of 4.3 µM and a Ki of 6.4 µM. K145 is inactive against SphK1 and other protein kinases. K145 induces cell apoptosis and has potently antitumor activity.
  • HY-15779A
    K145 hydrochloride

    		SphK Apoptosis Cancer
    K145 hydrochloride is a selective, substrate-competitive and orally active SphK2 inhibitor with an IC50 of 4.3 µM and a Ki of 6.4 µM. K145 hydrochloride is inactive against SphK1 and other protein kinases. K145 hydrochloride induces cell apoptosis and has potently antitumor activity.
  • HY-N2150
    Psammaplin A

    		HDAC DNA Methyltransferase DNA/RNA Synthesis Bacterial Cancer Infection
    Psammaplin A, a marine metabolite, is a potent inhibitor of HDAC and DNA methyltransferases. Psammaplin A ia a highly potent and selective DAC1 inhibitor with an IC50 of 0.9 nM. Psammaplin A possess the antimicrobial effect on the Gram-positive bacteria and inhibits DNA synthesis and DNA gyrase activity. Antitumor Activity.
  • HY-131902
    MLT-231

    		MALT1 Cancer
    MLT-231 is a potent, highly selective allosteric MALT1 Inhibitor with an IC50 of 9 nM. MLT-231 specifically prevents endogenous BCL10 cleavage with IC50 of 160 nM. MLT-231 shows antitumor activity in an ABC-DLBCL type xenograft model in mouse.
  • 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-15196
    TAK-285

    		EGFR Cancer
    TAK-285 is a potent, selective, ATP-competitive and orally active HER2 and EGFR(HER1) inhibitor with IC50 of 17 nM and 23 nM, respectively. TAK-285 is >10-fold selectivity for HER1/2 than HER4, and less potent to MEK1/5, c-Met, Aurora B, Lck, CSK etc. TAK-285 has effective antitumor activity. TAK-285 can cross the blood-brain barrier (BBB).
  • HY-131454A
    SR-717 free acid

    		STING Cancer Inflammation/Immunology
    SR-717 free acid is a non-nucleotide STING agonist with EC50s of 2.1 μM and 2.2 μM in ISG-THP1 (WT) and ISG-THP1 cGAS KO (cGAS KO) cell lines, respectively. SR-717 free acid is a stable cyclic guanosine monophosphate-adenosine monophosphate (cGAMP) mimetic. Antitumor activity.
  • 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-P9976
    Isatuximab

    		Apoptosis Cancer
    Isatuximab is a monoclonal antibody targeting the transmembrane receptor and ectoenzyme CD38, a protein highly expressed on hematological malignant cells, including those in multiple myeloma (MM). Isatuximab has antitumor activity via multiple biological mechanisms, including antibody-dependent cellular-mediated cytotoxicity, complement-dependent cytotoxicity, antibody-dependent cellular phagocytosis, and direct induction of apoptosis without crosslinking. Isatuximab also directly inhibits CD38 ectoenzyme activity, which is implicated in many cellular functions.
  • HY-138565
    K-975

    		YAP Cancer
    K-975 is a potent, selective and orally active TEAD inhibitor, with a strong inhibitory effect against protein-protein interactions between YAP1/TAZ and TEAD. K-975 covalently binds to Cys359 located in the palmitate-binding pocket of TEAD via an acrylamide structure. K-975 exhibits antitumor activity on malignant pleural mesothelioma.
  • HY-13680
    Meisoindigo

    Dian III; N-Methylisoindigotin; Natura-α

    		 Apoptosis Cancer
    Meisoindigo (Dian III), a derivative of Indirubin (HY-N0117), halts the cell cycle at the G0/G1 phase and induces apoptosis in primary acute myeloid leukemia (AML) cells. Meisoindigo exhibits high antitumor activity.
  • HY-18619
    YL-109

    		Aryl Hydrocarbon Receptor Cancer
    YL-109 is an antitumor agent that can induce carboxyl terminus of Hsp70-interacting protein (CHIP) expression through aryl hydrocarbon receptor (AhR) signaling. YL-109 has ability to inhibit breast cancer cell growth and invasiveness.
  • HY-133017
    Amcenestrant

    SAR439859

    		 Estrogen Receptor/ERR Cancer
    SAR439859 (compound 43d) is an orally active, nonsteroidal and selective estrogen receptor degrader (SERD). SAR439859 is a potent ER antagonist and has ER degrading activity with an EC50 of 0.2 nM for ERα degradation. SAR439859 demonstrates robust antitumor efficacy and limited cross-resistance in ER + breast cancer.
  • HY-131906
    JAK2-IN-7

    		JAK FLT3 Cancer
    JAK2-IN-7 is a selective JAK2 inhibitor with IC50s of 3, 11.7, and 41 nM for JAK2, SET-2, and Ba/F3 V617F cells, respectively. JAK2-IN-7 possesses >14-fold selectivity over JAK1, JAK3, FLT3. JAK2-IN-7 stimulates cell cycle arrest in the G0/G1 phase and induces tumor cellapoptosis. Antitumor activities.
  • HY-111790
    M3258

    		Proteasome Apoptosis Cancer
    M3258 is an orally bioavailable, potent, reversible and highly selective immunoproteasome subunit LMP7 (β5i) inhibitor. M3258 exerts high biochemical (IC50=3.6 nM) and cellular (IC50=3.4 nM) potency against the LMP7 subunit. M3258 shows strong antitumor efficacy in multiple myeloma xenograft models. M3258 leads to a significant and prolonged suppression of tumor LMP7 activity and ubiquitinated protein turnover and the induction of apoptosis in multiple myeloma cells.
  • HY-119257
    ABT-100

    		Farnesyl Transferase Apoptosis Cancer
    ABT-100 is a potent, highly selective and orally active farnesyltransferase inhibitor. ABT-100 inhibits cell proliferation (IC50s of 2.2 nM, 3.8 nM, 5.9 nM, 6.9 nM, 9.2 nM, 70 nM and 818 nM for EJ-1, DLD-1, MDA-MB-231, HCT-116, MiaPaCa-2, PC-3, and DU-145 cells, respectively), increases apoptosis and decreases angiogenesis. ABT-100 possesses broad-spectrum antitumor activity.
  • HY-13302
    CP-547632

    		VEGFR FGFR Cancer
    CP-547632 is an orally active, ATP-competitive and potent VEGFR-2 and FGF kinases inhibitor with IC50s of 11 nM and 9 nM, respectively. CP-547632 is selective for VEGFR2 and bFGF over EGFR, PDGFRβ, and related tyrosine kinases (TKs). CP-547632 has antitumor efficacy.
  • HY-13302B
    CP-547632 hydrochloride

    		VEGFR FGFR Cancer
    CP-547632 hydrochloride is an orally active, ATP-competitive and potent VEGFR-2 and FGF kinases inhibitor with IC50s of 11 nM and 9 nM, respectively. CP-547632 hydrochloride is selective for VEGFR2 and bFGF over EGFR, PDGFRβ, and related tyrosine kinases (TKs). CP-547632 hydrochloride has antitumor efficacy.
  • HY-101029
    MBM-55

    		Apoptosis Cancer
    MBM-55 is a potent NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 1 nM. MBM-55 shows a 20-fold or greater selectivity in most kinases with the exception of RSK1 (IC50=5.4 nM) and DYRK1a (IC50=6.5 nM). MBM-55 effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis. MBM-55 shows antitumor activities, and no obvious toxicity to mice.
  • HY-13811
    NSC697923

    		E1/E2/E3 Enzyme Apoptosis Cancer
    NSC697923 is a potent UBE2N (ubiquitin-conjugating enzyme E2 N, Ubc13) inhibitor. NSC697923 induces neuroblastoma (NB) cell death via promoting nuclear importation of p53 in p53 wild-type NB cells. NSC697923 also induces cell death in p53 mutant NB cells by activation of JNK-mediated apoptotic pathway. NSC697923 inhibits DNA damage and NF-κB signaling. Antitumor activity.
  • HY-W058849
    MT 63-78

    		AMPK mTOR Apoptosis Cancer
    MT 63-78 is a specific and potent direct AMPK activator with an EC50 of 25 μM. MT 63–78 also induces cell mitotic arrest and apoptosis. MT 63-78 blocks prostate cancer growth by inhibiting the lipogenesis and mTORC1 pathways. MT 63-78 has antitumor effects.
  • HY-123587
    PR-924

    		Proteasome Apoptosis Cancer
    PR-924 is a selective tripeptide epoxyketone immunoproteasome subunit LMP-7 inhibitor with an IC50 of 22 nM. PR-924 covalently modifies proteasomal N-terminal threonine active sites. PR-924 inhibits growth and triggers apoptosis in multiple myeloma (MM) cells. PR-924 has antitumor activities.
  • HY-124828
    CMLD-2

    		Apoptosis Cancer
    CMLD-2, an inhibitor of HuR-ARE interaction, competitively binds HuR protein disrupting its interaction with adenine-uridine rich elements (ARE)-containing mRNAs (Ki=350 nM). CMLD-2 induces apoptosis exhibits antitumor activity in different cancer cells as colon, pancreatic, thyroid and lung cancer cell lines. Hu antigen R (HuR) is an RNA binding protein, can regulate target mRNAs stability and translation.
  • HY-B0537A
    Pentamidine dihydrochloride

    MP-601205 dihydrochloride

    		 Parasite Fungal Phosphatase Bacterial Antibiotic Cancer Infection
    Pentamidine dihydrochloride (MP-601205 dihydrochloride) is an antimicrobial agent and interferes with DNA biosynthetics. Pentamidine dihydrochloride inhibits parasite Leishmania infantum with an IC50 of 2.5 μM. Pentamidine dihydrochloride is a potent and selective protein tyrosine phosphatases (PTPases) and phosphatase of regenerating liver (PRL) inhibitor. Pentamidine dihydrochloride has the potential for Gambian trypanosomiasis, antimony-resistant leishmaniasis, and Pneumocystis carinii pneumonia treatment. Antitumor and antibacterial activities.
  • HY-B0537
    Pentamidine

    MP-601205

    		 Parasite Fungal Phosphatase Bacterial Antibiotic Cancer Infection
    Pentamidine (MP-601205) is an antimicrobial agent and interferes with DNA biosynthetics. Pentamidine inhibits parasite Leishmania infantum with an IC50 of 2.5 μM. Pentamidine is a potent and selective protein tyrosine phosphatases (PTPases) and phosphatase of regenerating liver (PRL) inhibitor. Pentamidine has the potential for Gambian trypanosomiasis, antimony-resistant leishmaniasis, and Pneumocystis carinii pneumonia treatment. Antitumor and antibacterial activities.
  • HY-13302C
    CP-547632 TFA

    		VEGFR FGFR Cancer
    CP-547632 TFA is an orally active, ATP-competitive and potent VEGFR-2 and FGF kinases inhibitor with IC50s of 11 nM and 9 nM, respectively. CP-547632 TFA is selective for VEGFR2 and bFGF over EGFR, PDGFRβ, and related tyrosine kinases (TKs). CP-547632 TFA has antitumor efficacy.
  • HY-50936
    Trabectedin

    Ecteinascidin 743; ET-743

    		 Reactive Oxygen Species Apoptosis Cancer Inflammation/Immunology
    Trabectedin (Ecteinascidin 743; ET-743) is a tetrahydroisoquinoline alkaloid with potent antitumor activity. Trabectedin binds to the minor groove of DNA, blocks transcription of stress-induced proteins, induces DNA backbone cleavage and cancer cells apoptosis, and increases the generation of ROS in MCF-7 and MDA-MB-453 cells. Trabectedin has the potential for soft tissue sarcoma and ovarian cancer research.
  • HY-101029A
    MBM-55S

    		Ribosomal S6 Kinase (RSK) DYRK Apoptosis Cancer
    MBM-55S is a potent NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 1 nM. MBM-55S shows a 20-fold or greater selectivity in most kinases with the exception of RSK1 (IC50=5.4 nM) and DYRK1a (IC50=6.5 nM). MBM-55S effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis. MBM-55S shows antitumor activities, and no obvious toxicity to mice.
  • 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-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-17389
    Genipin

    (+)-Genipin

    		 Autophagy Cancer Metabolic Disease Inflammation/Immunology Neurological Disease
    Genipin ((+)-Genipin) is a natural crosslinking reagent derived from Gardenia jasminoides Ellis fruits. Genipin inhibits UCP2 (uncoupling protein 2) in cells. Genipin has a variety of bioactivities, including modulation on proteins, antitumor, anti-inflammation, immunosuppression, antithrombosis, and protection of hippocampal neurons. Genipin also can be used for type 2 diabetes research.
  • HY-100195
    SAR-020106

    		Checkpoint Kinase (Chk) Cancer
    SAR-020106 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC50 of 13.3 nM for human CHK1. SAR-020106 shows excellent selectivity over CHK2. SAR-020106 significantly enhances the cell killing of Gemcitabine and SN38 by 3- to 29-fold in several colon tumor lines and in a p53-dependent fashion. SAR-020106 can enhance antitumor activity with selected anticancer drugs.
  • HY-B0537B
    Pentamidine isethionate

    MP-601205 isethionate

    		 Parasite Fungal Phosphatase Bacterial Antibiotic Infection Cancer
    Pentamidine isethionate (MP-601205 isethionate) is an antimicrobial agent and interferes with DNA biosynthetics. Pentamidine isethionate inhibits parasite Leishmania infantum with an IC50 of 2.5 μM. Pentamidine isethionate is a potent and selective protein tyrosine phosphatases (PTPases) and phosphatase of regenerating liver (PRL) inhibitor. Pentamidine isethionate has the potential for Gambian trypanosomiasis, antimony-resistant leishmaniasis, and Pneumocystis carinii pneumonia treatment. Antitumor and antibacterial activities.
  • 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-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-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-17499
    EGFR-IN-12

    		EGFR Apoptosis Cancer
    EGFR-IN-12 is a 4,6-disubstituted pyrimidine and is a potent, ATP-competitive, irreversible and highly selective EGFR inhibitor with an IC50of 21 nM. EGFR-IN-12 also inhibits mutant EGFR L858R and EGFR L861Q with IC50s of 63 nM and 4 nM, respectively. EGFR-IN-12 displays strong selectivity for EGFR over HER4 (IC50 = 7640 nM) and a panel of 55 other kinases. EGFR-IN-12 induces cells apoptosis and has antitumor activity.
  • HY-12895
    SKI V

    		SphK PI3K Apoptosis Cancer
    SKI V is a noncompetitive and potent non-lipid sphingosine kinase (SPHK; SK) inhibitor with an IC50 of 2 μM for GST-hSK. SKI V potently inhibits PI3K with an IC50 of 6 μM for hPI3k. SKI V decreases formation of the mitogenic second messenger sphingosine-1-phosphate (S1P). SKI V induces apoptosis and has antitumor activity.
  • HY-121496
    3M-011

    		Toll-like Receptor (TLR) Influenza Virus Cancer Infection Inflammation/Immunology
    3M-011 is a potent dual toll-like receptor TLR7/8 agonist and a cytokine inducer. 3M-011 significantly inhibits H3N2 influenza viral replication in the nasal cavity. 3M-011 is also a potent adjuvant to radiotherapy that induces local and profound systemic immune responses during radiotherapy. 3M-011 strongly has antitumor action.
  • HY-135887
    ZX-29

    		ALK Apoptosis Autophagy Cancer
    ZX-29 is a potent and selective ALK inhibitor with an IC50 of 2.1 nM, 1.3 nM and 3.9 nM for ALK, ALK L1196M and ALK G1202R mutations, respectively. ZX-29 is inactive against EGFR. ZX-29 induces apoptosis by inducing endoplasmic reticulum (ER) stress and overcomes cell resistance caused by an ALK mutation. ZX-29 also induces protective autophagy and has antitumor effect.
  • HY-N7503
    Psoralenoside

    		Histamine Receptor CaMK Calcium Channel Cancer Infection Metabolic Disease
    Psoralenoside is a benzofuran glycoside from Psoralea corylifolia. Psoralenoside exhibits high binding affinities against histaminergic H1, calmodulin, and voltage-gated L-type calcium channels (E-value≥-6.5 Kcal/mol). Psoralenoside shows estrogen-like activity, osteoblastic proliferation accelerating activity, antitumor effects and antibacterial activity.
  • 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-108632
    BYK204165

    		PARP Cancer
    BYK204165 is a potent and selective PARP1 inhibitor. BYK204165 inhibits cell-free recombinant human PARP-1 (hPARP-1) with a pIC50 of 7.35 (pKi=7.05), and murine PARP-2 (mPARP-2) with a pIC50 of 5.38, respectively. BYK204165 displays 100-fold selectivity for PARP-1.
  • 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-135960
    BO-264

    		FGFR Apoptosis Cancer
    BO-264 is a highly potent and orally active transforming acidic coiled-coil 3 (TACC3) inhibitor with an IC50 of 188 nM and a Kd of 1.5 nM. BO-264 specifically blocks the function of FGFR3-TACC3 fusion protein. BO-264 induces spindle assembly checkpoint (SAC)-dependent mitotic arrest, DNA damage and apoptosis. BO-264 has broad-spectrum antitumor activity.
  • HY-119906
    Conglobatin

    FW-04-806

    		 HSP Apoptosis Cancer
    Conglobatin (FW-04-806), a macrolide dilactone, is isolated from the culture of Streptomyces conglobatus. Conglobatin is an orally active Hsp90 inhibitor. Conglobatin can bind to the N-terminal domain of Hsp90 and disrupt Hsp90-Cdc37 complex formation. Conglobatin induces apoptosis in human breast cancer cells and esophageal squamous cell carcinoma cells, and exhibits antitumor activity in vivo.
  • HY-N0891
    Tubeimoside II

    Tubeimoside-B

    		 Others Cancer
    Tubeimoside II(Tubeimoside-B) is a natural analogue of oleanane type of triterpenoid saponin; show anti-inflammatory, antitumor, and antitumor-promoting effects.
  • HY-125269
    TED-347

    		YAP Cancer
    TED-347 is a potent, irreversible, covalent and allosteric inhibitor at YAP-TEAD protein-protein interaction with an EC50 of 5.9 μM for TEAD4⋅Yap1 protein-protein interaction. TED-347 specifically and covalently bonds with Cys-367 within the central pocket of TEAD4 with a Ki of 10.3 μM. TED-347 blocks TEAD transcriptional activity and has antitumor activity.
  • HY-17576
    Satraplatin

    BMS182751; BMY45594; JM216

    		 DNA Alkylator/Crosslinker Cancer
    Satraplatin is an alkylating agent, with potent antitumor effect.
  • HY-103693
    NAZ2329

    		Phosphatase Cancer
    NAZ2329, the first cell-permeable inhibitor of R5 subfamily of receptor-type protein tyrosine phosphatases (RPTPs), allosterically and preferentially inhibits PTPRZ (IC50=7.5 µM for hPTPRZ1) and PTPRG (IC50=4.8 µM for hPTPRG) over other PTPs. NAZ2329 binds to the active D1 domain and more potently inhibits PTPRZ-D1 fragment (IC50 of 1.1 µM) than the whole intracellular (D1 + D2) fragment (IC50 of 7.5 µM). NAZ2329 can effectively inhibit tumor growth of the glioblastoma cells and suppress stem cell-like properties.
  • HY-17574
    Thio-TEPA

    		DNA Alkylator/Crosslinker Bacterial Antibiotic Cancer Infection
    Thio-TEPA is a DNA alkylating agent, with antitumor activity.
  • HY-12202
    MEK inhibitor

    		MEK Cancer
    MEK inhibitor is a potent MEK inhibitor with antitumor potency.
  • HY-19791
    N-Acetyl-Calicheamicin

    N-Acetyl-Calicheamicin γ; N-Acetyl-γ-calicheamicin

    		 Bacterial Cancer Infection
    N-Acetyl-Calicheamicin is a potent enediyne antitumor antibiotic.
  • HY-N0865
    Ingenol

    (-)-Ingenol

    		 PKC Cancer
    Ingenol is a PKC activator, with a Ki of 30 μM, with antitumor activity.
  • HY-14821
    Namitecan

    ST-1968

    		 Topoisomerase Cancer
    Namitecan is a potent topoisomerase I inhibitor, with antitumor property.
  • HY-N0156
    Oleanolic Acid

    Oleanic acid; Caryophyllin

    		 Autophagy Endogenous Metabolite HIV Cancer
    Oleanolic acid (Caryophyllin) is a natural compound from plants with anti-tumor activities.
  • HY-N1366
    Herniarin

    7-Methoxycoumarin; Methyl umbelliferyl ether

    		 Others Cancer
    Herniarin is a natural coumarin occurs in some flowering plants, with antitumor effect.
  • HY-13727
    Pixantrone

    BBR 2778

    		 Topoisomerase Cancer
    Pixantrone is a topoisomerase II inhibitor and DNA intercalator, with anti-tumor activity.
  • HY-13669
    Lomustine

    CCNU; NSC 79037

    		 DNA Alkylator/Crosslinker Autophagy Apoptosis Cancer
    Lomustine (CCNU; NSC 79037) is a DNA alkylating agent, with antitumor activity.
  • HY-101604
    Atrimustine

    Bestrabucil; KM2210

    		 Others Cancer
    Atrimustine is a conjugate of chlorambucil and β-estradiol benzoate with the antitumor activity.
  • HY-14798
    Palifosfamide

    Isophosphoramide mustard; IPM; ZIO-201

    		 DNA Alkylator/Crosslinker Drug Metabolite Cancer
    Palifosfamide is a novel DNA alkylator and the active metabolite of ifosfamide, with antitumor activity.
  • HY-13585
    Carmustine

    		DNA Alkylator/Crosslinker Cancer
    Carmustine is an antitumor chemotherapeutic agent, which works by akylating DNA and RNA.
  • HY-128920
    Phortress free base

    		Cytochrome P450 Cancer
    Phortress free base (NSC 710305) is a P450 CYP1A1-activated antitumor prodrug with antitumor activity. Phortress free base leads to DNA damage and cell cycle arrest.
  • HY-17411
    Limonin

    Limonoic acid 3,19:16,17 dilactone

    		 HIV Apoptosis Endogenous Metabolite Infection Cancer
    Limonin is a triterpenoid enriched in citrus fruits, which has antivirus and antitumor ability.
  • HY-15721
    FH535

    		PPAR Wnt β-catenin Cancer
    FH535 is an inhibitor of Wnt/β-catenin and PPAR, with anti-tumor activities.
  • HY-32364
    3-arylisoquinolinamine derivative

    		Others Cancer
    3-arylisoquinolinamine derivative is a 3-arylisoquinolinamine derivative with antitumor activity.
  • HY-16509
    UNBS5162

    		CXCR Autophagy Cancer Endocrinology
    UNBS5162 is a pan-antagonist of CXCL chemokine expression, with anti-tumor activity.
  • HY-13644A
    Gusperimus trihydrochloride

    Spanidin; NKT-01; BMS181173

    		 Others Cancer Inflammation/Immunology
    Gusperimus trihydrochloride (Spanidin) is a derivative of the antitumor antibiotic spergualin with immunosuppressant activity.
  • HY-100875
    Bisantrene

    CL216942

    		 Topoisomerase Cancer
    Bisantrene is a highly effective antitumor drug, targets eukaryotic type II topoisomerases.
  • HY-B1960
    Canthaxanthin

    E 161g; all-trans-Canthaxanthin

    		 Reactive Oxygen Species Cancer Inflammation/Immunology
    Canthaxanthin is a red-orange carotenoid with various biological activities, such as antioxidant, antitumor properties.
  • HY-U00337
    Datelliptium chloride

    		DNA/RNA Synthesis Cancer
    Datelliptium chloride is a DNA-intercalating agent derived from ellipticine, with anti-tumor activities.
  • HY-13727A
    Pixantrone dimaleate

    BBR 2778 dimaleate

    		 Topoisomerase Cancer
    Pixantrone dimaleate is a topoisomerase II inhibitor and DNA intercalator, with anti-tumor activity.
  • HY-10940
    Pifithrin-μ

    PFTμ; 2-Phenylethynesulfonamide

    		 MDM-2/p53 HSP Autophagy Cancer Neurological Disease
    Pifithrin-μ is an inhibitor of p53 and HSP70, with antitumor and neuroprotective activity.
  • HY-N4304
    Gambogellic acid

    		Others Cancer
    Gambogellic acid is an xanthone isolated from the processed gamboge, with antitumor activity.
  • HY-107769
    Duocarmycin TM

    		ADC Cytotoxin DNA Alkylator/Crosslinker Antibiotic Cancer
    Duocarmycin TM is an exceptionally potent antitumor antibiotic. Duocarmycin TM is a DNA alkylator.
  • HY-108359
    Alsterpaullone

    9-Nitropaullone; NSC 705701

    		 CDK GSK-3 Apoptosis Cancer
    Alsterpaullone (9-Nitropaullone) is a potent CDK inhibitor, with IC50s of 35 nM, 15 nM, 200 nM and 40 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E and CDK5/p35, respectively. Alsterpaullone also competes with ATP for binding to GSK-3alpha/GSK-3beta with IC50s of both 4 nM. Alsterpaullone has antitumor activity, and possesses potential for the study in neurodegenerative and proliferative disorders. Alsterpaullone induces apoptosis in leukemia cell line.
  • HY-112570
    CC-90003

    		ERK Cancer
    CC-90003 is an irreversible and selective inhibitor of ERK 1/2 with antitumor activity.
  • HY-10249A
    AKT Kinase Inhibitor

    		Akt Cancer
    AKT Kinase Inhibitor is an Akt kinase inhibitor with anti-tumor activity.
  • HY-N0351
    p-Coumaric acid

    trans-4-Hydroxycinnamic acid

    		 Endogenous Metabolite Cancer
    p-Coumaric acid is the abundant isomer of cinnamic acid which has antitumor and anti-mutagenic activities.
  • HY-N0235
    Bakuchiol

    (S)-(+)-Bakuchiol

    		 p38 MAPK Autophagy Cancer
    Bakuchiol is a phytoestrogen isolated from the seeds of Psoralea corylifolia L; has anti-tumor effects.
  • HY-N4257
    Yadanzioside A

    		Others Cancer
    Yadanziolide A, a quassinoid glycoside from Brucea javanica, has antitumor activity.
  • HY-16568
    Irinotecan hydrochloride trihydrate

    (+)-Irinotecan hydrochloride trihydrate; CPT-11 hydrochloride trihydrate

    		 Topoisomerase Autophagy Cancer
    Irinotecan hydrochloride trihydrate ((+)-Irinotecan hydrochloride trihydrate) is a topoisomerase I inhibitor with antitumor activity.
  • HY-113450
    10Z-Nonadecenoic acid

    		Endogenous Metabolite Metabolic Disease Cancer
    10Z-Nonadecenoic acid is a kind of long-chain fatty acid with anti-tumor activity.
  • HY-16513
    VAL-083

    Dianhydrodulcitol; Dianhydrogalactitol

    		 DNA Alkylator/Crosslinker Cancer
    VAL-083 is an alkylating agent that creates N7 methylation on DNA, with antitumor activity.
  • HY-14947
    Balamapimod

    MKI 833

    		 MEK Cancer
    Balamapimod (MKI 833) is a reversible Ras/Raf/MEK inhibitor with potential anti-tumor activity.
  • HY-15456
    NVP-BVU972

    		c-Met/HGFR Cancer
    NVP-BVU972 is a selective and potent Met inhibitor (IC50 = 14 nM). Antitumor agents.
  • HY-N1944
    Nerolidol

    		Bacterial Fungal Parasite Endogenous Metabolite Cancer Infection
    Nerolidol is a natural membrane-active sesquiterpene, with antitumor, antibacterial, antifungal and antiparasitic activity.
  • HY-16496
    Thiarabine

    OSI-7836

    		 DNA/RNA Synthesis Cancer Inflammation/Immunology
    Thiarabine (OSI-7836) shows potent anti-tumor activity and inhibition of DNA synthesis.
  • HY-100453
    HO-3867

    		STAT Apoptosis Cancer
    HO-3867 is a selective and potent STAT3 inhibitor and shows good antitumor activity.
  • HY-N8197
    Epigambogic acid

    		Others Cancer
    Epigambogic acid is a natural anti-tumor, antitussive, expectorant and anti-inflammatory compound.
  • HY-U00379
    LM985

    		Others Cancer
    LM985 is one of a series of compounds based on the flavone ring structure, with anti-tumor activities.
  • HY-100033
    NSC5844

    RE-640

    		 Parasite Cancer Infection
    NSC5844 (RE-640) is a 4-aminoquinoline derivative, with antitumor and antimalarial activity.
  • HY-N0123
    Aloin

    Aloin-A; Barbaloin-A

    		 Others Cancer
    Aloin(Aloin-A; Barbaloin-A) is a natural antitumor anthraquinone glycoside with iron chelating and non-atherogenic activities.
  • HY-N4124
    Poricoic acid B

    		Others Cancer
    Poricoic acid B, isolated from Poria cocos, possesses anti-tumor activity.
  • HY-N9400
    Lucidenic acid F

    		Others Cancer Inflammation/Immunology
    Lucidenic acid F, a natural triterpenoid, possesses anti-Inflammatory and anti-tumor activity.
  • HY-111411
    IZCZ-3

    		c-Myc Autophagy Cancer
    IZCZ-3 is a potent c-MYC transcription inhibitor with antitumor activity.
  • HY-108986
    JFD00244

    		Sirtuin Cancer
    JFD00244 is a sirtuin 2 (SIRT2) inhibitor. Anti-tumor effect.
  • HY-N6988
    Cimigenol

    		Others Cancer
    Cimigenol is an active compound isolated from Cimicifuga, with potent anti-tumor activity.
  • HY-117244
    AZD7507

    		c-Fms Cancer
    AZD7507 is a potent and orally active CSF-1R inhibitor, with antitumor activity.
  • HY-N0184
    Glycyrrhizic acid

    Glycyrrhizin

    		 Virus Protease Cancer Metabolic Disease
    Glycyrrhizic acid is a triterpenoid saponinl, acting as a direct HMGB1 antagonist, with anti-tumor, anti-diabetic activities.
  • HY-111783
    AZD-7648

    		DNA-PK Cancer
    AZD-7648 is a potent and selective DNA-PK inhibitor. Anti-tumor activity.
  • HY-N8038
    Isoanthricin

    (Rac)-Deoxypodophyllotoxin

    		 Others Others
    Isoanthricin ((Rac)-Deoxypodophyllotoxin) is the racemate of Deoxypodophyllotoxin. Deoxypodophyllotoxin is a potent antitumor and anti-inflammatory agent.
  • HY-N2596
    Isoscabertopin

    		Others Cancer Inflammation/Immunology
    Isoscabertopin is a sesquiterpene lactone isolated from Elephantopus scaber L and shows anti-tumor activities.
  • HY-14944
    Homoharringtonine

    Omacetaxine mepesuccinate; HHT

    		 STAT Cancer
    Homoharringtonine (Omacetaxine mepesuccinate;HHT) is a cytotoxic alkaloid with antitumor properties which acts by inhibiting translation elongation.
  • HY-124916
    Lycopsamine

    		Others Cancer
    Lycopsamine, a pyrrolizidine alkaloid, is a potential antitumor agent isolated from Eupatorium maculatum L..
  • HY-128937
    EC1454

    		Others Cancer
    EC1454 is an anti-tumor compound, extracted from US20170348376A1.
  • HY-N3125
    Osajin

    CID 95168; NSC 21565

    		 Apoptosis Cancer Metabolic Disease Inflammation/Immunology Cardiovascular Disease
    Osajin is the major bioactive isoflavone present in the fruit of Maclura pomifera with antitumor, antioxidant and anti-inflammatory activities.
  • HY-101275
    EMT inhibitor-1

    		Hippo (MST) TGF-beta/Smad Wnt Cancer
    EMT inhibitor-1 is an inhibitor of of Hippo, TGF-β, and Wnt signaling pathways with antitumor activities.
  • HY-B1436
    Nifuroxazide

    		STAT Bacterial Cancer Infection
    Nifuroxazide is an effective inhibitor of STAT3, also exerts potent anti-tumor and anti-metastasis activity.
  • HY-N9390
    Wilforlide B

    		Others Cancer
    Wilforlide B, a natural norditerpenoid, possesses anti-tumor activity in human cancer cells.
  • HY-10818
    LY309887

    		Antifolate Cancer
    LY309887 is a potent inhibitor of glycinamide ribonucleotide formyltransferase (GARFT), with a Ki of 6.5 nM, and has antitumor activity.
  • HY-N0189
    Aloe emodin

    Rhabarberone; 3-Hydroxymethylchrysazine

    		 Autophagy Cancer
    Aloe emodin is a hydroxyanthraquinone present in Aloe vera leaves, has a specific in vitro and in vivo antitumor activity.
  • HY-16212
    FR901464

    		Others Cancer
    FR901464 is a potent spliceosome inhibitor with prominent anti-tumor and anti-cancer effects.
  • HY-14846
    Litronesib

    LY2523355

    		 Kinesin Cancer
    Litronesib (LY2523355) is a selective mitosis-specific kinesin Eg5 inhibitor, with antitumor activity.
  • HY-16111
    BMS-214662

    		Farnesyl Transferase Cancer
    BMS-214662 is a potent and selective farnesyl transferase inhibitor with potent antitumor activity with an IC50 of 1.35 nM.
  • HY-N0706
    Gracillin

    		Others Cancer
    Gracillin is a kind of steroidal saponin isolated from the root bark of wild yam Dioscorea nipponica with antitumor agent.
  • HY-19994
    ML264

    		KLF Cancer
    ML264 is an antitumor agent that potently and selectively inhibits Krüppel-like factor five (KLF5) expression.
  • HY-N0370
    Bergapten

    5-Methoxypsoralen

    		 Cytochrome P450 Autophagy Cancer
    Bergapten is a natural anti-inflammatory and anti-tumor agent. Bergapten is inhibitory towards mouse and human CYP isoforms.
  • HY-17565
    Bleomycin sulfate

    		DNA/RNA Synthesis Antibiotic Cancer
    Bleomycin sulfate is a DNA synthesis inhibitor. Bleomycin hydrochloride is a DNA damaging agent. Bleomycin sulfate is an antitumor antibiotic.
  • HY-N6722
    Swainsonine

    Tridolgosir

    		 Bacterial Antibiotic Cancer Infection
    Swainsonine is an alkaloid isolated from Astragalus, acts as an inhibitor of α-mannosidase, with anti-tumor activity.
  • HY-128939
    EC0488

    		Antifolate Cancer
    EC0488 is used to synthesize EC0531 with folate receptor (FR)-specific and anti-tumor activities.
  • HY-N0428
    Obacunone

    		Apoptosis Cancer
    Obacunone, isolated from seeds of Marsh White grapefruit, exhibits anti-tumor activity by the induction of apoptosis.
  • HY-N0421
    Cinobufagin

    Cinobufagine

    		 Autophagy Apoptosis Cancer
    Cinobufagin, a kind of Chinese materia medica with antitumor effect, is widely used in clinical practice, especially in anti-liver cancer.
  • HY-N4255
    Resibufagin

    		Others Cancer
    Resibufagin is a kind of bufadienolide isolated from the venom of Bufo bufo gargarizans, has anti-tumor activities.
  • HY-N0140
    Ursolic acid

    Prunol; Urson; Malol

    		 Autophagy Endogenous Metabolite Cancer
    Ursolic acid (Prunol) is a natural pentacyclic triterpenoid carboxylic acid, exerts anti-tumor effects and is an effective compound for cancer prevention and therapy.
  • HY-N1318
    Salvigenin

    		Autophagy Cancer Inflammation/Immunology Neurological Disease
    Salvigenin is a natural polyphenolic compound, with neuroprotective effect. Salvigenin has antitumor cytotoxic and immunomodulatory properties.
  • HY-N6015
    Bacopasaponin C

    		Others Cancer
    Bacopasaponin C is an indigenous glycoside isolated from Bacopa monniera, with antitumor and anti-leishmanial activities.
  • HY-U00155
    NCI172112

    NSC172112; NSC268497

    		 Others Cancer
    NCI172112 is a classical bifunctional alkylating agent synthesized in an effort to develop antitumor agents effective against CNS tumors.
  • HY-70003
    Carboxypeptidase G2 (CPG2) Inhibitor

    CPG2 Inhibitor

    		 Carboxypeptidase Cancer
    Carboxypeptidase G2 (CPG2) Inhibitor is a novel Carboxypeptidase G2 (CPG2) Inhibitor, Antitumor agents.
  • HY-131088
    N3-PEG8-Phe-Lys-PABC-Gefitinib

    		Drug-Linker Conjugates for ADC Cancer
    N3-PEG8-Phe-Lys-PABC-Gefitinib is a drug-linker conjugate for ADC with potent antitumor activity by using the anti-tumor agent, Gefitinib (orally active EGFR tyrosine kinase inhibitor), linked via the cleavable linker N3-PEG8-Phe-Lys-PABC.
  • HY-130116
    IACS-8779

    		STING Cancer
    IACS-8779 is a highly potent stimulator of interferon genes (STING) agonist with robust systemic antitumor efficacy.
  • HY-112588
    dBET6

    		PROTAC and Building Blocks Epigenetic Reader Domain Apoptosis Cancer
    dBET6 is a highly potent, selective and cell-permeable degrader of BET based on PROTAC, with an IC50 of 14 nM, and has antitumor activity.
  • HY-N8204
    Siaresinolic acid 28-O-β-D-glucopyranosyl ester

    		Others Cancer Metabolic Disease
    Siaresinolic acid 28-O-β-D-glucopyranosyl ester possesses anti-tumor and antidiabetic effect activity.
  • HY-N2623
    Alloimperatorin

    Prangenidin

    		 Others Cancer
    Alloimperatorin (Prangenidin), a coumarin compound, is extracted from Angelica dahurica. Alloimperatorin (Prangenidin) has antitumor activity.
  • HY-19609
    Calicheamicin

    Calicheamicin γ1

    		 DNA Alkylator/Crosslinker ADC Cytotoxin Bacterial Apoptosis Antibiotic Cancer Infection
    Calicheamicin, an antitumor antibiotic, is a cytotoxic agent that causes double-strand DNA breaks. Calicheamicin is a DNA synthesis inhibitor.
  • HY-N0743
    Senkyunolide A

    		Others Cancer
    Senkyunolide A, isolated from Ligusticum chuanxiong Hort, has cytoprotective and antiproliferative activities. Anti-tumor activity.
  • HY-N8091
    Lehmannine

    		Bacterial Cancer Infection
    Lehmannine is a quinolizidine bioalkaloid isolated from S. alopecuroides L, has antibacterial, anti-inflammatory and anti-tumor activities.
  • HY-N2322
    Khasianine

    		Others Cancer
    Khasianine is a steroidal glycoalkaloid which is obtained from black nightshade (Solanum Nigrum L.), which displays antitumor activity.
  • HY-105529
    Indicine N-oxide

    (+)-Indicine N-oxide; NSC 132319

    		 Others Cancer
    Indicine N-oxide (NSC 132319), a pyrrolizidine alkaloid, is an antitumor agent for pediatric cancer and solid tumors research.
  • HY-101773
    c-Met-IN-2

    		c-Met/HGFR Cancer
    c-Met-IN-2 is a potent, selective and orally available c-Met inhibitor, with an IC50 of 0.6 nM, with antitumor activity.
  • HY-P1613A
    Cyclo(Arg-Gly-Asp-D-Phe-Val) TFA

    		Integrin Cancer
    Cyclo(Arg-Gly-Asp-D-Phe-Val) (TFA) is an inhibitor of integrin αvβ3, with antitumor activity.
  • HY-16674
    10-Oxo Docetaxel

    Docetaxel Impurity 1

    		 Microtubule/Tubulin Cancer
    10-Oxo Docetaxel (Docetaxel Impurity 1) is a novel taxoid having remarkable anti-tumor properties and a Docetaxel intermediate.
  • HY-N0863
    Methyl protodioscin

    NSC-698790; Smilax saponin B

    		 Apoptosis Cancer
    Methyl protodioscin(NSC-698790) is a furostanol bisglycoside with antitumor properties; shows to reduce proliferation, cause cell cycle arrest.
  • HY-N8131
    Pangelin

    		Bacterial Cancer Infection
    Pangelin is a coumarin that can be found in Ducrosia anethifolia. Pangelin exhibits anti-mycobacterial and anti-tumor activities.
  • HY-N2242
    Hosenkoside G

    		Others Cancer
    Hosenkoside G, a baccharane glycoside isolated from the seeds of Impatiens Balsamina L., possesses anti-tumor activity.
  • HY-N7596
    Isoverticine

    		Others Cancer
    Isoverticine, a bioactive isosteroidal alkaloid isolated from bulbus of Fritillaria pallidiflora, displays significant cytotoxicity.
  • HY-15865
    FR901463

    		Others Cancer
    FR901463 is a potent anti-cancer agent and can be used for cancer research. FR901463 enhances the transcriptional activity of the promoter of SV40 DNA virus.
  • HY-134653
    5-Ph-IAA

    		Others Cancer
    5-Ph-IAA is a derivative of IAA. 5-Ph-IAA, a ligand, establishes the auxin-inducible degron 2 (AID2) system together with an OsTIR1 (F74G) mutant. AID2 induces rapid and efficient depletion of mAID-fused proteins to study protein function in living cells, causing tumor suppression.
  • HY-N3940
    Gelsevirine

    		Others Cancer Neurological Disease
    Gelsevirine is the major alkaloid in Gelsemium elegans with potent anxiolytic effects. The anxiolytic mechanism of Gelsevirine may be involved in the agonist action of the glycine receptor in the brain. Gelsevirine has anti-proliferation activity with IC50 values of 1.41 mM and 1.22 mM for SW480 cells and MGC80-3 cells, respectively.
  • HY-126147
    J22352

    		HDAC Cancer
    J22352 is a PROTAC (proteolysis-targeting chimeras)-like and highly selective HDAC6 inhibitor with an IC50 value of 4.7 nM. J22352 promotes HDAC6 degradation and induces anticancer effects by inhibiting autophagy and eliciting the antitumor immune response in glioblastoma cancers, and leading to the restoration of host antitumor activity by reducing the immunosuppressive activity of PD-L1.
  • HY-139106
    N-Demethylansamitocin P-3

    		Others Others
    N-Demethylansamitocin P-3 can be prepared from Ansamitocin (an antitumor ansamycin antibiotic) by Streptomyces minutiscleroticus IFO 13361.
  • HY-U00248
    LMP744

    MJ-III65; NSC706744

    		 Topoisomerase Cancer
    LMP744 (MJ-III65) is a DNA intercalator and Topoisomerase I (Top1) inhibitor with antitumor activity.
  • HY-101486
    LF3

    		β-catenin Cancer
    LF3 is an antagonist of the β-Catenin/TCF4 interaction with antitumor activity; has an IC50 of 1.65 μM.
  • HY-107363
    FT-1518

    		mTOR Cancer
    FT-1518 is a new generation selective, potent and oral bioavailable mTORC1 and mTORC2 inhibitor, and exhibits antitumor activity.
  • HY-N0114
    Evodiamine

    (+)-Evodiamine; d-Evodiamine

    		 Others Cancer
    Evodiamine is an alkaloid isolated from the fruit of Evodia rutaecarpa Bentham with diverse biological activities including anti-inflammatory, anti-obesity, and antitumor.
  • HY-135317
    CA-4948

    		IRAK FLT3 Cancer Inflammation/Immunology
    CA-4948 is a potent IRAK4/FLT3 inhibtor with anti-tumor activity.
  • HY-112167A
    GDC-0575 dihydrochloride

    ARRY-575 dihydrochloride; RG7741 dihydrochloride

    		 Checkpoint Kinase (Chk) Cancer
    GDC-0575 dihydrochloride (ARRY-575 dihydrochloride) is an orally bioavailable CHK1 inhibitor, with an IC50 of 1.2 nM, and has antitumor activity.
  • HY-N2542
    Tubeimoside III

    		Others Cancer Inflammation/Immunology
    Tubeimoside III, a triterpenoid saponin, shows anti-inflammatory, anti-tumor, anti-tumorigenic activities, and acute toxicity in vivo.
  • HY-U00248A
    LMP744 hydrochloride

    MJ-III65 hydrochloride; NSC706744 hydrochloride

    		 Topoisomerase Cancer
    LMP744 hydrochloride (MJ-III65 hydrochloride) is a DNA intercalator and Topoisomerase I (Top1) inhibitor with antitumor activity.
  • HY-N2604
    Loureirin C

    		Others Cancer Infection Metabolic Disease Inflammation/Immunology Neurological Disease
    Loureirin C has anti-bacterial, anti-spasmodic, anti-inflammatory, analgesic, anti-diabetic, and anti-tumor activities.
  • HY-N6075
    Specneuzhenide

    Nuezhenide

    		 Others Cancer
    Specneuzhenide (Nuezhenide) is a phenol glycoside isolated from Ligustrum sinense. Specneuzhenide (Nuezhenide) possesses anti-tumor activity.
  • HY-N0400
    Wogonin

    		CDK Wnt Autophagy Apoptosis Cancer Inflammation/Immunology
    Wogonin is a naturally occurring mono-flavonoid, can inhibit the activity of CDK8 and Wnt, and exhibits anti-inflammatory and anti-tumor effects.
  • HY-114313
    Microtubule inhibitor 1

    		Microtubule/Tubulin Cancer
    Microtubule inhibitor 1 is an antitumor agent with microtubule polymerization inhibitory activity, with an IC50 value of 9-16 nM in cancer cells.
  • HY-N0271
    Echinocystic acid

    		Reactive Oxygen Species Apoptosis Inflammation/Immunology Cancer
    Echinocystic acid a pentacyclic triterpene isolated from the fruits of Gleditsia sinensis Lam, has potent antioxidant, anti-inflammatory and anti-tumor properties.
  • HY-101031
    c-met-IN-1

    		c-Met/HGFR Cancer
    c-met-IN-1 (compound 16) is a potent and selective c-Met inhibitor, with IC50 of 1.1 nM, with antitumor activity..
  • HY-P1728
    Super-TDU (1-31)

    		YAP Cancer
    Super-TDU (1-31) is a peptide of Super-TDU, which is an inhibitor of YAP-TEADs, shows potent anti-tumor activity.
  • HY-15184
    Elaiophylin

    Azalomycin B; Gopalamicin; Efomycin E

    		 Autophagy Cancer
    Elaiophylin (Azalomycin B; Gopalamicin; Efomycin E) is an autophagy inhibitor, exerts antitumor activity as a single agent in ovarian cancer cells.
  • HY-N2283
    Deltonin

    		ERK Akt Endogenous Metabolite Cancer
    Deltonin, a steroidal saponin, isolated from Dioscorea zingiberensis Wright, with antitumor activity; Deltonin inhibits ERK1/2 and AKT activation.
  • HY-15739
    Ansamitocin P-3

    Antibiotic C 15003P3; Maytansinol isobutyrate

    		 Microtubule/Tubulin ADC Cytotoxin Bacterial Antibiotic Cancer Infection
    Ansamitocin P-3 (Antibiotic C 15003P3) is a microtubule inhibitor. Ansamitocin P-3 is a macrocyclic antitumor antibiotic.
  • HY-129180
    XY028-133

    		PROTAC and Building Blocks CDK Cancer
    XY028-133 (example 14) is a PROTAC-based CDK4/6 degrader with anti-tumor activity.
  • HY-109104
    Telratolimod

    MEDI9197; 3M-052

    		 Toll-like Receptor (TLR) Cancer
    Telratolimod (MEDI9197) is a potent toll like receptors 7/8 (TLR7/8) agonist, with antitumor activity.
  • HY-P1728A
    Super-TDU (1-31) (TFA)

    		YAP Cancer
    Super-TDU (1-31) is a peptide of Super-TDU, which is an inhibitor of YAP-TEADs, shows potent anti-tumor activity.
  • HY-124584
    Minnelide

    		Apoptosis Cancer
    Minnelide is a prodrug of triptolide that shows potent antitumor activity in a number of tumor types, particularly in pancreatic cancer. Minnelide promotes apoptosis.
  • HY-15096
    MKT-077

    FJ-776

    		 HSP Cancer
    MKT-077 is a rhodacyanine dye and also a heat shock protein 70 (Hsp70) inhibitor which exhibits significant antitumor activity.
  • HY-N0714
    Berbamine

    		NF-κB Autophagy Cancer
    Berbamine is a natural compound extracted from traditional Chinese medicine Barberry with anti-tumor, immunomodulatory and cardiovascular effects. Berbamine is a calcium channel blocker.
  • HY-119367
    ODM-203

    		FGFR VEGFR Cancer
    ODM-203 is a potent FGFR and VEGFR families inhibitor with IC50s of 11, 16, 6, 35 nM towards recombinant FGFR1, FGFR2, FGFR3 and FGFR4 as well as 26, 9, 5 nM towards VEGFR1, VEGFR2 and VEGFR3, respectively. ODM-203 exhibits strong anti-tumor activity and induces anti-tumor immunity.
  • HY-128580
    FAK inhibitor 2

    		FAK Cancer
    FAK inhibitor 2 is a potent focal adhesion kinase (FAK) inhibitor with an IC50  of 0.07 nM, with antitumor and anti-angiogenesis activities.
  • HY-N2389
    Formosanin C

    		Apoptosis Cancer
    Formosanin C is a diosgenin saponin isolated from Paris formosana Hayata and an immunomodulator with antitumor activity. Formosanin C induces apoptosis.
  • HY-13468
    KW-2478

    		HSP Cancer
    KW-2478 is an inhibitor of Hsp90α, with an IC50 of 3.8 nM, and has antitumor activity against various human hematological tumor cells.
  • HY-N0580
    Fraxetin

    		Apoptosis Cancer Inflammation/Immunology
    Fraxetin is isolated from Cortex Fraxini. Fraxetin has antitumor, anti-oxidation effects and anti-inflammory effects. Fraxetin induces apoptosis.
  • HY-12045
    HMN-214

    IVX-214

    		 Polo-like Kinase (PLK) Cancer
    HMN-214, an orally bioavailable prodrug of HMN-176, is an inhibitor of polo-like kinase-1 (plk1), with antitumor activity.
  • HY-Y0247
    6-Chloropurine

    6-Chloro-9H-purine

    		 Others Cancer
    6-Chloropurine is a building block in chemical synthesis. Intermediate in the preparation of 9-alkylpurines and 6-rnercaptopurine. Antitumor activities.
  • HY-N0834
    Pulsatilla saponin D

    SB365; Hederacolchiside A

    		 Apoptosis Cancer
    Pulsatilla saponin D (SB365), isolated from the root of Pulsatilla koreana Nakai, is an anti-tumor agent.
  • HY-15359
    Episilvestrol

    		Eukaryotic Initiation Factor (eIF) Autophagy Cancer
    Episilvestrol is a derivative of silvestrol, isolated from the fruits and twigs of Aglaia silvestris, and is a specific eIF4A-targeting translation inhibitor, with antitumor activity.
  • HY-115568
    BETd-246

    		PROTAC and Building Blocks Epigenetic Reader Domain Cancer
    BETd-246 is a second-generation and PROTAC-based BET bromodomain (BRD) inhibitor, exhibiting superior selectivity, potency and antitumor activity.
  • HY-18931A
    NSC305787 hydrochloride

    		Others Cancer
    NSC305787 hydrochloride is an inhibitor of ezrin with a Kd of 5.85 μM, inhibits the phosphorylation of ezrin caused by PKCΙ with an IC50 of 8.3 μM, has antitumor activity.
  • HY-N4189
    Isocucurbitacin B

    		Others Cancer
    Isocucurbitacin B is a potent cytotoxic compound isolated from Helicteres rswa L. (Sterculiaceae). Isocucurbitacin B possesses anti-tumor acticity.
  • HY-U00097
    L-4-Oxalysine hydrochloride

    		Fungal Cancer Infection
    L-4-Oxalysine hydrochloride is a natural product isolated from the culture media of Streptomyces roseovirdofuscus in China which has shown antitumor activities.
  • HY-126330
    SS-208

    		HDAC Cancer
    SS-208 is a selective HDAC6 inhibitor, with an IC50 of 12 nM. SS-208 possesses anti-tumor activity in melanoma.
  • HY-12395
    Ecteinascidin-Analog-1

    		Others Cancer
    Ecteinascidin-Analog-1 is a useful intermediate for chemical sythesis of Ecteinascidin analogues; Ecteinascidins is a family of tetrahydroisoquinoline alkaloids with wide range of antitumor and antimicrobial activities.
  • HY-132179
    Fucoidan

    		Glucosidase Cancer Metabolic Disease Cardiovascular Disease
    Fucoidan, a biologically active polysaccharide, is an efficient inhibitor of α-amylase and α-glucosidase. Anticoagulant, antitumor, antioxidant and antisteatotic activities.
  • HY-P1009
    Z-YVAD-FMK

    		Caspase Cancer
    Z-YVAD-FMK is a cell-permeable caspase-1 and -4 inhibitor with anti-inflammatory and anti-tumor activities.
  • HY-N1166
    Tephrosin

    Deguelinol I; Hydroxydeguelin

    		 EGFR Cancer
    Tephrosin is a natural rotenoid which has potent antitumor activities. Tephrosin induces degradation of of EGFR and ErbB2 by inducing internalization of the receptors.
  • HY-18931
    NSC305787

    		Others Cancer
    NSC305787 is an inhibitor of ezrin with a Kd of 5.85 μM, inhibits the phosphorylation of ezrin caused by PKCΙ with an IC50 of 8.3 μM, has antitumor activity.
  • HY-129651
    SHMT-IN-1

    		Others Cancer
    SHMT-IN-1 (compound (±)-46) is a potent inhibitor of plasmodial serine hydroxymethyltransferase (SHMT). SHMT-IN-1 has antitumor activity.
  • HY-N8207
    Gypenoside LI

    		Apoptosis MicroRNA Cancer
    Gypenoside LI, a gypenoside monomer, possesses anti-tumor activity. Gypenoside LI induces cell apoptosis, cell cycle and migration.
  • HY-N4109
    Decursinol

    		Others Cancer Inflammation/Immunology
    Decursinol, isolated from the roots of Angelica gigas, possesses antinociceptive effect with orally bioavailability. Decursinol possesses anti-tumor and anti-metastasis activity.
  • HY-W015490
    1,4-Naphthoquinone

    		Others Cancer
    1,4-Naphthoquinone is a potential pharmacophore for inhibition of both MAO (monoamine oxidase) and DNA topoisomerase activities, this latter associated with antitumor activity.
  • HY-N2997
    Ganoderic acid LM2

    		Others Cancer
    Ganoderic acid LM2 is a natural terpenoid isolated from the Fungus Ganoderma lucidum. Ganoderic acid LM2 possesses potential anti-tumor activity.
  • HY-137442
    Inupadenant

    EOS-850

    		 Adenosine Receptor Cancer
    Inupadenant is an orally active, highly selective A2A receptor antagonist. Inupadenant is not brain-penetrant. Inupadenant has potent anti-tumor activity.
  • HY-N0174
    Cryptotanshinone

    Cryptotanshinon; Tanshinone c

    		 STAT Autophagy Cancer
    Cryptotanshinone is a natural compound extracted from the root of Salvia miltiorrhiza Bunge that shows antitumor activities. Cryptotanshinone inhibits STAT3 with an IC50 of 4.6 μM.
  • HY-D0803
    Thymoquinone

    		Others Inflammation/Immunology
    Thymoquinone is a nature product isolated from N. sativa. Thymoquinone possess antioxidant, anti-inflammatory, anti-cancer, antitumor activities and hepatoprotective properties.
  • HY-14573
    SJG-136

    NSC-694501

    		 DNA Alkylator/Crosslinker ADC Cytotoxin Cancer
    SJG-136 is a DNA cross-linking agent, with an XL50 of 45 nM for pBR322 DNA. SJG-136 has potent antitumor activity.
  • HY-100506
    GLPG0187

    		Integrin Cancer
    GLPG0187 is a broad spectrum integrin receptor antagonist with antitumor activity; inhibits αvβ1-integrin with an IC50 of 1.3 nM.
  • HY-N6004
    (Rac)-Shikonin

    Shikalkin

    		 Others Cancer
    (Rac)-Shikonin (Shikonin) possesses anti-tumor activity. (Rac)-Shikonin (Shikonin) circumvents cancer drug resistance by induction of a necroptotic death.
  • HY-N0488
    Vincristine sulfate

    Leurocristine sulfate; NSC-67574 sulfate; 22-Oxovincaleukoblastine sulfate

    		 Microtubule/Tubulin Apoptosis Cancer
    Vincristine sulfate is an antitumor vinca alkaloid which inhibits microtubule formation in mitotic spindle, resulting in an arrest of dividing cells at the metaphase stage. It binds to microtubule with a Ki of 85 nM.
  • HY-112897
    IITZ-01

    		Autophagy PI3K Apoptosis Cancer
    IITZ-01 is a potent lysosomotropic autophagy inhibitor with single-agent antitumor activity, with an IC50 of 2.62 μM for PI3Kγ.
  • HY-N0021
    Verbascoside

    Acteoside; Kusaginin; TJC160

    		 PKC Apoptosis Bacterial HSV Cancer Inflammation/Immunology Neurological Disease
    Verbascoside is isolated from Lantana camara, acts as an ATP-competitive inhibitor of PKC, with an IC50 of 25 µM, and has antitumor, anti-inflammatory and antineuropathic pain activity.
  • HY-14934
    Rosabulin

    STA 5312

    		 Microtubule/Tubulin Cancer
    Rosabulin (STA 5312) is a potent and orally active microtubule inhibitor that inhibits microtubule assembly. Rosabulin has broad-spectrum anti-tumor activity.
  • HY-N0429
    Diosbulbin B

    		Others Cancer
    Diosbulbin B is a diterpene lactone isolated from D. bulbifera L., with anti-tumor activity. Diosbulbin B can induce liver injury.
  • HY-139326
    NHS-MMAF

    		Others Cancer
    NHS-MMAF is a modified MMAF extracted from patent WO2012143499, intermediat 219. MMAF is a potent tubulin polymerization inhibitor and is used as a antitumor agent
  • HY-N4116
    Xanthyletin

    		Fungal Cancer Infection
    Xanthyletin is a coumarin isolated from Citrus, with anti-tumor and anti-bacterial activities. Xanthyletin also inhibits symbiotic fungus cultivated by leaf-cutting ants.
  • HY-N3442
    Juglanin

    		JNK Apoptosis Autophagy Cancer Inflammation/Immunology
    Juglanin, a natural occurring flavonoid, is a JNK acticator, with inflammation and anti-tumor activities. Juglanin can induce apoptosis and autophagy on human breast cancer cells.
  • HY-N1931
    Epifriedelanol

    		Others Cancer
    Epifriedelanol is a triterpenoid isolated from the root bark of Ulmus davidiana, with antitumor activity. Epifriedelanol inhibits cellular senescence in human primary cells.
  • HY-117260
    Coformycin

    		Adenosine Deaminase Bacterial Cancer Infection
    Coformycin, a nucleoside antibiotic, is a potent inhibitor of adenosine deaminase (ADA) from Streptomyces species. Coformycin possesses anti-tumor and anti-bacterial activity.
  • HY-128959
    MCC-Modified Daunorubicinol

    		Drug-Linker Conjugates for ADC Cancer
    Daunorubicinol is a drug-linker conjugate for ADC with potent antitumor activity by using Aur0101 (DNA Topoisomerase II inhibitor), linked via the ADC linker.
  • HY-126532
    Fmoc-Val-Cit-PAB-Duocarmycin TM

    		Drug-Linker Conjugates for ADC Cancer
    Fmoc-Val-Cit-PAB-Duocarmycin TM is a drug-linker conjugate for ADC by using the antitumor antibiotic, Duocarmycin TM, linked via Fmoc-Val-Cit-PAB.
  • HY-129467
    Minerval

    2-Hydroxyoleic acid; 2-OHOA

    		 Apoptosis Cancer
    Minerval (2-Hydroxyoleic acid) is a synthetic oleic acid (OA) derivative that binds to the plasma membrane and alters lipid organization. Minerval has anti-tumor effect.
  • HY-N2104
    Daurinoline

    		Others Cancer
    Daurinoline is an alkaloid that can be isolated from the roots of Menispermum dauricum. Daurinoline may be a potential anti-tumor agent or chemosensitizer for chemo-resistant NSCLC research.
  • 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-111381
    BI-3812

    		Bcl-2 Family Cancer
    BI-3812 is potent and efficacious BCL6 inhibitor, inhibiting the BTB domain of BCL6, with an IC50 of ≤3 nM; BI-3812 has antitumor activity.
  • HY-15159
    Cyclapolin 9

    		Polo-like Kinase (PLK) Cancer
    Cyclapolin 9 is a potent, selective and ATP-competitive polo-like kinase 1 (PLK1) inhibitor with an IC50 of 500 nM. Cyclapolin 9 is inactive against other kinases.
  • HY-20403
    PF-562271 hydrochloride

    		FAK Pyk2 Cancer
    PF-562271 hydrochloride is a potent, ATP-competitive and reversible FAK and Pyk2 kinase inhibitor with IC50s of 1.5 nM and 13 nM, respectively.
  • HY-10459
    PF-562271

    		FAK Pyk2 Cancer
    PF-562271 is a potent, ATP-competitive and reversible FAK and Pyk2 kinase inhibitor with IC50s of 1.5 nM and 13 nM, respectively.
  • HY-130850
    CDK9-IN-10

    		CDK Ligand for Target Protein for PROTAC Cancer
    CDK9-IN-10 is a potent CDK9 inhibitor. CDK9-IN-10 is the ligand for the PROTAC CDK9 degrader-2 (HY-112811).
  • HY-13772
    Valrubicin

    AD-32

    		 PKC Cancer Inflammation/Immunology
    Valrubicin is a chemotherapy agent, inhibits TPA- and PDBu-induced PKC activation with IC50s of 0.85 and 1.25 μM, respectively, and has antitumor and antiinflammatory activity.
  • 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-101414
    L-DABA

    L-2,4-Diaminobutyric acid

    		 GABA Receptor Endogenous Metabolite Neurological Disease Cancer
    L-DABA (L-2,4-Diaminobutyric acid) is a week GABA transaminase inhibitor with an IC50 of larger than 500 μM; exhibits antitumor activity in vivo and in vitro.
  • HY-133117A
    (Rac)-BAY-985

    		IKK Cancer
    (Rac)-BAY-985 (Compound Example 100.01) is a potent, ATP-competitive and selective TBK1 inhibitor with an IC50 of 1.5 nM. Antitumor efficacy.
  • HY-N4322
    Decursinol angelate

    		PKC Cancer Inflammation/Immunology
    Decursinol angelate, a cytotoxic and protein kinase C (PKC) activating agent from the root of Angelica gigas, possesses anti-tumor and anti-inflammatory activities.
  • HY-P9905
    Cetuximab

    C225

    		 EGFR Cancer
    Cetuximab (C225) is a monoclonal antibody that inhibits epidermal growth factor receptor (EGFR), with a Kd of 0.201 nM for EGFR by SPR. Cetuximab has potent antitumor activity.
  • HY-103088
    E7046

    		Prostaglandin Receptor Cancer Endocrinology
    E7046 is an orally bioavailable and specific EP4 antagonist, with IC50 of 13.5 nM and Ki of 23.14 nM. E7046 exhibits anti-tumor activities.
  • HY-112805
    FCHFHS-ST7612AA1

    		Drug-Linker Conjugates for ADC Cancer
    FCHFHS-ST7612AA1 is a part of antibody drug conjugates (ADCs) charged with HDAC inhibitor by a linker, shows antitumor activity.
  • HY-128599
    NMS-P515

    		PARP Cancer
    NMS-P515 is a potent, orally active and stereospecific PARP-1 inhibitor, with a Kd of 16 nM and an IC50 of 27 nM (in Hela cells). Anti-tumor activity.
  • HY-N0011
    Baohuoside I

    Icariin-II; Icariside-II

    		 CXCR Apoptosis Cancer Inflammation/Immunology Endocrinology
    Baohuoside I, a flavonoid isolated from Epimedium koreanum Nakai, acts as an inhibitor of CXCR4, downregulates CXCR4 expression, induces apoptosis and shows anti-tumor activity.
  • HY-111502
    Y06036

    		Epigenetic Reader Domain Cancer
    Y06036 is a potent and selective BET inhibitor, which binds to the BRD4(1) bromodomain with Kd value of 82 nM. Antitumor activity.
  • HY-129181
    FGFR4-IN-4

    		FGFR Cancer
    FGFR4-IN-4 (compound 693) is a FGFR4 inhibitor with anti-tumor activity, extracted from patent WO2018113584A1.
  • HY-N0344
    Farrerol

    		Others Cancer Inflammation/Immunology Neurological Disease
    Farrerol is a bioactive constituent of Rhododendron, with broad activities such as anti-oxidative, anti-inflammatory, anti-tumor, neuroprotective and hepatoprotective effects.
  • HY-N0102
    Isoliquiritigenin

    GU17; ISL; Isoliquiritigen

    		 Aldose Reductase Influenza Virus Autophagy Apoptosis Cancer Infection Inflammation/Immunology
    Isoliquiritigenin is an anti-tumor flavonoid from the root of Glycyrrhiza glabra, which inhibits aldose reductase with an IC50 of 320 nM. Isoliquiritigenin is a potent inhibitor of influenza virus replication with an EC50 of 24.7 μM.
  • HY-100510
    RAF709

    		Raf Cancer
    RAF709 is a potent, selective, and efficacious RAF inhibitor with IC50s of 0.4 nM and 0.5 nM for BRAF and CRAF, respectively. Antitumor efficacy.
  • HY-12460
    SPDB-DM4

    		Drug-Linker Conjugates for ADC Cancer
    SPDB-DM4 is a drug-linker conjugate for ADC by using the maytansinebased payload (DM4, a tubulin inhibitor) via a SPDB linker, exhibiting potent anti-tumor activity.
  • HY-N0017
    Bergenin

    Cuscutin

    		 Autophagy Apoptosis Bacterial Fungal Virus Protease Cancer Infection Inflammation/Immunology
    Bergenin is a cytoprotective and antioxidative polyphenol found in many medicinal plants. Bergenin has a wide spectrum activities such as hepatoprotective, antiinflammatory, immunomodulatory, antitumor, antiviral, and antifungal properties.
  • HY-102087
    JPM-OEt

    		Cathepsin Cancer
    JPM-OEt is a broad spectrum cysteine cathepsin inhibitor. JPM-OEt binds covalently in the active site, and irreversibly inhibits the cysteine cathepsin family. Antitumor activity.
  • HY-N2432
    Paederoside

    		HBV Cancer Infection
    Paederoside is a monoterpene S-methyl thiocarbonate isolated from Paederia pertomentosa. Paederoside shows a high anti-tumor promoting activity against the Epstein-Barr virus activation.
  • HY-126218
    HSV-TK substrate

    		HSV Cancer
    HSV-TK substrate is a substrate for HSV-TK, and induces multi-log cytotoxicity in HSV-TK-expressing and bystander cells. HSV-TK substrate shows antitumor activity.
  • HY-101978
    CPI-444

    V81444; ciforadenant

    		 Adenosine Receptor Cancer
    CPI-444 (V81444) is a potent, orally active and selective adenosine A2A receptor (A2AR) antagonist, which induces antitumor responses.
  • HY-128957
    Vc-seco-DUBA

    SYD985

    		 Drug-Linker Conjugates for ADC Cancer
    Vc-seco-DUBA is a drug-linker conjugate for ADC with potent antitumor activity by using DUBA (DNA alkylating agent), linked via the ADC linker Vc-seco.
  • HY-128896
    Nitro-PDS-Tubulysin M

    		Drug-Linker Conjugates for ADC Cancer
    Nitro-PDS-Tubulysin M is a drug-linker conjugate for ADC with potent antitumor activity by using Tubulysin M (a tubulin polymerization inhibitor), linked via the ADC linker Nitro-PDS.
  • HY-N4111
    Wushanicaritin

    		Others Cancer Inflammation/Immunology
    Wushanicaritin exhibits significant antioxidant activity (IC50=35.3 μM) in DPPH radical scavenging activity tests. Antitumor effects and anti-inflammatory property.
  • HY-112786
    MC-Val-Cit-PAB-MMAF

    		Drug-Linker Conjugates for ADC Microtubule/Tubulin Cancer
    MC-Val-Cit-PAB-MMAF is a drug-linker conjugate for ADC with antitumor activity by using the tubulin inhibitor, MMAF, linked via cathepsin cleavable MC-Val-Cit-PAB.
  • HY-N0205
    Pulchinenoside C

    Anemoside B4

    		 Others Cancer
    Pulchinenoside C (Anemoside B4) is Pulsatilla koreana Nakai that have many numerous biological effects in vitro, including enhancing hypoglycemic, anti-tumor, neuroprotective and anti-angiogenic activity.
  • HY-15582
    Auristatin E

    		Microtubule/Tubulin ADC Cytotoxin Cancer
    Auristatin E is a cytotoxic tubulin modifier with potent and selective antitumor activity; MMAE analog and cytotoxin in Antibody-drug conjugates. Auristatin E inhibits cell division by blocking the polymerisation of tubulin.
  • 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-101568
    Roblitinib

    FGF-401

    		 FGFR Cancer
    Roblitinib (FGF-401) is an orally active and highly selective FGFR4 inhibitor with an IC50 of 1.9 nM. Roblitinib has antitumor activity.
  • HY-N0622
    Morusin

    Mulberrochromene

    		 NF-κB STAT Bacterial Cancer Infection Inflammation/Immunology
    Morusin is a prenylated flavonoid isolated from M. australis with various biological activities, such as antitumor, antioxidant, and anti-bacteria property. Morusin could inhibit NF-κB and STAT3 activity.
  • 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-N6049
    Lup-20(29)-en-28-oic acid

    		Others Cancer Inflammation/Immunology
    Lup-20(29)-en-28-oic acid, a triterpenoid saponins of Pulsatilla koreana Root, possesses anti-inflammatory and anti-tumor effect.
  • HY-107366
    SGN-2FF

    		Others Cancer
    SGN-2FF is a potent and orally active inhibitor of fucosylation, directly inhibits fucosyltransferase activity. SGN-2FF possesses antitumor activity.
  • HY-131096
    L-Proline 4-methoxy-β-naphthylamide hydrochloride

    H-Pro-4MβNA hydrochloride

    		 Others Cancer
    L-Proline 4-methoxy-β-naphthylamide hydrochloride (H-Pro-4MβNA hydrochloride) can be used for Fap-activated anti-tumor compounds preparaction.
  • HY-112806
    MAC-VC-PABC-ST7612AA1

    		Drug-Linker Conjugates for ADC Cancer
    MAC-VC-PABC-ST7612AA1 is a part of antibody drug conjugates (ADCs) charged with HDAC inhibitor by a linker, shows antitumor activity.
  • HY-139105
    20-O-Demethyl-AP3

    		Microtubule/Tubulin Cancer Infection
    20-O-Demethyl-AP3 is a minor metabolite of Ansamitocin P-3. Ansamitocin P-3, a microtubule inhibitor, is a macrocyclic antitumor antibiotic.
  • HY-136317
    MC-betaglucuronide-MMAE-1

    		Microtubule/Tubulin Drug-Linker Conjugates for ADC Cancer
    MC-betaglucuronide-MMAE-1 is a drug-linker conjugate for ADC with potent antitumor activity by using MMAE (a tubulin polymerization inhibitor), linked via the cleavable ADC linker MC-betaglucuronide.
  • HY-136321
    MC-betaglucuronide-MMAE-2

    		Microtubule/Tubulin Drug-Linker Conjugates for ADC Cancer
    MC-betaglucuronide-MMAE-2 is a drug-linker conjugate for ADC with potent antitumor activity by using MMAE (a tubulin polymerization inhibitor), linked via the cleavable ADC linker MC-betaglucuronide.
  • HY-136350
    BRD9500

    		Phosphodiesterase (PDE) Cancer
    BRD9500 is an orally active phosphodiesterases 3 (PDE3) inhibitor with IC50s of 10 and 27 nM for PDE3A and PDE3B, respectively. Antitumor activity.
  • HY-126685
    Mal-PEG4-VA-PBD

    		Drug-Linker Conjugates for ADC Cancer
    Mal-PEG4-VA-PBD is a drug-linker conjugate for ADC by using the antitumor antibiotic, Pyrrolobenzodiazepine (PBD), linked via Mal-PEG4-VA.
  • HY-N7022
    Eclalbasaponin I

    		Others Cancer
    Eclalbasaponin I is isolated from Eclipta prostrata L with antitumor activity. Eclalbasaponin I inhibits the proliferation of hepatoma cell smmc-7721 with an IC50 value of 111.1703 μg/ml.
  • HY-126494
    DM4-SMCC

    		Drug-Linker Conjugates for ADC Cancer
    DM4-SMCC is a drug-linker conjugate for ADC with antitumor activity by using DM4 (an antitubulin agent), linked via the non-cleavable SMCC linker.
  • HY-N6656
    6-Hydroxycoumarin

    		Others Cancer Inflammation/Immunology
    6-Hydroxycoumarin is a coumarin which has anti-inflammatory, anti-pyretic, anti-oxidant, vasodilator, anti-amoebic, anti-bacterial, anti-fungal, bacteriostatic and antitumor activity.
  • HY-N8253
    Spiraeoside

    Quercetin 4′-O-glucoside

    		 Reactive Oxygen Species Cancer Inflammation/Immunology
    Spiraeoside, an orally active natural compound, exerts antioxidant activity, inhibits reactive oxygen species (ROS) and malondialdehyde production. Spiraeoside possesses antiallergic, anti-inflammatory and antitumor activities.
  • HY-126692
    Mal-VC-PAB-ABAEP-Azonafide

    		Drug-Linker Conjugates for ADC Cancer
    Mal-VC-PAB-ABAEP-Azonafide is a drug-linker conjugate for ADC with with potent antitumor activity by using Azonafide (a cytotoxin), linked via the ADC linker Mal-VC-PAB.
  • HY-112732B
    Sparfosic acid trisodium

    		Others Cancer Metabolic Disease
    Sparfosic acid trisodium, is a potent inhibitor of aspartate transcarbamoyl transferase, with anti-tumor and antimetabolite activity. Aspartate transcarbamoyl transferase catalyzes the second step of de novo pyrimidine biosynthesis.
  • HY-18295
    Erteberel

    LY500307

    		 Estrogen Receptor/ERR Neurological Disease
    Erteberel (LY500307) is a potent and selective estrogen receptor beta (ERβ) agonist with Ki and EC50 of 1.54 nM and 3.61 nM, respectively. Anti-tumor activities.
  • HY-114277A
    Sotorasib racemate

    AMG-510 racemate

    		 Ras Cancer
    Sotorasib (AMG-510) racemate is the racemate of Sotorasib (AMG-510). AMG-510 is a potent, orally bioavailable, and selective KRAS G12C covalent inhibitor with anti-tumor activity.
  • HY-107324
    β-Elemene

    (-)-β-Elemene; Levo-β-elemene

    		 Apoptosis Cancer
    β-Elemene ((-)-β-Elemene; Levo-β-elemene) is isolated from natural plant Curcuma wenyujin with an antitumor activity. β-Elemene can induce cell apoptosis.
  • HY-N6892
    3'-​O-​Acetylhamaudol

    		Others Cancer
    3'-O-Acetylhamaudol, isolated from Angelica japonica roots, exhibits anti-tumor activity through dual actions, anti-angiogenesis and intestinal intraepithelial lymphocyte activation.
  • HY-137450
    Senaparib

    IMP4297

    		 PARP Cancer
    Senaparib (IMP4297) is a highly potent, selective and orally active PARP1/2 inhibitor. Senaparib (IMP4297) exhibits strong antitumor activity in animal models.
  • HY-128906
    MC-Val-Cit-PAB-Retapamulin

    		Drug-Linker Conjugates for ADC Cancer
    MC-Val-Cit-PAB-Retapamulin is a drug-linker conjugate for ADC with potent antitumor activity by using Retapamulin (a ribosome inhibitor), linked via the ADC linker MC-Val-Cit-PAB.
  • HY-108488
    KB SRC 4

    		Src Cancer
    KB SRC 4 is a potent, and highly selective c-Src inhibitor, with a Ki of 44 nM and a Kd of 86 nM, and shows no inhibition on c-Abl up to 125 μM; KB SRC 4 has antitumor activity.
  • HY-128903
    MC-Val-Cit-PAB-carfilzomib

    		Drug-Linker Conjugates for ADC Cancer
    MC-Val-Cit-PAB-carfilzomib is a drug-linker conjugate for ADC with potent antitumor activity by using carfilzomib (an irreversible proteasome inhibitor), linked via the ADC linker MC-Val-Cit-PAB.
  • HY-130233
    S516

    		Microtubule/Tubulin Cancer
    S516 (Compound 22) is an active metabolite of CKD-516 and a potent tubulin polymerization inhibitor with an IC50 of 4.29 μM. S516 has marked antitumor activity.
  • HY-107999
    CADD522

    		Others Cancer
    CADD522 is a potent inhibitor of runt-related transcription factor-2 (RUNX2)-DNA binding with an IC50 of 10 nM. CADD522 exhibits antitumor activity.
  • HY-B1714A
    NSC 601980

    		Others Cancer
    NSC601980 shows antitumor activity in the yeast screening experiment, which can inhibit cell proliferation in the COLO 205 and HT29 with Log GI 50 of -6.6 and -6.9 respectively.
  • HY-128907
    MC-Val-Cit-PAB-clindamycin

    		Drug-Linker Conjugates for ADC Cancer
    MC-Val-Cit-PAB-clindamycin is a drug-linker conjugate for ADC with potent antitumor activity by using clindamycin (a protein synthesis inhibitor), linked via the ADC linker MC-Val-Cit-PAB.
  • HY-N6958
    2-O-β-D-Glucopyranosyl-L-ascorbic acid

    AA-2βG

    		 Others Cancer Metabolic Disease
    2-O-β-D-Glucopyranosyl-L-ascorbic acid (AA-2βG), isolated from Lycium Fruit, is a stable vitamin C analog with anti-tumor activity.
  • HY-128968
    PEG4-aminooxy-MMAF

    		Microtubule/Tubulin Drug-Linker Conjugates for ADC Cancer Inflammation/Immunology
    PEG4-aminooxy-MMAF is a drug-linker conjugate for ADC with potent antitumor activity by using the potent antitubulin agent MMAF, linked via the noncleavable PEG4.
  • HY-10231
    PX-478

    		HIF/HIF Prolyl-Hydroxylase Autophagy Cancer
    PX-478 is an orally active HIF-1α inhibitor with potent antitumor activities. PX-478 can cross the blood-brain barrier.
  • HY-128902
    MC-Val-Cit-PAB-vinblastine

    		Drug-Linker Conjugates for ADC Cancer
    MC-Val-Cit-PAB-vinblastine is a drug-linker conjugate for ADC with potent antitumor activity by using vinblastine (an microtubule protein inhibitor), linked via the ADC linker MC-Val-Cit-PAB.
  • HY-136684
    BrBzGCp2

    S-p-Bromobenzylglutathione cyclopentyl diester

    		 Others Cancer Neurological Disease
    BrBzGCp2 is a Glyoxalase 1 (GLO1) inhibitor, with a GC50 of 4.23 μM in HL-60 cells. BrBzGCp2 possesses antitumor and neuroprotective activity.
  • HY-126491
    SPP-DM1

    		Drug-Linker Conjugates for ADC Cancer
    SPP-DM1 is a drug-linker conjugate for ADC with potent antitumor activity by using DM1 (a potent microtubule-disrupting agent), linked via the ADC linker SPP.
  • HY-100760
    Toxoflavin

    Xanthothricin; Toxoflavine; PKF-118-310

    		 β-catenin Bacterial Antibiotic Cancer Infection
    Toxoflavin (Xanthothricin) is an antagonist of transcription factor 4 (TCF4)/β-catenin complex, also acts as an inhibitor of KDM4A, with antitumor activity. Antibiotic properties.
  • HY-12823
    BLU9931

    		FGFR Cancer
    BLU9931 is a potent, highly selective, and irreversible fibroblast growth factor receptor 4 (FGFR4) inhibitor with an IC50 of 3 nM and a Kd of 6 nM. BLU9931 has significant antitumor activity.
  • HY-110244
    Tilfrinib

    		Others Cancer
    Tilfrinib (compound 4f) is a potent and selective inhibitor of breast tumor kinase (Brk) with an IC50 of 3.15 nM, which displays anti-proliferative activity and acts as a promising antitumor agent.
  • HY-128961
    MC-Alkyl-Hydrazine Modified MMAF

    		Drug-Linker Conjugates for ADC Microtubule/Tubulin Cancer
    MC-Alkyl-Hydrazine Modified MMAF is a drug-linker conjugate for ADC with potent antitumor activity by using the Modified MMAF (a tubulin inhibitor), linked via the noncleavable MC-Alkyl-Hydrazine.
  • HY-16961
    Sitravatinib

    MGCD516; MG-516

    		 VEGFR c-Kit FLT3 Discoidin Domain Receptor Trk Receptor Cancer Inflammation/Immunology
    Sitravatinib (MGCD516) is an orally bioavailable receptor tyrosine kinase (RTK) inhibitor with IC50s of 1.5 nM, 2 nM, 2 nM, 5 nM, 6 nM, 6 nM, 8 nM, 0.5 nM, 29 nM, 5 nM, and 9 nM for Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT, FLT3, DDR2, DDR1, TRKA, TRKB, respectively. Sitravatinib shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment.
  • HY-101150
    DGN462

    		DNA Alkylator/Crosslinker Cancer
    DGN462, a potent DNA-alkylating agent, shows anti-tumor activity, such as acute myeloid leukemia (AML). DGN462 can be used as a cytotoxic component of antibody-drug conjugates (ADCs).
  • HY-101150A
    sulfo-DGN462 sodium

    		DNA Alkylator/Crosslinker ADC Cytotoxin Cancer
    sulfo-DGN462 sodium is degraded to DGN462 in culture medium and plasma. DGN462, a potent DNA-alkylating agent, shows anti-tumor activity, such as acute myeloid leukemia (AML).
  • HY-136645
    EP4 receptor antagonist 2

    		Prostaglandin Receptor Cancer
    EP4 receptor antagonist 2 (compound 2-13) is a potent EP4 receptor antagonist with an IC50 of 7.8 nM. EP4 receptor antagonist 2 shows antitumor activity.
  • HY-136289
    MB-VC-MGBA

    		Drug-Linker Conjugates for ADC Cancer
    MB-VC-MGBA is a drug-linker conjugate for ADC with potent antitumor activity by using MGBA (minor-groove-binding DNA-alkylating agent), linked via the ADC linker MB-VC.
  • HY-136640
    BCL6-IN-4

    		Bcl-2 Family Cancer
    BCL6-IN-4 is a potent B-cell lymphoma 6 (BCL6) inhibitor with an IC50 of 97 nM. BCL6-IN-4 has anti-tumor activities.
  • HY-133433
    DBCO-PEG4-VA-PBD

    		Drug-Linker Conjugates for ADC Cancer
    DBCO-PEG4-VA-PBD is a drug-linker conjugate for ADC by using the antitumor antibiotic, Pyrrolobenzodiazepine (PBD), linked via DBCO-PEG4-VA.
  • HY-16126
    Carboxyamidotriazole

    L-651582; CAI

    		 Calcium Channel Cancer Inflammation/Immunology
    Carboxyamidotriazole (L-651582) is a cytostatic inhibitor of nonvoltage-operated calcium channels and calcium channel-mediated signaling pathways. Carboxyamidotriazole shows anti-tumor, anti-inflammatory and antiangiogenic effects.
  • HY-136316
    MC-VC-PAB-MMAD

    		Microtubule/Tubulin Drug-Linker Conjugates for ADC Cancer
    MC-VC-PAB-MMAD is a drug-linker conjugate for ADC with potent antitumor activity by using MMAD (a potent tubulin inhibitor), linked via the cleavable ADC linker MC-VC-PAB.
  • HY-N1451
    Betulonic acid

    Betunolic acid; Liquidambaric acid; (+)-Betulonic acid

    		 Parasite HSV Cancer Infection Inflammation/Immunology
    Betulonic acid (Betunolic acid), a naturally occurring triterpene, is found in many plants. Betulonic acid has anti-tumor, anti-inflammatory, antiparasitic and anti-viral (HSV-1) activities.
  • HY-135815
    Mobocertinib

    TAK-788; AP32788

    		 EGFR Cancer
    Mobocertinib (TAK-788) is a potent and orally active inhibitor of EGFR and HER2 oncogenic mutants, including exon 20 insertions, with selectivity over WT EGFR. Antitumor activity.
  • HY-14949
    Cevipabulin

    TTI-237

    		 Microtubule/Tubulin Cancer
    Cevipabulin (TTI-237) is an oral, microtubule-active antitumor compound and inhibits the binding of [ 3H] vinblastine to tubulin, with an IC50 of 18-40 nM for cytotoxicity in human tumor cell line.
  • HY-136315
    OSu-Glu-VC-PAB-MMAD

    		Microtubule/Tubulin Drug-Linker Conjugates for ADC Cancer
    OSu-Glu-VC-PAB-MMAD is a drug-linker conjugate for ADC with potent antitumor activity by using MMAD (a potent tubulin inhibitor), linked via the cleavable ADC linker OSu-Glu-VC-PAB.
  • HY-128955
    MC-VC-PABC-Aur0101

    		Drug-Linker Conjugates for ADC Cancer
    MC-VC-PABC-Aur0101 is a drug-linker conjugate for ADC with potent antitumor activity by using Aur0101 (an auristatin microtubule inhibitor), linked via the ADC linker MC-VC-PABC.
  • HY-128893
    MC-Sq-Cit-PAB-Gefitinib

    		Drug-Linker Conjugates for ADC Cancer
    MC-Sq-Cit-PAB-Gefitinib is a drug-linker conjugate for ADC with potent antitumor activity by using Gefitinib (an EGFR tyrosine kinase inhibitor), linked via the ADC linker MC-Sq-Cit-PAB.
  • HY-129188
    CCT369260

    		Bcl-2 Family Cancer
    CCT369260 (compound 1) is an orally avtive B-cell lymphoma 6 (BCL6) inhibitor with anti-tumor activity. CCT369260 (compound 1) exhibits an IC50 of 520 nM.
  • HY-19095
    TNP-351

    		Antifolate Cancer
    TNP-351 is an antifolate. TNP-351, a dihydrofolate reductase (DHFR) inhibitor, has potent antitumor activity against not only leukemia cells but also solid tumor cells in vitro and in vivo.
  • HY-133492
    DBCO-PEG4-MMAF

    		Drug-Linker Conjugates for ADC Cancer
    DBCO-PEG4-MMAF is a drug-linker conjugate for ADC with potent antitumor activity by using the tubulin polymerization inhibitor, MMAF, linked via the cleavable linker DBCO-PEG4.
  • HY-P1599
    Valorphin

    		Opioid Receptor Cancer Neurological Disease
    Valorphin is an endogenous hemoglobin β-chain (33-39) fragment with opioid analgesic activity, binds to rat mu-opioid receptor, with an IC50 of 14 nM; Valorphin also shows anti-tumor activity.
  • 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-101820
    Simotinib

    		EGFR Cancer
    Simotinib is a selective, specific, and orally bioavailable EGFR tyrosine kinase inhibitor, with an IC50 of 19.9 nM. Antineoplastic activities.
  • HY-128908
    MC-Val-Cit-PAB-Indibulin

    		Drug-Linker Conjugates for ADC Cancer
    MC-Val-Cit-PAB-Indibulin is a drug-linker conjugate for ADC with potent antitumor activity by using Indibulin (an orally applicable inhibitor of tubulin assembly), linked via the ADC linker MC-Val-Cit-PAB.
  • HY-128899
    MC-Val-Cit-PAB-Auristatin E

    		Drug-Linker Conjugates for ADC Cancer
    MC-Val-Cit-PAB-Auristatin E is a drug-linker conjugate for ADC with potent antitumor activity by using Auristatin E (a cytotoxic tubulin modifier), linked via the ADC linker MC-Val-Cit-PAB.
  • HY-114233
    MC-GGFG-DX8951

    		Drug-Linker Conjugates for ADC Cancer
    MC-GGFG-DX8951 is a drug-linker conjugate for ADC with antitumor activity by using DX8951 (a DNA topoisomerase I inhibitor), linked via the protease cleavable MC-GGFG linker.
  • HY-126492
    Vat-Cit-PAB-Monomethyl Dolastatin 10

    		Drug-Linker Conjugates for ADC Microtubule/Tubulin Cancer
    Vat-Cit-PAB-Monomethyl Dolastatin 10 is a drug-linker conjugate for ADC with potent antitumor activity by using Monomethyl Dolastatin 10 (a potent tubulin inhibitor), linked via the ADC linker Vat-Cit-PAB.
  • HY-117288A
    S55746 hydrochloride

    BCL201 hydrochloride

    		 Bcl-2 Family Cancer
    S55746 hydrochloride (BCL201 hydrochloride) is a potent, orally active and selective BCL-2 inhibitor, with a Ki of 1.3 nM and a Kd of 3.9 nM. S55746 hydrochloride (BCL201 hydrochloride) has antitumor activity with low toxicity.
  • HY-107271
    Imperialine 3-β-D-glucoside

    		Others Cancer
    Imperialine 3-β-D-glucoside is the glycoside of Imperialine. Imperialine 3-β-D-glucoside may exhibit anti-tumor properties against multi-drug resistant tumor cells.
  • HY-122493
    Illudin M

    		DNA Alkylator/Crosslinker Apoptosis Cancer
    Illudin M is a cytotoxic fungal sesquiterpene that can be isolated from the culture medium of Omphalotus olearius mushrooms. Illudin M can alkylate DNA. Illudin M has anti-tumor activities.
  • 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-128897
    MC-VC-PABC-DNA31

    		Drug-Linker Conjugates for ADC Cancer
    MC-VC-PABC-DNA31 is a drug-linker conjugate for ADC with potent antitumor activity by using DNA31 (a potent RNA polymerase inhibitor), linked via the ADC linker MC-VC-PABC.
  • HY-N2490
    Dehydrotrametenolic acid

    		Caspase Apoptosis Cancer Inflammation/Immunology
    Dehydrotrametenolic acid is a sterol isolated from the sclerotium of Poria cocos. Dehydrotrametenolic acid induces apoptosis through caspase-3 pathway. Dehydrotrametenolic acid has anti-tumor activity, anti-inflammatory, anti-diabetic effects.
  • HY-107777
    LLY-283

    		Histone Methyltransferase Cancer
    LLY-283 is a potent, selective and oral protein arginine methyltransferase 5 (PRMT5) inhibitor, with an IC50 of 22 nM and a Kd of 6 nM for PRMT5:MEP50 complex, and shows antitumor activity.
  • HY-102026
    Formycin A

    NSC 102811

    		 HIV Nucleoside Antimetabolite/Analog Antibiotic Cancer Infection
    Formycin A (NSC 102811), a purine nucleoside antibiotic, is a potent human immunodeficiency virus type 1 (HIV-1) inhibitor with an EC50 of 10 μM. Formycin A shows antitumor and antiviral activities.
  • 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-101021
    Ascochlorin

    Ilicicolin D

    		 STAT Apoptosis Cancer Inflammation/Immunology
    Ascochlorin (Ilicicolin D), an isoprenoid antibiotic, mediates its anti-tumor effects predominantly through the suppression of STAT3 signaling cascade. Ascochlorin induces apoptosis. Anti-inflammatory activity.
  • HY-B2230
    Hinokitiol

    β-Thujaplicin

    		 Keap1-Nrf2 DNA Methyltransferase Virus Protease Cancer Infection
    Hinokitiol is a component of essential oils isolated from Chymacyparis obtusa, reduces Nrf2 expression, and decreases DNMT1 and UHRF1 mRNA and protein expression, with anti-infective, anti-oxidative, and anti-tumor activities.
  • HY-N2380
    N-Benzoyl-(2R,3S)-3-phenylisoserine

    		Others Cancer
    N-Benzoyl-(2R,3S)-3-phenylisoserine is a Taxol C-13 Side Chain and crucial for the strong antitumor activity of Taxol.
  • HY-16062
    ARQ 621

    		Kinesin Cancer
    ARQ 621 is an allosteric, potent and selective inhibitor of Eg5, a microtubule-based ATPase motor protein involved in cell division. Anti-tumor activity. ARQ 621 is a kinesin inhibitor.
  • HY-117288
    S55746

    BCL201

    		 Bcl-2 Family Cancer
    S55746 (BCL201) is a potent, orally active and selective BCL-2 inhibitor, with a Ki of 1.3 nM and a Kd of 3.9 nM. S55746 (BCL201) has antitumor activity with low toxicity.
  • HY-128909
    MC-Val-Cit-PAB-rifabutin

    		Drug-Linker Conjugates for ADC Cancer
    MC-Val-Cit-PAB-rifabutin is a drug-linker conjugate for ADC with potent antitumor activity by using rifabutin (an DNA-dependent RNA polymerase inhibitor), linked via the ADC linker MC-Val-Cit-PAB.
  • HY-129545
    DS-1001b

    		Isocitrate Dehydrogenase (IDH) Cancer
    DS-1001b is a mutant IDH-1 (Isocitrate Dehydrogenase-1) inhibitor extracted from patent WO2016052697A1, Example 168, and has antitumor activity.
  • HY-137552
    MKI-1

    MASTL Kinase Inhibitor-1

    		 Others Cancer
    MKI-1, an inhibitor of MASTL (microtubule-associated serine/threonine kinase-like) with an IC50 of 9.9 μM, exerts antitumor and radiosensitizer activities through PP2A activation in breast cancer.
  • HY-136320
    MC-VC-PABC-SP 141

    		Drug-Linker Conjugates for ADC MDM-2/p53 Cancer
    MC-VC-PABC-SP 141 is a drug-linker conjugate for ADC with potent antitumor activity by using SP 141 (a potent MDM2 inhibitor), linked via the cleavable ADC linker MC-VC-PABC.
  • HY-N0103A
    Sophocarpine monohydrate

    		Autophagy Apoptosis PI3K Akt Influenza Virus Cancer Infection Inflammation/Immunology
    Sophocarpine (monohydrate) is one of the significant alkaloid extracted from the traditional herb medicine Sophora flavescens which has many pharmacological properties such as anti-virus, anti-tumor, anti-inflammatory. Sophocarpine (monohydrate) significantly inhibits the growth of gastric cancer (GC) cells through multiple mechanisms such as induction of autophagy, activation of cell apoptosis and down-regulation of cell survival PI3K/AKT signaling pathway. Sophocarpine (monohydrate) has been demonstrated to have anti-tumor activity in various cancer cells, including hepatocellular carcinoma, prostate cancer and colorectal cancer.
  • HY-16961A
    Sitravatinib malate

    MGCD516 malate; MG-516 malate

    		 VEGFR c-Kit FLT3 Discoidin Domain Receptor Trk Receptor Cancer Inflammation/Immunology
    Sitravatinib malate (MGCD516 malate) is an orally bioavailable receptor tyrosine kinase (RTK) inhibitor with IC50s of 1.5 nM, 2 nM, 2 nM, 5 nM, 6 nM, 6 nM, 8 nM, 0.5 nM, 29 nM, 5 nM, and 9 nM for Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT, FLT3, DDR2, DDR1, TRKA, TRKB, respectively. Sitravatinib malate shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment.
  • HY-N0103
    Sophocarpine

    		Autophagy Apoptosis PI3K Akt Influenza Virus Cancer Infection Inflammation/Immunology
    Sophocarpine is one of the significant alkaloid extracted from the traditional herb medicine Sophora flavescens which has many pharmacological properties such as anti-virus, anti-tumor, anti-inflammatory. Sophocarpine significantly inhibits the growth of gastric cancer (GC) cells through multiple mechanisms such as induction of autophagy, activation of cell apoptosis and down-regulation of cell survival PI3K/AKT signaling pathway. Sophocarpine has been demonstrated to have anti-tumor activity in various cancer cells, including hepatocellular carcinoma, prostate cancer and colorectal cancer.
  • HY-101566A
    Elimusertib hydrochloride

    BAY 1895344 hydrochloride

    		 ATM/ATR Cancer
    Elimusertib (BAY 1895344) hydrochloride is a potent, orally active and selective ATR inhibitor with an IC50 of 7 nM. Elimusertib hydrochloride has anti-tumor activity. Elimusertib hydrochloride can be used for the research of solid tumors and lymphomas.
  • HY-12628
    GNE-618

    		NAMPT Cancer
    GNE-618 is a potent, orally active nicotinamide phosphoribosyl transferase (NAMPT) inhibitor with an IC50 of 6 nM. GNE-618 depletes NAD levels and induces tumor cell death. Anti-tumor activity.
  • HY-10981A
    Lenvatinib mesylate

    E7080 mesylate

    		 VEGFR FGFR PDGFR RET c-Kit Cancer
    Lenvatinib mesylate (E7080 mesylate), an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities.
  • HY-125506
    NP-G2-044

    		Others Cancer
    NP-G2-044 is a potent, orally active fascin inhibitor, with an IC50 of ~2 μM. NP-G2-044 blocks tumor metastasis and increases antitumor immune response.
  • HY-116446
    Pironetin

    		Microtubule/Tubulin Cancer
    Pironetin is an α/β unsaturated lactone isolated from Streptomyces species. Pironetin binds to α-tubulin and is a potent inhibitor of microtubule polymerization, and has cell cycle arrest and antitumor activity.
  • HY-126682
    Mal-VC-PAB-DM1

    		Drug-Linker Conjugates for ADC Cancer
    Mal-VC-PAB-DM1 is a drug-linker conjugate for ADC with potent antitumor activity by using DM1 (a potent microtubule-disrupting agent), linked via the ADC linker Mal-VC-PAB .
  • HY-B0109
    Dorzolamide

    L671152; MK507

    		 Carbonic Anhydrase Cancer
    Dorzolamide (L671152) is a potent carbonic anhydrase II inhibitor, with IC50 values of 0.18 nM and 600 nM for red blood cell CA-II and CA-I respectively. Dorzolamide possesses anti-tumor activity.
  • HY-114244
    USL311

    		CXCR Cancer Endocrinology
    USL311 is a selective CXCR4 antagonist, with anti-tumor activity. USL311 prevents the binding of stromal-cell derived factor-1 (SDF-1 or CXCL12) to CXCR4.
  • HY-125916
    Pseurotin A

    		Others Cancer
    Pseurotin A, a secondary metabolite of Aspergillus and other fungi, is a competitive inhibitor of chitin synthase and a neuritogenic agent. Pseurotin A inhibits IgE production (IC50=3.6 μM). Antitumor activity.
  • HY-126693
    SC-VC-PAB-DM1

    		Drug-Linker Conjugates for ADC Cancer
    SC-VC-PAB-DM1 is a drug-linker conjugate for ADC with with potent antitumor activity by using DM1 (Mertansine, a tubulin inhibitor) , linked via the ADC linker SC-VC-PAB.
  • HY-10981
    Lenvatinib

    E7080

    		 VEGFR FGFR PDGFR c-Kit RET Cancer
    Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities.
  • HY-N2113
    Glaucocalyxin B

    		Autophagy Cancer
    Glaucocalyxin B is an ent kaurane diterpenoid isolated from the Chinese traditional medicine Rabdosia japonica with anticancer and antitumor activity; decreases the growth of HL-60 cells with an IC50 of approximately 5.86 μM at 24 h.
  • HY-B0109A
    Dorzolamide hydrochloride

    L671152 hydrochloride; MK507 hydrochloride

    		 Carbonic Anhydrase Others
    Dorzolamide (L671152) hydrochloride is a potent carbonic anhydrase II inhibitor, with IC50 values of 0.18 nM and 600 nM for red blood cell CA-II and CA-I respectively. Dorzolamide possesses anti-tumor activity.
  • HY-128904
    MC-Val-Cit-PAB-duocarmycin

    		Drug-Linker Conjugates for ADC Cancer
    MC-Val-Cit-PAB-duocarmycin is a drug-linker conjugate for ADC with potent antitumor activity by using duocarmycin (a DNA minor groove binding alkylating agent), linked via the ADC linker MC-Val-Cit-PAB.
  • HY-135145
    CB-103

    		Notch Cancer
    CB-103 is a first-in-class, orally active protein-protein interaction (PPI) inhibitor of the NOTCH transcriptional activation complex. CB-103 has anti-tumor activity.
  • HY-N4210
    Yadanziolide A

    		Others Cancer Infection
    Yadanziolide A, isolated from the cultivated dry seeds of Brucea javanica, has strong antiviral activities with IC50 of 5.5 μM against tobacco mosaic virus. Yadanziolide A shows significant antitumor effects.
  • HY-N6990
    Anhydrosecoisolariciresinol

    		Others Cancer
    Anhydrosecoisolariciresinol is from the flower of Wedelia biflora, has anti-tumor activities. Anhydrosecoisolariciresinol decreases the growth of human breast cancer MCF-7 and MDA-MB-231 cell lines.
  • HY-135815A
    Mobocertinib succinate

    TAK-788 succinate; AP32788 succinate

    		 EGFR Cancer
    Mobocertinib succinate (TAK-788 succinate) is a potent and orally active inhibitor of EGFR and HER2 oncogenic mutants, including exon 20 insertions, with selectivity over WT EGFR. Antitumor activity.
  • HY-128894
    MC-Sq-Cit-PAB-Dolastatin10

    		Drug-Linker Conjugates for ADC Cancer
    MC-Sq-Cit-PAB-Dolastatin10 is a drug-linker conjugate for ADC with potent antitumor activity by using Dolastatin10 (a tubulin polymerization inhibitor), linked via the ADC linker MC-Sq-Cit-PAB.
  • HY-N0250
    Saikosaponin D

    		STAT NF-κB Estrogen Receptor/ERR Bacterial Cancer Infection Inflammation/Immunology
    Saikosaponin D is a triterpene saponin isolated from Bupleurum, with anti-inflammatory, anti-bacterial, anti-tumor, and anti-allergic activities; Saikosaponin D inhibits selectin, STAT3 and NF-kB and activates estrogen receptor-β.
  • HY-111407
    MK-8353

    SCH900353

    		 ERK Cancer
    MK-8353 (SCH900353) is a potent, selective and orally available ERK1/2 inhibitor, with IC50s of 23.0 nM and 8.8 nM, respectively; MK-8353 has antitumor activity.
  • HY-77554
    Cephalomannine

    		Microtubule/Tubulin Cancer
    Cephalomannine is a Paclitaxel (HY-B0015) alkaloidal analog and isolated from most Cephalotaxus species. Cephalomannine is an orally active anti-tumor agent and can be used as a chemotherapy agent for cancer research.
  • HY-14949C
    Cevipabulin fumarate

    TTI-237 fumarate

    		 Microtubule/Tubulin Cancer
    Cevipabulin fumarate (TTI-237 fumarate) is an oral, microtubule-active, antitumor compound and inhibits the binding of [ 3H]NSC 49842 to tubulin, with an IC50 of 18-40 nM for cytotoxicity in human tumor cell line.
  • HY-N2357
    Eudesmin

    (-)-Eudesmin; Eudesmine; (-)-Eudesmine

    		 Ribosomal S6 Kinase (RSK) Cancer Infection Metabolic Disease Inflammation/Immunology
    Eudesmin ((-)-Eudesmin) impairs adipogenic differentiation via inhibition of S6K1 signaling pathway. Eudesmin possesses diverse therapeutic effects, including anti-tumor, anti-inflammatory, and anti-bacterial activities.
  • HY-N0405
    Orientin

    		Others Cancer Neurological Disease
    Orientin is a naturally occurring bioactive flavonoid that possesses diverse biological properties, including anti-inflammation, anti-oxidative, anti-tumor, and cardio protection. Orientin is a promising neuroprotective agent suitable for therapy for neuropathic pain.
  • HY-15579A
    MMAF hydrochloride

    Monomethylauristatin F hydrochloride

    		 Microtubule/Tubulin ADC Cytotoxin Cancer
    MMAF (Monomethylauristatin F) hydrochloride is a potent tubulin polymerization inhibitor and is used as a antitumor agent. MMAF hydrochloride is widely used as a cytotoxic component of antibody-drug conjugates (ADCs) such as Vorsetuzumab mafodotin and SGN-CD19A.
  • HY-111192
    IPR-803

    		Ser/Thr Protease Cancer
    IPR-803 is a potent inhibitor of the uPAR•uPA protein-protein interaction (PPI). IPR-803 binds directly to uPAR with sub-micromolar affinity. IPR-803 displays anti-tumor activity.
  • HY-P1404
    R8-T198wt

    		Pim Cancer
    R8-T198wt is a cell-permeable carboxyl-terminal p27 Kip1 peptide exhibits anti-tumor activity by inhibiting Pim-1 kinase.
  • HY-N2108
    7-Ethylcamptothecin

    		Others Cancer
    7-Ethylcamptothecin is one of camptothecin analogues. camptothecin (CPT), a cytotoxic alkaloid isolated from Camptotheca acuminate, is shown to have strong antitumor activity against L1210 leukemia and Walker 256 carcinosarcoma models.
  • HY-108472
    Loxoribine

    7-Allyl-8-oxoguanosine; RWJ 21757

    		 Toll-like Receptor (TLR) Influenza Virus Cancer Infection
    Loxoribine (7-Allyl-8-oxoguanosine) is a guanosine analog with anti-viral and anti-tumor activities. Loxoribine is an orally bioavailable and selective Toll-like receptor (TLR) 7 agonist.
  • HY-105019A
    Melflufen hydrochloride

    Melphalan flufenamide hydrochloride

    		 DNA Alkylator/Crosslinker Apoptosis Cancer
    Melflufen (Melphalan flufenamide) hydrochloride, a dipeptide prodrug of Melphalan, is an alkylating agent. Melflufen hydrochloride shows antitumor activity against multiple myeloma (MM) cells and inhibits angiogenesis. Melflufen hydrochloride induces irreversible DNA damage and cytotoxicity in MM cells.
  • HY-101566
    Elimusertib

    BAY 1895344

    		 ATM/ATR Cancer
    Elimusertib (BAY-1895344) is a potent, orally active and selective ATR inhibitor with an IC50 of 7 nM. Elimusertib has anti-tumor activity. Elimusertib can be used for the research of solid tumors and lymphomas.
  • HY-N1984
    Artemisic acid

    Qing Hao acid; Artemisinic acid; Arteannuic acid

    		 Bacterial Cancer Infection Metabolic Disease Inflammation/Immunology
    Artemisinic acid (Qing Hao acid), an amorphane sesquiterpene isolated from Artemisia annua L., possesses a variety of pharmacological activity, such as antimalarial activity, anti-tumor activity, antipyretic effect, antibacterial activity, allelopathy effect and anti-adipogenesis effect.
  • HY-105019
    Melflufen

    Melphalan flufenamide

    		 DNA Alkylator/Crosslinker Apoptosis Cancer
    Melflufen (Melphalan flufenamide), a dipeptide prodrug of Melphalan, is an alkylating agent. Melflufen shows antitumor activity against multiple myeloma (MM) cells and inhibits angiogenesis. Melflufen induces irreversible DNA damage and cytotoxicity in MM cells.
  • HY-129167
    Menin-MLL inhibitor 4

    		Epigenetic Reader Domain Cancer
    Menin-MLL inhibitor 4 is an inhibitor of Menin- MLL (mixed-lineage leukemia protein) interaction extracted from patent WO2017214367, compound example 1. Menin-MLL inhibitor 4 has antitumor activity.
  • HY-128759
    DYRKs-IN-2

    		DYRK Cancer
    DYRKs-IN-2 (Example 132) is a potent DYRKs inhibitor with IC50s of 30.6 nM and 12.8 nM for DYRK1B and DYRK1A, respectively. DYRKs-IN-2 has antitumor activity.
  • HY-100763
    Mcl1-IN-12

    		Bcl-2 Family Cancer
    Mcl1-IN-12 (Compound F) is a selective Mcl-1 inhibitor, less potent at Bcl-2, with Kis of 0.29 and 3.1 μM, respectively. Anti-tumor activity.
  • HY-N2000
    Bellidifolin

    		HIV Cancer Infection Inflammation/Immunology
    Bellidifolin is a xanthone isolated from the stems of Swertia punicea, with hepatoprotective, hypoglycemic, anti-oxidation, anti-inflammatory and antitumor activities. Bellidifolin also acts as a viral protein R (Vpr) inhibitor.
  • HY-N1373
    Sophoridine

    		Apoptosis Cancer
    Sophoridine is a quinolizidine alkaloid isolated from leafs of Leguminous plant Sophora alopecuroides.L. Sophoridine induces apoptosis. Sophoridine has the potential to be a novel, potent and selective antitumor drug candidate for pancreatic cancer with well-tolerated toxicity.
  • HY-111183
    Neocarzinostatin

    		DNA/RNA Synthesis Bacterial Apoptosis Antibiotic Cancer Infection
    Neocarzinostatin, a potent DNA-damaging, anti-tumor antibiotic, recognizes double-stranded DNA bulge and induces DNA double strand breaks (DSBs). Neocarzinostatin induces apoptosis. Neocarzinostatin has potential for EpCAM-positive cancers treatment .
  • HY-N7766
    Rubropunctatin

    		Apoptosis Cancer Inflammation/Immunology
    Rubropunctatin, an orange azaphilone pigment, is isolated from the extracts of Monascus pilosus-fermented rice (red-mold rice). Rubropunctatin has anti-inflammatory, immunosuppressive and antioxidative effects, and also exhibits anti-tumor activity.
  • HY-P1687
    Siomycin A

    		Bacterial Apoptosis Cancer
    Siomycin A is a thiopeptide antibiotic and is a Forkhead box M1(FOXM1) selective inhibitor without affecting other members of the Forkhead box family. Siomycin A has anti-tumor and promotes apoptosis.
  • HY-10991
    MGCD-265 analog

    		c-Met/HGFR VEGFR Apoptosis Cancer
    MGCD-265 analog is a potent and oral active inhibitor of c-Met and VEGFR2 tyrosine kinases, with IC50s of 29 nM and 10 nM, respectively. MGCD-265 analog has significant antitumor activity.
  • HY-126681
    SC-VC-PAB-MMAE

    		Drug-Linker Conjugates for ADC Cancer
    SC-VC-PAB-MMAE is a drug-linker conjugate for ADC with potent antitumor activity by using the anti-mitotic agent, monomethyl auristatin E (MMAE, a tubulin inhibitor), linked via the cleavable linker SC-VC-PAB.
  • HY-N2135
    Puerarin 6''-O-Xyloside

    		Apoptosis Cancer Inflammation/Immunology
    Puerarin 6''-O-Xyloside, isolated from radix of Pueraria lobata (Willd.), possesses snti-osteoporotic and anti-tumor activity. Puerarin 6''-O-Xyloside induces the mitochondria-mediated apoptosis pathway..
  • HY-126683
    Mal-C6-α-Amanitin

    		Drug-Linker Conjugates for ADC Cancer
    Mal-C6-α-Amanitin is a drug-linker conjugate for ADC with potent antitumor activity by using α-Amanitin (an RNA polymerase II inhibitor), linked via the ADC linker Mal-C6.
  • HY-108477
    TMPyP4 tosylate

    TMP 1363

    		 G-quadruplex Telomerase Cancer
    TMPyP4 tosylate (TMP 1363) is a quadruplex-specific ligand, which inhibits the interaction between G-quadruplexes and IGF-1. TMPyP4 tosylate (TMP 1363) is a telomerase inhibitor with antitumor effects in osteosarcoma cell lines.
  • HY-N1376
    (20R)-Ginsenoside Rg3

    (20R)-Propanaxadiol; R-ginsenoside Rg3

    		 Others Cancer
    (20R)-ginsenoside Rg3 ((20R)-Propanaxadiol), one of the active compounds present in ginseng root, inhibits vascular endothelial growth factor (VEGF)(IC50=10 nM) and antitumor activities.
  • HY-15575
    VcMMAE

    mc-vc-PAB-MMAE

    		 Drug-Linker Conjugates for ADC Microtubule/Tubulin Cancer
    VcMMAE (mc-vc-PAB-MMAE) is a drug-linker conjugate for ADC with potent antitumor activity by using the anti-mitotic agent, monomethyl auristatin E (MMAE, a tubulin inhibitor), linked via the lysosomally cleavable dipeptide, valine-citrulline (vc).
  • HY-138696
    XL092

    		TAM Receptor c-Met/HGFR Cancer
    XL092 is a potent inhibitor of the activity of Axl, Mer and C-Met kinase with IC50s of <10 nM, respectively. XL092 exhibits anti-tumor activity and has the potential for kinase-dependent diseases and conditions research.
  • HY-N2420
    Flavokawain A

    		Apoptosis Cancer
    Flavokawain A, a proming anticarcinogenic agent, is a chalcone from kava extract with anti-tumor activity. Flavokawain A induces cell apoptosis by involvement of Bax protein-dependent and mitochondria-dependent apoptotic pathway. Flavokawain A has the potential for the study of bladder cancer.
  • HY-13744
    Rubitecan

    RFS 2000; 9-Nitrocamptothecin

    		 Topoisomerase Cancer
    Rubitecan (RFS 2000), a Camptothecin derivative, is an orally active topoisomerase I inhibitor with broad antitumor activity, and induces protein-linked DNA single-strand breaks, thereby blocking DNA and RNA synthesis in dividing cells.
  • HY-15579B
    MMAF sodium

    Monomethylauristatin F sodium

    		 Microtubule/Tubulin ADC Cytotoxin Cancer
    MMAF sodium (Monomethylauristatin F sodium) is a potent tubulin polymerization inhibitor and is used as a antitumor agent. MMAF sodium (Monomethylauristatin F sodium) is widely used as a cytotoxic component of antibody-drug conjugates (ADCs) such as Vorsetuzumab mafodotin and SGN-CD19A.
  • HY-N3085
    Phellamurin

    		P-glycoprotein Apoptosis Cancer Metabolic Disease
    Phellamurin is a plant flavonone glycoside from the leaves of Phellodendron amurense and inhibits intestinal P-glycoprotein. Phellamurin also inhibits egg laying by Papilio protenor. Phellamurin induces cells apoptosis and has anti-tumor activity.
  • HY-124711
    TBOPP

    		Others Cancer
    TBOPP is a selective inhibitor of DOCK1 with an IC50 of 8.4 μM. TBOPP binds to the DOCK1 DHR-2 domain with high affinity (Kd of 7.1 μM), has anti-tumor activity for broader types of tumors.
  • HY-107981
    LSN 3213128

    		Antifolate Cancer
    LSN 3213128 is a selective, nonclassical, orally bioavailable antifolate with potent and specific inhibitory activity for aminoimidazole-4-carboxamide ribonucleotide formyltransferase (AICARFT), with IC50 of 16 nM for AICARFT enzyme inhibiton and 19 nM in cells. Anti-tumor activity.
  • HY-N6961
    Lapachol

    		Bacterial Fungal Influenza Virus Parasite Cancer Infection Inflammation/Immunology
    Lapachol is a naphthoquinone that was first isolated from Tabebuia avellanedae (Bignoniaceae). Lapachol shows anti-abscess, anti-ulcer, antileishmanial, anticarcinomic, antiedemic, anti-inflammatory, antimalarial, antiseptic, antitumor, antiviral, antibacterial, antifungal and pesticidal activities.
  • HY-B0486
    Lonidamine

    AF-1890; Diclondazolic Acid; DICA

    		 Hexokinase Mitochondrial Metabolism Apoptosis Cancer
    Lonidamine (AF-1890), an antitumor agent, is a hexokinase, mitochondrial pyruvate carrier (Ki 2.5 μM in isolated rat liver mitochondria) and plasma membrane monocarboxylate transporters inhibitor, which also inhibits mitochondrial complex II.
  • HY-122306
    Ansatrienin B

    Mycotrienin II

    		 Antibiotic Bacterial Cancer Infection
    Ansatrienin B (Mycotrienin II) is an ansamycin antibiotic isolated from Streptomyces. Ansatrienin B is active against fungi and yeasts, but inactive against bacteria.Ansatrienin B displays antitumor antibiotic activity and can be used as an ADC Toxin.
  • HY-129055
    Isoeleutherin

    		Fungal Inflammation/Immunology
    Isoeleutherin is a naphthopyran derivative isolated from E. americana Merr. Et Heyne with anti-fungal, anti-viral, and anti-tumor activities. Isoeleutherin plays an important role in selective modulation of T helper cell-mediated immune responses.
  • HY-112607
    Tubulin inhibitor 1

    		Microtubule/Tubulin Apoptosis Cancer
    Tubulin inhibitor 1 is a tubulin inhibitor, inhibits tubulin polymerization. Tubulin inhibitor 1 shows potent anti-tumor activity, casues cellular mitotic arrest in the G2/M phase, and induces cellular apoptosis.
  • HY-B1714
    NSC 601980 (analog)

    		Others Cancer
    NSC 601980 analog is the analog of the NSC601980, NSC601980 shows antitumor activity in the yeast screening experiment, which can inhibit cell proliferation in the COLO 205 and HT29 with Log GI 50 of -6.6 and -6.9 respectively.
  • HY-15579
    MMAF

    Monomethylauristatin F

    		 Microtubule/Tubulin ADC Cytotoxin Cancer
    MMAF (Monomethylauristatin F) is a potent tubulin polymerization inhibitor and is used as a antitumor agent. MMAF (Monomethylauristatin F) is widely used as a cytotoxic component of antibody-drug conjugates (ADCs) such as vorsetuzumab mafodotin and SGN-CD19A.
  • HY-15528
    kb NB 142-70

    		PKD Cancer
    kb NB 142-70 is a potent PKD inhibitor, with IC50s of 28.3, 58.7 and 53.2 nM for PKD1, PKD2, and PKD3, respectively. kb NB 142-70 also has antitumor activity.
  • HY-N6011
    9-Methoxycamptothecin

    		Topoisomerase Apoptosis Cancer
    9-Methoxycamptothecin (MCPT), isolated from Nothapodytes foetida, has antitumor activities through topoisomerase inhibition. 9-Methoxycamptothecin (MCPT) induces strong G2/M arrest and apoptosis in cancer.
  • HY-N0835
    (20S)-Protopanaxatriol

    20(S)-APPT; g-PPT

    		 Glucocorticoid Receptor Estrogen Receptor/ERR LXR Apoptosis Endocrinology Cardiovascular Disease
    (20S)-Protopanaxatriol is a metabolite of ginsenoside, works through the glucocorticoid receptor (GR) and oestrogen receptor (ER), and is also a LXRα inhibitor. (20S)-Protopanaxatriol shows a broad spectrum of antitumor effects.
  • HY-130812
    Gemcitabine-O-Si(di-iso)-O-Mc

    		Drug-Linker Conjugates for ADC Cancer
    Gemcitabine-O-Si(di-iso)-O-Mc is a drug-linker conjugate for ADC with potent antitumor activity by using Gemcitabine (a pyrimidine nucleoside analog antimetabolite and an antineoplastic agent; HY-17026), linked via the ADC linker.
  • HY-126684
    Mal-PEG4-VC-PAB-DMEA-Seco-Duocarmycin SA

    		Drug-Linker Conjugates for ADC Cancer
    Mal-PEG4-VC-PAB-DMEA-Seco-Duocarmycin SA is a drug-linker conjugate for ADC by using the antitumor antibiotic, Duocarmycin SA, linked via Mal-PEG4-VC-PAB-DMEA-Seco.
  • HY-N7046
    Silybin B

    		Amyloid-β Cancer Neurological Disease
    Silybin B, a flavonolignan separated from Silybum marianum, has anti-tumor activity. Silybin B is the most potent antifibrillogenic and anti-oligomeric component of silymarin and proposes it as a promising anti Alzheimer’s disease drug candidate.
  • HY-100219
    CB1151

    		VD/VDR Cancer
    CB1151 is a 20-epi analogue of 1,25 dihydroxyvitamin D3 (VD) with potent anti-tumor effects. CB1151 inhibits MCF-7 cell growth with an IC50 value of 0.82 nM.
  • HY-131003A
    Taletrectinib free base

    DS-6051b free base; AB-106 free base

    		 ROS Cancer
    Taletrectinib (DS-6051b) free base is a potent, orally active, and new-generation selective ROS1/NTRK inhibitor. Taletrectinib free base potently inhibits recombinant ROS1, NTRK1, and NTRK3 with IC50s of 0.207, 0.622, 2.28, and 0.98 nM, respectively. Taletrectinib free base also inhibits ROS1 G2032R and other Crizotinib-resistant ROS1 mutants.
  • HY-129478
    TC11

    		Caspase Bcl-2 Family CDK Cancer
    TC11 is a MCL1 degradator and Caspase-9 and CDK1 activator. TC11 structurally relates to immunomodulatory drugs as phenylphthalimide derivative. TC11 induces apoptotic death caused by degradation of MCL1 during prolonged mitotic arrest.
  • HY-141512
    JB170

    		PROTAC and Building Blocks Aurora Kinase Cancer
    JB170 is a potent and highly specific PROTAC-mediated AURORA-A degrader (DC50=28 nM) by linking Alisertib, to the CEREBLON-binding molecule Thalidomide. JB170 preferentially binds AURORA-A (EC50=193 nM) over AURORA-B (EC50=1.4 µM). JB170-mediated S-phase arrest is caused specifically by AURORA-A depletion. JB170 has excellent ability to inhibit non-catalytic function of AURORA-A kinase.
  • HY-109015S
    Tucidinostat D4

    Chidamide D4; HBI-8000 D4; CS 055 D4

    		 HDAC Cancer
    Tucidinostat D4 (Chidamide D4) is the deuterium labeled Tucidinostat. Tucidinostat is a potent and orally bioavailable HDAC enzymes class I (HDAC1/2/3) and class IIb (HDAC10) inhibitor, with IC50s of 95, 160, 67 and 78 nM, respectively.
  • HY-D0713
    7ACC2

    		Monocarboxylate Transporter Mitochondrial Metabolism Cancer
    7ACC2 is a potent monocarboxylate transporter (MCT) inhibitor with an IC50 of 11 nM for inhibition of [ 14C]-lactate influx. 7ACC2 is also a potent inhibitor of mitochondrial pyruvate transport. 7ACC2 is an anticancer agent through inhibition of lactate flux.
  • HY-131188
    PROTAC Bcl-xL degrader-1

    		PROTAC and Building Blocks Bcl-2 Family Cancer
    PROTAC Bcl-xL degrader-1 is a PROTAC that comprises a Bcl-xL ligand binding group, a linker and an IAP E3 ligases binding group. PROTAC Bcl-xL degrader-1 is a potent Bcl-xL degrader, and shows toxicity for human platelets and MyLa 1929 cells with IC50 values of 62 nM and 8.5 μM, respectively.
  • HY-13775
    XL019

    		JAK Apoptosis Cancer
    XL019 is a potent, orally active, and selective JAK2 inhibitor, with IC50s of 2.2, 134.3, and 214.2 nM for JAK2, JAK1 and JAK3, respectively. XL019 shows 50-fold or greater selectivity for JAK2, versus a panel of over 100 serine/threonine and tyrosine kinases, including other members of the JAK family. XL019 potently inhibits STAT3 and STAT5 phosphorylation in cells harboring either JAK2V617F or wild-type JAK2.
  • HY-131003
    Taletrectinib

    DS-6051b; AB-106

    		 ROS Cancer
    Taletrectinib (DS-6051b) is a potent, orally active, and new-generation selective ROS1/NTRK inhibitor. Taletrectinib potently inhibits recombinant ROS1, NTRK1, and NTRK3 with IC50s of 0.207, 0.622, 2.28, and 0.98 nM, respectively. Taletrectinib also inhibits ROS1 G2032R and other Crizotinib-resistant ROS1 mutants.
  • HY-130518
    Cdc7-IN-6

    		CDK Cancer
    Cdc7-IN-6 (compound I-D) is a potent Cdc7 kinase inhibitor (IC50=4 nM), extracted from patent WO2019165473A1, compound I- D, has anti-tumor activity.
  • HY-N4121
    Isocurcumenol

    		Estrogen Receptor/ERR Apoptosis Cancer
    Isocurcumenol, an estrogen receptor alpha (ERα) inhibitor isolated from Curcuma zedoaria Rhizomes, possesses anti-tumor acticity, with IC50 values of 99.1µg/mL and 178.2 µg/mL in DLA and KB cells, respectively.
  • HY-N2463
    Kushenol E

    		Indoleamine 2,3-Dioxygenase (IDO) Cancer
    Kushenol E is a class of flavonoids isolated from Sophora flavescens and is a non-competitive indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor with an IC50 of 7.7 µM and a Ki of 9.5 µM, has anti-tumor activity.
  • HY-N6674
    Diazepinomicin

    ECO-4601; TLN-4601; BU 4664L

    		 Ras Apoptosis Cancer
    Diazepinomicin (TLN-4601) is a secondary metabolite produced by Micromonospora sp. Diazepinomicin (TLN-4601) inhibits the EGF-induced Ras-ERK MAPK signaling pathway and induces apoptosis. An anti-tumor agent for K-Ras mutant models.
  • HY-101291
    Iberdomide

    CC-220

    		 Ligand for E3 Ligase Apoptosis Inflammation/Immunology Cancer
    Iberdomide (CC-220) is an orally active and potent cereblon (CRBN) E3 ligase modulator (CELMoD) with an IC50 of ~150 nM for cereblon-binding affinity. Iberdomide, a derivative of Thalidomide (HY-14658), has antitumor and immunostimulatory activities.
  • HY-128758
    DYRKs-IN-1

    		DYRK Cancer
    DYRKs-IN-1 is a potent DYRKs (Dual-specificity tyrosine-phosphorylation-regulated kinases) inhibitor with IC50s of 5 nM and 8 nM for DYRK1A and DYRK1B, respectively. DYRKs-IN-1 has antitumor activity.
  • HY-128766
    CHK1-IN-4

    		Checkpoint Kinase (Chk) Cancer
    CHK1-IN-4 (Compound 3) is a potent checkpoint kinase 1 (chk1) inhibitor, and potently inhibits chk1 phosphorylation in the tumor cells. CHK1-IN-4 has anti-tumor activity.
  • HY-131704
    FGFR4-IN-5

    		FGFR Cancer
    FGFR4-IN-5 is a potent and selective covalent FGFR4 inhibitor with an IC50 of 6.5 nM. FGFR4-IN-5 exhibits strong anti-tumor activity in vivo and can be used for hepatocellular carcinoma research.
  • HY-N6884
    Bixin

    		Reactive Oxygen Species Cancer Inflammation/Immunology Cardiovascular Disease
    Bixin (BX), isolated from the seeds of Bixa orellana, is a carotenoid, possessing anti-inflammatory, anti-tumor and anti-oxidant activities. Bixin treatment ameliorated cardiac dysfunction through inhibiting fibrosis, inflammation and reactive oxygen species (ROS) generation.
  • HY-128758A
    DYRKs-IN-1 hydrochloride

    		DYRK Cancer
    DYRKs-IN-1 hydrochloride is a potent DYRKs (Dual-specificity tyrosine-phosphorylation-regulated kinases) inhibitor with IC50s of 5 nM and 8 nM for DYRK1A and DYRK1B, respectively. DYRKs-IN-1 hydrochloride has antitumor activity.
  • HY-109019
    Vorolanib

    CM082; X-82

    		 VEGFR PDGFR Cancer Cardiovascular Disease
    Vorolanib (CM082) is an orally active, potent multikinase VEGFR/PDGFR inhibitor. Vorolanib is a potent ATP-binding cassette (ABC) transporter inhibitor. Vorolanib is an angiogenesis inhibitor and has antitumor activity combined with ZD1839 (HY-50895).
  • HY-75161
    (-)-Menthol

    		TRP Channel Endogenous Metabolite Cancer
    (-)-Menthol is a key component of peppermint oil that binds and activates transient receptor potential melastatin 8 (TRPM8), a Ca 2+-permeable nonselective cation channel, to increase [Ca 2+]i. Antitumor activity.
  • HY-N2995
    Poricoic acid A

    Poricoic acid A(F)

    		 Others Cancer
    Poricoic acid A, isolated from Poria cocos, possesses anti-tumor activity. Poricoic acid A enhances melatonin inhibition of AKI-to-CKD transition by regulating Gas6/AxlNFκB/Nrf2 axis.
  • HY-N2040
    (20R)-Protopanaxadiol

    		Bacterial Cancer Infection
    (20R)-Protopanaxadiol is a triterpenoid saponin metabolite of 20(R)-ginsenoside Rg3 in black ginseng. (20R)-Protopanaxadiol exhibits anti-tumor activity and cytotoxicity, and potently inhibits the growth of Helicobacter pylori.
  • HY-16106
    Talazoparib

    BMN-673; LT-673

    		 PARP Cancer
    Talazoparib (BMN-673) is a highly potent, orally active PARP1/2 inhibitor.Talazoparib inhibits PARP1 and PARP2 enzyme activity with Kis of 1.2 nM and 0.87 nM, respectively. Talazoparib has antitumor activity.
  • HY-135967
    MTH1-IN-2

    		DNA/RNA Synthesis Cancer
    MTH1-IN-2 is a MutT homolog 1 (MTH1) inhibitor extracted from patent WO2016135138A1, Compound (6), MTH1-IN-2 can be used for the research of cancer. Anti-tumor activity.
  • HY-111554
    AcLys-PABC-VC-Aur0101

    		Microtubule/Tubulin Drug-Linker Conjugates for ADC Cancer
    AcLys-PABC-VC-Aur0101 is a drug-linker conjugate for ADC (anti-CXCR4 ADC) with potent antitumor activity by using Aur0101 (an auristatin microtubule inhibitor), linked via the cleavable linker AcLys-PABC-VC.
  • HY-N0889
    Ginkgetin

    		Wnt Apoptosis Autophagy Inflammation/Immunology Cancer
    Ginkgetin, a biflavone, is isolated from Ginkgo biloba leaves. Ginkgetin exhibit anti-tumor, anti-inflammatory, neuroprotective, anti-fungal activities. Ginkgetin is also a potent inhibitor of Wnt signaling, with an IC50 of 5.92 μΜ.
  • HY-107367
    Epertinib

    S-22611

    		 EGFR Cancer
    Epertinib (S-22611) is a potent, oral, reversible, and selective tyrosine kinase inhibitor of EGFR, HER2 and HER4, with IC50s of 1.48 nM, 7.15 nM and 2.49 nM, respectively. Epertinib shows potent antitumor activity.
  • HY-N7698B
    Hexa-N-acetylchitohexaose

    		Others Cancer Inflammation/Immunology
    Hexa-N-acetylchitohexaose is an inducer of disease resistance in crop plants, which could elicit an increase of lignification-related and antioxidative enzymes in soybean plants. Hexa-N-acetylchitohexaose is a substrate of lysozyme. Hexa-N-acetylchitohexaose shows antitumor effect.
  • HY-124036
    DS-7423

    		PI3K mTOR Cancer
    DS-7423 is a dual PI3K and mTOR inhibitor, with IC50 values of 15.6 nM, 34.9 nM for PI3Kα and mTOR, respectively. DS-7423 possesses anti-tumor activity.
  • HY-106381
    Aurothiomalate sodium

    		PKC Cancer Inflammation/Immunology
    Aurothiomalate sodium is a potent and selective oncogenic PKCι signaling inhibitor. Aurothiomalate sodium inhibits tumor cell proliferation and not cell apoptosis. Aurothiomalate sodium is a potent thioredoxin reductase (TrxR) inhibitor. Aurothiomalate sodium, an anti-rheumatoid agent, exhibits potent anti-tumor activity.
  • HY-N0004
    Oridonin

    NSC-250682; Isodonol

    		 Akt Bacterial Cancer Infection Inflammation/Immunology
    Oridonin (NSC-250682), a diterpenoid isolated from Rabdosia rubescens, acts as an inhibitor of AKT, with IC50s of 8.4 and 8.9 μM for AKT1 and AKT2; Oridonin possesses anti-tumor, anti-bacterial and anti-inflammatory effects.
  • HY-123055
    Adenosine dialdehyde

    		Nucleoside Antimetabolite/Analog Cancer
    Adenosine dialdehyde, a purine nucleoside analogue, is a potent inhibitor of S-Adenosylhomocysteine hydrolase (SAHH) (Ki=3.3 nM). Adenosine Dialdehyde exhibits potent anti-tumor activity in vivo and can be used for the cancer research.
  • HY-N1934
    Dihydroberberine

    		Potassium Channel HSP Cancer Inflammation/Immunology Cardiovascular Disease
    Dihydroberberine inhibits human ether-a-go-go-related gene (hERG) channels and remarkably reduces heat shock protein 90 (Hsp90) expression and its interaction with hERG. Dihydroberberine has anti-inflammatory, anti-atherosclerotic, hypolipidemic and antitumor activities.
  • HY-N0211
    Cyasterone

    		EGFR Apoptosis Cancer
    Cyasterone, a natural EGFR inhibitor, mainly isolated from Ajuga decumbens Thunb (Labiatae). Cyasterone manifests anti-proliferation effect by induced apoptosis and cell cycle arrests. Cyasterone may serves as a therapeutic anti-tumor agent against human tumors.
  • HY-108697
    PT2399

    		HIF/HIF Prolyl-Hydroxylase Cancer
    PT2399 is a potent and selective HIF-2α antagonist, which directly binds to HIF-2α PAS B domain with an IC50 of 6 nM. PT2399 displays potent antitumor activity in vivo.
  • HY-125286
    AB-680

    		CD73 Cancer
    AB-680 is a highly potent, reversible and selective inhibitor of CD73 (an ecto-nucleotidase), with a Ki of 4.9 pM for hCD73, displays >10,000-fold selectivity over related ecto-nucleotidases CD39. Anti-tumor activity.
  • HY-N0126
    Xanthone

    		Bacterial Influenza Virus Fungal Apoptosis Cancer Infection Inflammation/Immunology
    Xanthone is isolated from Mangosteen and is known to control cell division and growth, apoptosis, inflammation, and metastasis in different stages of carcinogenesis. Xanthone has anti-oxidant, anti-tumor, anti-allergic, anti-inflammatory, anti-bacterial, anti-fungal, and anti-viral activities.
  • HY-16261
    Aldoxorubicin

    INNO-206; DOXO-EMCH

    		 Topoisomerase ADC Cytotoxin Cancer
    Aldoxorubicin (INNO-206) is an albumin-binding prodrug of Doxorubicin (DNA topoisomerase II inhibitor), which is released from albumin under acidic conditions. Aldoxorubicin (INNO-206) has potent antitumor activities in various cancer cell lines and in murine tumor models.
  • HY-B0180
    Imiquimod

    R 837

    		 Toll-like Receptor (TLR) Autophagy SARS-CoV HSV Cancer Infection Inflammation/Immunology
    Imiquimod (R 837), an immune response modifier, is a selective toll like receptor 7 (TLR7) agonist. Imiquimod exhibits antiviral and antitumor effects in vivo. Imiquimod can be used for the research of external genital, perianal warts, cancer and COVID-19.
  • HY-B0180A
    Imiquimod hydrochloride

    R 837 hydrochloride

    		 Toll-like Receptor (TLR) Autophagy SARS-CoV HSV Cancer Infection Inflammation/Immunology
    Imiquimod hydrochloride (R 837 hydrochloride), an immune response modifier, is a selective toll like receptor 7 (TLR7) agonist. Imiquimod hydrochloride exhibits antiviral and antitumor effects in vivo. Imiquimod hydrochloride can be used for the research of external genital, perianal warts, cancer and COVID-19.
  • HY-136270
    Gartisertib

    VX-803; ATR inhibitor 2

    		 ATM/ATR Cancer
    ATR inhibitor 2 is an ATP-competitive, orally active, and selective ATR inhibitor, with a Ki of <150 pM. ATR inhibitor 2 potently inhibits ATR-driven phosphorylated checkpoint kinase-1 (Chk1) phosphorylation with an IC50 of 8 nM. Antitumor activity.
  • HY-110120
    DSR-6434

    		Toll-like Receptor (TLR) Cancer
    DSR-6434 is a potent and selective Toll-like receptor 7 (TLR7) agonist, with EC50s of 7.2 nM and 4.6 nM for human and mice TLR7, respectively. DSR-6434 has a strong antitumor effect.
  • HY-111388
    SEL120-34A

    		CDK Cancer
    SEL120-34A is a potent, selective, orally available, ATP-competitive CDK8 inhibitor, with IC50s of 4.4 nM and 10.4 nM for CDK8/CycC and CDK19/CycC, respectively, with antitumor activity.
  • HY-B0180B
    Imiquimod maleate

    R 837 maleate

    		 Toll-like Receptor (TLR) Autophagy SARS-CoV HSV Cancer Infection Inflammation/Immunology
    Imiquimod maleate (R 837 maleate), an immune response modifier, is a selective toll like receptor 7 (TLR7) agonist. Imiquimod maleate exhibits antiviral and antitumor effects in vivo. Imiquimod maleate can be used for the research of external genital, perianal warts, cancer and COVID-19.
  • HY-111388B
    SEL120-34A HCl

    		CDK Cancer
    SEL120-34A HCl is a potent, selective, orally available, ATP-competitive CDK8 inhibitor, with IC50s of 4.4 nM and 10.4 nM for CDK8/CycC and CDK19/CycC, respectively, with antitumor activity.
  • HY-12678
    Entrectinib

    NMS-E628; RXDX-101

    		 ROS Trk Receptor ALK Autophagy Cancer
    Entrectinib (NMS-E628) is a potent, orally available, and CNS-active pan-Trk, ROS1, and ALK inhibitor. Entrectinib inhibits TrkA, TrkB, TrkC, ROS1 and ALK with IC50 values of 1, 3, 5, 12 and 7 nM, respectively. Antitumor activity.
  • HY-107367A
    Epertinib hydrochloride

    S-22611 hydrochloride

    		 EGFR Cancer
    Epertinib hydrochloride (S-22611 hydrochloride) is a potent, orally active, reversible, and selective tyrosine kinase inhibitor of EGFR, HER2 and HER4, with IC50s of 1.48 nM, 7.15 nM and 2.49 nM, respectively. Epertinib hydrochloride shows potent antitumor activity.
  • HY-N0289
    Lycorine hydrochloride

    		Autophagy Bacterial Virus Protease Cancer Inflammation/Immunology
    Lycorine hydrochloride is the main active ingredient of the herbal medicine derived from Lycoris radia and is also a melanoma vasculogenic inhibitor and has anti-tumor activity. Lycorine hydrochloride effectively inhibits mitotic proliferation of Hey1B cells (IC50 of 1.2 μM).
  • HY-N6623
    Malvidin-3-galactoside chloride

    		Apoptosis ROS Cancer
    Malvidin-3-galactoside chloride, an anthocyanin monomer, induces hepatocellular carcinoma (HCC) cells cycle arrest and apoptosis. Malvidin-3-galactoside chloride inhibits the production and accumulation of ROS. Malvidin-3-galactoside chloride has anti-tumor function.
  • HY-N8213
    Rapanone

    		Apoptosis Phospholipase Bacterial Parasite Cancer Infection Inflammation/Immunology
    Rapanone is a natural benzoquinone. Rapanone exhibits a broad spectrum of biological actions, including anti-tumor, antioxidant, anti-inflammatory, antibacterial and antiparasitic. Rapanone also is a potent and selective human synovial PLA2 inhibitor, with an IC50 of 2.6 μM.
  • HY-129393
    AB928

    		Adenosine Receptor Inflammation/Immunology
    AB928 is an orally bioavailable, selective dual adenosine receptor (A2aR/A2bR) antagonist. AB928 relieves adenosine-mediated immune suppression. AB928 has immunomodulatory and antitumor activities.
  • HY-122312
    BAY-8002

    		Monocarboxylate Transporter Cancer
    BAY-8002 is a potent, selective, orally active inhibitor of monocarboxylate transporter 1 (MCT1), with an IC50 of 85 nM in the MCT1-expressing DLD-1 cells, displays excellent selectivity against MCT4. Anti-tumor activity.
  • HY-120356A
    T-1101 tosylate

    TAI-95 tosylate

    		 Apoptosis Cancer
    T-1101 tosylate (TAI-95 tosylate) is a Hec1/Nek2 (Highly expressed in cancer 1 / NIMA-related kinase 2) inhibitor with antitumor activity. T-1101 tosylate is inactive toward normal cells, kinases and hERG
  • HY-112642
    9-Methoxycanthin-6-one

    		Others Cancer
    9-Methoxycanthin-6-one, a canthin-6-one alkaloid, is present in intact plant parts and in callus tissues of different explants. 9-Methoxycanthin-6-one shows anti-tumor activity.
  • HY-15794
    Nemorubicin

    Methoxymorpholinyl doxorubicin; FCE 23762; PNU 152243

    		 Others Cancer
    Nemorubicin (Methoxymorpholinyl doxorubicin) is a Doxorubicin derivative with potent antitumor activity. Nemorubicin is highly cytotoxic to a variety of tumor cell lines presenting a multidrug-resistant phenotype. Nemorubicin requirs an intact nucleotide excision repair (NER) system to exert its activity.
  • HY-133586
    N3-PEG4-DYKDDDD-Doxorubicin

    		Drug-Linker Conjugates for ADC Cancer
    N3-PEG4-DYKDDDD-Doxorubicin is a drug-linker conjugate for ADC with potent antitumor activity by using the cytotoxic anthracycline antibiotic, Doxorubicin, linked via the cleavable linker N3-PEG4-DYKDDDD.
  • HY-114334
    Glutaminase-IN-1

    CB839 derivative

    		 Glutaminase Cancer
    Glutaminase-IN-1 (CB839 derivative), a CB839 derivative, is an allosteric inhibitor of 1,3,4-selenadiazole-containing kidney-type glutaminase (KGA), with an IC50 of 1 nM. Glutaminase-IN-1 (CB839 derivative) shows improved cellular uptake and antitumor activity.
  • HY-N0158
    Oxymatrine

    		TGF-beta/Smad Influenza Virus Cancer Infection Inflammation/Immunology
    Oxymatrine, an alkaloid from the roots of Sophora species, with anti-inflammatory, antifibrosis, and antitumor effects, inhibits the iNOS expression and TGF-β/Smad pathway. Oxymatrine inhibits bocavirus minute virus of canines (MVC) replication, reduces viral gene expression and decreases apoptosis induced by viral infection.
  • HY-125286A
    AB-680 ammonium

    		CD73 Cancer
    AB-680 ammonium is a highly potent, reversible and selective inhibitor of CD73 (an ecto-nucleotidase), with a Ki of 4.9 pM for hCD73, displays >10,000-fold selectivity over related ecto-nucleotidases CD39. Anti-tumor activity.
  • HY-131090
    N3-PEG4-YPYDVPDYA-Doxorubicin

    		Drug-Linker Conjugates for ADC Cancer
    N3-PEG4-YPYDVPDYA-Doxorubicin is a drug-linker conjugate for ADC with potent antitumor activity by using the cytotoxic anthracycline antibiotic, Doxorubicin, linked via the cleavable linker N3-PEG4-YPYDVPDYA.
  • HY-10619B
    Niraparib tosylate

    MK-4827 tosylate

    		 PARP Apoptosis Cancer
    Niraparib tosylate (MK-4827 tosylate) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with an IC50 of 3.8 and 2.1 nM, respectively. Niraparib tosylate leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity.
  • HY-109176
    Giredestrant

    GDC-9545

    		 Estrogen Receptor/ERR Cancer
    Giredestrant (GDC-9545), a non-steroidal estrogen receptor (ER) ligand, is an orally active and selective ER antagonist. Giredestrant potently competes with Estradiol for binding and induces a conformational change within the ER ligand binding domain. Giredestrant has anti-tumor activity.
  • HY-10008
    SNS-032

    BMS-387032

    		 CDK Apoptosis Cancer
    SNS-032 (BMS-387032) is a potent and selective inhibitor of CDK2, CDK7, and CDK9 with IC50s of 38 nM, 62 nM and 4 nM, respectively. SNS-032 has antitumor effect.
  • HY-138294
    RAS/RAS-RAF-IN-1

    		Ras Raf Cancer
    RAS/RAS-RAF-IN-1 is a potent RAS and RAS-RAF inhibitor. RAS/RAS-RAF-IN-1 has a KD of 5.0 μΜ-15 μΜ for cyclophilin A (CYPA) binding affinity. RAS/RAS-RAF-IN-1 has antitumor activity.
  • HY-120697
    MSAB

    		Wnt β-catenin Cancer
    MSAB is a potent and selective inhibitor of Wnt/β-catenin signaling. MSAB binds to β-catenin promoting its degradation, and specifically downregulates Wnt/β-catenin target genes. MSAB exhibits potent anti-tumor effects selectively on Wnt-dependent cancer cells.
  • HY-100492
    Fisogatinib

    BLU-554

    		 FGFR Cancer
    Fisogatinib (BLU-554) is a potent, highly selective and orally active fibroblast growth factor receptor 4 (FGFR4) inhibitor with an IC50 of 5 nM. Fisogatinib has significant anti-tumor activity in models of hepatocellular carcinoma (HCC) that are dependent on FGFR4 signalling.
  • HY-114311
    FGFR1/DDR2 inhibitor 1

    		FGFR Discoidin Domain Receptor Cancer
    FGFR1/DDR2 inhibitor 1 is an orally active inhibitor of fibroblast growth factor receptor 1 (FGFR1) and discoindin domain receptor 2 (DDR2), with IC50 values of 31.1 nM and 3.2 nM, respectively. Antitumor activity.
  • HY-14833
    Atiratecan

    TP300

    		 Others Cancer
    Atiratecan (TP300) is a prodrug of camptothecin analog CH0793076 (HY-107096). Atiratecan does not inhibit acetylcholinesterase (AChE) activities. Atiratecan shows antitumor activity against both breast cancer resistance protein (BCRP)-positive and -negative xenografts in mouse xenograft models.
  • HY-125827
    13-Methylberberine chloride

    13-Methylberberinium chloride

    		 Others Cancer Metabolic Disease
    13-Methylberberine chloride (13-Methylberberinium chloride), a berberine analogue, has anti-adipogenic and antitumor activities. 13-Methylberberine chloride (13-Methylberberinium chloride) increases production of IL-12 and inhibits the expression of iNOS at posttranscriptional level in macrophages activated with LPS.
  • 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-100544
    FLLL32

    		STAT JAK Apoptosis Cancer
    FLLL32, a synthetic analog of curcumina, is a JAK2/STAT3 dual inhibitor with anti-tumor activity. FLLL32 can inhibit the induction of STAT3 phosphorylation by IFNα and IL-6 in breast cancer cells.
  • HY-50846
    SCH772984

    		ERK Cancer
    SCH772984 is a highly selective and ATP-competitive ERK inhibitor, with IC50s of 4 and 1 nM for ERK1 and ERK2, respectively. SCH772984 has antitumor activity in MAPK inhibitor-naïve and MAPK inhibitor-resistant cells containing BRAF or RAS mutations.
  • HY-N1231
    Sophoraflavanone G

    Kushenol F

    		 Apoptosis Cancer
    Sophoraflavanone G (Kushenol F) is iaolated from Sophora flavescens and shows anti-tumor and anti-inflammatory properties.  Sophoraflavanone G (Kushenol F) induces MDA-MB-231 and HL-60 cells apoptosis through suppression of MAPK-related pathways.
  • HY-N0393
    Glabridin

    		PPAR Reactive Oxygen Species Bacterial Cancer Infection Inflammation/Immunology
    Glabridin is a natural isoflavan from Glycyrrhiza glabra, binds to and activates PPARγ, with an EC50 of 6115 nM. Glabridin exhibits antioxidant, anti-bacterial, anti-nephritic, anti-diabetic, anti-fungal, antitumor, anti-inflammatory, antiosteoporotic, cardiovascular protective, neuroprotective and radical scavenging activities.
  • HY-10529
    Betulinic acid

    Lupatic acid; Betulic acid

    		 Apoptosis Topoisomerase HIV Autophagy Mitophagy NF-κB Endogenous Metabolite Cancer Infection Inflammation/Immunology
    Betulinic acid is a natural pentacyclic triterpenoid, acts as a eukaryotic topoisomerase I inhibitor, with an IC50 of 5 μM, and possesses anti-HIV, anti-malarial, anti-inflammatory and anti-tumor properties. Betulinic acid acts as a new activator of NF-kB.
  • HY-B0719
    Ingenol Mebutate

    Ingenol 3-angelate; PEP005

    		 PKC Cancer Inflammation/Immunology
    Ingenol Mebutate is an active ingredient in Euphorbia peplus, acts as a potent PKC modulator, with Kis of 0.3, 0.105, 0.162, 0.376, and 0.171 nM for PKC-α, PKC-β, PKC-γ, PKC-δ, and PKC-ε, respectively, and has antiinflammatory and antitumor activity.
  • HY-135903
    Giredestrant tartrate

    GDC-9545 tartrate

    		 Estrogen Receptor/ERR Cancer
    Giredestrant tartrate (GDC-9545 tartrate), a non-steroidal ER ligand, is an orally active and selective estrogen receptor (ER) antagonist. Giredestrant tartrate potently competes with estradiol for binding and induces a conformational change within the ER ligand binding domain. Anti-tumor activity.
  • HY-N0368
    Linalool

    		iGluR Apoptosis Endogenous Metabolite Cancer Cardiovascular Disease
    Linalool is natural monoterpene in essential olis of coriander, acts as a competitive antagonist of Nmethyl d-aspartate (NMDA) receptor, with anti-tumor, anti-cardiotoxicity activity.Linalool is a PPARα ligand that reduces plasma TG levels and rewires the hepatic transcriptome and plasma metabolome.
  • HY-134723
    DBCO-PEG4-GGFG-DX8951

    		Drug-Linker Conjugates for ADC Cancer
    DBCO-PEG4-GGFG-DX8951 is a drug-linker conjugate for ADC with potent antitumor activity by using DX8951 (a DNA topoisomerase I inhibitor), linked via the non-cleavable ADC linker DBCO-PEG4-GGFG.
  • HY-10619
    Niraparib

    MK-4827

    		 PARP Apoptosis Cancer
    Niraparib (MK-4827) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC50s of 3.8 and 2.1 nM, respectively. Niraparib leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity.
  • HY-128775
    JHU395

    		Others Cancer
    JHU395 is an orally-bioavailable and a plasma stable lipophilic glutamine antagonists (GA) prodrug. JHU395 delivers 6-diazo-5-oxo-L-norleucine (DON) to malignant peripheral nerve sheath tumor (MPNST) in vitro and in vivo, and has antitumor activity in MPNST.
  • HY-10619A
    Niraparib hydrochloride

    MK-4827 hydrochloride

    		 PARP Apoptosis Cancer
    Niraparib hydrochloride (MK-4827 hydrochloride) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC50s of 3.8 and 2.1 nM, respectively. Niraparib hydrochloride leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity.
  • HY-17547
    NMS-E973

    		HSP Cancer
    NMS-E973 is a potent and selective inhibitor of HSP90. NMS-E973 binds to the ATP binding site of Hsp90α with a DC50 of <10 nM. NMS-E973 is able to cross the blood-brain barrier (BBB). Antitumor efficacy.
  • HY-N0488S
    Vincristine-d3 sulfate

    		Microtubule/Tubulin Apoptosis Cancer
    Vincristine-d3 (Leurocristine-d3) sulfate is the deuterium labeled Vincristine sulfate. Vincristine sulfate is an antitumor vinca alkaloid which inhibits microtubule formation in mitotic spindle, resulting in an arrest of dividing cells at the metaphase stage. It binds to microtubule with a Ki of 85 nM.
  • HY-N7507
    Sempervirine

    		Others Cancer
    Sempervirine is an indole alkaloid isolated from Gelsemium sempervirens with anti-tumor activities. Sempervirine is against sempervirine-sensitive tumor cells with EC50 values of 2.7 μM, 1.77 μM, and 1.96 μM for Raji, MDA-MB-231 and HeLa cells, respectively.
  • HY-126297
    c-Fms-IN-10

    		c-Fms Cancer Inflammation/Immunology
    c-Fms-IN-10 is the derivative of thieno [3,2-d] pyrimidine, an kinase inhibitor of FMS (Colony stimulating factor-1 receptor, CSF-1R) with IC50 of 2 nM. c-Fms-IN-10 has anti-tumor activity.
  • HY-114989
    Fluorizoline

    		Apoptosis Cancer
    Fluorizoline selectively and directly binds to prohibitin 1 (PHB1) and 2 (PHB2), and induces apoptosis. Fluorizoline reduces chronic lymphocytic leukemia (CLL) cell viability through the upregulation of NOXA and BIM. Fluorizoline exerts antitumor action in a p53-independent manner.
  • HY-128905
    MC-Val-Cit-PAB-dimethylDNA31

    		Drug-Linker Conjugates for ADC Cancer
    MC-Val-Cit-PAB-dimethylDNA31 is a drug-linker conjugate for ADC with potent antitumor activity by using dimethylDNA31, linked via the ADC linker MC-Val-Cit-PAB. DimethylDNA31 has effective bactericidal activity against persisters and stationary-phase S. aureus.
  • HY-135147
    ONC206

    		Dopamine Receptor Cancer Neurological Disease
    ONC206 is an analogue of TRAIL inducer ONC201. ONC206 is a selective antagonist of the D2-like dopamine receptors (DRD2/3/4) at nanomolar concentrations. ONC206 has broad-spectrum anti-tumor activity.
  • HY-20878
    Tyrphostin AG 879

    AG 879

    		 Trk Receptor EGFR Apoptosis Cancer
    Tyrphostin AG 879 (AG 879) is a tyrosine kinase inhibitor that inhibits TrKA phosphorylation (IC50 of 10 μM), but not TrKB and TrKC. Tyrphostin AG 879 is also a selective ErbB2 tyrosine kinase inhibitor with an IC50 of 1 μM, and has at least 500-fold higher selectivity to ErbB2 than EGFR. Tyrphostin AG 879 has anticancer activity.
  • HY-10985
    Marizomib

    Salinosporamide A; NPI-0052

    		 Proteasome Cancer
    Marizomib (Salinosporamide A) is a second-generation, irreversible, brain-penetrant, pan-proteasome inhibitor. Marizomib inhibits the CT-L (β5), CT-T-laspase-like (C-L, β1) and trypsin-like (T-L, β2) activities of the 20S proteasome (IC50=3.5, 28, and 430 nM, respectively).
  • HY-131364
    Nur77 modulator 1

    		Others Cancer
    Nur77 modulator 1 is a good Nur77 binder (KD = 3.58 μM). Nur77 modulator 1 up-regulates Nur77 expression, mediates sub-cellular localization of Nur77, induces Nur77-dependent ER stress and autophagy, and results in cell apoptosis. Anti-hepatoma activity.
  • HY-P2316
    Epinecidin-1 TFA

    		Bacterial Antibiotic Infection
    Epinecidin-1 TFA is a multi-functional antimicrobial peptide (AMP) from Orange-spotted grouper (Epinephelus coioides). Epinecidin-1 TFA has antibacterial, antifungal, antiviral, anti-tumor, and immunomodulatory effects. Epinecidin-1 TFA has the potential to be an alternative for current antibiotics.
  • HY-101246
    RPI-1

    		RET Cancer
    RPI-1 is a specific, orally available 2-indolinone Ret tyrosine kinase inhibitor. RPI-1 inhibits proliferation, Ret tyrosine phosphorylation, Ret protein expression, and the activation of PLCgamma, ERKs and AKT in human medullary thyroid carcinoma TT cells. Antitumor activity.
  • HY-P9921
    Trastuzumab emtansine

    Ado-Trastuzumab emtansine; PRO132365; T-DM 1

    		 Antibody-Drug Conjugate (ADC) EGFR Cancer
    Trastuzumab emtansine (Ado-Trastuzumab emtansine) is an antibody-drug conjugate (ADC) that incorporates the HER2-targeted antitumor properties of trastuzumab with the cytotoxic activity of the microtubule-inhibitory agent DM1 (derivative of maytansine). Trastuzumab emtansine can be used for the research of advanced breast cancer.
  • HY-N0462
    Corilagin

    		Reverse Transcriptase Bacterial Cancer Infection Inflammation/Immunology
    Corilagin, a gallotannin, inhibits activity of reverse transcriptase of RNA tumor viruses. Corilagin inhibits the growth of Staphylococcus aureus with a MIC of 25 μg/mL. Corilagin shows good anti-tumor activity on hepatocellular carcinoma and ovarian cancer. Corilagin shows a low level of toxicity toward normal cells and tissues.
  • HY-16590
    X-376

    		ALK c-Met/HGFR Cancer
    X-376 is a potent and highly specific ALK tyrosine kinase inhibitor (TKI) (IC50=0.61 nM). X-376 is a less potent inhibitor of MET (IC50=0.69 nM). X-376 displays potent anti-tumor activity.
  • HY-N5020
    Carabrone

    		Bacterial Infection
    Carabrone is isolated from the fruits of Carpesium abrotanoides , is a well-known sesquiterpene and exhibits significant anti-bacterial and anti-tumor activities. Carabrone exhibits antifungal activities in vitro and in vivo against Botrytis cinerea, Colletotrichum lagenarium(EC50=7.10 μg/mL) and Erysiphe graminis.
  • HY-N0488S1
    Vincristine-d3-ester sulfate

    		Microtubule/Tubulin Apoptosis Cancer
    Vincristine-d3-ester (Leurocristine-d3-ester) sulfate is the deuterium labeled Vincristine sulfate. Vincristine sulfate is an antitumor vinca alkaloid which inhibits microtubule formation in mitotic spindle, resulting in an arrest of dividing cells at the metaphase stage. It binds to microtubule with a Ki of 85 nM .
  • HY-N2112
    Glaucocalyxin A

    		PI3K Akt Apoptosis Cancer
    Glaucocalyxin A, an ent-kauranoid diterpene from Rabdosia japonica var., induces apoptosis in osteosarcoma by inhibiting nuclear translocation of Five-zinc finger Glis 1 (GLI1) via regulating PI3K/Akt signaling pathway. Glaucocalyxin A has antitumor effect.
  • HY-N7422
    Kauran-16,17-diol

    ent-Kauran-16β,17-diol

    		 Apoptosis Cancer Inflammation/Immunology
    Kauran-16,17-diol (ent-Kauran-16β,17-diol), a natural diterpene, posseses anti-tumor and inducing-apoptosis activity, with a IC50 of 17 μM on inhibiting NO production in LPS-stimulated RAW 264.7 macrophages.
  • HY-137506
    XST-14

    		ULK p38 MAPK TGF-β Receptor ALK CaMK Cancer
    XST-14 is a potent, competitive and highly selective ULK1 inhibitor with an IC50 of 26.6 nM. XST-14 induces autophagy inhibition by reducing the phosphorylation of the ULK1 downstream substrate. XST-14 induces apoptosis in hepatocellular carcinoma (HCC) cells and has antitumor effects.
  • HY-N1517
    Ganoderic acid C2

    		Others Cancer
    Ganoderic acid C2 is a bioactive triterpenoid in Ganoderma lucidum. Ganoderic acid C2 possesses the potential anti-tumor bioactivity, antihistamine, anti-aging and cytotoxic effects. Ganoderic acid C2 exhibits high inhibitory activity against the rat lens aldose reductase (RLAR) with an IC50 of 3.8 µM.
  • HY-13582
    Carbendazim

    		Fungal Infection Cancer
    Carbendazim is a potent and orally active broad-spectrum benzimidazole fungicide and can be acts as a pesticide for fungal diseases research, such as Seproria, Fusarium and Sclerotina. Carbendazim is a benzimidazole (HY-Y1825) derivative with antitumor activity and used for cancer research, especially advanced solid tumors and lymphoma.
  • HY-N0646
    Silydianin

    		Phosphatase Cancer
    Silydianin is an active constituent of Silybium marianum, with exhibit anti-collagenase, antitumor and anti-elastase activities. Silydianin is a natural protein tyrosine phosphatase 1B (PTP1B) with an IC50 of 17.38 μM. Silydianin has inhibitory effect on the in vitro production and release of oxidative products.
  • HY-N9398
    3β,6α,12β-Dammar-E-20(22)-ene-3,6,12,25-tetraol

    		Sirtuin Cancer
    3β,6α,12β-Dammar-E-20(22)-ene-3,6,12,25-tetraol, a SIRT1 activator, exhibits significant stimulation of SIRT1 activity. Anti-tumor activity.
  • HY-N5112
    (Rac)-Arnebin 1

    (Rac)-β,β-Dimethylacrylalkannin; (Rac)-β,β-​Dimethylacrylshikonin

    		 Others Others
    (Rac)-Arnebin 1 ((Rac)-β,β-Dimethylacrylalkannin) is the racemate of β,β-Dimethylacrylalkannin and/or β,β-Dimethylacrylshikonin. β,β-Dimethylacrylalkannin and β,β-Dimethylacrylshikonin are napthoquinones isolated from Arnebia nobilis. β,β-Dimethylacrylshikonin has anti-tumor activity.
  • HY-N0446
    10-Methoxycamptothecin

    		Others Cancer
    10-Methoxycamptothecin is a natural bioactive derivative of camptothecin (CPT) isolated from Camptotheca acuminata, and has been confirmed to possess high anti-cancer properties. 10-Methoxycamptothecin has higher cytotoxicity than 10-hydroxycamptothecin by testing antitumor activity against 2774 cell lines.
  • HY-N6775
    Sonolisib

    PX-866

    		 PI3K Cancer
    Sonolisib (PX-866), an improved Wortmannin analogue, is an oral, irreversible, and pan-isoform inhibitor of PI3K (IC50=0.1 nM (p110α), 1.0 nM (p120γ), 2.9 nM (p110δ)). Antitumor activity.
  • HY-115400
    1V209

    TLR7 agonist T7

    		 Toll-like Receptor (TLR) Cancer
    1V209 (TLR7 agonist T7) is a Toll-like receptor 7 (TLR7) agonist and has anti-tumor effects. 1V209 can be conjugated with various polysaccharides to improve its water solubility, and enhance its efficacy, and maintain low toxicity.
  • HY-100862
    BRCA1-IN-2

    		PARP Cancer
    BRCA1-IN-2 (compound 15) is a cell-permeable protein-protein interaction (PPI) inhibitor for BRCA1 with an IC50 of 0.31 μM and a Kd of 0.3 μM, which shows antitumor activities via the disruption of BRCA1 (BRCT)2/protein interactions.
  • HY-12456
    Duocarmycin SA

    		ADC Cytotoxin DNA Alkylator/Crosslinker Cancer
    Duocarmycin SA is a potent antitumor antibiotic with an IC50 of 10 pM. Duocarmycin SA is an extremely potent cytotoxic agent capable of inducing a sequence-selective alkylation of duplex DNA. Duocarmycin SA demonstrates synergistic cytotoxicity against glioblastoma multiforme (GBM) cells treated with proton radiation in vitro.
  • HY-B0986
    Hexylresorcinol

    4-Hexylresorcinol

    		 Parasite Bacterial Apoptosis Glucosidase Cancer Infection Metabolic Disease
    Hexylresorcinol (4-Hexylresorcinol) is a natural compound found in plants with antimicrobial, anthelmintic, antiseptic and antitumor activities. Hexylresorcinol can induce apoptosis in squamous carcinoma cells. Hexylresorcinol is a reversible and noncompetitive inhibitor of α-glucosidase. Hexylresorcinol has protective effects against oxidative DNA damage.
  • HY-121993
    Combretastatin A-1

    		Microtubule/Tubulin Cancer
    Combretastatin A-1 is a microtubule polymerization inhibitor that binds to the colchicine-binding site of tubulin. Combretastatin A-1 inhibits the Wnt/β-catenin pathway through tubulin depolymerization mediated AKT deactivation. Combretastatin A-1 exhibits anti-tumor and anti-vascular effects.
  • HY-100874
    N3-PEG3-vc-PAB-MMAE

    		Drug-Linker Conjugates for ADC Cancer
    N3-PEG3-vc-PAB-MMAE is a synthesized drug-linker conjugate for ADC that incorporates the MMAE (a tubulin inhibitor ) and 3-unit PEG linker. N3-PEG3-vc-PAB-MMAE shows potent antitumor activity.
  • HY-18030A
    CEP-28122 mesylate salt

    		ALK Cancer
    CEP-28122 mesylate salt, a diaminopyrimidine derivative, is a potent, selective, and orally bioavailable ALK inhibitor, with an IC50 value of 1.9 nM for recombinant ALK kinase activity. CEP-28122 has antitumor activity in experimental models of ALK-positive human cancers. CEP-28122 mesylate salt has good pharmacodynamic and pharmacokinetic activity.
  • HY-19828
    Herboxidiene

    GEX1A

    		 DNA/RNA Synthesis Cancer
    Herboxidiene (GEX1A) is a potent phytotoxic polyketide from Streptomyces sp. A7847 with a diverse range of activities, including herbicidal, anti-cholesterol, anti-tumor effects. Herboxidiene inhibits the pre-mRNA splicing process by binding to spliceosome-associated protein (SAP) 155, a subunit of SF3b, in the splicesome.
  • HY-W009156
    Hydroxycitric acid tripotassium hydrate

    Potassium citrate monohydrate

    		 ATP Citrate Lyase HIF/HIF Prolyl-Hydroxylase Cancer Metabolic Disease Inflammation/Immunology
    Hydroxycitric acid tripotassium hydrate (Potassium citrate monohydrate) is the major active ingredient of Garcinia cambogia and a derivative of citric acid. Hydroxycitric acid tripotassium hydrate competitively inhibits ATP citrate lyase with weight loss benefits. Hydroxycitric acid tripotassium hydrate effective inhibits stones formation and also inhibits HIF, and has antioxidation, anti-inflammation and anti-tumor effects.
  • HY-N0790
    Lupeol

    Clerodol; Monogynol B; Fagarasterol

    		 Androgen Receptor Apoptosis Cancer
    Lupeol (Clerodol; Monogynol B; Fagarasterol) is an active pentacyclic triterpenoid, has anti-oxidant, anti-mutagenic, anti-tumor and anti-inflammatory activity. Lupeol is a potent androgen receptor (AR) inhibitor and can be used for cancer research, especially prostate cancer of androgen-dependent phenotype (ADPC) and castration resistant phenotype (CRPC).
  • HY-139299
    WSD0922

    		EGFR Cancer
    WSD-0922 is a potent, selective, orally active, and BBB penetrable EGFR/EGFRVIII inhibitor. WSD-0922 is against EGFRm + (EGFRvIII/Del19/L858R) with an IC50 of <10 nM. WSD0922 shows good safety profile and preclinical anti-tumor efficacy.
  • HY-137894
    PF-07104091

    		CDK GSK-3 Cancer
    PF-07104091 is a potent and selective CDK2/cyclin E1 and GSK3β inhibitor, with Kis of 1.16 and 537.81 nM, respectively. PF-07104091 has anti-tumor activity for cyclin E1-amplified cancers. (patent WO2020157652A2).
  • HY-107365
    PQR530

    		PI3K mTOR Cancer
    PQR530 is a potent, ATP-competitive, orally bioavailable and brain-penetrant dual pan-PI3K/mTORC1/2 inhibitor, with a subnanomolar Kd toward PI3Kα and mTOR (0.84 and 0.33 nM, respectively). Antitumor activity.
  • HY-100429
    CAN508

    		CDK Cancer
    CAN508 is a potent, ATP-competitive CDK9/cyclin T1 inhibitor with an IC50 of 0.35 μM. CAN508 exhibits a 38-fold selectivity for CDK9/cyclin T over other CDK/cyclin complexes. Antitumor activity.
  • HY-13454
    CID 2011756

    		PKD Cancer
    CID 2011756 is an ATP competitive PKD inhibitor, with an IC50 of 3.2 µM for PKD1 in cell free assay, and also shows cellular pan-PKD inhibitory activity against PKD2 and PKD3 (IC50, 0.6 and 0.7 µM, respectively). CID 2011756 also has antitumor activity.
  • HY-133537
    Hygrolidin

    		Antibiotic Fungal ADC Cytotoxin Cancer Infection
    Hygrolidin is a 16-membered macrolide antibiotic produced by Streptomyces hygroscopicus D-1166. Hygrolidin has anti-fungus activity against Valsa ceratosperma. Hygrolidin induces p21 expression and abrogates cell cycle progression at G1 and S phases. Hygrolidin has antitumor activity.
  • HY-137894A
    PF-07104091 hydrate

    		CDK GSK-3 Cancer
    PF-07104091 hydrate is a potent and selective CDK2/cyclin E1 and GSK3β inhibitor, with Kis of 1.16 and 537.81 nM, respectively. PF-07104091 hydrate has anti-tumor activity for cyclin E1-amplified cancers. (patent WO2020157652A2).
  • HY-13636
    Fulvestrant

    ICI 182780; ZD 9238; ZM 182780

    		 Estrogen Receptor/ERR Autophagy Apoptosis Cancer
    Fulvestrant (ICI 182780) is a pure antiestrogen and a potent estrogen receptor (ER) antagonist with an IC50 of 9.4 nM. Fulvestrant is also a GPR30 agonist. Fulvestrant effectively inhibits the growth of ER-positive MCF-7 cells with an IC50 of 0.29 nM. Fulvestrant also induces autophagy and has antitumor efficacy.
  • HY-N5112B
    β,β-Dimethylacrylshikonin

    Isoarnebin I

    		 Others Cancer
    β,β-Dimethylacrylshikonin (Isoarnebin I) is a naphthoquinone derivative isolated from Arnebia nobilis, promotes angiogenesis by inducing eNOS, VEGF and HIF-1α expression through the PI3K-dependent pathway.β,β-Dimethylacrylshikonin has anti-tumor activity.
  • HY-18213
    EGFR-IN-9

    		EGFR Cancer
    EGFR-IN-9 (Compound 8) is a potent EGFR kinase inhibitor with IC50s of 7 nM, 28 nM for the wild type EGFR kinase and double mutant EGFR kinase (L858R/T790M). EGFR-IN-9 has antitumor activity.
  • HY-16125
    Carboxyamidotriazole Orotate

    L-651582 Orotate; CAI Orotate

    		 Calcium Channel Cancer Inflammation/Immunology
    Carboxyamidotriazole Orotate (L-651582 Orotate) is the orotate salt form of Carboxyamidotriazole (CAI), an orally bioavailable signal transduction inhibitor. Carboxyamidotriazole Orotate is a cytostatic inhibitor of nonvoltage-operated calcium channels and calcium channel-mediated signaling pathways. Carboxyamidotriazole Orotate shows anti-tumor, anti-inflammatory and antiangiogenic effects.
  • HY-N3028
    Taccalonolide B

    		Microtubule/Tubulin Cancer
    Taccalonolide B is microtubule stabilizer isolated from Tacca plantaginea, with antitumor activity. Taccalonolide B is effective in vitro against cell lines that overexpress P-glycoprotein (Pgp) and multidrug-resistance protein (MRP7). Taccalonolide B inhibits growth of SK-OV-3 cells with an IC50 of 208 nM.
  • HY-101775A
    9-Hydroxyellipticine hydrochloride

    		Topoisomerase Cancer Cardiovascular Disease
    9-Hydroxyellipticine hydrochloride is a inhibitor of Topo II and RyR. 9-Hydroxyellipticine hydrochloride exhibits antitumor, antioxidant and catecholamine-releasing activities. 9-Hydroxyellipticine hydrochloride exhibits IC50 values of 1.6 μM and 1.2μM in Hela S-3 and 293T cells, respectively.
  • HY-101494
    Temuterkib

    LY3214996

    		 ERK Cancer
    LY3214996 is a highly selective inhibitor of ERK1 and ERK2, with IC50 of 5 nM for both enzymes in biochemical assays. LY3214996 potently inhibits cellular p-RSK1 in BRAF and RAS mutant cancer cell lines. LY3214996 shows potent antitumor activities in cancer models with MAPK pathway alterations.
  • HY-N0255
    alpha-Hederin

    α-Hederin

    		 Apoptosis Others
    alpha-Hederin (α-Hederin), a monodesmosidic triterpenoid saponin, exhibits promising antitumor potential against a variety of human cancer cell lines. alpha-Hederin could inhibit the proliferation and induce apoptosis of gastric cancer accompanied by glutathione decrement and reactive oxygen species generation via activating mitochondrial dependent pathway.
  • HY-136291
    Sulfo-SPDB-DGN462

    		Drug-Linker Conjugates for ADC Cancer
    Sulfo-SPDB-DGN462 is a drug-linker conjugate for ADC. Sulfo-SPDB-DGN462 consists a toxin DGN462 (HY-101150) conjugated to the cleavable Sulfo-SPDB linker. DGN462, a potent DNA-alkylating agent, shows anti-tumor activity, such as acute myeloid leukemia (AML).
  • HY-W008859
    Tetrac

    Tetraiodothyroacetic acid; 3,3',5,5'-Tetraiodothyroacetic acid

    		 Integrin Endogenous Metabolite Cancer
    Tetrac (Tetraiodothyroacetic acid), a derivative of L-thyroxine (T4), is a thyrointegrin receptor antagonist. Tetrac blocks the actions of T4 and 3,5,3'-triiodo-L-thyronine (T3) at the cell surface receptor for thyroid hormone on integrin αvβ3. Tetra has anti-angiogenic and anti-tumor activities.
  • HY-P9968
    Nimotuzumab

    		EGFR Cancer
    Nimotuzumab is a humanized IgG1 monoclonal antibody targeting EGFR with a KD of 0.21 nM. Nimotuzumab is directed against the extracellular domain of the EGFR blocking the binding to its ligands. Nimotuzumab, a strong antitumor drug, is cytolytic on target tumors by its capacity to cause antibody dependent cell mediated cytotoxicity (ADCC) and complement dependent cytotoxicity (CDC).
  • HY-N6013
    Aloin(mixture of A&B)

    		MMP Bacterial Fungal Cancer Infection Inflammation/Immunology
    Aloin (mixture of A&B) is anthraquinone derivative isolated from Aloe vera. Aloin (mixture of A&B) has diverse biological activities such as anti-inflammatory, immunity, antidiabetic, antioxidant, antibacterial, antifungal, and antitumor activities. Aloin (mixture of A&B) also an effective inhibitor of stimulated granulocyte matrix metalloproteinases (MMPs).
  • HY-N0192
    Arbutin

    β-Arbutin

    		 Tyrosinase Cancer
    Arbutin (β-Arbutin) is a competitive inhibitor of tyrosinase in melanocytes, with Ki app values of 1.42 mM for monophenolase; 0.9 mM for diphenolase. Arbutin is also used as depigmenting agents. Arbutin is a natural polyphenol isolated from the bearberry plant Arctostaphylos uvaursi, possesses with anti-oxidant, anti-inflammatory and anti-tumor properties.
  • HY-N5077
    Sinapine

    		AChE P-glycoprotein Cancer Inflammation/Immunology Neurological Disease
    Sinapine is an alkaloid isolated from seeds of the cruciferous species. Sinapine exhibits anti-inflammatory, anti-oxidant, anti-tumor, anti-angiogenic and radio-protective effects. Sinapine is also an acetylcholinesterase (AChE) inhibitor and can be used for the research of Alzheimer’s disease, ataxia, myasthenia gravis, and Parkinson’s disease.
  • HY-111555
    AmPEG6C2-Aur0131

    		Microtubule/Tubulin Drug-Linker Conjugates for ADC Cancer
    AmPEG6C2-Aur0131 is a drug-linker conjugate for ADC (anti-CXCR4 ADC) with potent antitumor activity by using Aur0131 (an auristatin microtubule inhibitor), linked via the non-cleavable linker AmPEG6C2.
  • HY-10330
    Toceranib

    SU11654; PHA 291639E

    		 PDGFR VEGFR c-Kit Cancer
    Toceranib phosphate (SU11654 phosphate) is an orally active receptor tyrosine kinase (RTK) inhibitor, and it potently inhibits PDGFR, VEGFR, and Kit with Kis of 5 and 6 nM for PDGFRβ and Flk-1/KDR, respectively. Toceranib phosphate (SU11654 phosphate) has antitumor and antiangiogenic activity, and used in the treatment of canine mast cell tumors.
  • HY-15045
    INO-1001

    		PARP Cancer
    INO-1001 is a potent and selective poly (ADP-ribose) polymerase (PARP) inhibitor. INO-1001 is a potent enhancer of radiation sensitivity and enhances radiation-induced cell killing by interfering with DNA repair mechanisms, resulting in necrotic cell death. INO-1001 has anti-tumor effects.
  • HY-112698
    CA-5f

    		Autophagy Apoptosis Cancer
    CA-5f is a potent late-stage macroautophagy/autophagy inhibitor via inhibiting autophagosome-lysosome fusion. CA-5f increases LC3B-II (a marker to monitor autophagy) and SQSTM1 protein, and also increases ROS production. Anti-tumor activity.
  • HY-N0284
    Esculetin

    		PI3K Akt Cancer Inflammation/Immunology
    Esculetin is an active ingredient extracted mainly from the bark of Fraxinus rhynchophylla. Esculetin inhibits platelet-derived growth factor (PDGF)-induced airway smooth muscle cells (ASMCs) phenotype switching through inhibition of PI3K/Akt pathway. Esculetin has antioxidant, antiinflammatory, and antitumor activities.
  • HY-N7526
    Naphthazarin

    DHNQ; 5,8-Dihydroxy-1,4-naphthoquinone

    		 Apoptosis Cancer Neurological Disease
    Naphthazarin (DHNQ) is a naturally occurring compound. Naphthazarin is effective by various cellular mechanisms including oxidative stress, activation of mitochondrial apoptosis-inducing factor (AIF), depolymerization of microtubules, interference with lysosomal function and p53-dependent p21 activation. Naphthazarin triggers apoptosis and has anti-tumor effects.
  • HY-B0109S
    Dorzolamide-d5

    		Carbonic Anhydrase Cancer
    Dorzolamide-d5 (L671152-d5) is the deuterium labeled Dorzolamide. Dorzolamide (L671152) is a potent carbonic anhydrase II inhibitor, with IC50 values of 0.18 nM and 600 nM for red blood cell CA-II and CA-I respectively. Dorzolamide possesses anti-tumor activity.
  • HY-128910
    MC-VC(S)-PABQ-Tubulysin M

    		Drug-Linker Conjugates for ADC Cancer
    MC-VC(S)-PABQ-Tubulysin M is a drug-linker conjugate for ADC with potent antitumor activity by using Tubulysin M (a tubulin inhibitor), linked via the ADC linker MC-VC(S)-PABQ. MC-VC(S)-PABQ-Tubulysin M is effective against multidrug-resistant lymphoma cell lines and tumors.
  • HY-128778
    DBPR112

    		EGFR Cancer
    DBPR112 is an orally active furanopyrimidine-based EGFR inhibitor with IC50s of 15 nM and 48 nM for EGFR WT and EGFR L858R/T790M, respectively. DBPR112 can occupy the ATP-binding site. DBPR112 has significant antitumor efficacy.
  • HY-13404
    Capmatinib

    INC280; INCB28060

    		 c-Met/HGFR Apoptosis Cancer
    Capmatinib (INC280; INCB28060) is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC50=0.13 nM). Capmatinib (INC280; INCB28060) potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity.
  • HY-N4042
    Hirsutenone

    		PI3K ERK Cancer Inflammation/Immunology
    Hirsutenone is an active botanical diarylheptanoid present in Alnus species and exhibits many biological activities, including anti-inflammatory, anti-tumor promoting and anti-atopic dermatitis effects. Hirsutenone attenuates adipogenesis by binding directly to PI3K and ERK1 in a non-ATP competitive manner. Hirsutenone can be used for the study of obesity.
  • HY-109189
    Rezivertinib

    BPI-7711

    		 EGFR Cancer
    Rezivertinib (BPI-7711) is an orally active, highly selective and irreversible third-generation EGFR tyrosine kinase inhibitor (TKI). Rezivertinib exhibits high potency against the common activation EGFR and the resistance T790M mutations. Rezivertinib has excellent central nervous system (CNS) penetration and has antitumor activity.
  • HY-N0047
    Polyphyllin I

    		JNK mTOR Akt PDK-1 Autophagy Apoptosis Cancer
    Polyphyllin I is a bioactive constituent extracted from Paris polyphylla, has strong anti-tumor activity. Polyphyllin I is an activator of the JNK signaling pathway and is an inhibitor of PDK1/Akt/mTOR signaling. Polyphyllin I induces autophagy, G2/M phase arrest and apoptosis.
  • HY-N8211
    Gypenoside L

    		p38 MAPK ERK NF-κB Cancer Inflammation/Immunology
    Gypenoside L is a saponin that can be found in Gynostemma pentaphyllum. Gypenoside L increases the SA-β-galactosidase activity, promotes the production of senescence-associated secretory cytokines. Gypenoside L also can activate p38 and ERK MAPK pathways and NF-κB pathway to induce senescence. Gypenoside L exhibits anti-tumor and anti-inflammatory activities.
  • HY-12458
    Pyrindamycin A

    		DNA/RNA Synthesis Cancer Infection
    Pyrindamycin A is an antibiotic that inhibits DNA synthesis. Pyrindamycin A shows antitumor activities against murine leukemia, exhibits stronger cytotoxic activities towards murine and human tumor cell lines and especially towards doxorubicin-resistant cells, inhibits P388 and P388/ADR cells with the same IC50 of 3.9 μg/ml.
  • HY-10330A
    Toceranib phosphate

    SU11654 phosphate; PHA 291639E phosphate

    		 PDGFR VEGFR c-Kit Cancer
    Toceranib phosphate (SU11654 phosphate) is an orally active receptor tyrosine kinase (RTK) inhibitor, and it potently inhibits PDGFR, VEGFR, and Kit with Kis of 5 and 6 nM for PDGFRβ and Flk-1/KDR, respectively. Toceranib phosphate (SU11654 phosphate) has antitumor and antiangiogenic activity, and used in the treatment of canine mast cell tumors .
  • HY-15666
    Olverembatinib

    GZD824; HQP1351

    		 Bcr-Abl Cancer
    Olverembatinib (GZD824) is a potent and orally active pan-Bcr-Abl inhibitor. Olverembatinib potently inhibits a broad spectrum of Bcr-Abl mutants. Olverembatinib strongly inhibits native Bcr-Abl and Bcr-Abl T315I with IC50s of 0.34 nM and 0.68 nM, respectively. Olverembatinib has antitumor activity.
  • HY-119347
    Cirsilineol

    		IFNAR STAT Cancer Inflammation/Immunology
    Cirsilineol, a natural flavone compound, selectively inhibits IFN-γ/STAT1/T-bet signaling in intestinal CD4 + T cells. Cirsilineol has potent immunosuppressive and anti-tumor properties. Cirsilineol significantly ameliorates trinitro-benzene sulfonic acid (TNBS)-induced T-cell-mediated experimental colitis in mice.
  • HY-10251
    BMS-599626

    AC480

    		 EGFR Cancer
    BMS-599626 (AC480) is a selective and orally bioavailable HER1 and HER2 inhibitor, with IC50s of 20 and 30 nM, respectively. BMS-599626 displays ~8-fold less potent to HER4 (IC50=190 nM), >100-fold to VEGFR2, c-Kit, Lck, MEK. BMS-599626 inhibits tumor cell proliferation, and has potential to increase tumor response to radiotherapy.
  • HY-103442
    CGP52411

    DAPH

    		 EGFR Amyloid-β Cancer Neurological Disease
    CGP52411 (DAPH) is a high selective, potent, orally active and ATP-competitive EGFR inhibitor with an IC50 of 0.3 μM. CGP52411 blocks the toxic influx of Ca 2+ ions into neuronal cells, and dramatic inhibits and reverses the formation of β-amyloid (Aβ42) fibril aggregates associated with Alzheimer's disease.
  • HY-90006
    5-Fluorouracil

    5-FU

    		 Nucleoside Antimetabolite/Analog HIV Apoptosis Endogenous Metabolite Cancer
    5-Fluorouracil (5-FU) is an analogue of uracil and a potent antitumor agent. 5-Fluorouracil affects pyrimidine synthesis by inhibiting thymidylate synthetase thus depleting intracellular dTTP pools. 5-Fluorouracil induces apoptosis and can be used as a chemical sensitizer. 5-Fluorouracil also inhibits HIV.
  • HY-10971A
    Alisertib sodium

    MLN 8237 sodium

    		 Aurora Kinase Autophagy Apoptosis Cancer
    Alisertib (MLN 8237) sodium is an orally active and selective Aurora A kinase inhibitor (IC50=1.2 nM), which binds to Aurora A kinase resulting in mitotic spindle abnormalities, mitotic accumulation. Alisertib sodium induces apoptosis and autophagy through targeting the AKT/mTOR/AMPK/p38 pathway in leukemic cells. Antitumor activity.
  • HY-19564
    JX06

    		PDHK Apoptosis Cancer
    JX06 is a potent, selective and covalent inhibitor of PDK. JX06 inhibits PDK1, PDK2 and PDK3 with IC50s of 49 nM, 101 nM, and 313 nM, respectively. JX06 inhibits PDK1 activity via covalently binding to a cysteine residue in an irreversible manner. JX06 shows significant antitumor activity.
  • HY-17364
    Temozolomide

    NSC 362856; CCRG 81045; TMZ

    		 DNA Alkylator/Crosslinker Autophagy Apoptosis Cancer
    Temozolomide (NSC 362856) is an oral active DNA alkylating agent that crosses the blood-brain barrier. Temozolomide is also a proautophagic and proapoptotic agent. Temozolomide is effective against tumor cells that are characterized by low levels of O6-alkylguanine DNA alkyltransferase (OGAT) and a functional mismatch repair system. Temozolomide has antitumor and antiangiogenic effects.
  • HY-108705
    BI-3802

    		Bcl-2 Family Cancer
    BI-3802 is a highly potent BCL6 degrader and inhibits the Bric-à-brac (BTB) domain of BCL6 with an IC50 of ≤3 nM. BI-3802 induces the polymerization of BCL6 and promotes BCL6 degration depended on E3 ligase SIAH1. BI-3802 has antitumor 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-100789
    ON1231320

    		Polo-like Kinase (PLK) Apoptosis Cancer
    ON1231320 is a highly specific polo like kinase 2 (PLK2) inhibitor with an IC50 of 0.31 µM. ON1231320 blocks tumor cell cycle progression in the G2/M phase in mitosis, causing apoptotic cell death. ON1231320, an arylsulfonyl pyrido-pyrimidinone, has antitumor activity.
  • HY-119198
    NSC745885

    		Apoptosis Histone Methyltransferase Cancer
    NSC745885 an effective anti-tumor agent, shows selective toxicity against multiple cancer cell lines but not normal cells. NSC745885 is an effective down-regulator of EZH2 via proteasome-mediated degradation. NSC745885 provides possibilities for the study of advanced bladder and oral squamous cell carcinoma (OSCC) cancers.
  • HY-129189
    RAS GTPase inhibitor 1

    		Ras Cancer
    RAS GTPase inhibitor 1 (example 51) is a RAS GTPase inhibitor with anti-tumor activity, extracted from patent WO2018212774A1. RAS GTPase inhibitor 1 (example 51) exhibits an EC50 less than 1 μM for at least one nucleotide exchange and an IC50 less than 1 μM in H727 cells.
  • HY-N5077B
    Sinapine hydroxide

    		AChE P-glycoprotein Cancer Inflammation/Immunology Neurological Disease
    Sinapine hydroxide is an alkaloid isolated from seeds of the cruciferous species. Sinapine hydroxide exhibits anti-inflammatory, anti-oxidant, anti-tumor, anti-angiogenic and radio-protective effects. Sinapine hydroxide is also an acetylcholinesterase (AChE) inhibitor and can be used for the research of Alzheimer’s disease, ataxia, myasthenia gravis, and Parkinson’s disease.
  • HY-P2268
    RAGE antagonist peptide

    		Amyloid-β Cancer Inflammation/Immunology
    RAGE antagonist peptide is an advanced glycation end products (RAGE) antagonist. RAGE antagonist peptide prevents RAGE from binding with several of its most important ligands, including HMGB-1, S100P, and S100A4. RAGE antagonist peptide (RAP) possesses anti-tumor and anti-inflammatory activities.
  • HY-N2329
    Piperlongumine

    Piplartine

    		 ERK Reactive Oxygen Species Autophagy Apoptosis Bacterial Ferroptosis Cancer Infection Cardiovascular Disease
    Piperlongumine is a alkaloid, possesses ant-inflammatory, antibacterial, antiangiogenic, antioxidant, antitumor, and antidiabetic activities. Piperlongumine induces ROS, and induces apoptosis in cancer cell lines. Piperlongumine shows anti-cardiac fibrosis activity, suppresses myofibroblast transformation via suppression of the ERK1/2 signaling pathway.
  • HY-15656A
    Ceritinib dihydrochloride

    LDK378 dihydrochloride

    		 ALK Insulin Receptor IGF-1R Cancer Endocrinology
    Ceritinib dihydrochloride (LDK378 dihydrochloride) is a selective, orally bioavailable and ATP-competitive ALK tyrosine kinase inhibitor with an IC50 of 200 pM. Ceritinib dihydrochloride (LDK378 dihydrochloride) also inhibits IGF-1R, InsR, and STK22D with IC50 values of 8, 7, and 23 nM, respectively. Ceritinib dihydrochloride (LDK378 dihydrochloride) shows great antitumor potency.
  • HY-103665
    STING agonist-3

    		STING Cancer
    STING agonist-3, extracted from patent WO2017175147A1 (example 10), is a selective and non-nucleotide small-molecule STING agonist with a pEC50 and pIC50 of 7.5 and 9.5, respectively. STING agonist-3 has durable anti-tumor effect and tremendous potential to improve treatment of cancer.
  • HY-15505
    RWJ-67657

    JNJ 3026582

    		 p38 MAPK Cancer Inflammation/Immunology Cardiovascular Disease
    RWJ-67657 (JNJ 3026582) is an orally active and selective p38α and p38β MAPK inhibitor with IC50s of 1 and 11 μM, respectively. RWJ-67657 displays no activity at p38γ and p38δ, and exhibits cardio protective effect. Anti-inflammatory and anti-tumor activity.
  • HY-114302
    CCB02

    		Microtubule/Tubulin Cancer
    CCB02 is a selective CPAP-tubulin interaction inhibitor, binding to tubulin and competing for the CPAP binding site of β-tubulin, with an IC50 of 689 nM, and shows potent anti-tumor activity. CCB02 shows no inhibition on the cell cycle- and centrosome-related kinases, or the phosphorylation status of Aurora A, Plk1, Plk2, CDK2, and CHK1.
  • HY-14674
    CP-724714

    		EGFR Apoptosis Cancer
    CP-724714 is a potent, selective and orally active ErbB2 (HER2) tyrosine kinase inhibitor, with an IC50 of 10 nM. CP-724714 displays a marked selectivity against EGFR kinase (IC50=6400 nM). CP-724714 potently inhibits ErbB2 receptor autophosphorylation in intact cells. Antitumor activities.
  • HY-N0450
    Sinapine thiocyanate

    		P-glycoprotein AChE Cancer
    Sinapine thiocyanate is an alkaloid isolated from seeds of the cruciferous species. Sinapine thiocyanate exhibits anti-inflammatory, anti-oxidant, anti-tumor, anti-angiogenic and radio-protective effects. Sinapine thiocyanate is also an acetylcholinesterase (AChE) inhibitor and can be used for the research of Alzheimer’s disease, ataxia, myasthenia gravis, and Parkinson’s disease.
  • HY-15656
    Ceritinib

    LDK378

    		 ALK Insulin Receptor IGF-1R Cancer Endocrinology
    Ceritinib (LDK378) is a selective, orally bioavailable, and ATP-competitive ALK tyrosine kinase inhibitor with an IC50 of 200 pM. Ceritinib (LDK378) also inhibits IGF-1R, InsR, and STK22D with IC50 values of 8, 7, and 23 nM, respectively. Ceritinib (LDK378) shows great antitumor potency.
  • HY-103665A
    STING agonist-3 trihydrochloride

    		STING Cancer
    STING agonist-3 trihydrochloride, extracted from patent WO2017175147A1 (example 10), is a selective and non-nucleotide small-molecule STING agonist with a pEC50 and pEC50 of 7.5 and 9.5, respectively. STING agonist-3 trihydrochloride has durable anti-tumor effect and tremendous potential to improve treatment of cancer.
  • HY-12342
    ML216

    CID-49852229

    		 DNA/RNA Synthesis Cancer
    ML216 (CID-49852229) is a potent, selective and cell permeable inhibitor of the DNA unwinding activity of BLM helicase with IC50s of 2.98 μM and 0.97 μM for BLM full-length and BLM 636-1298, respectively. ML216 inhibits ssDNA-dependent ATPase activity of BLM with a Ki of 1.76 µM. Antitumor avtivity.
  • HY-137092
    IACS-13909

    		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-15491
    AG-024322

    		COX Apoptosis Cancer
    AG-024322 is a potent ATP-competitive pan-CDK inhibitor against cell cycle kinases CDK1, CDK2, and CDK4 with Ki values in the 1-3 nM range. AG-024322 displays broad-spectrum anti-tumor activity and clear target modulation in vivo. AG-024322 induces cell apoptosis.
  • HY-116000
    Glumetinib

    SCC244

    		 c-Met/HGFR Cancer
    Glumetinib (SCC244) is a highly selective, orally bioavailable, ATP-competitive c-Met inhibitor with an IC50 of 0.42 nM. Glumetinib has greater than 2400-fold selectivity for c-Met over those 312 kinases evaluated, including the c-Met family member RON and highly homologous kinases Axl, Mer, TyrO3. Antitumor activity.
  • HY-W040129
    Chromomycin A3

    		Bacterial Fungal Antibiotic Cancer Infection
    Chromomycin A3 is an aureolic acid-type antitumor antibiotic. Chromomycin A3 forms dimeric complexes with divalent cations, such as Mg 2+, which strongly binds to the GC rich sequence of DNA to inhibit DNA replication and transcription. Chromomycin A3 has a variety of utilities as a staining agent for human sperm chromatin, autophagy inducing agent, and apoptosis inhibitor.
  • HY-14452
    Fatostatin

    125B11

    		 Fatty Acid Synthase (FASN) Cancer
    Fatostatin (125B11), a specific inhibitor of SREBP activation, impairs the activation of SREBP-1 and SREBP-2. Fatostatin binds to SCAP (SREBP cleavage-activating protein), and inhibits the ER-Golgi translocation of SREBPs. Fatostatin decreases the transcription of lipogenic genes in cells. Fatostatin possesses antitumor properties, and lowers hyperglycemia in ob/ob mice.
  • HY-10220
    SF1126

    		PI3K Apoptosis Cancer
    SF1126 is a relevant pan and dual first-in-class PI3K/BRD4 inhibitor, has antitumor and anti-angiogenic activity. SF1126 is an RGDS-conjugated LY294002 prodrug, which is designed to exhibit increased solubility and bind to specific integrins within the tumor compartment. SF1126 induces cell apoptosis.
  • HY-100036
    MK-4101

    		Smo Apoptosis Hedgehog Cancer
    MK-4101 is a Smoothened (SMO) antagonist (IC50 of 1.1 µM for 293 cells ) and also a potent inhibitor of the hedgehog pathway (IC50 of 1.5 µM for mouse cells; IC50 of 1 µM for KYSE180 oesophageal cancer cells). MK-4101 has robust antitumor activity that inhibits tumor cell proliferation and induces extensive apoptosis.
  • HY-N0587
    Demethylzeylasteral

    		Apoptosis Cancer Inflammation/Immunology
    Demethylzeylasteral is a triterpene compound isolated from Tripterygium wilfordii Hook F, with anti-inflammatory, immunosuppressive and anti-tumor activities. Demethylzeylasteral can significantly alleviates atherosclerosis (AS). Demethylzeylasteral inhibits triple-negative breast cancer invasion by blocking the canonical and non-canonical TGF-β signaling pathways.
  • HY-108696
    GNE-781

    		Epigenetic Reader Domain Histone Acetyltransferase Cancer
    GNE-781 is an orally active, highly potent and selective CBP inhibitor with an IC50 of 0.94 nM in TR-FRET assay. GNE-781 also inhibits BRET and BRD4(1) with IC50s of 6.2 nM and 5100 nM, respectively. GNE-781 displays antitumor activity in an MOLM-16 AML xenograft model.
  • HY-12203
    PFK-158

    		Autophagy Apoptosis Cancer
    PFK-158 is a potent and selective PFKFB3 inhibitor with an IC50 value 137 nM. PFK-158 reduces glucose uptake, ATP production, lactate release, and induces apoptosis and autophagy in cancer cells. PFK-158 has broad anti-tumor activity. PFK-158 can also enhance Colistin's resistance to bacteria.
  • HY-N6246
    Asperulosidic Acid

    		NF-κB ERK Cancer Inflammation/Immunology
    Asperulosidic Acid (ASPA), a bioactive iridoid glycoside, is extracted from the herbs of Hedyotis diffusa Willd. Asperulosidic Acid (ASPA) has anti-tumor, anti-oxidant, and anti-inflammatory activities. ASPA is related to the inhibition of inflammatory cytokines (TNF-α, IL-6) and mediators via suppression of the NF-κB and mitogen-activated protein kinase (MAPK) signaling pathways.
  • HY-128590
    PHT-7.3

    		Ras Cancer
    PHT-7.3 is a selective inhibitor of connector enhancer of kinase suppressor of Ras 1 (Cnk1) pleckstrin homology (PH) domain (Kd=4.7 μM). PHT-7.3 inhibits mut-KRas, but not wild-type KRas cancer cell and tumor growth and signaling. PHT-7.3 has antitumor activity.
  • HY-131970
    LSD1/HDAC6-IN-1

    		Histone Demethylase Cancer
    LSD1/HDAC6-IN-1 is an orally active dual inhibitor of lysine specific demethylase 1(LSD1)/Histone deacetylase 6 (HDAC6), with anti-tumor activity. LSD1/HDAC6-IN-1 can be used for the research of multiple myeloma (MM).
  • HY-10971
    Alisertib

    MLN 8237

    		 Aurora Kinase Autophagy Apoptosis Cancer
    Alisertib (MLN 8237) is an orally active and selective Aurora A kinase inhibitor (IC50=1.2 nM), which binds to Aurora A kinase resulting in mitotic spindle abnormalities, mitotic accumulation. Alisertib (MLN 8237) induces apoptosis and autophagy through targeting the AKT/mTOR/AMPK/p38 pathway in leukemic cells. Antitumor activity.
  • HY-104066
    Theliatinib

    Xiliertinib; HMPL-309

    		 EGFR Cancer
    Theliatinib (HMPL-309) is a potent, ATP-competitive, orally active and highly selective EGFR inhibitor with a Ki of 0.05 nM and an IC50 of 3 nM. Theliatinib has an IC50 of 22 nM for EGFR T790M/L858R mutant. Theliatinib shows >50-fold selectivity for EGFR than other kinases. Anti-tumor activity.
  • HY-101597
    NVX-207

    		Apoptosis Cancer
    NVX-207, a Betulinic acid-derived anti-cancer compound, shows anti-tumor activity (mean IC50=3.5 μM) against various human and canine cell lines. NVX-207-induced apoptosis is associated with activation of the intrinsic apoptotic pathway via cleavage of caspases -9, -3, -7 and of PARP.
  • HY-P2268A
    RAGE antagonist peptide TFA

    		Amyloid-β Cancer Inflammation/Immunology
    RAGE antagonist peptide TFA is an advanced glycation end products (RAGE) antagonist. RAGE antagonist peptide TFA prevents RAGE from binding with several of its most important ligands, including HMGB-1, S100P, and S100A4. RAGE antagonist peptide TFA possesses anti-tumor and anti-inflammatory activities.
  • HY-14621
    Zingerone

    Vanillylacetone; Gingerone

    		 NF-κB Cancer Metabolic Disease Inflammation/Immunology
    Zingerone (Vanillylacetone) is a nontoxic methoxyphenol isolated from Zingiber officinale, with potent anti-inflammatory, antidiabetic, antilipolytic, antidiarrhoeic, antispasmodic and anti-tumor properties. Zingerone alleviates oxidative stress and inflammation, down-regulates NF-κB mediated signaling pathways. Zingerone acts as an anti-mitotic agent, and inhibits the growth of neuroblastoma cells.
  • HY-15666A
    Olverembatinib dimesylate

    GZD824 dimesylate; HQP1351 dimesylate

    		 Bcr-Abl Cancer
    Olverembatinib (GZD824) dimesylate is a potent and orally active pan-Bcr-Abl inhibitor. Olverembatinib dimesylate potently inhibits a broad spectrum of Bcr-Abl mutants. Olverembatinib dimesylate strongly inhibits native Bcr-Abl and Bcr-Abl T315I with IC50s of 0.34 nM and 0.68 nM, respectively. Olverembatinib dimesylate has antitumor activity.
  • HY-W088075
    Acriflavine hydrochloride

    Acriflavinium chloride hydrochloride

    		 HIF/HIF Prolyl-Hydroxylase Bacterial SARS-CoV Cancer Infection
    Acriflavine hydrochloride (Acriflavinium chloride hydrochloride) is a fluorescent acridine dye that can be used to label nucleic acid. Acriflavine hydrochloride is an antiseptic. Acriflavine hydrochloride is a potent HIF-1 inhibitor, with antitumor activity. Acriflavine hydrochloride has antimicrobial and antiviral activities. Acriflavine hydrochloride is a potent papain-like protease (PL pro) inhibitor, which inhibits SARS-CoV-2
  • HY-N7691
    3,29-O-Dibenzoyloxykarounidiol

    Karounidiol dibenzoate

    		 Others Cancer Infection
    3,29-O-Dibenzoyloxykarounidiol (Karounidiol dibenzoate) is a triterpene benzoate isolated from the fruit of Momordica grosvenori. 3,29-O-Dibenzoyloxykarounidiol has potent inhibitory effects on Epstein-Barr virus early antigen (EBV-EA) induced by tumor promoter 12-O-tetradecanoylphorbol-13-acetate (TPA).
  • HY-138298
    Trastuzumab deruxtecan

    DS-8201; DS-8201a

    		 Antibody-Drug Conjugate (ADC) EGFR Cancer
    Trastuzumab deruxtecan (DS-8201a) is an anti-human epidermal growth factor receptor 2 (HER2) antibody-drug conjugate (ADC). Trastuzumab deruxtecan is composed of a humanized anti-HER2 antibody, an enzymatically cleavable peptide-linker, and a topoisomerase I inhibitor. Trastuzumab deruxtecan can be used for the research of HER2-positive breast cancer and gastric cancer.
  • 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-12137A
    Volasertib trihydrochloride

    BI 6727 trihydrochloride

    		 Polo-like Kinase (PLK) Apoptosis Cancer
    Volasertib (BI 6727) trihydrochloride is an orally active, highly potent and ATP-competitive Polo-like kinase 1 (PLK1) inhibitor with an IC50 of 0.87 nM. Volasertib trihydrochloride inhibits PLK2 and PLK3 with IC50s of 5 and 56 nM, respectively. Volasertib trihydrochloride induces mitotic arrest and apoptosis. Volasertib trihydrochloride, a dihydropteridinone derivative, shows marked antitumor activity in multiple cancer models.
  • 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-N2274
    23-Hydroxylongispinogenin

    12-Oleanene-3β,16β,23,28-tetrol; 3β,16β-12-Oleanene-3, 16,23,28-tetrol

    		 Others Cancer
    23-Hydroxylongispinogenin (12-Oleanene-3β,16β,23,28-tetrol) is extracted from Lysimachia heterogenea Klatt. Lysimachia heterogenea Klatt is a perennial herb, which is used as a folk medicine in subduing swelling and detoxicating in China. The effective fraction LH-1 of L. heterogene has antitumor activity.
  • HY-12040
    Elesclomol

    STA-4783

    		 Reactive Oxygen Species Apoptosis Cancer
    Elesclomol (STA-4783) is an oxidative stress inducer that induces cancer cell apoptosis. Elesclomol is a reactive oxygen species (ROS) inducer. Elesclomol shows antitumor activity against a broad range of cancer cell types. Elesclomol is also a highly lipophilic Cu 2+-binding molecule. Elesclomol can be used for Menkes and associated disorders of hereditary copper deficiency research.
  • HY-129179
    Lisaftoclax

    APG-2575; Bcl-2/Bcl-xl inhibitor 1

    		 Bcl-2 Family Cancer
    Bcl-2/Bcl-xl inhibitor 1 (compound 6) is a dual Bcl-2 and Bcl-xl inhibitor with anti-tumor activity, extracted from patent WO2018027097A1. Bcl-2/Bcl-xl inhibitor 1 exhibits IC50 values of 2 nM and 5.9 nM for Bcl-2 and Bcl-xl, respectively.
  • HY-B0091A
    Adapalene sodium salt

    CD 271 sodium salt

    		 RAR/RXR Autophagy Apoptosis Cancer Inflammation/Immunology Neurological Disease
    Adapalene (CD271) sodium salt, a third-generation synthetic retinoid, is widely used for the research of acne. Adapalene sodium salt is a potent RAR agonist, with AC50s of 2.3 nM, 9.3 nM, and 22 nM for RARβ, RARγ, RARα, respectively. Adapalene sodium salt also inhibits the enzymatic activity of GOT1 in a non-competitive manner. Adapalene sodium salt exhibits anti-tumor activity.
  • HY-139018
    TLR7/8 agonist 4 hydroxy-PEG10-acid

    		Drug-Linker Conjugates for ADC Cancer
    TLR7/8 agonist 4 hydroxy-PEG10-acid (compound 9) is a drug-linker conjugate for ADC with potent antitumor activity by using TLR7/8 agonist 4 (HY-139018; a TLR7/8 agonist), linked via the cleavable ADC linker hydroxy-PEG10-acid (HY-133307).
  • HY-128862
    EGFR-IN-7

    		EGFR Cancer
    EGFR-IN-7 (compound 34) is a selective and potent EGFR kinase inhibitor extracted from patent WO2019015655A1, has IC50s of 7.92 nM and 0.218 nM for EGFR (WT) and EGFR (mutant C797S/T790M/L858R) respectively, and shows anti-tumor activity.
  • HY-129603
    SI-109

    		STAT Ligand for Target Protein for PROTAC Cancer
    SI-109 is a potent STAT3 SH2 domain inhibitor (Ki=9 nM) with antitumor activity. SI-109 effectively inhibits the transcriptional activity of STAT3 (IC50=3 μM). SI-109 and an analog of CRBN ligand lenalidomide have been used to design PROTAC STAT3 degrader SD-36.
  • HY-121508
    (E/Z)-IT-603

    		NF-κB Cancer Inflammation/Immunology
    (E/Z)-IT-603 is a mixture of E-IT-603 and Z-IT-603 (IT-603). IT-603 is a c-Rel inhibitor with an IC50 of 3 μM. IT-603 has anti-tumor activity. (E/Z)-IT-603 is a promising modulator of T-cell responses in the context of graft-versus-host disease (GVHD) and malignant diseases.
  • HY-12137
    Volasertib

    BI 6727

    		 Polo-like Kinase (PLK) Apoptosis Cancer
    Volasertib (BI 6727) is an orally active, highly potent and ATP-competitive Polo-like kinase 1 (PLK1) inhibitor with an IC50 of 0.87 nM. Volasertib inhibits PLK2 and PLK3 with IC50s of 5 and 56 nM, respectively. Volasertib induces mitotic arrest and apoptosis. Volasertib, a dihydropteridinone derivative, shows marked antitumor activity in multiple cancer models.
  • HY-B0091
    Adapalene

    CD271

    		 RAR/RXR Autophagy Apoptosis Cancer Inflammation/Immunology Neurological Disease
    Adapalene (CD271), a third-generation synthetic retinoid, is widely used for the research of acne. Adapalene is a potent RAR agonist, with AC50s of 2.3 nM, 9.3 nM, and 22 nM for RARβ, RARγ, RARα, respectively. Adapalene also inhibits the enzymatic activity of GOT1 in a non-competitive manner. Adapalene exhibits anti-tumor activity.
  • HY-105226
    CI-988

    PD134308

    		 Cholecystokinin Receptor Cancer Neurological Disease
    CI-988 (PD134308) is a potent, selective and orally active CCK2R (cholecystokinin 2 receptor) antagonist with an IC50 of 1.7 nM for mouse cortex CCK2. CI-988 shows >1600-fold selectivity for CCK2 over CCK1 receptor. CI-988 has anxiolytic and anti-tumor effects.
  • HY-N1440
    Koumine

    		Others Cancer Inflammation/Immunology
    Koumine is an alkaloid separated from Gelsemium elegans, shows potent anti-tumor activity. Koumine up-regulates the Bax/Bcl-2 ratio and caspase-3 expression in human breast cancer cells. Koumine has anxiolytic, antistress, antipsoriatic, and analgesic activities, protects against the development of arthritis in Rheumatoid arthritis (RA) animal models.
  • HY-135691
    hnRNPK-IN-1

    		c-Myc Apoptosis Cancer
    hnRNPK-IN-1 is a heterogeneous nuclear ribonucleoprotein K (hnRNPK) binding ligand with Kd values of 4.6 μM and 2.6 μM measured with SPR and MST, respectively. hnRNPK-IN-1 inhibits c-myc transcription by disrupting the binding of hnRNPK and c-myc promoter. hnRNPK-IN-1 induces Hela cells apoptosis and has strongly anti-tumor activities.
  • HY-P1812
    AUNP-12

    NP-12

    		 PD-1/PD-L1 Cancer
    AUNP-12 (NP-12) is a peptide antagonist of the PD-1 signaling pathway, displays equipotent antagonism toward PD-L1 and PD-L2 in rescue of lymphocyte proliferation and effector functions. AUNP-12 exhibits immune activation, excellent antitumor activity, and potential for better management of immune-related adverse events (irAEs).
  • HY-125858
    MI-1061

    		MDM-2/p53 E1/E2/E3 Enzyme Apoptosis Cancer
    MI-1061 is a potent, orally bioavailable, and chemically stable MDM2 (MDM2-p53 interaction) inhibitor (IC50=4.4 nM; Ki=0.16 nM). MI-1061 potently activates p53 and induces apoptosis in the SJSA-1 xenograft tumor tissue in mice. Anti-tumor activity.
  • HY-138293
    CDK7-IN-3

    		CDK Apoptosis Cancer
    CDK7-IN-3 is a selective CDK7 inhibitor with a KD of 0.059 nM. CDK7-IN-3 shows poor inhibition on CDK2 (Ki=390 nM), CDK9 (Ki=290 nM), CDK12 (Ki=78 nM). CDK7-IN-3 induce apoptosis in tumor cells and has antitumor activity.
  • HY-N2359
    Chelerythrine

    		PKC Bcl-2 Family Apoptosis Autophagy Cancer Metabolic Disease Inflammation/Immunology
    Chelerythrine is a natural alkaloid, acts as a potent and selective Ca 2+/phospholopid-dependent PKC antagonist, with an IC50 of 0.7 μM. Chelerythrine has antitumor, antidiabetic and anti-inflammatory activity. Chelerythrine inhibits the BclXL-Bak BH3 peptide binding with IC50 of 1.5 μM and displaces Bax from BclXL. Chelerythrine triggers apoptosis and autophagy.
  • HY-18174A
    Prexasertib dihydrochloride

    LY2606368 dihydrochloride

    		 Checkpoint Kinase (Chk) Apoptosis Cancer
    Prexasertib dihydrochloride (LY2606368 dihydrochloride) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib dihydrochloride inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib dihydrochloride causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib dihydrochloride shows potent anti-tumor activity.
  • HY-17408
    Mevastatin

    Compactin; ML236B

    		 HMG-CoA Reductase (HMGCR) Bacterial Autophagy Apoptosis Antibiotic Cancer Infection Metabolic Disease Neurological Disease Cardiovascular Disease
    Mevastatin (Compactin) is a first HMG-CoA reductase inhibitor that belongs to the statins class. Mevastatin is a lipid-lowering agent, and induces apoptosis, arrests cancer cells in G0/G1 phase. Mevastatin also increases endothelial nitric oxide synthase (eNOS) mRNA and protein levels. Mevastatin has antitumor activity and has the potential for cardiovascular diseases treatment.
  • HY-117273
    AZ304

    		Raf Autophagy Cancer
    AZ304 is an ATP-competitive dual BRAF kinase inhibitor, potently inhibits wild type BRAF, V600E mutant BRAF and wild type CRAF, with IC50s of 79 nM, 38 nM and 68 nM, respectively. AZ304 also has significant effect on other kinases, such as p38 (IC50, 6 nM), CSF1R (IC50, 35 nM). Anti-tumor activity.
  • HY-19827
    Aeroplysinin 1

    (+)-Aeroplysinin-1

    		 Bacterial HIV Apoptosis Cancer Infection
    Aeroplysinin 1 ((+)-Aeroplysinin-1), a secondary metabolite isolated from marine sponges, shows potent antibiotic effects on Gram-positive bacteria and exerts antiviral activity against HIV-1 (IC50=14.6 μM). Aeroplysinin 1 has anti-inflammatory, anti-angiogenic and anti-tumor activities. Aeroplysinin 1 induces apoptosis in endothelial cells.
  • HY-12455
    Duocarmycin A

    		ADC Cytotoxin Apoptosis Caspase Cancer
    Duocarmycin A, which is one of well-known antitumor antibiotics, is a DNA alkylator and efficiently alkylates adenine N3 at the 3′ end of AT-rich sequences in the DNA. Duocarmycin A, as a chemotherapeutic agent, results HLC-2 cells typically apoptotic changes, including chromatin condensation, sub-G1 accumulation in DNA histogram pattern, and decrease in procaspase-3 and 9 levels.
  • HY-134901
    WM-3835

    		Histone Acetyltransferase Apoptosis Cancer
    WM-3835 is a potent and high-specific HBO1 (KAT7 or MYST2) inhibitor and binds directly to the acetyl-CoA binding site of HBO1 33. WM-3835 activates apoptosis while inhibits osteosarcoma (OS) cell proliferation, migration and invasion. WM-3835 has antitumor activity and potently inhibits pOS-1 xenograft growth in mice.
  • HY-W046353
    2-Methoxycinnamaldehyde

    o-Methoxycinnamaldehyde

    		 Apoptosis Cancer
    2-Methoxycinnamaldehyde (o-Methoxycinnamaldehyde) is a natural compound of Cinnamomum cassia, with antitumor activity. 2-Methoxycinnamaldehyde inhibits proliferation and induces apoptosis by mitochondrial membrane potential (ΔΨm) loss, activation of both caspase-3 and caspase-9. 2-Methoxycinnamaldehyde effectively inhibits platelet-derived growth factor (PDGF)-induced HASMC migration.
  • HY-14452A
    Fatostatin hydrobromide

    125B11 hydrobromide

    		 Fatty Acid Synthase (FASN) Cancer
    Fatostatin hydrobromide (125B11 hydrobromide), a specific inhibitor of SREBP activation, impairs the activation of SREBP-1 and SREBP-2. Fatostatin hydrobromide binds to SCAP (SREBP cleavage-activating protein), and inhibits the ER-Golgi translocation of SREBPs. Fatostatin hydrobromide decreases the transcription of lipogenic genes in cells. Fatostatin hydrobromide possesses antitumor properties, and lowers hyperglycemia in ob/ob mice.
  • 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-125858A
    MI-1061 TFA

    		MDM-2/p53 E1/E2/E3 Enzyme Apoptosis Cancer
    MI-1061 TFA is a potent, orally bioavailable, and chemically stable MDM2 (MDM2-p53 interaction) inhibitor (IC50=4.4 nM; Ki=0.16 nM). MI-1061 TFA potently activates p53 and induces apoptosis in the SJSA-1 xenograft tumor tissue in mice. Anti-tumor activity.
  • HY-N2259
    Curcumenol

    (+)-Curcumenol

    		 Cytochrome P450 Cancer Inflammation/Immunology Neurological Disease
    Curcumenol ((+)-Curcumenol) is a potent CYP3A4 inhibitor with an IC50 of 12.6 μM, which is one of constituents in the plants of medicinally important genus of Curcuma zedoaria, with neuroprotection, anti-inflammatory, anti-tumor and hepatoprotective activities. Curcumenol ((+)-Curcumenol) suppresses Akt-mediated NF-κB activation and p38 MAPK signaling pathway in LPS-stimulated BV-2 microglial cells.
  • HY-18174B
    Prexasertib Mesylate Hydrate

    LY2606368 Mesylate Hydrate; LY2940930

    		 Checkpoint Kinase (Chk) Apoptosis Cancer
    Prexasertib Mesylate Hydrate (LY2606368 Mesylate Hydrate) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib Mesylate Hydrate inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib Mesylate Hydrate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib Mesylate Hydrate shows potent anti-tumor 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 inudces autophagy and has antitumor activity.
  • HY-N6856
    4-Hydroxycoumarin

    		Endogenous Metabolite Bacterial Infection
    4-Hydroxycoumarin, a coumarin derivative, is one of the most versatile heterocyclic scaffolds and is frequently applied in the synthesis of various organic compounds. 4-Hydroxycoumarin possesses both electrophilic and nucleophilic properties. 4-Hydroxycoumarin derivatives are employed as the anticoagulant, antibacterial, antifungal, antiviral, antitumor, antiprotozoal, insecticidal, antimycobacterial, antimutagenic, antioxidant, anti-inflammatory agents, HIV protease inhibitors and tyrosine kinase inhibitors.
  • HY-18174
    Prexasertib

    LY2606368

    		 Checkpoint Kinase (Chk) Apoptosis Cancer
    Prexasertib (LY2606368) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib shows potent anti-tumor activity.
  • HY-18285
    Longdaysin

    		Casein Kinase ERK CDK Cancer
    Longdaysin is a inhibitor of the Wnt/β-catenin signaling pathway, which exerts antitumor effect through blocking CK1δ/ε-dependent Wnt signaling. Longdaysin inhibits CK1α, CK1δ, CDK7, and ERK2 with IC50s of  5.6 µM, 8.8 µM, 29 µM, and 52 µM, respectively.
  • HY-15149
    Romidepsin

    FK 228; FR 901228; NSC 630176

    		 HDAC Apoptosis Cancer
    Romidepsin (FK 228) is a Histone deacetylase (HDAC) inhibitor with anti-tumor activities. Romidepsin (FK 228) inhibits HDAC1, HDAC2, HDAC4, and HDAC6 with IC50s of 36 nM, 47 nM, 510 nM and 1.4 μM, respectively. Romidepsin (FK 228) is produced by Chromobacterium violaceum, induces cell G2/M phase arrest and apoptosis.
  • HY-132229
    LPM4870108

    		Trk Receptor Cancer
    LPM4870108 is a potent and orally active pan-Trk (WT and MT) inhibitor, with IC50s of 0.2 nM, 2.4 nM, 3.5 nM and 2.3 nM for TrkC, TrkA, TrkA G595R and TrkA G667C, respectively. LPM4870108 shows selectivity for Trk over ALK (IC50=182 nM). LPM4870108 exhibits anti-tumor activity.
  • HY-N0222
    Avicularin

    		Others Cancer Inflammation/Immunology
    Avicularin is a bio-active flavonoid from plants, anti-inflammatory, anti-allergic, anti-oxidant, hepatoprotective, and anti-tumor activities. Avicularin exhibits anti-inflammatory activity through the suppression of ERK signaling pathway in LPS-stimulated RAW 264.7 macrophage cells. Avicularin ameliorates human hepatocellular carcinoma via the regulation of NF κB (p65), COX 2 and PPAR γ activities.
  • HY-13543
    Tretazicar

    CB 1954

    		 DNA Alkylator/Crosslinker Cancer
    Tretazicar (CB 1954), an antitumor prodrug, is highly selective against the Walker 256 rat tumour line. Tretazicar is enzymatically activated to generate a bifunctional agent, which can form DNA-DNA interstrand cross-links. Tretazicar in rat cells involves the reduction of its 4-nitro group to a 4-hydroxylamine by the enzyme NAD(P)H:quinone oxidoreductase 1 (NQO1).
  • HY-P1812A
    AUNP-12 TFA

    NP-12 TFA

    		 PD-1/PD-L1 Cancer
    AUNP-12 TFA (NP-12 TFA) is a peptide antagonist of the PD-1 signaling pathway, displays equipotent antagonism toward PD-L1 and PD-L2 in rescue of lymphocyte proliferation and effector functions. AUNP-12 TFA exhibits immune activation, excellent antitumor activity, and potential for better management of immune-related adverse events (irAEs).
  • HY-16559A
    Riviciclib

    P276-00 free base

    		 CDK Cancer
    Riviciclib (P276-00 free base) is a potent cyclin-dependent kinase (CDK) inhibitor, which inhibits CDK9-cyclinT1, CDK4-cyclin D1, and CDK1-cyclinB with IC50s of 20 nM, 63 nM, and 79 nM, respectively. Riviciclib shows antitumor activity on cisplatin-resistant cells.
  • HY-129601
    MYCi975

    NUCC-0200975

    		 c-Myc Cancer Inflammation/Immunology
    MYCi975 (NUCC-0200975) is an orally active MYC inhibitor, which disrupts MYC/MAX interaction, promotes MYC T58 phosphorylation and MYC degradation, and impairs MYC driven gene expression. MYCi975 (NUCC-0200975) exhibits potent anti-tumor efficacy with good tolerability, increases tumor immune cell infiltration, and sensitizes tumors to anti-PD1 immunotherapy.
  • HY-100237
    SZL P1-41

    		E1/E2/E3 Enzyme Apoptosis Cancer
    SZL P1-41 is a specific Skp2 inhibitor, binds to the F-box domain of Skp2 to prevent Skp1 association and Skp2 SCF complex formation. SZL P1-41, like Skp2 deficiency, augments p27-mediated apoptosis/senescence, while it impairs Akt-driven glycolysis. Anti-tumor activities.
  • HY-11107
    PHA-665752

    		c-Met/HGFR Autophagy Apoptosis Cancer
    PHA-665752 is a selective, ATP-competitive, and active-site inhibitor of the catalytic activity of c-Met kinase (Ki=4 nM; IC50=9 nM). PHA-665752 exhibits >50-fold selectivity for c-Met compared with a panel of diverse tyrosine and serine-threonine kinases. PHA-665752 induces apoptosis and cell cycle arrest, and exhibits cytoreductive antitumor activity.
  • HY-16146
    Combretastatin A-1 phosphate tetrasodium

    OXi-4503 tetrasodium

    		 Microtubule/Tubulin Cancer
    Combretastatin A-1 phosphate (OXi-4503) tetrasodium, a prodrug of Combretastatin A-1, is a microtubule polymerization inhibitor that binds to the colchicine-binding site of tubulin. Combretastatin A-1 phosphate tetrasodium inhibits the Wnt/β-catenin pathway through tubulin depolymerization mediated AKT deactivation. Combretastatin A-1 phosphate tetrasodium exhibits anti-tumor and anti-vascular effects.
  • HY-N0095
    (S)-10-Hydroxycamptothecin

    10-HCPT; 10-Hydroxycamptothecin

    		 Topoisomerase Apoptosis Cancer
    (S)-10-Hydroxycamptothecin (10-HCPT;10-Hydroxycamptothecin) is a DNA topoisomerase I inhibitor of isolated from the Chinese plant Camptotheca accuminata. (S)-10-Hydroxycamptothecin exhibits a remarkable apoptosis-inducing effect. (S)-10-Hydroxycamptothecin has the potential for hepatoma, gastric carcinoma, colon cancer and leukaemia treatment.
  • HY-106014
    Tezacitabine

    		DNA/RNA Synthesis Nucleoside Antimetabolite/Analog Apoptosis Cancer
    Tezacitabine is a cytostatic and cytotoxic antimetabolite and a nucleoside analogue. Tezacitabine irreversibly inhibits the ribonucleotide reductase and interferes with DNA replication and repair. Tezacitabine effectively induces cells apoptotic. Tezacitabine has the potential for leukemias and solid tumors (carcinomas) treatment.
  • HY-16559
    Riviciclib hydrochloride

    P276-00

    		 CDK Apoptosis Cancer
    Riviciclib hydrochloride (P276-00) is a potent cyclin-dependent kinase (CDK) inhibitor, which inhibits CDK9-cyclinT1, CDK4-cyclin D1, and CDK1-cyclinB with IC50s of 20 nM, 63 nM, and 79 nM, respectively. Riviciclib hydrochloride (P276-00) shows antitumor activity on cisplatin-resistant cells.
  • HY-N2959
    Brevilin A

    		JAK STAT Apoptosis Autophagy Cancer
    Brevilin A is a sesquiterpene lactone isolated from Centipeda minima with anti-tumor activity. Brevilin A is a selective inhibitor of JAK-STAT signal pathway by attenuating the JAKs activity and blocking STAT3 signaling (IC50 = 10.6 µM) in Cancer Cells. Brevilin A induces apoptosis and autophagy via mitochondrial pathway and PI3K/AKT/mTOR inactivation in colon adenocarcinoma cell CT26.
  • HY-N2205
    Esculentoside H

    		NF-κB JNK Cancer
    Esculentoside H (EsH) is a saponin isolated from the root extract of perennial plant Phytolacca esculenta. Esculentoside H (EH) has anti-tumor activity, the mechanism is related to the capacity for TNFrelease. Esculentoside H (EsH) suppresses colon cancer cell migration through blockage of the JNK1/2 and NF-κB signaling-mediated matrix metalloproteinases-9 (MMP-9) expression.
  • HY-10524
    GSK1904529A

    		IGF-1R Insulin Receptor Apoptosis Cancer Endocrinology
    GSK1904529A is a potent, selective, orally active, and ATP-competitive inhibitor of insulin-like growth factor-1 receptor (IGF-1R) and insulin receptor (IR), with IC50s of 27 and 25 nM, respectively. GSK1904529A shows poor activity (IC50>1 μM) in 45 other serine/threonine and tyrosine kinases. GSK1904529A exhibits anti-tumor activity.
  • HY-13440
    AMG 511

    		PI3K Cancer
    AMG 511 is a potent and orally available pan inhibitor of class I PI3Ks, with Kis of 4 nM, 6 nM, 2 nM and 1 nM for PI3Kα, β, δ and γ, respectively. AMG 511 significantly suppresses PI3K signaling that is indicated by p-Akt (Ser473) decrease. AMG 511 exhibits anti-tumor activity in mouse glioblastoma xenograft model.
  • 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-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-103441
    JNJ28871063 hydrochloride

    		EGFR Cancer
    JNJ28871063 hydrochloride is an orally active, highly selective and ATP competitive pan-ErbB kinase inhibitor with IC50 values of 22 nM, 38 nM, and 21 nM for ErbB1, ErbB2, and ErbB4, respectively. JNJ28871063 hydrochloride inhibits phosphorylation of functionally important tyrosine residues in both EGFR and ErbB2. JNJ28871063 hydrochloride crosses the blood-brain barrier and has antitumor activity in human tumor xenograft models that overexpress EGFR and ErbB2.
  • HY-16438
    RRx-001

    		Apoptosis Parasite Cancer Infection Inflammation/Immunology
    RRx-001, a hypoxia-selective epigenetic agent and studied as a radio- and chem-sensitizer, triggers apoptosis and overcomes drug resistance in myeloma. RRx-001 exhibits potent anti-tumor activity with minimal toxicity. RRx-001 is a dual small molecule checkpoint inhibitor by downregulating CD47 and SIRP-α. RRx-001 is a potent inhibitor of G6PD and shows potent antimalarial activity.
  • HY-N6796
    Manumycin A

    		Farnesyl Transferase Ras Apoptosis Phospholipase Cancer Infection
    Manumycin A is an antibiotic. Manumycin A acts as a selective, competitive inhibitor of protein farnesyltransferase (FTase) with respect to farnesylpyrophosphate (Ki =1.2 μM), and as a noncompetitive inhibitor with respect to the Ras protein. Manumycin A induces apoptosis and exerts antitumor activity . Manumycin A suppresses exosome biogenesis and secretion via targeted inhibition of Ras/Raf/ERK1/2 signaling. Manumycin A is a nSMase inhibitor (EC50=0.25 μM).
  • HY-126249
    AAPK-25

    		Aurora Kinase Polo-like Kinase (PLK) Apoptosis Cancer
    AAPK-25 is a potent and selective Aurora/PLK dual inhibitor with anti-tumor activity, which can cause mitotic delay and arrest cells in a prometaphase, reflecting by the biomarker histone H3 Ser10 phosphorylation and followed by a surge in apoptosis. AAPK-25 targets Aurora-A, -B, and -C with Kd values ranging from 23-289 nM, as well as PLK-1, -2, and -3 with Kd values ranging from 55-456 nM.
  • HY-112429
    HJB97

    		Epigenetic Reader Domain Cancer
    HJB97 is a high-affinity BET inhibitor with Kis of 0.9 nM (BRD2 BD1), 0.27 nM (BRD2 BD2), 0.18 nM (BRD3 BD1), 0.21 nM (BRD3 BD2), 0.5 nM (BRD4 BD1), 1.0 nM (BRD4 BD2), respectively. HJB97 is employed for the design of potential PROTAC BET degrader and has antitumor activity.
  • HY-10201
    Sorafenib

    Bay 43-9006

    		 Raf VEGFR FLT3 Autophagy Apoptosis Ferroptosis Cancer
    Sorafenib (Bay 43-9006) is a potent and orally active Raf inhibitor with IC50s of 6 nM and 20 nM for Raf-1 and B-Raf, respectively. Sorafenib is a multikinase inhibitor with IC50s of 90 nM, 15 nM, 20 nM, 57 nM and 58 nM for VEGFR2, VEGFR3, PDGFRβ, FLT3 and c-Kit, respectively. Sorafenib induces autophagy and apoptosis. Sorafenib has anti-tumor activity. Sorafenib is a ferroptosis activator.
  • HY-103712A
    Samuraciclib hydrochloride

    CT7001 hydrochloride; ICEC0942 hydrochloride

    		 CDK Apoptosis Cancer
    Samuraciclib hydrochloride (CT7001 hydrochloride) is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC50 of 41 nM. Samuraciclib hydrochloride displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC50 of 578 nM), CDK5 and CDK9, respectively. Samuraciclib hydrochloride inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 µM. Samuraciclib hydrochloride has anti-tumor effects.
  • HY-50936S
    Trabectedin D3

    Ecteinascidin 743 D3; ET-743 D3

    		 Reactive Oxygen Species Apoptosis Cancer Inflammation/Immunology
    Trabectedin D3 (Ecteinascidin 743 D3) is deuterium labeled Trabectedin. Trabectedin is a tetrahydroisoquinoline alkaloid with potent antitumor activity. Trabectedin binds to the minor groove of DNA, blocks transcription of stress-induced proteins, induces DNA backbone cleavage and cancer cells apoptosis, and increases the generation of ROS in MCF-7 and MDA-MB-453 cells. Trabectedin has tje potential for soft tissue sarcoma and ovarian cancer treatment.
  • HY-126350
    CL2-SN-38

    		Drug-Linker Conjugates for ADC Cancer
    CL2-SN-38 is a part of the antibody drug conjugate (ADC), can conjugate with the anti-Trop-2-humanized antibody hRS7. SN-38 is a DNA topoisomerase I inhibitor. The anti-Trop-2 hRS7-CL2A-SN-38 ADC provides significant and specific antitumor effects against a range of human solid tumor types.
  • HY-10330S
    Toceranib-d8

    		PDGFR VEGFR c-Kit Cancer
    Toceranib-d8 (SU11654-d8) is the deuterium labeled Toceranib. Toceranib (SU11654) is an orally active receptor tyrosine kinase (RTK) inhibitor, and it potently inhibits PDGFR, VEGFR, and Kit with Kis of 5 and 6 nM for PDGFRβ and Flk-1/KDR, respectively. Toceranib (SU11654) has antitumor and antiangiogenic activity, and used in the treatment of canine mast cell tumors.
  • HY-131347
    PD-1/PD-L1-IN-NP19

    		PD-1/PD-L1 Cancer Inflammation/Immunology
    PD-1/PD-L1-IN-NP19 is a PD-1/PD-L1 inhibitor, with an IC50 of 12.5 nM for human PD-1/PD-L1 interaction. PD-1/PD-L1-IN-NP19 could activate the immune microenvironment in tumor, which may contribute to its antitumor effects.
  • HY-18174E
    Prexasertib dimesylate

    LY2606368 dimesylate

    		 Checkpoint Kinase (Chk) Apoptosis Cancer
    Prexasertib dimesylate (LY2606368 dimesylate) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib dimesylate inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib dimesylate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib dimesylate shows potent anti-tumor activity.
  • HY-112610
    CF53

    		Epigenetic Reader Domain Histone Acetyltransferase Cancer
    CF53 is a highly potent, selective and orally active inhibitor of BET protein, with a Ki of <1 nM, Kd of 2.2 nM and an IC50 of 2 nM for BRD4 BD1. CF53 binds to both the BD1 and BD2 domains of BRD2, BRD3, BRD4, and BRDT BET proteins with high affinities, very selective over non-BET bromodomain-containing proteins. CF53 shows potent anti-tumor activity both in vitro and in vivo.
  • HY-17364S
    Temozolomide-d3

    		DNA Alkylator/Crosslinker Autophagy Apoptosis Cancer
    Temozolomide-d3 (NSC 362856-d3) is the deuterium labeled Temozolomide. Temozolomide (NSC 362856) is an oral active DNA alkylating agent that crosses the blood-brain barrier. Temozolomide is also a proautophagic and proapoptotic agent. Temozolomide is effective against tumor cells that are characterized by low levels of O6-alkylguanine DNA alkyltransferase (OGAT) and a functional mismatch repair system. Temozolomide has antitumor and antiangiogenic effects.
  • HY-119940
    MC180295

    (rel)-MC180295

    		 CDK Cancer
    MC180295 ((rel)-MC180295) is a potent and selective CDK9-Cyclin T1 inhibitor, with an IC50 of 5 nM, at least 22-fold more selective for CDK9 over other CDKs. MC180295 also inhibits GSK-3α and GSK-3β. MC180295 ((rel)-MC180295) has potent anti-tumor effect.
  • HY-N2348
    Tubulysin D

    		Microtubule/Tubulin Apoptosis Cancer
    Tubulysin D is one of the most potent derivatives among the tubulysins isolated from the myxobacterial species Archangium geophyra and Angiococcus disciformis. Tubulysin D is a novel tetrapeptide that displays potent antitumor activity and leads to cell cycle arrest and apoptosis by inhibiting tubulin polymerization with an IC50 of 1.7 μM. Tubulysin displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the lower nanomolar range.
  • HY-101561
    Avapritinib

    BLU-285

    		 c-Kit PDGFR Cancer
    Avapritinib (BLU-285) is a highly potent, selective, and orally active KIT and PDGFRA activation loop mutant kinases inhibitor with IC50s of 0.27 and 0.24 nM for KIT D816V and PDGFRA D842V, respectively. Avapritinib (BLU-285) binds the active conformation of the kinase and shows antitumor activity. Avapritinib (BLU-285) attenuates the transport function of both ABCB1 and ABCG2.
  • HY-136927
    MSA-2

    		STING Cancer Inflammation/Immunology
    MSA-2, a potent and orally available non-nucleotide STING agonist, is bound to STING as a noncovalent dimer with nanomolar affinity. MSA-2 shows EC50s of 8.3 and 24 μM for human STING isoforms WT and HAQ, respectively. MSA-2 stimulates interferon-β secretion in tumors, induces tumor regression with durable antitumor immunity, and synergizes with anti-PD-1 in syngeneic mouse tumor models.
  • HY-10201A
    Sorafenib Tosylate

    Bay 43-9006 Tosylate

    		 Raf VEGFR FLT3 Autophagy Ferroptosis Apoptosis Cancer
    Sorafenib Tosylate (Bay 43-9006 Tosylate) is a potent and orally active Raf inhibitor with IC50s of 6 nM and 20 nM for Raf-1 and B-Raf, respectively. SorafenibTosylate is a multikinase inhibitor with IC50s of 90 nM, 15 nM, 20 nM, 57 nM and 58 nM for VEGFR2, VEGFR3, PDGFRβ, FLT3 and c-Kit, respectively. Sorafenib Tosylate induces autophagy and apoptosis. Sorafenib Tosylate has anti-tumor activity. Sorafenib Tosylate is a ferroptosis activator.
  • HY-103712B
    Samuraciclib trihydrochloride

    CT7001 trihydrochloride; ICEC0942 trihydrochloride

    		 CDK Apoptosis Cancer
    Samuraciclib (CT7001) trihydrochloride is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC50 of 41 nM. Samuraciclib trihydrochloride displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC50 of 578 nM), CDK5 and CDK9, respectively. Samuraciclib trihydrochloride inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 µM. Samuraciclib trihydrochloride has anti-tumor effects.
  • HY-114778
    Fluzoparib

    SHR3162; Fuzuloparib

    		 PARP Cancer
    Fluzoparib (SHR3162) is a potent and orally active PARP1 inhibitor (IC50=1.46±0.72 nM, a cell‐free enzymatic assay) with superior antitumor activity. Fluzoparib selectively inhibits the proliferation of homologous recombination repair (HR)‐deficient cells, and sensitizes both HR‐deficient and HR‐proficient cells to cytotoxic agents. Fluzoparib exhibits good pharmacokinetic properties in vivo and can be used for BRCA1/2-mutant relapsed ovarian cancer research.
  • HY-107691
    GR 159897

    		Neurokinin Receptor Cancer Endocrinology Neurological Disease
    GR 159897 is a highly potent, selective, competitive, brain-penetrated non-peptide neurokinin 2 (NK2) receptor antagonist. GR 159897 has little or no affinity for NK1 and NK3 receptors. GR 159897 inhibits binding of [ 3H]GR100679 to human NK2 (hNK2)-CHO cells and rat colon membranes with pKis of 9.51 and 10, respectively. Antagonizes bronchoconstriction. Anxiolytic-like and anti-tumor effects.
  • HY-116749
    Ethaselen

    BBSKE

    		 Others Cancer
    Ethaselen (BBSKE) is an orally active, selective thioredoxin reductase (TrxR) inhibitor with IC50s of 0.5 and 0.35 μM for the wild-type human TrxR1 and rat TrxR1, respectively. Ethaselen specifically binds to the unique selenocysteine-cysteine redox pair in the C-terminal active site of mammalian TrxR1. Ethaselen, an organoselenium compound, is a potent antitumor candidate that exerts potent inhibition on non-small cell lung cancer (NSCLC) by targeting TrxR.
  • HY-N6924
    Zingibroside R1

    		HIV Infection Metabolic Disease
    Zingibroside R1 is dammaranae-type triterpenoid saponin, isolated from rhizomes, taproots, and lateral roots of Panax japonicas C. A. Meyer, shows excellent anti-tumor effects as well as anti-angiogenic activity. Zingibroside R1 possesses some anti-HIV-1 activity. Zingibroside R1 has inhibitory effects on the 2-deoxy-D-glucose (2-DG) uptake by EAT cells (IC50=91.3 μM).
  • HY-113914
    9-ING-41

    		GSK-3 Apoptosis Autophagy Cancer
    9-ING-41 is a maleimide-based ATP-competitive and selective glycogen synthase kinase-3β (GSK-3β) inhibitor with an IC50 of 0.71 μM. 9-ING-41 significantly leads to cell cycle arrest, autophagy and apoptosis in cancer cells. 9-ING-41 has anticancer activity and has the potential for enhancing the antitumor effects of chemotherapeutic drugs.
  • HY-121618
    α-Thujone

    		GABA Receptor Reactive Oxygen Species Parasite Apoptosis Autophagy Cancer Infection Neurological Disease
    α-Thujone is a monoterpene isolated from Thuja occidentalis essential oil with potent anti-tumor activities. α-Thujone is a reversible modulator of the GABA type A receptor and the IC50 for α-Thujone is 21 μM in suppressing the GABA-induced currents. α-Thujone induces ROS accumulation-dependent cytotoxicity, also induces cell apoptosis and autophagy. α-Thujone has antinociceptive, insecticidal, and anthelmintic activity, and easily penetrates the blood-brain barrier.
  • HY-128769
    M2N12

    		CDK Cancer
    M2N12 is a potent and highly selective cell division cycle 25C protein phosphatase (Cdc25C) inhibitor with an IC50 value of 0.09  μM. M2N12 also has promising activity against Cdc25A and Cdc25B with IC50 values of  0.53  μM and 1.39 μM, respectively. M2N12 has anti-tumor activity and can be used for cancer research.
  • HY-N0166
    Gramine

    Donaxine

    		 Adiponectin Receptor Adrenergic Receptor Reverse Transcriptase Cancer Infection Metabolic Disease Endocrinology
    Gramine (Donaxine) is a natural alkaloid isolated from giant reed, acts as an active adiponectin receptor (AdipoR) agonist, with IC50s of 3.2 and 4.2 µM for AdipoR2 and AdipoR1, respectively. Gramine is also a human and mouse β2-Adrenergic receptor (β2-AR) agonist. Gramine (Donaxine) has anti-tumor, anti-viral and anti-inflammatory properties.
  • 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-112611
    H3B-5942

    		Estrogen Receptor/ERR Cancer
    H3B-5942 is a selective, irreversible and orally active estrogen receptor covalent antagonist, inactivates both wild-type and mutant ERα by targeting Cys530, with Kis of 1 nM and 0.41 nM, respectively. H3B-5942 reduces ERα target gene GREB1, shows potent antitumor activity both in multiple cell lines or animals bearing ERα WT or ERα mutations.
  • HY-12170
    Prinomastat

    AG3340; KB-R9896

    		 MMP Apoptosis Cancer
    Prinomastat (AG3340) is a broad spectrum, potent, orally active metalloproteinase (MMP) inhibitor with IC50s of 79, 6.3 and 5.0 nM for MMP-1, MMP-3 and MMP-9, respectively. Prinomastat inhibits MMP-2, MMP-3 and MMP-9 with Kis of 0.05 nM, 0.3 nM and 0.26 nM, respectively. Prinomastat crosses blood-brain barrier. Antitumor avtivity.
  • HY-12170A
    Prinomastat hydrochloride

    AG3340 hydrochloride; KB-R9896 hydrochloride

    		 MMP Apoptosis Cancer
    Prinomastat hydrochloride (AG3340 hydrochloride) is a broad spectrum, potent, orally active metalloproteinase (MMP) inhibitor with IC50s of 79, 6.3 and 5.0 nM for MMP-1, MMP-3 and MMP-9, respectively. Prinomastat hydrochloride inhibits MMP-2, MMP-3 and MMP-9 with Kis of 0.05 nM, 0.3 nM and 0.26 nM, respectively. Prinomastat hydrochloride can cross blood-brain barrier. Antitumor avtivity.
  • HY-114263
    NXT629

    		PPAR Cancer
    NXT629 is a potent, selective, and competitive PPAR-α antagonist, with an IC50 of 77 nM for human PPARα, shows high selectivity over other nuclear hormone receptor, such as PPARδ, PPARγ, ERβ, GR and TRβ, IC50s are 6.0, 15, 15.2, 32.5 and >100 μM, respectively. NXT629 has potent anti-tumor activity and inhibits experimental metastasis of cancer cell in animal models.
  • HY-14572
    PR-104A

    SN 27858

    		 DNA Alkylator/Crosslinker Cancer
    PR-104A (SN 27858) is the alcohol metabolite of phosphate prodrug PR-104. PR-104A is a hypoxia-selective DNA cross-linking agent/DNA-damaging agent and cytotoxin. Antitumor Activity. PR-104A is metabolized under hypoxia by the 1-electron NADPH:cytochrome P450 oxidoreductase. PR-104A can be used for the research of relapsed/refractory T-lineage acute lymphoblastic leukemia (T-ALL).
  • HY-123986
    CTPI-2

    		Mitochondrial Metabolism Cancer Inflammation/Immunology
    CTPI-2 is a third-generation mitochondrial citrate carrier SLC25A1 inhibitor with a KD of 3.5 μM. CTPI-2 inhibits glycolysis, PPARγ, and its downstream target the glucose transporter GLUT4. CTPI-2 halts salient alterations of NASH reverting steatosis, preventing the evolution to steatohepatitis, reducing inflammatory macrophage infiltration in the liver and adipose tissue, and starkly mitigating obesity induced by a high-fat diet. Antitumor activity.
  • HY-132307
    Mcl-1 inhibitor 6

    		Bcl-2 Family Apoptosis Cancer
    Mcl-1 inhibitor 6 is an orally active, selective myeloid cell leukemia 1 (Mcl-1) protein inhibitor with a Kd of 0.23 nM and a Ki of 0.02 μM. Mcl-1 inhibitor 6 possesses superior selectivity over other Bcl-2 family members (Bcl-2, Bcl2A1, Bcl-xL, and Bcl-w, Kd>10 μM). Mcl-1 inhibitor 6 is a potent antitumor agent.
  • HY-116624
    MAZ51

    		VEGFR Apoptosis Cancer
    MAZ51 is a selective inhibitor of VEGFR-3 (Flt-4) tyrosine kinase. MAZ51 inhibits VEGF-C-induced activation of VEGFR-3 without blocking VEGF-C-mediated stimulation of VEGFR2. MAZ51 had no effect on ligand-induced autophosphorylation of EGFR, IGF-1R and PDGFRβ. MAZ51 blocks proliferation and induces apoptosis in a wide variety of tumor cells. Antitumor activity.
  • HY-16749
    Pexidartinib

    PLX-3397

    		 c-Fms c-Kit Apoptosis Cancer
    Pexidartinib (PLX-3397) is a potent, orally active, selective, and ATP-competitive colony stimulating factor 1 receptor (CSF1R or M-CSFR) and c-Kit inhibitor, with IC50s of 20 and 10 nM, respectively. Pexidartinib (PLX-3397) exhibits 10- to 100-fold selectivity for c-Kit and CSF1R over other related kinases. Pexidartinib (PLX-3397) induces cell apoptosis and has anti-tumor activity.
  • HY-132192
    PD-1/PD-L1-IN-9

    		PD-1/PD-L1 Cancer
    PD-1/PD-L1-IN-9 is a potent and orally active inhibitor of PD-1/PD-L1 interaction, with an IC50 of 3.8 nM. PD-1/PD-L1-IN-9 can enhance the killing activity of tumor cells by immune cells. PD-1/PD-L1-IN-9 also exhibits significant in vivo antitumor activity in a CT26 mouse model.
  • HY-101249
    L-732138

    		Neurokinin Receptor Cancer Neurological Disease
    L-732138 is a selective, potent and competitive neurokinin-1 (NK-1) receptor antagonist with an IC50 of 2.3 nM. L-732138 has 200-fold more potent in cloned human NK-1 receptors than cloned rat NK-1 receptors, and has > 1000-fold more potent than human NK-2 and NK-3 receptors. L-732138 can reduce hyperalgesia and has antitumor action.
  • HY-W009732
    Sinapinic acid

    Sinapic acid

    		 HDAC Angiotensin-converting Enzyme (ACE) Reactive Oxygen Species Apoptosis Cancer Metabolic Disease
    Sinapinic acid (Sinapic acid) is a phenolic compound isolated from Hydnophytum formicarum Jack. Rhizome, acts as an inhibitor of HDAC, with an IC50 of 2.27 mM, and also inhibits ACE-I activity. Sinapinic acid posssess potent anti-tumor activity, induces apoptosis of tumor cells. Sinapinic acid shows antioxidant and antidiabetic activities. Sinapinic acid reduces total cholesterol, triglyceride, and HOMA-IR index, and also normalizes some serum parameters of antioxidative abilities and oxidative damage in ovariectomized rats.
  • HY-14571
    E7820

    ER68203-00

    		 Integrin Cancer
    E7820 (ER68203-00), an orally active aromatic sulfonamide derivative, is a unique angiogenesis inhibitor suppressing an expression of integrin alpha2 subunit on endothelium. E7820 inhibits rat aorta angiogenesis with an IC50 of 0.11 μg/ml. E7820 modulates α-1, α-2, α-3, and α-5 integrin mRNA expression. Antiangiogenic and antitumor activity.
  • HY-135805
    JBJ-04-125-02

    		EGFR Cancer
    JBJ-04-125-02 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor with an IC50 of 0.26 nM for EGFR L858R/T790M. JBJ-04-125-02 can inhibit cancer cell proliferation and EGFR L858R/T790M/C797S signaling. JBJ-04-125-02 has anti-tumor activities.
  • HY-N2187
    Deoxyshikonin

    		Bacterial HIF/HIF Prolyl-Hydroxylase Cancer Infection Cardiovascular Disease
    Deoxyshikonin is isolated from Lithospermum erythrorhizon Sieb with antitumor activity. Deoxyshikonin increases the expression of VEGF-C and VEGF-A mRNA in HMVEC-dLy, promotes HIF-1α and HIF-1β subunit interaction and binds to specific DNA sequences targeted by HIF, indicates a prolymphangiogenesis as well as a proangiogenesis effect in vitro. Deoxyshikonin shows significant synergic antimicrobial activity against S. pneumonia (MIC=17 μg/mL), also shows significantly inhibitory activities against MRSA.
  • HY-111508
    PI3K/mTOR Inhibitor-2

    		PI3K mTOR Cancer
    PI3K/mTOR Inhibitor-2 is a potent dual pan-PI3K/mTOR inhibitor with IC50s of 3.4/34/16/1 nM for PI3Kα/PI3Kβ/PI3Kδ/PI3Kγ and 4.7 nM for mTOR. Antitumor activity.
  • 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-N3032
    Xanthatin

    		Apoptosis VEGFR Lipoxygenase Bacterial Cancer Infection Inflammation/Immunology
    Xanthatin is isolated from Xanthium strumarium leaves. Xanthatin exhibits strong antitumor activities against a variety of cancer cells through apoptosis persuasion and shows anti-inflammatory activities by inhibiting PGE2 synthesis and 5-lipoxygenase activity. Xanthatin is a potent and orally active inhibitor of VEGFR2 kinase activity with an IC50 of 3.8 μM and prominently blocks the phosphorylation of VEGFR2 at Tyr951 site. Xanthatin inhibits angiogenesis and has the potential for the investigation of breast 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-112602
    PI3K/mTOR Inhibitor-1

    		PI3K mTOR Cancer
    PI3K/mTOR Inhibitor-1 is a potent, orally bioavailable dual PI3K/mTOR inhibitor with IC50s of 20/376/204/46 nM and 186 nM for PI3Kα/PI3Kβ/PI3Kγ/PI3Kδ and mTOR, respectively. Antitumor activity.
  • HY-111553
    TAS0728

    		EGFR Cancer
    TAS0728 is a potent, selective, orally active, irreversible and covalent-binding HER2 inhibitor, binds to HER2 at C805, inhibits its kinase activity, with an IC50 of 13 nM. TAS0728 shows IC50s of 4.9, 8.5, 31, 65, 33, 25, 86 and 36 nM for BMX, HER4, BLK, EGFR, JAK3, SLK, LOK and human HER2, respectively. TAS0728 also inhibits the phosphorylation of HER2, HER3, and downstream effectors, shows no obvious effect on EGFR. Antitumor activity.
  • HY-P2657
    Verucopeptin

    		HIF/HIF Prolyl-Hydroxylase Proton Pump Endogenous Metabolite Cancer
    Verucopeptin is a potent HIF-1 (IC50=0.22 μM) inhibitor and decreases the expression of HIF-1 target genes and HIF-1α protein levels. Verucopeptin strongly inhibits v-ATPase activity by directly targeting the v-ATPase ATP6V1G subunit but not ATP1V1B2 or ATP6V1D. Verucopeptin exhibits antitumor activity against multidrug resistance (MDR) cancers and can be used for cancer research.
  • HY-19896
    COTI-2

    		MDM-2/p53 Apoptosis Cancer
    COTI-2, an anti-cancer drug with low toxicity, is an orally available third generation activator of p53 mutant forms. COTI-2 acts both by reactivating mutant p53 and inhibiting the PI3K/AKT/mTOR pathway. COTI-2 induces apoptosis in multiple human tumor cell lines. COTI-2 exhibits antitumor activity in HNSCC through p53-dependent and -independent mechanisms. COTI-2 converts mutant p53 to wild-type conformation.
  • HY-15514A
    Merestinib dihydrochloride

    LY2801653 dihydrochloride

    		 c-Met/HGFR FLT3 ROS Discoidin Domain Receptor Cancer
    Merestinib dihydrochloride (LY2801653 dihydrochloride) is a potent, orally bioavailable c-Met inhibitor (Ki=2 nM) with anti-tumor activities. Merestinib dihydrochloride also has potent activity against MST1R (IC50=11 nM), FLT3 (IC50=7 nM), AXL (IC50=2 nM), MERTK (IC50=10 nM), TEK (IC50=63 nM), ROS1, DDR1/2 (IC50=0.1/7 nM) and MKNK1/2 (IC50=7 nM).
  • HY-N1940
    β-Anhydroicaritin

    		Interleukin Related TNF Receptor MMP Inflammation/Immunology
    β-Anhydroicaritin is isolated from Boswellia carterii Birdware, has important biological and pharmacological effects, such as antiosteoporosis, estrogen regulation and antitumor properties. β-Anhydroicaritin ameliorates the degradation of periodontal tissue and inhibits the synthesis and secretion of TNF-α and MMP-3 in diabetic rats. β-Anhydroicaritin decreases the overproduction of NO, IL-10, TNF-α, MCP-1 and IL-6 in inperitonitis mice. β-Anhydroicaritin inhibits the elevation of intracellular Ca 2+, and markedly decreases iNOS protein expression.
  • HY-15514
    Merestinib

    LY2801653

    		 c-Met/HGFR FLT3 ROS Discoidin Domain Receptor Cancer
    Merestinib (LY2801653) is a potent, orally bioavailable c-Met inhibitor (Ki=2 nM) with anti-tumor activities. Merestinib (LY2801653) also has potent activity against MST1R (IC50=11 nM), FLT3 (IC50=7 nM), AXL (IC50=2 nM), MERTK (IC50=10 nM), TEK (IC50=63 nM), ROS1, DDR1/2 (IC50=0.1/7 nM) and MKNK1/2 (IC50=7 nM).
  • HY-N1992
    Theaflavin 3,3'-digallate

    TF-3; ZP10

    		 Virus Protease HSV HIV Cancer Infection
    Theaflavin 3,3'-digallate (TF-3) is a potent Zika virus (ZIKV) protease inhibitor with an IC50 of 2.3 μM. Theaflavin 3,3'-digallat directly binds to ZIKVpro (Kd=8.86 µM) and inhibits ZIKV replication. Theaflavin 3,3'-digallat inhibits the activity of gp41 and NS2B-3 protease and has antiviral activity against HSV and HIV-1. Theaflavin 3,3'-digallate, the typical pigment in black tea, is a potent antitumor agent.
  • HY-112614
    ATM Inhibitor-1

    		ATM/ATR Cancer
    ATM Inhibitor-1 is a highly potent, selective and orally active ATM inhibitor, with an IC50 of 0.7 nM, shows weak activity against mTOR (IC50, 21 μM), DNAPK (IC50, 2.8 μM), PI3Kα (IC50, 3.8 μM), PI3Kβ (IC50, 10.3 μM), PI3Kγ (IC50, 3 μM) and PI3Kδ (IC50, 0.73 μM). ATM Inhibitor-1 exhibits anti-tumor activity.
  • HY-100513A
    Dehydroaltenusin

    		Apoptosis DNA/RNA Synthesis Antibiotic Cancer
    Dehydroaltenusin is a small molecule selective inhibitor of eukaryotic DNA polymerase α, a type of antibiotic produced by a fungus with an IC50 value of 0.68 μM. The inhibitory mode of action of dehydroaltenusin against mammalian pol α activity is competitive with respect to the DNA template primer (Ki=0.23 µM) and non-competitive with respect to the 2'-deoxyribonucleoside 5'-triphosphate substrate (Ki=0.18 µM). Dehydroaltenusin arrests the cancer cell cycle at the S-phase and triggers apoptosis. Dehydroaltenusin possesses anti-tumor activity against human adenocarcinoma tumor in vivo.
  • HY-128946
    CL2A-SN-38

    		Drug-Linker Conjugates for ADC Cancer Inflammation/Immunology
    CL2A-SN-38 is a drug-linker conjugate composed of a potent a DNA Topoisomerase I inhibitor SN-38 and a linker CL2A to make antibody drug conjugate (ADC). CL2A-SN-38 provides significant and specific antitumor effects against a range of human solid tumor types. CL2A is a nonclaevable complicated PEG8- and triazole-containing PABC-peptide-mc linker. CL2A is cleavable through pH sensitivity, giving rise to bystander effect, and binds the antibody at a cysteine residue via a disulfide bond.
  • HY-126251
    CDK9-IN-7

    		CDK Apoptosis Cancer
    CDK9-IN-7 (compound 21e) is a selective, highly potent, and orally active CDK9/cyclin T inhibitor (IC50=11 nM), which exhibits more potent over other CDKs (CDK4/cyclinD=148 nM; CDK6/cyclinD=145 nM). CDK9-IN-7 shows antitumor activity without obvious toxicity. CDK9-IN-7 induces NSCLC cell apoptosis, arrests the cell cycle in the G2 phase, and suppresses the stemness properties of NSCLC.
  • HY-134472
    PI3Kδ-IN-8

    		PI3K Cancer
    PI3Kδ-IN-8 is a potent, selective and orally active PI3Kδ inhibitor, with an IC50 of 3.3 nM. PI3Kδ-IN-8 shows selectivity for PI3Kδ over PI3Kα, PI3Kβ, and PI3Kγ (IC50=377.2, 241.6, 17.9 nM, respectively). PI3Kδ-IN-8 has anti-tumor activity.
  • HY-128860
    Mutated EGFR-IN-2

    		EGFR Cancer
    Mutated EGFR-IN-2 (compound 91) is a mutant-selective EGFR inhibitor extracted from patent WO2017036263A1, which potently inhibits single-mutant EGFR (T790M) and double-mutant EGFR (including L858R/T790M (IC50=＜1nM) and ex19del/T790M), and can suppress activity of single gain-of-function mutant EGFR (including L858R and ex19del) as well. Mutated EGFR-IN-2 shows anti-tumor antivity.
  • HY-15730
    Poziotinib

    HM781-36B; NOV120101

    		 EGFR Apoptosis Cancer
    Poziotinib (HM781-36B) is an orally active, irreversible pan-HER inhibitor, which effectively inhibits EGFR wt, HER-2 and HER-4 with IC50s of 3.2, 5.3 and 23.5 nM, respectively. Poziotinib (HM781-36B) also shows excellent inhibitory activities against mutated EGFRs, including EGFR T790M and EGFR L858R/T790M, with IC50s of 4.2 and 2.2 nM, respectively. Excellent antitumor activity.
  • HY-129602
    SD-36

    		PROTAC and Building Blocks STAT Apoptosis Cancer
    SD-36 is a potent and efficacious PROTAC STAT3 degrader (Kd=~50 nM), and demonstrates high selectivity over other STAT members. SD-36 also effectively degrades mutated STAT3 proteins in cells and suppresses the transcriptional activity of STAT3 (IC50=10 nM). SD-36 exerts robust anti-tumor activity, and achieves complete and long-lasting tumor regression in mouse tumor models. SD-36 is composed of the STAT3 inhibitor SI-109, a linker, and an analog of CRBN ligand Lenalidomide for E3 ubiquitin ligase.
  • HY-136065
    bpV(phen)

    		PTEN Phosphatase Parasite Apoptosis Cancer Infection Metabolic Disease Inflammation/Immunology
    bpV(phen), a insulin-mimetic agent, is a potent protein tyrosine phosphatase (PTP) and PTEN inhibitor with IC50s of 38 nM, 343 nM and 920 nM for PTEN, PTP-β and PTP-1B, respectively. bpV(phen) inhibits proliferation of the protozoan parasite Leishmania in vitro. bpV(phen) strongly induces the secretion of a large number of chemokines and pro-inflammatory cytokines, and it activates a Th1-type pathway (IL-12, IFNγ). bpV(phen) can also induce cell apoptosis, and has anti-angiogenic and anti-tumor activity.
  • HY-122818
    bpV(phen) trihydrate

    		PTEN Phosphatase Parasite Apoptosis Cancer Infection Metabolic Disease Inflammation/Immunology
    bpV(phen) trihydrate, a insulin-mimetic agent, is a potent protein tyrosine phosphatase (PTP) and PTEN inhibitor with IC50s of 38 nM, 343 nM and 920 nM for PTEN, PTP-β and PTP-1B, respectively. bpV(phen) trihydrate inhibits proliferation of the protozoan parasite Leishmania in vitro. bpV(phen) trihydrate strongly induces the secretion of a large number of chemokines and pro-inflammatory cytokines, and it activates a Th1-type pathway (IL-12, IFNγ). bpV(phen) trihydrate can also induce cell apoptosis, and has anti-angiogenic and anti-tumor activity.
  • HY-111388A
    SEL120-34A monohydrochloride

    		CDK Cancer
    SEL120-34A monohydrochloride is an ATP-competitive and selective CDK8 inhibitor, inhibits kinase activities of CDK8/CycC and CDK19/CycC complexes with IC50s of 4.4 nM and 10.4 nM, respectively, with a Kd of 3 nM for CDK8. SEL120-34A monohydrochloride weakly inhibits CDK9 (calculated IC50=1070 nM), but shows no obvious activity against CDK1, 2, 4, 6, 5, 7. SEL120-34A monohydrochloride inhibits phosphorylation of STAT1 S727 and STAT5 S726. Has anti-tumor activity.
  • HY-11080A
    PKI-179 hydrochloride

    		PI3K mTOR Cancer
    PKI-179 hydrochloride is a potent and orally active dual PI3K/mTOR inhibitor, with IC50s of 8 nM, 24 nM, 74 nM, 77 nM, and 0.42 nM for PI3K-α, PI3K-β, PI3K-γ, PI3K-δ and mTOR, respectively. PKI-179 hydrochloride also exhibits activity over E545K and H1047R, with IC50s of 14 nM and 11 nM, respectively. PKI-179 hydrochloride shows anti-tumor activity in vivo.
  • HY-11080
    PKI-179

    		PI3K mTOR Cancer
    PKI-179 is a potent and orally active dual PI3K/mTOR inhibitor, with IC50s of 8 nM, 24 nM, 74 nM, 77 nM, and 0.42 nM for PI3K-α, PI3K-β, PI3K-γ, PI3K-δ and mTOR, respectively. PKI-179 also exhibits activity over E545K and H1047R, with IC50s of 14 nM and 11 nM, respectively. PKI-179 shows anti-tumor activity in vivo.
  • HY-N2515
    Ginsenoside Rk1

    		NF-κB PI3K JAK Apoptosis Cancer Inflammation/Immunology
    Ginsenoside Rk1 is a unique component created by processing the ginseng plant (mainly Sung Ginseng, SG) at high temperatures. Ginsenoside Rk1 has anti-inflammatory effect, suppresses the activation of Jak2/Stat3 signaling pathway and NF-κB. Ginsenoside Rk1 has anti-tumor effect, antiplatelet aggregation activities, anti-insulin resistance, nephroprotective effect, antimicrobial effect, cognitive function enhancement, lipid accumulation reduction and prevents osteoporosis. Ginsenoside Rk1 induces cell apoptosis by triggering intracellular reactive oxygen species (ROS) generation and blocking PI3K/Akt pathway.
  • HY-12307
    (-)-Indolactam V

    Indolactam V

    		 PKC Cancer
    (-)-Indolactam V is a PKC activator, with Kis of 3.36 nM, 1.03 μM for η-CRD2 (PKCη surrogate peptide), γ-CRD2 (PKCγ surrogate peptide), and Kds of 5.5 nM (η-C1B), 7.7 nM (ε-C1B), 8.3 nM (δ-C1B), 18.9 nM (β-C1A-long), 20.8 nM (α-C1A-long), 137 nM (β-C1B), 138 nM (γ-C1A), 213 nM (γ-C1B), and has antitumor activity.
  • HY-10587
    BIX-01294

    		Histone Methyltransferase Autophagy Cancer
    BIX-01294 is a reversible and highly selective G9a Histone Methyltransferase inhibitor, with an IC50 of 2.7 μM in DELFIA assay. BIX-01294 specifically inhibits G9a (H3K9me2) and GLP enzyme (H3K9me3), with IC50s of 1.7 μM and 38 μM, respectively. BIX-01294 inhibits G9a/GLP by competing for binding with the amino acids N-terminal of the substrate lysine residue. BIX-01294, a (1H-1,4-diazepin-1-yl)-quinazolin-4-yl amine derivative, induces necroptosis and autophagy. BIX-01294 has antitumor activity in recurrent tumor cells.