Search Result
Results for "
proliferative activity
" in MedChemExpress (MCE) Product Catalog:
5
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-156285
-
|
Histone Methyltransferase
Apoptosis
|
Cancer
|
ZZM-1220 is a histone lysine methyltransferase G9a/GLP covalent inhibitor with IC50s of of 458 nM and 924 nM, respectively. ZZM-1220 inhibits H3K9me2 in cells and significantly induces apoptosis of triple-negative breast cancer (TNBC) cells and blocks the cell cycle in the G2/M phase .
|
-
-
- HY-148185
-
|
ADC Cytotoxin
|
Cancer
|
T01-1 is an anticancer agent (camptothecin derivative) with good anti-proliferative activity .
|
-
-
- HY-115980
-
|
Apoptosis
|
Cancer
|
Anticancer agent 39 (compound B12), a fluorescent derivative of Jiyuan Oridonin A (JOA), induces the collapse of mitochondrial membrane potential (MMP)and thus induced apoptosis.Anticancer agent 39 inhibits cell cloning and migration.Anticancer agent 39 exhibits promising anti-proliferative activity against HGC-27 cells with IC50 value of 0.39 μM .
|
-
-
- HY-U00345
-
-
-
- HY-N8239
-
|
Others
|
Others
|
Cepharanoline is a compound isolated from Stephania cepharantha Hayata. Cepharanoline has proliferative activities .
|
-
-
- HY-153753
-
|
Others
|
Cancer
|
Wnt pathway inhibitor 4 (compound 16D) is an anticancer agent that has anti-proliferative activity .
|
-
-
- HY-N0202
-
Asterolide
|
Apoptosis
|
Cancer
|
Atractylenolide II is a sesquiterpene compound isolated from the dried rhizome of Atractylodes macrocephala (Baizhu in Chinese); anti-proliferative activity.
|
-
-
- HY-B0421S
-
-
-
- HY-N3355
-
|
Others
|
Cancer
|
Lupeolic acid can be isolated from Boswellia sacra. Lupeolic acid has anti-proliferative activity and can be used in cancer research .
|
-
-
- HY-N8477
-
-
-
- HY-147747
-
|
HSP
|
Cancer
|
Among vibsanin a analogues, vibsanin a analog C (VAC) showed anti proliferative effect on various cancer cell lines, and the anti proliferative activity was the strongest among vibsanin a analogues. In addition, VAC fluctuated the amount of hsp90 related proteins in cells and inhibited hsp90 mediated protein refolding of luciferase in vitro.
|
-
-
- HY-146506
-
|
Microtubule/Tubulin
|
Cancer
|
isoCA-4, a Combretastatin A4 derivative, is a tubulin polymerization inhibitor. isoCA-4 has anti-proliferative activities .
|
-
-
- HY-N10699
-
|
Others
|
Cancer
|
6-Methoxykaempferol is a flavone that can be found in brazilian propolis. 6-Methoxykaempferol shows anti-proliferative activity for cancer cells .
|
-
-
- HY-N11136
-
|
Others
|
Cancer
|
Schizolaenone C is a natural product that can be found in Schizolaena hystrix. Schizolaenone C exhibits anti-proliferative and anti-oxidative activities .
|
-
-
- HY-W013032A
-
Sodium oxamate
|
Lactate Dehydrogenase
Apoptosis
|
Cancer
|
Oxamic acid (oxamate) sodium salt is a lactate dehydrogenase-A (LDH-A) inhibitor. Oxamic acid sodium salt shows anti-tumor activity, and anti-proliferative activity against cancer cells, and can induce apoptosis .
|
-
-
- HY-N3527
-
|
Others
|
Cancer
|
Calyxin B can be extracted from the seeds of Alpinia blepharocalyx. Calyxin B has anti-proliferative activity and can be used in cancer research .
|
-
-
- HY-N3428
-
|
Others
|
Cancer
|
Kamebanin can be isolated from the leaves of Isodon weisiensis C. Y. Wu. Kamebanin has anti-proliferative activity and can be used in cancer research .
|
-
-
- HY-143250
-
|
Microtubule/Tubulin
|
Cancer
|
Tubulin inhibitor 12 (Hit 9) is a novel tubulin inhibitor (IC50=25.3 μM). Tubulin inhibitor 12 shows anti-tumor activity and anti-proliferative activity .
|
-
-
- HY-W013332
-
|
HIV
|
Infection
Inflammation/Immunology
|
3-Deazaadenosine is an inhibitor of S-adenosylhomocysteine hydrolase, with a Ki of 3.9 µM; 3-Deazaadenosine has anti-inflammatory, anti-proliferative and anti-HIV activity.
|
-
-
- HY-W013332A
-
|
HIV
|
Infection
Inflammation/Immunology
|
3-Deazaadenosine (hydrochloride) is an inhibitor of S-adenosylhomocysteine hydrolase, with a Ki of 3.9 µM; 3-Deazaadenosine has anti-inflammatory, anti-proliferative and anti-HIV activity.
|
-
-
- HY-100757
-
|
Histone Methyltransferase
|
Cancer
|
CPUY074020 is a potent and oral bioavailable inhibitor of histone methyltransferase G9a, with an IC50 of 2.18 μM. CPUY074020 possesses anti-proliferative activity .
|
-
-
- HY-N10393
-
|
PKC
HSP
|
Cancer
|
Vibsanin A, a protein kinase C (PKC) activator, exhibits anti-proliferative activity against human cancer cell lines. Vibsanin A is also a HSP90 inhibitor .
|
-
-
- HY-152001
-
|
Carbonic Anhydrase
|
Cancer
|
hCA IX-IN-2 is a potent and selectively hCA IX inhibitor with an KI value of 32.1 nM. hCA IX-IN-2 shows anti-proliferative activity .
|
-
-
- HY-15605
-
LGX818
|
Raf
|
Cancer
|
Encorafenib (LGX818) is a highly potent BRAF inhibitor with selective anti-proliferative and apoptotic activity in cells expressing BRAF V600E (EC50=4 nM).
|
-
-
- HY-117737A
-
|
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-146889
-
|
Others
|
Cancer
|
ATX inhibitor 16 is a potent ATX inhibitor with an IC50 of 0.0021 µM. ATX inhibitor 16 shows excellent anti-proliferative activities in breast cancer cells .
|
-
-
- HY-146890
-
|
Others
|
Cancer
|
ATX inhibitor 17 is a potent ATX inhibitor with an IC50 of 0.019 µM. ATX inhibitor 17 shows excellent anti-proliferative activities in breast cancer cells .
|
-
-
- HY-155094
-
|
DNA/RNA Synthesis
|
Others
|
DNA polymerase-IN-3 (Compd 5b) is a coumarin derivative that exhibits inhibitory activity against Taq DNA polymerase and can be used in proliferative disease research .
|
-
-
- HY-161057
-
-
-
- HY-W005130
-
|
NF-κB
|
Metabolic Disease
|
2,4,6-Trihydroxybenzaldehyde is an orally active NF-ĸB inhibitor. 2,4,6-Trihydroxybenzaldehyde shows anti-tumor activity, anti-cancer cell proliferative activity and anti-obesity activity .
|
-
-
- HY-N2198
-
|
|
|
Podocarpusflavone A is a DNA topoisomerase I inhibitor. Podocarpusflavone A has moderated anti-proliferative activity and induces cell apoptosis in MCF-7. Podocarpusflavone A is developing anti-tumor agents .
|
-
-
- HY-N10670
-
Methylpluviatolide
|
Apoptosis
|
Cancer
|
Bursehernin (Methylpluviatolide) is an antitumor agent. Bursehernin induces Apoptosis and cell cycle arrest at G2/M phase. Bursehernin shows anti-proliferative activity .
|
-
-
- HY-152091
-
|
Fungal
|
Infection
Cancer
|
Antiproliferative agent-18 (Compound 5k) is an anti-proliferative agent. Antiproliferative agent-18 also displays moderate anti-bacterial and anti-fungi activity .
|
-
-
- HY-151996
-
|
Microtubule/Tubulin
|
Cardiovascular Disease
|
Tubulin inhibitor 31 is a potent tubulin inhibitor with an IC50 value of 4 µM. Tubulin inhibitor 31 shows anti-proliferative activity. Tubulin inhibitor 31 inhibits the HUVEC migration .
|
-
-
- HY-152512
-
|
Androgen Receptor
|
Cancer
|
RLA-4842 is an iron activator containing anti-androgen. RLA-4842 has anti-proliferative activity on metastatic castration-resistant prostate cancer (mCRPC) cell line .
|
-
-
- HY-152520
-
|
Androgen Receptor
|
Cancer
|
RLA-5331 is an iron activator containing anti-androgen. RLA-5331 has anti-proliferative activity on metastatic castration-resistant prostate cancer (mCRPC) cell line .
|
-
-
- HY-153982
-
|
PPAR
|
Metabolic Disease
|
PPARγ agonist 8 is an agonist of PPARγ. PPARγ agonist 8 induces peroxisome proliferator response element (PPRE)-luciferase activity with an EC50 of 0.2 μM .
|
-
-
- HY-N12601
-
|
Apoptosis
|
Cancer
|
Diselaginellin B (compound 2) is a natural product isolated from Selaginella Pulvinata, which exhibits anti-proliferative, apoptosis-inducing and antimetastatic activities against human carcinoma hepatocellular cells .
|
-
-
- HY-N7640
-
|
Others
|
Inflammation/Immunology
Cancer
|
Desoxylimonin is an orally active triterpenoid compound found from grapefruit seed. Desoxylimonin shows anti-proliferative activities to breast cancer cells. Desoxylimonin derivatives shows better anticancer, analgesic and anti-inflammatory activity than the lead compound .
|
-
-
- HY-19937
-
|
PPAR
|
Metabolic Disease
|
Saroglitazar is a novel peroxisome proliferator-activated receptor (PPAR) agonist with predominant PPARα and moderate PPARγ activity with EC50 values of 0.65 pM and 3 nM in HepG2 cells, respectively.
|
-
-
- HY-N10392
-
|
Apoptosis
|
Cancer
|
(S)-Erypoegin K is a potent anticancer agent. (S)-Erypoegin K shows potent anti-proliferative activity against HL-60 cells. (S)-Erypoegin K induces apoptosis .
|
-
-
- HY-147318
-
|
Apoptosis
|
Cancer
|
PBENZ-DBRMD is a potent iodothyronine deiodinase type 3 (DIO3) inhibitor. PBENZ-DBRMD has anti-proliferative activity and induces apoaptosis. PBENZ-DBRMD can be used for cancer research .
|
-
-
- HY-149927
-
|
Others
|
Cancer
|
Antitumor agent-91 is a cyclic phosphate ester derivative with anticancer and anti-proliferative activities. Antitumor agent-91 has potential application in human castration resistant prostate cancer and pancreatic cancer .
|
-
-
- HY-N2959
-
|
JAK
STAT
Apoptosis
Autophagy
|
Cancer
|
Brevilin A is an orally active STAT3/JAK inhibitor (STAT3 IC50= 10.6 µM). Brevilin A shows anti-tumor activity, anti-proliferative activity to cancer cells, and can induce apoptosis and autophagy .
|
-
-
- HY-N0578
-
Apigenin-7-O-β-D-glucopyranoside; Cosmosiin; Apigetrin
|
Reactive Oxygen Species
|
Cancer
|
Apigenin-7-glucoside (Apigenin-7-O-β-D-glucopyranoside) exhibits significant anti-proliferative and antioxidant activity and scavenges reactive oxygen species (ROS) .
|
-
-
- HY-19937A
-
|
PPAR
|
Metabolic Disease
|
Saroglitazar magnesium is a novel peroxisome proliferator-activated receptor (PPAR) agonist with predominant PPARα and moderate PPARγ activity with EC50 values of 0.65 pM and 3 nM in HepG2 cells, respectively.
|
-
-
- HY-147887
-
|
Microtubule/Tubulin
|
Cancer
|
Tubulin inhibitor 28 (compound 2g) is a potent tubulin inhibitor with an IC50 value of 1.2 µM. Tubulin inhibitor 28 shows anti-proliferative activity for MCF-7 cells .
|
-
-
- HY-N3646
-
|
Others
|
Others
Neurological Disease
Inflammation/Immunology
Cancer
|
Cudratricusxanthone A is isolated from Cudrania tricuspidata, and has anti-inflammatory, hepatoprotective, and anti-proliferative activities. Cudratricusxanthone A inhibits osteoclast differentiation and function in RAW 264.7 cells and mouse bone marrow monocytes .
|
-
-
- HY-156450
-
|
ERK
|
Cancer
|
ERK5-IN-5 (compound 4a) is an ERK5 kinase inhibitor with anticancer activity. ERK5-IN-5 exhibits good anti-proliferative activity with the IC50 value of 6.23 µg/mL for A549 cells .
|
-
-
- HY-12424
-
ABT-578; A 179578
|
Others
|
Cardiovascular Disease
Cancer
|
Zotarolimus (ABT-578) is a derivative of rapamycin (HY-10219), with anti-proliferative activity. Zotarolimus is an immunosuppressant. Zotarolimus is developed specifically for local delivery from stents for the prevention of coronary artery restenosis .
|
-
- HY-N3845
-
|
Bacterial
|
Inflammation/Immunology
Cancer
|
Ergosterol peroxide is a steroid derivative and can be isolated from a variety of fungi, yeast, lichens or sponges. Ergosterol peroxide has anti-tumour, proapoptotic, anti-inflammatory, anti-mycobacterial, and anti-proliferative activities .
|
-
- HY-148109
-
|
FAK
|
Cancer
|
FAK-IN-7 (compound 5r) is a FAK inhibitor (IC50=11.72 µM). FAK-IN-7 has good anti-proliferative activity and can be used in cancer research .
|
-
- HY-148110
-
|
FAK
|
Cancer
|
FAK-IN-8 (compound 5h) is a FAK inhibitor (IC50=5.32 µM). FAK-IN-8 has good anti-proliferative activity and can be used in cancer research .
|
-
- HY-126423
-
Isorhamnetin 3-O-glucuronide
|
Others
|
Cancer
|
Isorhamnetin 3-glucuronide is a potent anticancer agent. Isorhamnetin 3-glucuronide shows anti-proliferative activity. Isorhamnetin 3-glucuronide induces Apoptosis and cell cycle arrest at S-phase .
|
-
- HY-149100
-
-
- HY-155748
-
|
MELK
Apoptosis
|
Cancer
|
Antitumor agent-116 (compound 6C) is an anti-tumor agent with anti-proliferative activities. Antitumor agent-11 induces cell apoptosis, and shows the binding affinity against the MELK receptor .
|
-
- HY-120607
-
|
Parasite
|
Infection
Cancer
|
Chevalone C, a meroterpenoid fungal metabolite, shows antimalarial activity with IC50 value of 25.00 μg/mL. Chevalone C has anti-proliferative activity on colon HCT116, liver HepG2 and melanoma A375 cancer cell lines .
|
-
- HY-N3451
-
|
Lipoxygenase
|
Cancer
|
Isothymusin is a potent anti-oxidant agent. Isothymusin shows radical scavenging activities. Isothymusin shows anti-proliferative activities in cancer cell lines. Isothymusin inhibited the enzymes associated with the promotion stage of cancer, including cycloxygenase- 2 and lipoxygenase-5 .
|
-
- HY-147322
-
|
YAP
|
Cancer
|
YAP/TAZ inhibitor-2 is a potent and orally active TEAD-YAP/TAZ inhibitor with an EC50 value of 3 nM. YAP/TAZ inhibitor-2 shows anti-proliferative activity. YAP/TAZ inhibitor-2 shows antitumor activity .
|
-
- HY-146209
-
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
Tubulin polymerization-IN-13 (Compound 4f) is a tubulin polymerization inhibitor (IC50=0.37 μM). Tubulin polymerization-IN-13 shows anti-proliferative activity against cancer cells, induces apoptosis and potential antivascular activity .
|
-
- HY-156451
-
|
ERK
|
Cancer
|
ERK5-IN-6 (compound 5J) is an ERK5 kinase inhibitor with anticancer activity. ERK5-IN-6 exhibits good anti-proliferative activity with the IC50 value of 4.56 µg/mL for A549 cells .
|
-
- HY-15187
-
ARRY-520
|
Kinesin
Apoptosis
|
Cancer
|
Filanesib (ARRY-520) is a selective and noncompetitive kinesin spindle protein (KSP) inhibitor, with an IC50 of 6 nM for human KSP. Filanesib induces cell death by apoptosis in vitro. Filanesib has potent anti-proliferative activity .
|
-
- HY-114323
-
|
PROTACs
FLT3
Apoptosis
|
Cancer
|
PROTAC FLT-3 degrader 1 is a von Hippel-Lindau-based PROTAC FLT-3 internal tandem duplication (ITD) degrader with an IC50 0.6 nM. Anti-proliferative activity; apoptosis induction .
|
-
- HY-110244
-
|
BRK
|
Cancer
|
Tilfrinib (compound 4f) is a potent and selective Brk/PTK6 inhibitor with an IC50 value of 3.15 nM for Brk. Tilfrinib shows good anti-proliferative activity and has potential of anti-tumour .
|
-
- HY-N3005
-
|
Apoptosis
Autophagy
|
Inflammation/Immunology
Cancer
|
Britannin, isolated from Inula aucheriana, is a sesquiterpene lactone. Britannin induces apoptosis and autophagy by activating AMPK regulated by ROS in liver cancer cells. Britannin has anti-proliferative and anti-inflammatory activities .
|
-
- HY-N7015
-
|
EBV
Caspase
Apoptosis
Bacterial
|
Infection
|
Zerumbone is an orally active natural cyclic sesquiterpene and can be isolated from Zingiber zerumbet. Zerumbone has anti-proliferative, anti-inflammation, anti-cancer, anti-bacterial and anti-mutagenic activity .
|
-
- HY-B1394
-
|
|
|
Khellin is a furochromone that can be isolated from Ammi visnuga L.. Khellin is an EGFR inhibitor with an IC50 of 0.15 µM. Khelline has anti-proliferative activity in vitro. Khellin has antispasmodic and coronary vasodilator effects .
|
-
- HY-124012
-
|
DNA/RNA Synthesis
|
Cancer
|
PCNA-I1 is a potent PCNA (proliferating cell nuclear antigen) inhibitor. PCNA-I1 directly binds PCNA trimers with a Kd of 0.41 μM and exhibits antitumor activity both in vitro and in vivo .
|
-
- HY-151191
-
|
Histone Demethylase
|
Cancer
|
LSD1-IN-22 is a potent Lysine-specific demethylase 1 (LSD1) inhibitor with a Ki value of 98 nM. LSD1-IN-22 has anti-proliferative activity against certain cancer cells .
|
-
- HY-15587
-
|
DNA/RNA Synthesis
|
Cancer
|
L82 is a selective and uncompetitive DNA ligase 1 (DNA Lig1) inhibitor (hLig1 IC50=12 μM). L82 shows anti-proliferative activity to breast cancer cells .
|
-
- HY-152748
-
|
Apoptosis
Caspase
|
Cancer
|
Caspase-3/7 activator 1 is an effective activator of Caspase-3/7. Caspase-3/7 activator 1 has tumor selectivity, anti-proliferative activity and high Apoptosis-inducing ability .
|
-
- HY-152756
-
|
Apoptosis
Caspase
|
Cancer
|
Caspase-3/7 activator 2 is an effective activator of Caspase-3/7. Caspase-3/7 activator 2 has tumor selectivity, anti-proliferative activity and high Apoptosis-inducing ability .
|
-
- HY-152758
-
|
Apoptosis
Caspase
|
Cancer
|
Caspase-3/7 activator 3 is an effective activator of Caspase-3/7. Caspase-3/7 activator 3 has tumor selectivity, anti-proliferative activity and high Apoptosis-inducing ability .
|
-
- HY-161236
-
|
Ras
|
Cancer
|
KRAS ligand 4 (Compound 2) is a bifunctional depressant based on SOS1. KRAS ligand 4 reduces the downstream signaling markers pERK and pS6 and shows anti-proliferative activity in multiple KRAS mutated cells .
|
-
- HY-163275
-
|
MDM-2/p53
Apoptosis
|
Cancer
|
MDM2-IN-24 (compound A3f) exhibits MDM2-inhibiting and MDMX-activating properties in triple-negative breast cancer (TNBC) cells, with apoptotic and anti-proliferative activities .
|
-
- HY-15187C
-
ARRY-520 hydrochloride
|
Kinesin
Apoptosis
|
Neurological Disease
|
Filanesib (ARRY-520) hydrochloride is a selective and noncompetitive kinesin spindle protein (KSP) inhibitor, with an IC50 of 6 nM for human KSP. Filanesib induces cell death by apoptosis in vitro. Filanesib has potent anti-proliferative activity .
|
-
- HY-P99218
-
Sch 717454; 19D12
|
IGF-1R
|
Cancer
|
Robatumumab (Sch 717454) is an anti-human IGF-1R (insulin-like growth factor receptor-1) antibody. Robatumumab shows anti-tumor activity and anti-proliferative activity to cancer cells. Robatumumab can be used in osteosarcoma and Ewing sarcoma research .
|
-
- HY-151480
-
|
STAT
Apoptosis
|
Cancer
|
HP590 is an orally active, novel and potent STAT3 inhibitor (STAT3 luciferase activity: IC50=27.8 nM; ATP inhibition: IC50=24.7 nM). HP590 shows anti-proliferative activity to gastric cancer cells and induces apoptosis .
|
-
- HY-161123
-
|
WDR5
|
Cancer
|
WDR5-IN-8 is a WDR5 inhibitor with IC50 value of 15.5 nM. WDR5-IN-8 shows good anti-proliferative activity in two human acute leukemia cell lines. WDR5-IN-8 has antitumor activity .
|
-
- HY-15187B
-
ARRY-520 TFA
|
Kinesin
|
Cancer
|
Filanesib TFA (ARRY-520 TFA) is a selective kinesin spindle protein (KSP) inhibitor, with an IC50 of 6 nM for human KSP. Filanesib TFA induces cell death by apoptosis in vitro. Filanesib TFA has potent anti-proliferative activity .
|
-
- HY-150730
-
|
FAK
|
Cancer
|
FAK-IN-6 is a potent FAK inhibitor with an IC50 value of 1.415 nM. FAK-IN-6 has anti-proliferative activity against certain cancer cell lines. FAK-IN-6 can be used for researching pancreatic cancer .
|
-
- HY-149402
-
|
Carbonic Anhydrase
|
Cancer
|
hCA XII-IN-6 (compound 4d) is a potent hCA XII inhibitor with a Ki value of 84.2 nM. hCA XII-IN-6 has anti-proliferative activity. hCA XII-IN-6 can be used in research of cancer .
|
-
- HY-N12503
-
|
Apoptosis
Caspase
|
Cancer
|
Patuletin is a flavonol, that can be isolated from the flowers of Tagetes patula. Patuletin shows anti-proliferative activity against cancer cells. Patuletin causes significant nuclear fragmentation and has a great capacity to induce caspase-3 activation .
|
-
- HY-10082A
-
(E)-PAN-811; (E)-NSC# 663249; (E)-OCX191
|
DNA/RNA Synthesis
|
Cancer
|
(E)-3-AP is the E configuration of 3-AP. 3-AP is a potent ribonucleotide reductase inhibitor. 3-AP shows anti-proliferative activity. 3-AP shows anticancer activity in L1210 leukemia model. 3-AP inhibits RR activity and DNA synthesis .
|
-
- HY-17037
-
LS 519; Pirenzepin dihydrochloride; Gastrozepin dihydrochloride
|
mAChR
|
Metabolic Disease
Cancer
|
Pirenzepine (LS 519) dihydrochloride is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist. Pirenzepine dihydrochloride reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine dihydrochloride shows anti-proliferative activity to cancer cells .
|
-
- HY-A0143
-
DGLA; all-cis-8,11,14-Eicosatrienoic acid
|
|
|
Dihomo-γ-linolenic acid (DGLA) is a 20-carbon ω-6 fatty acid, with anti-inflammatory and anti-proliferative activities. Dihomo-γ-linolenic acid attenuates atherosclerosis in the apolipoprotein E deficient mouse model system .
|
-
- HY-112316
-
|
Epigenetic Reader Domain
|
Cancer
|
BAY1238097 is a potent and selective inhibitor of BET binding to histones and has strong anti-proliferative activity in different AML (acute myeloid leukemia) and MM (multiple myeloma) models through down-regulation of c-Myc levels and its downstream transcriptome (IC50 <100 nM).
|
-
- HY-132167
-
AZD5305
|
PARP
|
Cancer
|
Saruparib (AZD5305) is a potent, orally active and selective PARP inhibitor and trapper with IC50 values of 3 nM and 1400 nM for PARP1 and PARP2, respectively. Saruparib has anti-proliferative activity and inhibits growth in cells with deficiencies in DNA repair .
|
-
- HY-156919
-
|
MDM-2/p53
|
Cancer
|
p53 Activator 8 (compound 5) is a p53 activator. p53 Activator 8 has potent anti-proliferative activity against MCF7 breast cancer cell lines with an IC 50 value of 0.5 μM .
|
-
- HY-14543
-
-
- HY-15605S
-
LGX818-13C,d3
|
Isotope-Labeled Compounds
Raf
|
Cancer
|
Encorafenib- 13C,d3 is the 13C- and deuterium labeled Encorafenib. Encorafenib (LGX818) is a highly potent BRAF inhibitor with selective anti-proliferative and apoptotic activity in cells expressing BRAFV600E (EC50=4 nM).
|
-
- HY-128359
-
ACBI1
4 Publications Verification
|
PROTACs
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
ACBI1 is a potent and cooperative SMARCA2, SMARCA4 and PBRM1 degrader with DC50s of 6, 11 and 32 nM, respectively. ACBI1 is a PROTAC degrader. ACBI1 shows anti-proliferative activity. ACBI1 induces apoptosis .
|
-
- HY-147928
-
|
Apoptosis
Caspase
Bcl-2 Family
|
Cancer
|
Apoptotic agent-2 (compound 14b) induces apoptosis by down-regulation of Bcl-2 and up-regulation of Bax and caspase-3. Apoptotic agent-2 exhibits anti-proliferative activities and can be used for cancer research .
|
-
- HY-157137
-
|
PARP
Caspase
Apoptosis
|
Cancer
|
PARP1-IN-17 is a PARP-1 inhibitor (IC50 = 19.24 nM for PARP-1 and = 32.58 nM for PARP-2) and induce apoptosis. PARP1-IN-17 shows excellent anti-proliferative activity .
|
-
- HY-111551
-
FT113
1 Publications Verification
|
Fatty Acid Synthase (FASN)
|
Cancer
|
FT113 is a potent and orally active fatty acid synthase (FASN) inhibitor, with an IC50 of 213 nM for full-length recombinant human FASN enzyme. In cell-based assay, FT113 blocks FASN activity in BT474 cells (IC50, 90 nM). FT113 shows anti-proliferative activity, and exhibits anti-cancer activity both in vitro and in vivo .
|
-
- HY-B0356
-
-
- HY-B0356B
-
Bay-09867 hydrochloride monohydrate
|
Topoisomerase
Apoptosis
Antibiotic
Bacterial
Mitochondrial Metabolism
Reactive Oxygen Species
|
Infection
Cancer
|
Ciprofloxacin (Bay-09867) hydrochloride monohydrate is a potent, orally active topoisomerase IV inhibitor. Ciprofloxacin hydrochloride monohydrate induces mitochondrial DNA and nuclear DNA damage and lead to mitochondrial dysfunction, ROS production. Ciprofloxacin hydrochloride monohydrate has anti-proliferative activity and induces apoptosis. Ciprofloxacin hydrochloride monohydrate is a fluoroquinolone antibiotic, exhibiting potent antibacterial activity .
|
-
- HY-151576
-
|
Others
|
Cancer
|
PRMT5:MEP50 PPI is a novel PRMT5:MEP50 protein-protein interaction (PRMT5:MEP50 PPI) inhibitor, shows anti-tumor activity and anti-proliferative activity of lung and prostate cancer cells .
|
-
- HY-149252
-
|
Apoptosis
Microtubule/Tubulin
|
Cancer
|
Tubulin inhibitor 32 is a potent and orally active tubulin inhibitor. Tubulin inhibitor 32 shows anti-proliferative activity and inhibits microtubule polymerization. Tubulin inhibitor 32 induces Apoptosis and cell cycle arrest at G2/M phase. Tubulin inhibitor 32 shows anti-tumor activity .
|
-
- HY-123159
-
|
Aurora Kinase
|
Cancer
|
AKI603 is an inhibitor of Aurora kinase A (AurA), with an IC50 of 12.3 nM. AKI603 is developed to overcome resistance mediated by BCR-ABL-T315I mutation. AKI603 exhibits strong anti-proliferative activity in leukemic cells .
|
-
- HY-115928
-
|
Bcl-2 Family
|
Cancer
|
M24 is a Mcl-1 selective inhibitor. M24 exhibits good binding affinity against Mcl-1 with Ki value of 0.33 μM. M24 exhibits good anti-proliferative activity and induce apoptosis in HepG2 cells .
|
-
- HY-146188
-
|
Topoisomerase
|
Cancer
|
Topoisomerase II inhibitor 8 (compound 22) is a potent topoisomerase II inhibitor, with an IC50 of 0.52 μM. Topoisomerase II inhibitor 8 exhibits good anti-proliferative activities and can arrest the cell cycle at G2/M phase .
|
-
- HY-143280
-
|
Topoisomerase
|
Cancer
|
Topoisomerase II inhibitor 4 (compound E17) is a potent Topoisomerase II inhibitor. Topoisomerase II inhibitor 4 triggers G2/M cell cycle arrest and shows anti-tumor activity with strong cytotoxic and anti-proliferative effect .
|
-
- HY-151106
-
-
- HY-17037A
-
LS 519 free base; Pirenzepin; Gastrozepin
|
|
|
Pirenzepine (LS 519 free base) is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist. Pirenzepine reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine shows anti-proliferative activity to cancer cells .
|
-
- HY-156553
-
|
Btk
|
Inflammation/Immunology
Cancer
|
BTK-IN-27 (example 8) is a BTK inhibitor (IC50: 0.2 nM). BTK-IN-27 shows anti-proliferative activity in TMD8 cells (IC50: < 5 nM). BTK-IN-27 can be used for research of cancer, lymphoma, leukemia and immunological diseases .
|
-
- HY-112316A
-
|
Epigenetic Reader Domain
|
Cancer
|
(R)-BAY1238097 is the R-isomer with lower activity of BAY1238097. BAY1238097 is a potent and selective inhibitor of BET binding to histones and has strong anti-proliferative activity in different AML (acute myeloid leukemia) and MM (multiple myeloma) models through down-regulation of c-Myc levels and its downstream transcriptome .
|
-
- HY-128587
-
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-N0448
-
|
Others
|
Inflammation/Immunology
Cancer
|
10-Gingerol is a major pungent constituent in the ginger oleoresin from fresh rhizome, with anti-inflammatory, antioxidant and anti-proliferative activities. 10-Gingerol inhibits the proliferation of MDA-MB-231 tumor cell line with an IC50 of 12.1 μM .
|
-
- HY-N7072
-
|
Apoptosis
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
Grape seed extract is a natural product, with anti-inflammatory and anti-proliferative effects. Grape seed extract shows inhibitory activity on the fat-metabolizing enzymes pancreatic lipase and lipoprotein lipase. Grape seed extract induces apoptotic in human colorectal cancer cells .
|
-
- HY-N2920
-
11-Oxo-β-amyrin
|
Cytochrome P450
|
Inflammation/Immunology
Cancer
|
β-Amyrenonol (11-Oxo-β-amyrin), an oleanolic-type triterpenoid in licorice roots, is a precursor of Glycyrrhetinic acid. β-Amyrenonol has anti-proliferative and anti-inflammatory activities, and β-Amyrenonol could function as the skeleton for the synthesis of many triterpenoids .
|
-
- HY-147741
-
|
JAK
Btk
EGFR
|
Inflammation/Immunology
Cancer
|
DPPY (compound 6) is a potent PTK inhibitor with IC50 values of <10, <10, <10 nM for EGFR, BTK, JAK3, respectively. DPPY shows anti-proliferative activity against B-cell lymphoma cells. DPPY has the potential for the research of idiopathic pulmonary fibrosis (IPF) .
|
-
- HY-153339
-
|
Others
|
Cancer
|
E235 is an expression regulator of activates transcription factor 4 (ATF4). E235 reduces cell viability by activating integrated stress response (ISR) and DNA damage response signals. E235 has anti-proliferative activity and can be used for tumor research .
|
-
- HY-122989
-
|
DYRK
|
Inflammation/Immunology
|
Aristolactam BIII is a potent DYRK1A inhibitor and inhibits the kinase activity of DYRK1A in vitro (IC50= 9.67 nM. Aristolactam BIII rescues the proliferative defects of DYRK1A transgenic (TG) mouse-derived fibroblasts and neurological and phenotypic defects of DS-like Drosophila models .
|
-
- HY-163402
-
|
EGFR
Apoptosis
|
Cancer
|
EGFR-IN-108 chloride (Compound Ru3S) is an EGFR inhibitor with an IC50 value of 5.8 nM for hEGFR. EGFR-IN-108 chloride induces apoptosis and has anti-proliferative activity against cancer cells. EGFR-IN-108 chloride also has anti-angiogenic effects .
|
-
- HY-15456
-
|
c-Met/HGFR
|
Cancer
|
NVP-BVU972 is an selective and potent Met inhibitor, with an IC50 of 14 nM. NVP-BVU972 also exhibits good anti-proliferative activity against Met with drug-resistant mutations and inhibits phosphorylation. NVP-BVU972 can be used in study of cancer .
|
-
- HY-N6797
-
|
Bacterial
c-Met/HGFR
Antibiotic
|
Infection
Cancer
|
Meleagrin is a roquefortine C-derived alkaloid produced by fungi of the genus Penicillium and has antimicrobial and anti-proliferative activities. Meleagrin is a class of FabI inhibitor. Meleagrin is a lead c-Met inhibitory entity useful for the control of c-Met-dependent metastatic and invasive breast malignancies .
|
-
- HY-N3523
-
|
Others
|
Cancer
|
3-O-Beta-D-Glucopyranosylplatycodigenin is an oleanane-type triterpenoid isolated from roots of Platycodon grandiflorum. 3-O-Beta-D-Glucopyranosylplatycodigenin exhibits anti-proliferative activities against HSC-T6 cell line with an IC50 of 13.36 μM .
|
-
- HY-121538
-
|
Epoxide Hydrolase
PPAR
|
Cardiovascular Disease
|
CUDA is a potent inhibitor of soluble epoxide hydrolase (sEH), with IC50s of 11.1 nM and 112 nM for mouse sEH and human sEH, respectively . CUDA selectively increases peroxisome proliferator-activated receptor (PPAR) alpha activity. CUDA may be valuable for the research of cardiovascular disease .
|
-
- HY-N0181A
-
9β,10α-Ergosterol
|
Endogenous Metabolite
|
Metabolic Disease
|
Lumisterol (9β,10α-Ergosterol), a steroid compound, is the (9β,10α)-stereoisomer of Ergosterol (HY-N0181). Lumisterol is a photoprotective agent against UVB-induced DNA damage and anti-proliferative activities .
|
-
- HY-146227
-
|
Topoisomerase
Apoptosis
|
Cancer
|
DNA topoisomerase II inhibitor 1 (compound 8ed) is a potent DNA topoisomerase II inhibitor. DNA topoisomerase II inhibitor 1 shows anti-proliferative activity. DNA topoisomerase II inhibitor 1 induces apoptosis and cell cycle arrest at sub G1 phase .
|
-
- HY-147929
-
|
Apoptosis
Caspase
Bcl-2 Family
|
Cancer
|
Apoptotic agent-3 (compound 15f) promotes apoptosis through the potential mitochondria-mediated Bcl-2/Bax pathway and activation of the Caspase 3 pathway. Apoptotic agent-3 exhibits anti-proliferative activities and can be used for cancer research .
|
-
- HY-151914
-
|
Atg7
Autophagy
|
Cancer
|
Antitumor agent-82 (compound 6g) is a potent anti-tumor agent. Antitumor agent-82 shows anti-proliferative activity. Antitumor agent-82 induces cell Autophagy by the ATG5/ATG7 signaling pathway .
|
-
- HY-148489
-
|
Others
|
Cancer
|
CSNK1-IN-1 is a CSNK1A1 inhibitor. CSNK1-IN-1 has inhibitory activity for CSNK1A1 kinase with IC50 values of 21 μM. CSNK1-IN-1 can be used for the research of proliferative disorders .
|
-
- HY-B0356A
-
Bay-09867 monohydrochloride
|
Topoisomerase
Apoptosis
Antibiotic
Bacterial
Mitochondrial Metabolism
Reactive Oxygen Species
|
Infection
Cancer
|
Ciprofloxacin (Bay-09867) monohydrochloride is a potent, orally active topoisomerase IV inhibitor. Ciprofloxacin monohydrochloride induces mitochondrial DNA and nuclear DNA damage and lead to mitochondrial dysfunction, ROS production. Ciprofloxacin monohydrochloride has anti-proliferative activity and induces apoptosis. Ciprofloxacin monohydrochloride is a fluoroquinolone antibiotic, exhibiting potent antibacterial activity .
|
-
- HY-12847
-
|
Raf
Src
Apoptosis
|
Cancer
|
CCT241161 is an orally active pan-RAF inhibitor with IC50s of 3, 6, 10, 15 and 30 nM for LCK, CRAF, SRC, V600E-BRAF and BRAF, respectively. CCT241161 shows good activity to in BRAF and NRAS mutant melanomas. CCT241161 also exhibits anticancer cell proliferative activity .
|
-
- HY-W040298
-
Bay-09867 lactate
|
Topoisomerase
Apoptosis
Antibiotic
Bacterial
Mitochondrial Metabolism
Reactive Oxygen Species
|
Infection
Cancer
|
Ciprofloxacin (Bay-09867) lactate is a potent, orally active topoisomerase IV inhibitor. Ciprofloxacin lactate induces mitochondrial DNA and nuclear DNA damage and lead to mitochondrial dysfunction, ROS production. Ciprofloxacin lactate has anti-proliferative activity and induces apoptosis. Ciprofloxacin lactate is a fluoroquinolone antibiotic, exhibiting potent antibacterial activity .
|
-
- HY-155704
-
|
Others
|
Others
|
DPP-IV-IN-5 is isolated from the fruits of Lycium barbarum. DPP-IV-IN-5 exerts moderate agonistic activities for peroxisome proliferator-activated receptor (PPARγ) with EC50 values of 10.09 - 44.26 μM and also presents inhibitory activity on dipeptidyl peptidase-4 (DPPIV) with an IC50 value of 47.13 μM .
|
-
- HY-147030
-
|
PARP
|
Cancer
|
PARP1-IN-8 (compound 11c) is a potent and BBB-penetrated PARP1 inhibitor, with an IC50 of 97 nM. PARP1-IN-8 shows significantly potent anti-proliferative activity against Human lung adenocarcinoma epithelial cell line A549 .
|
-
- HY-122594
-
|
Topoisomerase
|
Cancer
|
BNS-22 is a DNA topoisomerase II (TOP2) catalytic inhibitor with the IC50 values of 2.8 μM and 0.42 μM for human TOP2α and TOP2β, respectively. BNS-22 induces abnormal division and has anti-proliferative activity .
|
-
- HY-148491
-
|
Others
|
Cancer
|
CSNK1-IN-2 is a CSNK1A1 inhibitor. CSNK1-IN-1 has inhibitory activity for CSNK1A1 kinase with IC50 values of 2.52 μM. CSNK1-IN-2 can be used for the research of proliferative disorders .
|
-
- HY-146368
-
|
PROTACs
VEGFR
|
Cancer
|
PROTAC VEGFR-2 degrader-1(PROTAC-1), a PROTAC VEGFR-2 degrader, exhibits little VEGFR-2 inhibition (IC50> 1 μM) and anti-proliferative activity against EA.hy926 cells (IC50> 100 μM) .
|
-
- HY-146369
-
|
PROTACs
VEGFR
|
Cancer
|
PROTAC VEGFR-2 degrader-2(PROTAC-4), a PROTAC VEGFR-2 degrader, exhibits little VEGFR-2 inhibition (IC50> 1 μM) and anti-proliferative activity against EA.hy926 cells (IC50> 100μM) .
|
-
- HY-N6635
-
|
Fungal
|
Infection
Cancer
|
trans-Nerolidol is a sesquiterpene alcohol. It can be isolated from f aerial parts of Warionia saharae ex Benth. trans-Nerolidol improves the anti-proliferative effect of Doxorubicin (HY-15142A) against intestinal cancer cells in vitro. trans-Nerolidol also has anti-fungal activity .
|
-
- HY-19937S1
-
|
Isotope-Labeled Compounds
|
Others
|
Saroglitazar-d4 is the deuterium-labeled Saroglitazar (HY-19937). Saroglitazar-d4 is a novel peroxisome proliferator-activated receptor (PPAR) agonist with predominant PPARα and moderate PPARγ activity with EC50 values of 0.65 pM and 3 nM in HepG2 cells, respectively.
|
-
- HY-147742
-
|
JAK
|
Inflammation/Immunology
|
Thi-DPPY (compound 8e) is a potent and orally active JAK3 inhibitor with IC50 values of 62.4, 1.38 nM for BTK, JAK, respectively. Thi-DPPY shows anti-proliferative activity against HBE cells. Thi-DPPY shows anti-inflammatory activity in vivo. Thi-DPPY has the potential for the research of idiopathic pulmonary fibrosis (IPF) .
|
-
- HY-101870B
-
INCB053914 phosphate
|
Pim
|
Cancer
|
Uzansertib (INCB053914) phosphate is an orally active, ATP-competitive pan-PIM kinase inhibitor with IC50s of 0.24 nM, 30 nM, 0.12 nM for PIM1, PIM2, PIM3, respectively. Uzansertib phosphate has broad anti-proliferative activity against a variety of hematologic tumor cell lines .
|
-
- HY-137977
-
DMU-212
1 Publications Verification
|
ERK
Apoptosis
|
Cancer
|
DMU-212 is a methylated derivative of Resveratrol (HY-16561), with antimitotic, anti-proliferative, antioxidant and apoptosis promoting activities. DMU-212 induces mitotic arrest via induction of apoptosis and activation of ERK1/2 protein. DMU-212 has orally active .
|
-
- HY-101870
-
INCB053914
|
Pim
|
Cancer
|
Uzansertib (INCB053914) is an orally active, ATP-competitive pan-PIM kinase inhibitor with IC50s of 0.24 nM, 30 nM, 0.12 nM for PIM1, PIM2, PIM3, respectively. Uzansertib has broad anti-proliferative activity against a variety of hematologic tumor cell lines .
|
-
- HY-115994
-
|
Carbonic Anhydrase
|
Cancer
|
Carbonic anhydrase inhibitor 10 is a potent hCA IX inhibitor with a Ki value of 6.2 nM. Carbonic anhydrase inhibitor 10 exhibits anti-proliferative activity against MCF-7 cancer cell line with an IC50 of 11.9 μM. Carbonic anhydrase inhibitor 10 can be used for cancer research .
|
-
- HY-147703
-
|
Aurora Kinase
|
Cancer
|
Aurora kinase inhibitor-9 (compound 9d) is a potent AURKA/B dual aurora kinase inhibitor with IC50s of 0.093, 0.09 µM for Aurora A, Aurora B, respectively. Aurora kinase inhibitor-9 shows broad spectrum anti-proliferative activity .
|
-
- HY-163282
-
|
HDAC
Epigenetic Reader Domain
|
Cancer
|
NB512 (compound 39a) is a dual inhibitor for BET and HDAC, which exhibits a efficient binding affinity with BRD4 bromodomains and HDAC1/2, with EC50s of 100-400 nM. NB512 exhibits an anti-proliferative activity towards cancer cells PaTu8988T and NMC .
|
-
- HY-107551
-
|
Gli
|
Cancer
|
GLI antagonist-1 is a potent GLI antagonist with an IC50 value of 1.1 µM. GLI antagonist-1 shows anti-proliferative activity. GLI antagonist-1 decreases the GLI1 mRNA expression. GLI antagonist-1 inhibits colony formation in a dose-dependent manner .
|
-
- HY-150611
-
|
EGFR
|
Cancer
|
EGFR-IN-70 (compound 18j) is a potent EGFR inhibitor with IC50 values of 23.6 and 307.5 nM for EGFR LR/TM/CS and EGFR WT, respectively. EGFR-IN-70 has anti-proliferative activity and suppresses phosphorylation of the EGFR. EGFR-IN-70 can be used for cancer research .
|
-
- HY-122844
-
BI-853520; IN-10018
|
FAK
|
Cancer
|
Ifebemtinib (BI 853520) is an orally active and potent focal adhesion kinase (FAK) inhibitor (recombinant FAK IC50=1 nM). Ifebemtinib shows anti-proliferative activity against cancer cells. Ifebemtinib inhibits FER Kinase and FES Kinase with IC50s of 900 nM and 1040 nM, respectively .
|
-
- HY-123024
-
BL-S-640; SK&F 60771
|
Apoptosis
Bacterial
Antibiotic
|
Infection
Cancer
|
Cefatrizine (BL-S-640) is an orally active and broad-spectrum cephalosporin antibiotic. Cefatrizine is also a eEF2K inhibitor, with anti-proliferative activity in human breast cancer cells, which could induce ER stress, leading to cell death. Cefatrizine can be used in studies of cancer and bacterial infection .
|
-
- HY-151519
-
|
Sirtuin
|
Cancer
|
SIRT2-IN-9 (compound 12) is a selective inhibitor of SRIT2 with an IC50 value of 1.3 μM. SIRT2-IN-9 inhibits proliferative activity of MCF-7 breast cancer cells. SIRT2-IN-9 can be used for the research of cancer .
|
-
- HY-A0143A
-
DGLA sodium; all-cis-8,11,14-Eicosatrienoic acid sodium
|
Endogenous Metabolite
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
Dihomo-γ-linolenic acid (DGLA; all-cis-8,11,14-Eicosatrienoic acid) sodium is a 20-carbon ω-6 fatty acid, with anti-inflammatory and anti-proliferative activities. Dihomo-γ-linolenic acid (sodium) attenuates atherosclerosis in the apolipoprotein E deficient mouse model system .
|
-
- HY-N8519
-
|
Bacterial
Fungal
Antibiotic
|
Infection
Cancer
|
Urdamycin B is an antibiotic that effectively inhibits fungi and bacteria. Urdamycin B also exhibits anti-proliferative activity against mouse leukemia cells L1210. Urdamycin B can be obtained from the metabolic products of Streptomyces fradiae. Urdamycin B can be used for research on cancer as well as bacterial and fungal infections .
|
-
- HY-160698
-
|
MALT1
|
Cancer
|
SGR-1505 is an orally active MALT1 allosteric inhibitor. SGR-1505 inhibits MALT1 enzymatic activity and shows anti-proliferative activity in BTK inhibitor (BTKi)-sensitive and BTKi-resistant activated B cell-like diffuse large B cell lymphoma (ABC-DLBCL) cell lines. SGR-1505 can be used for research of B-cell lymphomas .
|
-
- HY-B0644
-
Sucrose octasulfate-aluminum complex
|
Bacterial
|
Infection
Inflammation/Immunology
Cancer
|
Sucralfate (Sucrose octasulfate-aluminum complex) is a potent and orally active gastroprotectant with no systemic effects. Sucralfate inhibits peptic activity and binds to negatively charged subepithelial proteins exposed during mucosal injury, forming a viscous layer that protects the vascular bed and proliferative zone. Sucralfate is used for prevention and research of several gastrointestinal diseases in vivo .
|
-
- HY-128588
-
|
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-137756
-
|
JAK
|
Cancer
|
JAK2-IN-6, a multiple-substituted aminothiazole derivative, is a potent and selective JAK2 inhibitor with an IC50 of 22.86 μg/mL. JAK2-IN-6 shows no activity against JAK1 and JAK3. JAK2-IN-6 has anti-proliferative effect against cancer cells .
|
-
- HY-124822
-
COH-SR4
1 Publications Verification
|
AMPK
|
Metabolic Disease
Cancer
|
COH-SR4 is an AMPK activator. COH-SR4 shows potent anti-proliferative activities against leukemia, melanoma, breast and lung cancers. COH-SR4 inhibits adipocyte differentiation via AMPK activation. COH-SR4 can be used for the research of obesity and related metabolic disorders .
|
-
- HY-150595
-
|
HDAC
Microtubule/Tubulin
|
Cancer
|
HDAC6-IN-10 is a highly selective HDAC6 inhibitor with the IC50 of 0.73 nM. HDAC6-IN-10 has 144~10941-fold selectivity over other HDAC isoforms. HDAC6-IN-10 shows anti-proliferative activities against multiple myeloma cells .
|
-
- HY-147298
-
CYC140
|
Polo-like Kinase (PLK)
|
Cancer
|
Plogosertib (CYC140) is a selective, potent, and orally active ATP-competitive PLK1 inhibitor (IC50: 3 nM). Plogosertib is an anti-cancer agent with anti-proliferative activity. Plogosertib can be used in the research of several tumors, including esophageal, gastric, leukemia, non–small cell lung cancer, ovarian, and squamous cell cancers .
|
-
- HY-151277
-
|
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
ALK5-IN-29 is an selective activin receptor-like kinase (ALK) inhibitor. ALK5-IN-29 can inhibit the activity of ALK5 with an IC50 value of ≤10 nM. ALK5-IN-29 also has inhibitory of tumor growth and can be used for the research of proliferative diseases, such as cancer .
|
-
- HY-152945
-
|
NF-κB
|
Cancer
|
Antiproliferative agent-22 (compound 2) is an anticancer agent. Antiproliferative agent-22 shoes anti-proliferative activities against MCF-7, MDA-MB-231 and MDA-MB-468 cells with IC50 values of 6.2 μM, 3.3 μM and 3.3 μM, respectively .
|
-
- HY-152019
-
|
EGFR
|
Cancer
|
EGFR/C797S-IN-1 is a potent EGFR-C797S inhibitor with an IC50 value of 0.128 µM. EGFR/C797S-IN-1 shows anti-proliferative activity and anti-tumor activity. EGFR/C797S-IN-1 inhibits the expression of p-EGFR in a dose-dependent manner .
|
-
- HY-110144
-
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
TC-E 5008 is a potent mutant IDH1 inhibitor with Ki values of 190 nM and 120 nM for R132H and R132C IDH1 mutants, respectively. TC-E 5008 exhibits very weak activity against WT-IDH1 with a Ki value of 12.3 μM. TC-E 5008 has anti-proliferative activity on multiple ER positive breast cancer cell lines .
|
-
- HY-142945
-
|
Ras
|
Cancer
|
KRAS G12C inhibitor 43 (compound 59) is a potent KRAS G12C inhibitor. KRAS G12C inhibitor 43 shows antimigration and anti-proliferative activity with IC50s of 0.001-1 µM, >1 µM, >1 µM for H358, A549, HCC cells ,respectively .
|
-
- HY-146354
-
|
Apoptosis
Reactive Oxygen Species
|
Cancer
|
Antiproliferative agent-4 (compound 2y) has excellent anti-proliferative activity against certain cancer cell lines. Antiproliferative agent-4 reduces the mitochondrial membrane potential, and increases the apoptosis rate and the level of ROS on EC109. Antiproliferative agent-4 inhibits tumour growth in nude mice, with low toxicity .
|
-
- HY-147892
-
|
HDAC
Apoptosis
|
Cancer
|
HDAC-IN-42 (compound 14f) is a potent and selective HDAC inhibitor with IC50 values of 0.19 and 4.98 µM for HDAC1 and HDAC6, respectively. HDAC-IN-42 shows anticancer and anti-proliferative activity. HDAC-IN-42 induces apoptosis and cell cycle arrest at G2/M phase .
|
-
- HY-147966
-
|
HDAC
PI3K
mTOR
|
Cancer
|
HDAC-IN-43 is a potent HDAC 1/3/6 inhibitor with IC50 values of 82, 45, and 24 nM, respectively. HDAC-IN-43 is a weak PI3K/mTOR inhibitors with IC50 values of 3.6 and 3.7 μM, respectively. HDAC-IN-43 shows broad anti-proliferative activity .
|
-
- HY-150694
-
|
HDAC
|
Cancer
|
HDAC6-IN-11 (Compound 9) is a selective HDAC6 inhibitor with the IC50 value of 20.7 nM. HDAC6-IN-11 has more than 300-fold selectivity over HDAC other isoforms. HDAC6-IN-11 shows anti-proliferative activities against cancer cells .
|
-
- HY-150615
-
|
SphK
Apoptosis
|
Cancer
|
SphK1-IN-2 is a potent, selective SphK1 inhibitor with IC50 values of 19.81 nM and >10 μM for SphK1 and SphK2, respectively. SphK1-IN-2 exhibits anti-proliferative activities and induces cell cycle arrest and apoptosis. SphK1-IN-2 can be used for cancer research .
|
-
- HY-134601
-
|
HuR
|
Cancer
|
KH-3 is a potent RNA-binding protein Hu antigen R (HuR) inhibitor with an IC50 value of 0.35 μM. KH-3 has anti-proliferative activity. KH-3 suppresses breast cancer cell invasion as well as delays the initiation of lung colonies by disrupting HuR-FOXQ1 mRNA interaction .
|
-
- HY-155074
-
|
EGFR
|
Cancer
|
EGFR-IN-79 (compound 21) is an EGFR inhibior with antitumor activity. EGFR-IN-79 induces ROS-independent apoptosis and EGFR/AKT/mTOR-mediated autophagy. EGFR-IN-79 induces cell death at both proliferating and quiescent zones of EJ28 spheroids. EGFR-IN-79 exhibits safety profile in the zebrafish-based model .
|
-
- HY-149889
-
|
Apoptosis
EGFR
|
Cancer
|
EGFR-IN-78 (compound A5),a 2-aminopyrimidine derivative,is a reversible inhibitor of EGFR C797S-TK,and also an inducer of apoptosis. EGFR-IN-78 shows anti-proliferative activity,inhibits EGFR phosphorylation and arrests cell cycle at G2/M phase .
|
-
- HY-143400
-
|
HSP
Hedgehog
|
Cancer
|
HSP70-IN-3 is a potent HSP70 inhibitor (IC50s of 1.1 and 1.9 μM in ASZ001 and C3H10T1/2, respectively). HSP70-IN-3 has anti-Hh (Hedgehog signaling) activity and anti-proliferative activity and reduces expression of the oncogenic transcription factor GLI1 .
|
-
- HY-50767
-
PD 0332991
|
CDK
|
Cancer
|
Palbociclib (PD 0332991) is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma .
|
-
- HY-150791
-
|
Reactive Oxygen Species
DNA/RNA Synthesis
|
Cancer
|
FLDP-5 is a blood-brain barrier (BBB) penetrant curcuminoid analogues. FLDP-5 can induce production of ROS (Reactive Oxygen Species), DNA damage and cell cycle S phase arrest. FLDP-5 exhibits highly potent tumour-suppressive effects with anti-proliferative and anti-migratory activities on LN-18 cells .
|
-
- HY-50767B
-
PD-0332991 dihydrochloride
|
CDK
|
Cancer
|
Palbociclib (PD 0332991) dihydrochloride is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib dihydrochloride has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma .
|
-
- HY-151289
-
|
TGF-β Receptor
TGF-beta/Smad
|
Cancer
|
ALK5-IN-34 is an selective orally active activin receptor-like kinase (ALK) inhibitor. ALK5-IN-34 can inhibit the activity of ALK5-IN-34 with an IC50 value of ≤10 nM. ALK5-IN-34 also has inhibitory of tumor growth and can be used for the research of proliferative diseases, such as cancer .
|
-
- HY-50767C
-
PD-0332991 hydrochloride
|
CDK
|
Cancer
|
Palbociclib (PD 0332991) hydrochloride is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib hydrochloride has potent anti-proliferative activity and induces cell cycle arrest in cancer cells. Palbociclib hydrochloride can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma .
|
-
- HY-132578
-
|
Phosphatase
|
Cancer
|
M5N36 is a potent and selective Cdc25C inhibitor with IC50 values of 0.15, 0.19, 0.06 µM for Cdc25A, Cdc25B, Cdc25C, respectively. M5N36 shows anti-proliferative activity and increases the expression of p-CDK1 and p-CDK2 .
|
-
- HY-156084
-
|
CDK
PROTACs
Apoptosis
c-Myc
|
Cancer
|
LL-K9-3 is a potent small-molecule degrader of CDK9-cyclin T1. LL-K9-3 has anti-proliferative and pro-apoptotic activities and suppresses downstream signaling of CDK9 and AR. Moreover, LL-K9-3 inhibits AR and Myc-driven oncogenic transcriptional programs .
|
-
- HY-B0413
-
|
Parasite
HIF/HIF Prolyl-Hydroxylase
Microtubule/Tubulin
Antibiotic
|
Infection
|
Fenbendazole is an orally active benzimidazole anthelmintic agent, with a broad antiparasitic range. Fenbendazole is a microtubule destabilizing agent and acts on helminthes primarily by binding to tubulin and disrupting the tubulin microtubule equilibrium. Fenbendazole stabilizes the transcriptional activator HIF-1α. Fenbendazole possesses an efficient anti-proliferative activity and induces apoptosis. Fenbendazole causes cell-cycle arrest and mitotic cell death, and has antitumor activity in mice xenografted with wild-type p53 .
|
-
- HY-148278
-
|
Ras
|
Cancer
|
BI-0474 is a potent KRAS G12C inhibitor with an IC50 value of 7.0 nM for the GDP-KRAS::SOS1 protein-protein interaction. BI-0474 exhibits good anti-proliferative activity against NCI-H358 cells carrying the G12C mutation. BI-0474 also shows good anti-tumour activity in non-small cell lung cancer xenograft models .
|
-
- HY-50767A
-
PD 0332991 monohydrochloride
|
CDK
|
Cancer
|
Palbociclib (PD 0332991) monohydrochloride is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib monohydrochloride has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma .
|
-
- HY-B0360
-
OPC12759; Proamipide
|
COX
|
Inflammation/Immunology
Cancer
|
Rebamipide (OPC12759) is an orally active gastroprotective agent that enhances the production of endogenous PGs (especially intragastric PGE2) by inducing COX-2 expression, thereby protecting the gastric mucosa from injury. Rebamipide exerts anti-proliferative activity against gastric cancer cells. Rebamipide can be used in studies of mucosal protection, gastroduodenal ulcer, gastritis and gastric cancer .
|
-
- HY-15995
-
TubA
|
ADC Cytotoxin
Antibiotic
Microtubule/Tubulin
|
Cancer
|
Tubulysin A (TubA) is an anticancer and antiangiogenic agent with anti-microtubule, anti-mitosis and anti-proliferative activity against a variety of cancer cells with IC50 values in the pmol range. It can induce apoptosis of cancer cells and has no effect on normal cells. Tubulysins are a group of potent cytotoxins consisting of nine members (A-I). Tubulysin A can synthesize ADC as ADC Cytotoxin< b>ADC Cytotoxin .
|
-
- HY-A0065
-
PD 0332991 isethionate
|
CDK
|
Cancer
|
Palbociclib (PD 0332991) isethionate is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib isethionate has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma .
|
-
- HY-15856B
-
Flupenthixol dihydrochloride
|
Dopamine Receptor
PI3K
Apoptosis
|
Neurological Disease
Cancer
|
Flupentixol is an orally active D1/D2 dopamine receptor antagonist and new PI3K inhibitor (PI3Kα IC50=127 nM). Flupentixol shows anti-proliferative activity to cancer cells and induces apoptosis. Flupentixol can also be used in schizophrenia, anxiolytic and depressive research .
|
-
- HY-115672
-
KS15
1 Publications Verification
|
Cryptochrome
|
Cancer
|
KS15 is an inhibitor of the interactions between cryptochromes (CRYs: CRY1 and CRY2) and the CLOCK:BMAL1 heterodimer. KS15 impairs the feedback actions of CRYs on E-box-dependent transcription (EC50=4.9 μM) by CLOCK:BMAL1 heterodimer, an indispensable transcriptional regulator of the mammalian circadian clock. Anti-proliferative activity .
|
-
- HY-114491
-
|
ERK
Raf
|
Cancer
|
Rineterkib (compound B) is an orally available ERK1 and ERK2 inhibitor in the treatment of a proliferative disease characterized by activating mutations in the MAPK pathway. The activity is particularly related to the treatment of KRAS-mutant NSCLC, BRAF-mutant NSCLC, KRAS-mutant pancreatic cancer, KRAS-mutant colorectal cancer (CRC) and KRAS-mutant ovarian cancer. Rineterkib hydrochloride can also inhibit RAF .
|
-
- HY-114491A
-
|
ERK
Raf
|
Cancer
|
Rineterkib hydrochloride (compound B) is an orally available ERK1 and ERK2 inhibitor in the treatment of a proliferative disease characterized by activating mutations in the MAPK pathway. The activity is particularly related to the treatment of KRAS-mutant NSCLC, BRAF-mutant NSCLC, KRAS-mutant pancreatic cancer, KRAS-mutant colorectal cancer (CRC) and KRAS-mutant ovarian cancer. Rineterkib hydrochloride can also inhibit RAF .
|
-
- HY-144732
-
|
Trk Receptor
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
TRK/ALK-IN-1 (compound 21) is a potent and dual inhibitor of TRK and ALK. TRK/ALK-IN-1 in the enzymatic assays is in good accordance with anti-proliferative activity with IC50 values of 2.2, 9.3 and 38 nM towards TRKA, ALK WT and ALK L1196M, respectively. TRK/ALK-IN-1 has the potential for the research of cancer diseases .
|
-
- HY-147731
-
|
HDAC
|
Cancer
|
HDAC6-IN-9 (compound 12c) is a potent and selective HDAC6 inhibitor with IC50 values of 11.8, 15.2, 4.2, 139.6, 21.3 nM for HDAC1,HDAC3, HDAC6, HDAC8, HDAC10, respectively. HDAC6-IN-9 shows anti-proliferative activities .
|
-
- HY-147027
-
|
PARP
Caspase
Apoptosis
|
Cancer
|
PARP-1-IN-2 (compound 11g) is a potent and BBB-penetrated PARP1 inhibitor, with an IC50 of 149 nM. PARP1-IN-2 shows significantly potent anti-proliferative activity against Human lung adenocarcinoma epithelial cell line A549. PARP1-IN-2 can induce A549 cells apoptosis .
|
-
- HY-121333
-
|
Antibiotic
Wnt
β-catenin
|
Infection
Neurological Disease
Cancer
|
Dinactin, an antibiotic ionophore produced by Streptomyces species, as an effective small molecule targeting Wnt/β-catenin signaling pathway in cancer cells. Dinactin shows marked inhibition of HCT-116 cell growth with an IC50 of 1.1 µM. Dinactin shows anti-proliferative activity against the cancer cells in apoptosis-independent manner. Dinactin is also an effective agent for the research of neuropathic pain .
|
-
- HY-150695
-
|
Carbonic Anhydrase
Apoptosis
|
Cancer
|
hCAIX/XII-IN-5 (Coumarin 9a) a carbonic anhydrase (CA) inhibitor, and exhibits excellent hCA IX/XII selectivity (Ki=93.9 and 85.7 nM, respectively) over hCA I and hCA II. hCAIX/XII-IN-5 shows anti-proliferative activities to cancer cells. hCAIX/XII-IN-5 can delay cell cycle and induce apoptosis .
|
-
- HY-15856A
-
Flupenthixol
|
|
|
Flupentixol is an orally active D1/D2 dopamine receptor antagonist and new PI3K inhibitor (PI3Kα IC50=127 nM). Flupentixol shows anti-proliferative activity to cancer cells and induces apoptosis. Flupentixol can also be used in schizophrenia, anxiolytic and depressive research .
|
-
- HY-150654
-
|
Histone Methyltransferase
|
Cancer
|
WDR5-IN-5 is an orally active and selective inhibitor of WIN site of WD repeat domain 5 (WDR5). WDR5-IN-5 exhibits anti-proliferative activity towards cancer cells and good pharmacokinetics profile in mice. WDR5-IN-5 shows high affinity to WDR5 and the binding affinity Ki value <0.02 nM .
|
-
- HY-50767D
-
PD 0332991 orotate
|
CDK
|
Cancer
|
Palbociclib (PD 0332991) orotate is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib orotate has potent anti-proliferative activity and induces cell cycle arrest in cancer cells. Palbociclib orotate can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma .
|
-
- HY-150566
-
|
Bcr-Abl
|
Cancer
|
BCR-ABL-IN-5 (compound II) is a Bcr-Abl kinase (Breakpoint cluster region-Abelson) inhibitor. BCR-ABL-IN-5 inhibits Bcr-Abl WT and Bcr-Abl T3151 with the IC50 value of 0.014 μM and 0.45 μM, respectively. BCR-ABL-IN-5 has some anti-proliferative activity against leukemic cells .
|
-
- HY-13065
-
Corylifolinin; Isobacachalcone
|
Akt
Reactive Oxygen Species
Apoptosis
Autophagy
|
Cancer
|
Isobavachalcone (Corylifolinin) is derived from Psoralea corylifolia Linn. and is a potent inhibitor of Akt signaling pathway, which induces apoptosis in human cancer cells (Inhibits OVCAR-8 cell growth with an IC50 value of 7.92 μM). Isobavachalcone also induces Reactive Oxyen Species (ROS) generation in OVCAR-8 cells and has exhibit cancer anti-promotive and anti-proliferative activity .
|
-
- HY-131031
-
|
DNA Alkylator/Crosslinker
|
Cancer
|
KCC-07 is a potent, selective and brain-penetrant MBD2 (methyl-CpG-binding domain protein 2) inhibitor. KCC-07 prevents binding of MBD2 to methylated DNA and activates brain specific angiogenesis inhibitor 1 (BAI1) inducing anti-proliferative BAI1/p53/p21 signaling. Anticancer activity .
|
-
- HY-146061
-
|
Ras
|
Cancer
|
KRAS G12C inhibitor 48 (compound 6e) is a potent KRAS G12C inhibitor with an IC50 of 639.91 nM. KRAS G12C inhibitor 48 (0-50 µM) shows anti-proliferative activity with IC50s of 0.796, 6.33, 16.14 µM for H358, H23, A549 cells, respectively .
|
-
- HY-147575
-
|
TAM Receptor
c-Met/HGFR
|
Cancer
|
Axl-IN-8 (NO.1) is a potent AXL inhibitor, with an IC50 of <1 nM. Axl-IN-8 also inhibits c-MET, with an IC50 of 1-10 nM. Axl-IN-8 shows anti-proliferative activity against BaF3/TEL-AXL, MKN45, and EBC-1 cells, with IC50 values of <10, 226.6 and 120.3 nM, respectively .
|
-
- HY-151606
-
|
Akt
|
Cancer
|
Akt3 degrader 1 (compound 12l) is a selective Akt3 degrader that overcomes Osimertinib (HY-15772)-induced resistance in H1975OR NSCLC cells. Akt3 degrader 1 also has anti-proliferative activity and significantly inhibits tumour growth in mice. Akt3 degrader 1 can be used in the study of drug-resistant non-small cell lung cancer .
|
-
- HY-155542
-
|
ROR
|
Cancer
|
RORγ antagonist 1 (compound 22), a potent betulinic acid derivative, is an antagonist of RORγ (KD=0.18 μM). RORγ antagonist 1 exhibits anti-proliferative activity in HPAF-II pancreatic cancer xenograft model. RORγ antagonist 1 inhibits RAS/MAPK and AKT/mTORC1 pathway, and induces caspase-dependent apoptosis in pancreatic cancer cells .
|
-
- HY-155841
-
|
Microtubule/Tubulin
|
Cancer
|
Tubulin polymerization-IN-46 (compound 9q) is a microtubule/Tubulin inhibitor that inhibits tubulin polymerization and induces apoptosis. Tubulin polymerization-IN-46 inhibits mitosis and arrests MCF-7 cells in the G2/M phase. Tubulin polymerization-IN-46 has anti-proliferative activity against MCF-7 breast cancer cells with an IC50 of 10 nM .
|
-
- HY-163001
-
|
Autophagy
p62
Atg8/LC3
|
Cancer
|
Microcolin H is a marine lipopeptide and phosphatidylinositol transfer protein ligand that targets PITPα/β. Microcolin H increases the conversion of LC3I to LC3II and reduces p62 levels in cancer cells, leading to autophagy cell death (Autophagy). Microcolin H effectively inhibits tumor development and has anti-proliferative activity in nude mouse subcutaneous tumor models .
|
-
- HY-158016
-
|
EGFR
Apoptosis
|
Cancer
|
Antiproliferative agent-49 (Compound 5a) is a EGFR-TK inhibitor with an IC50 of 0.09 μM. Antiproliferative agent-49 is a anti-proliferative agent. Antiproliferative agent-49 displays good activities against HER3 and HER4 with IC50 values 0.18 and 0.37 µM. Antiproliferative agent-49 induces mitochondrial apoptotic pathway and increased accumulation of ROS .
|
-
- HY-B0988
-
-
- HY-B1625
-
-
- HY-161334
-
|
Histone Methyltransferase
Apoptosis
|
Cancer
|
CARM1-IN-4 (compound 11f) is a potent CARM1 inhibitor with IC50s of 9 nM and 56 nM for CARM1 and PRMT1, respectively. CARM1-IN-4 displays significant anti-proliferative effects on colorectal cancer cell lines. CARM1-IN-4 effectively inhibits the methyltransferase activity of CARM1 and prevents methylation of downstream proteins. CARM1-IN-4 induces apoptosis and shows antitumor activity .
|
-
- HY-100900
-
|
Deubiquitinase
|
Cancer
|
ML364 is a selective ubiquitin specific peptidase 2 (USP2) inhibitor (IC50=1.1 μM) with anti-proliferative activity, which direct binds to USP2 (Kd=5.2 μM), induces an increase in cellular cyclin D1 degradation and causes cell cycle arrest. ML364 increases the levels of mitochondrial ROS and decreases in the intracellular content of ATP .
|
-
- HY-N2787
-
|
Apoptosis
|
Cancer
|
8-prenylnaringenin is a prenylflavonoid isolated from hop cones Humulus lupulus, with cytotoxicity. 8-prenylnaringenin has anti-proliferative activity against HCT-116 colon cancer cells via induction of intrinsic and extrinsic pathway-mediated apoptosis. 8-Prenylnaringenin also promotes recovery from immobilization-induced disuse muscle atrophy through activation of the Akt phosphorylation pathway in mice .
|
-
- HY-147949
-
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
SKLB0565 is a potent tubulin inhibitor. SKLB0565 shows significant anti-proliferative activity against CRC (colorectal carcinoma) cell lines, with IC50 values ranging from 0.012 μM to 0.081 μM. SKLB0565 causes G2/M phase arrest and mitochondria-mediated intrinsic apoptosis. SKLB0565 inhibits cell migration and disrupted the tube formation of HUVECs .
|
-
- HY-15221
-
|
Apoptosis
Histone Demethylase
MDM-2/p53
|
Cardiovascular Disease
Cancer
|
Methylstat is a potent histone demethylases inhibitor. Methylstat shows anti-proliferative activity with low cytotoxicity. Methylstat induces apoptosis and cell cycle arrest at G0/G1 phase. Methylstat increases the expression of p53 and p21 protein levels. Methylstat inhibits angiogenesis induced by various cytokines. Methylstat can be used as a chemical probe for addressing its role in angiogenesis .
|
-
- HY-151110
-
|
PROTACs
CDK
|
Cancer
|
PROTAC CDK12/13 Degrader-1 (7f) is a highly selective cell cycle protein-dependent kinase CDK12/CDK13 dual degrader with the DC50 values of 2.2 nM and 2.1 nM, respectively. PROTAC CDK12/13 Degrader-1 has anti-proliferative activity and can be used in breast cancer research .
|
-
- HY-17037S1
-
LS 519-d8 dihydrochloride; Pirenzepin-d8 dihydrochloride; Gastrozepin-d8 dihydrochloride
|
Isotope-Labeled Compounds
|
Cancer
|
Pirenzepine-d8 (LS 519-d8; Pirenzepin-d8) dihydrochloride is a deuterium labeled Pirenzepine (dihydrochloride) (HY-17037). Pirenzepine (LS 519) dihydrochloride is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist. Pirenzepine dihydrochloride reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine dihydrochloride shows anti-proliferative activity to cancer cells .
|
-
- HY-N0234
-
7-O-Methylbavachin; Bavachinin A
|
Amyloid-β
PPAR
HIF/HIF Prolyl-Hydroxylase
|
Inflammation/Immunology
|
Bavachinin is agonist of pan-peroxisome proliferator-activated receptor (PPAR), with the IC50 value of 21.043 μM, 12.819 μM, and 0.622 μM to PPAR-α, RRAR-β/δ, and PPAR-γ, respectively. Bavachinin is an inhibitor of HIF-1α. Bavachinin exhibits antitumor activity against non-small cell lung cancer by targeting RRAR-γ. Bavachinin is a natural compound with anti-inflammatory and anti-angiogenic activities. Bavachinin has orally bioactivity. .
|
-
- HY-18684
-
5'-Isobutylthioadenosine; 5'-Deoxy-5'-isobutylthioadenosine
|
Nucleoside Antimetabolite/Analog
HSV
Parasite
|
Infection
Metabolic Disease
Cancer
|
SIBA (5'-Isobutylthioadenosine) is a transmethylation inhibitor (SAH (HY-19528) analogue), with potent anti-proliferative activity. SIBA reversibly inhibits the production of HSV-1 by blocking methylation, specifically by blocking the 5' end-capping of viral mRNA. SIBA also inhibits the growth of tumour cells in vitro and metastatic spread in vivo. SIBA can be used in cancer, HSV-1 infection and anti-malaria studies .
|
-
- HY-112083
-
|
AMPK
|
Cancer
|
BAY-3827 is a potent and selective AMPK inhibitor with IC50 values of 1.4 nM at low (10 µM ATP concentration) and 15 nM at high (2 mM ATP concentration). BAY-3827 shows over 500-fold selectivity for most of the 331 kinases. BAY-3827 prevents phosphorylation of acetyl-CoA carboxylase 1 and shows strongest anti-proliferative activity in androgen-dependent prostate cancer cell lines .
|
-
- HY-151110A
-
|
PROTACs
CDK
|
Cancer
|
PROTAC CDK12/13 Degrader-1 (7f) TFA is a highly selective cell cycle protein-dependent kinase CDK12/CDK13 dual degrader with the DC50 values of 2.2 nM and 2.1 nM, respectively. PROTAC CDK12/13 Degrader-1 TFA has anti-proliferative activity and can be used in breast cancer research .
|
-
- HY-155522
-
|
Carbonic Anhydrase
|
Cancer
|
WES-1 (Compound 8g) is an inhibitor of carbonic anhydrase IX (Ki: 55.9 μM). WES-1 has broad spectrum anti-proliferative activity against the cancer cells, such as leukemia (K-562 and MOLT-4), non-small cell lung cancer (NCI–H460), colon cancer (HCT 116 and HCT-15) and melanoma (LOX IMVI) cell lines .
|
-
- HY-156083
-
|
CDK
|
Cancer
|
PROTAC CDK9/CycT1 Degrader-1 (compounds 10) is a potent inhibitor of CDK9. PROTAC CDK9/CycT1 Degrader-1 can be used as a PROTAC target protein ligand for PROTAC synthesis. PROTAC CDK9/CycT1 Degrader-1 shows strong anti-proliferative activity in solid tumors .
|
-
- HY-157814
-
|
Apoptosis
Epigenetic Reader Domain
|
Cancer
|
Menin-MLL inhibitor-25 (compound A6) is a potent Menin-MLL interaction inhibitor with an IC50 value of 0.38 µM. Menin-MLL inhibitor-25 shows anti-proliferative activity. Menin-MLL inhibitor-25 induces apoptosis and cell cycle arrest at G0/G1 phase. Menin-MLL inhibitor-25 reverses the differentiation arrest .
|
-
- HY-163396
-
|
EGFR
Apoptosis
|
Cancer
|
EGFR-IN-107 (compound 3r) is an orally active EGFR inhibitor with IC50 values of 0.4333 μM for EGFR WT and 0.0438 μM for EGFR L858R/T790M. EGFR-IN-107 has anti-proliferative activity and can inhibit the proliferation of H1975 cells and induce their apoptosis. EGFR-IN-107 can be used in cancer research .
|
-
- HY-10209
-
AB1010
|
c-Kit
PDGFR
Src
FGFR
FAK
Apoptosis
|
Cancer
|
Masitinib (AB1010) is a potent, orally bioavailable, and selective inhibitor of c-Kit (IC50=200 nM for human recombinant c-Kit). It also inhibits PDGFRα/β (IC50s=540/800 nM), Lyn (IC50= 510 nM for LynB), Lck, and, to a lesser extent, FGFR3 and FAK. Masitinib (AB1010) has anti-proliferative, pro-apoptotic activity and low toxicity .
|
-
- HY-10209A
-
AB-1010 mesylate
|
c-Kit
PDGFR
Src
FGFR
Apoptosis
|
Cancer
|
Masitinib mesylate (AB-1010 mesylate) is a potent, orally bioavailable, and selective inhibitor of c-Kit (IC50=200 nM for human recombinant c-Kit). It also inhibits PDGFRα/β (IC50s=540/800 nM), Lyn (IC50= 510 nM for LynB), Lck, and, to a lesser extent, FGFR3 and FAK. Masitinib mesylate (AB-1010 mesylate) has anti-proliferative, pro-apoptotic activity and low toxicity .
|
-
- HY-A0143S
-
DGLA-d6; all-cis-8,11,14-Eicosatrienoic acid-d6
|
Endogenous Metabolite
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
Dihomo-γ-linolenic acid-d6 (DGLA-d6) is the deuterium labeled Dihomo-γ-linolenic acid. Dihomo-γ-linolenic acid (all-cis-8,11,14-Eicosatrienoic acid) is a 20-carbon ω-6 fatty acid, with anti-inflammatory and anti-proliferative activities. Dihomo-γ-linolenic acid attenuates atherosclerosis in the apolipoprotein E deficient mouse model system[1][2][3].
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-
- HY-144181
-
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Methionine Adenosyltransferase (MAT)
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Cancer
|
MAT2A-IN-5 is a potent inhibitor of MAT2A. The expression level of MAT2A is abnormally elevated in several types of tumors, including gastric, colon, liver and pancreatic cancers. MAT2A-IN-5 reduces the proliferative activity of MTAP-deficient cancer cells. MAT2A-IN-5 has the potential for the potential for the research of cancer diseases (extracted from patent WO2021254529A1, compound 1) .
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-
- HY-144184
-
|
Methionine Adenosyltransferase (MAT)
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Cancer
|
MAT2A-IN-6 is a potent inhibitor of MAT2A. The expression level of MAT2A is abnormally elevated in several types of tumors, including gastric, colon, liver and pancreatic cancers. MAT2A-IN-6 reduces the proliferative activity of MTAP-deficient cancer cells. MAT2A-IN-6 has the potential for the potential for the research of cancer diseases (extracted from patent WO2021254529A1, compound 18) .
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-
- HY-144185
-
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Methionine Adenosyltransferase (MAT)
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Cancer
|
MAT2A-IN-7 is a potent inhibitor of MAT2A. The expression level of MAT2A is abnormally elevated in several types of tumors, including gastric, colon, liver and pancreatic cancers. MAT2A-IN-7 reduces the proliferative activity of MTAP-deficient cancer cells. MAT2A-IN-7 has the potential for the potential for the research of cancer diseases (extracted from patent WO2021254529A1, compound 24) .
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-
- HY-142930
-
|
Somatostatin Receptor
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Cancer
|
MAT2A-IN-3 is a potent inhibitor of MAT2A. The expression level of MAT2A is abnormally high in several types of tumors, including gastric, colon, liver and pancreatic cancers. MAT2A-IN-3 reduces the proliferative activity of MTAP-deficient cancer cells. MAT2A-IN-3 has the potential for the research of cancer diseases (extracted from patent WO2019191470A1, compound 265) .
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- HY-142929
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Somatostatin Receptor
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Cancer
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MAT2A-IN-2 is a potent inhibitor of MAT2A. The expression level of MAT2A is abnormally high in several types of tumors, including gastric, colon, liver and pancreatic cancers. MAT2A-IN-2 reduces the proliferative activity of MTAP-deficient cancer cells. MAT2A-IN-2 has the potential for the research of cancer diseases (extracted from patent WO2020243376A1, compound 172) .
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- HY-142928
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Somatostatin Receptor
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Cancer
|
MAT2A-IN-1 is a potent inhibitor of MAT2A. The expression level of MAT2A is abnormally high in several types of tumors, including gastric, colon, liver and pancreatic cancers. MAT2A-IN-1 reduces the proliferative activity of MTAP-deficient cancer cells. MAT2A-IN-1 has the potential for the research of cancer diseases (extracted from patent WO2021139775A1, compound 64) .
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- HY-147839
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Topoisomerase
Apoptosis
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Cancer
|
Topoisomerase II inhibitor 10 (compound 32a) is a potent topoisomerase II inhibitor with an IC50 value of 7.45 μM. Topoisomerase II inhibitor 10 causes cell cycle arrest at G2-M phase and induces apoptosis of HepG-2 cells. Topoisomerase II inhibitor 10 has excellent anti-proliferative activities against HepG-2, MCF-7, and HCT-116 cells .
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- HY-146210
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EGFR
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Cancer
|
EGFR-IN-50 (Compound 9h) is a potent EGFR inhibitor against L858R resistance mutation (TEL-EGFR-L858R-BaF3: GI50=8 nM, TEL-EGFR-T790M-L858R-BaF3: GI50=6.03 μM). EGFR-IN-50 shows anti-proliferative activity to cancer cells .
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- HY-156003
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HDAC
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Cancer
|
HDAC-IN-64 (Compound 13) is a HDAC inhibitor. HDAC-IN-64 inhibits HDAC4/5/6/7/9 with IC50s of 24, 45, 85, 31, 37 nM. HDAC-IN-64 has anti-proliferative activity and anti-migration properties on prostate cancer (PCA) cells. HDAC-IN-64 inhibits LNCaP and RWPE-1 cell growth with GI50 of 0.32 and 1.1 μM respectively .
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- HY-15856BR
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Flupenthixol dihydrochloride (Standard)
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Dopamine Receptor
PI3K
Apoptosis
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Neurological Disease
Cancer
|
Flupentixol (dihydrochloride) (Standard) is the analytical standard of Flupentixol (dihydrochloride). This product is intended for research and analytical applications. Flupentixol is an orally active D1/D2 dopamine receptor antagonist and new PI3K inhibitor (PI3Kα IC50=127 nM). Flupentixol shows anti-proliferative activity to cancer cells and induces apoptosis. Flupentixol can also be used in schizophrenia, anxiolytic and depressive research .
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- HY-104048
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QC6352
4 Publications Verification
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Histone Demethylase
|
Cancer
|
QC6352 is an orally active KDM4 inhibitor with anti-tumor and anti-proliferative activity. QC6352 has in vivo inhibitory effects on PDX models of breast and colon cancer and reduces the number of chemoresistant cell populations. QC6352 inhibits KDM4 different isoforms with IC50s of 104 nM (KDM4A), 56 nM (KDM4B), 35 nM (KDM4C), and 104 nM (KDM4D), respectively. QC6352 has moderate inhibitory activity against KDM5 with an IC50 of 750 nM (KDM5B) .
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- HY-133121
-
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Histone Methyltransferase
Apoptosis
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Cancer
|
WDR5-IN-1 is a potent and selective WD repeat domain 5 (WDR5) inhibitor, with a Kd of <0.02 nM. WDR5-IN-1 inhibits MLL1 histone methyltransferase (HMT) activity with an IC50 of 2.2 nM. WDR5-IN-1 diminishes MYC recruitment at WDR5-displaced genes and exhibits potent anti-proliferative effects in CHP-134 (neuroblastoma) and Ramos (Burkitt’s lymphoma) lines .
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- HY-101144
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TCD-717
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Others
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Cancer
|
RSM-932A (TCD-717) is a specific ChoKα inhibitor with IC50s of 1 and 33 μM for human recombinant ChoKα and ChoKβ enzymes, respectively. RSM-932A acts as the “first in humans” compound targeting ChoKα. RSM-932A is potent in vitro anti-proliferative and in vivo anti-tumoral activity against human xenografts in mice, showing high efficacy with low toxicity profiles .
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-
- HY-146103
-
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Apoptosis
Reactive Oxygen Species
|
Cancer
|
Antiproliferative agent-7 (compound 8f) is a potent anti-proliferative agent. Antiproliferative agent-7 has antiproliferative activity against cancer cell lines MCF-7, MDA-MB-231, HCT-116 and FR-2 with IC50s of 3.5 μM, 15.54 μM, 30.43 μM and 34.8 μM, respectively. Antiproliferative agent-7 can increase ROS production and induce apoptosis .
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-
- HY-N12253
-
|
Others
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Cancer
|
(19R)-13-Deoxy-19-hydroxyenmein is the parent compound of enmein-type diterpenoid analogs. (19R)-13-Deoxy-19-hydroxyenmein has anti-proliferative activities with IC50 values of 0.41, 0.85, 0.43, 1.89 μM against human cancer cell lines K562, MGC-803, CaEs-17, and Bel-7402, respectively .
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-
- HY-400684
-
|
Others
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Cancer
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Tubulysin A intermediate-1 is an intermediate in the synthesis of the cytotoxic peptide Tubulysin A (HY-15995). Tubulysin A (TubA) is an antibiotic, anti-microtubule toxins, and apoptosis inducer isolated from myxobacteria. Tubulysin A has anti-angiogenic, anti-microtubule, anti-mitotic, and anti-proliferative activities. Tubulysin A arrests cells in the G2/M phase, effectively inhibits tubulin polymerization, and induces depolymerization of detached microtubules. Tubulysin A acts as an ADC cytotoxin (ADC Cytotoxin) to synthesize ADC .
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-
- HY-113831
-
|
CDK
SRPK
|
Cancer
|
LK1/2-IN-3 (compound 3) is a potent and selective CLK1 and CLK2 inhibitor with IC50 values of 1.1, 2.1, 130, 260, 260 nM for CLK1, CLK2, SRPK1, SRPK2, SRPK3, respectively. CLK1/2-IN-3 shows anti-proliferative activity. CLK1/2-IN-3 reduces the levels of endogenous phosphorylated SR proteins and increases the expression of S6K mRNAs .
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-
- HY-151477
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|
SARS-CoV
|
Infection
Cancer
|
SARS-CoV-2-IN-32 (compound 3g) is a COVID-19 inhibitor. SARS-CoV-2-IN-32 shows anti-proliferative activity against cancer cells. SARS-CoV-2-IN-32 exhibits comparatively high binding affinity (-8.8 Kcal/mole) to COVID-19 main protease (M pro) (PDB ID: 6LU7). SARS-CoV-2-IN-32 can be used in studies of cancer and COVID-19 .
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- HY-151478
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|
SARS-CoV
|
Infection
Cancer
|
SARS-CoV-2-IN-33 (compound 3m) is a COVID-19 inhibitor. SARS-CoV-2-IN-33 shows anti-proliferative activity against cancer cells. SARS-CoV-2-IN-33 exhibits comparatively good binding affinity (-8.0 Kcal/mole) to COVID-19 main protease (M pro) (PDB ID: 6LU7). SARS-CoV-2-IN-33 can be used in studies of cancer and COVID-19 .
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-
- HY-155808
-
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STAT
JAK
Apoptosis
COX
|
Cancer
|
STAT3-IN-18 (compound SPP) is a platinum (IV) complex with an axial ligand derived from sandalwood. STAT3-IN-18 inhibits the JAK2-STAT3 pathway in breast cancer (BC) cells, with anti-proliferative activity. STAT3-IN-18 activates caspase-3 and increases cleaved polyADP-ribose polymerase to induce apoptosis. STAT3-IN-18 promotes maturation and antigen presentation of dendritic cells and demonstrates safety in vivo.
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-
- HY-119944
-
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EGFR
|
Cancer
|
JND3229 is a reversible EGFR C797S inhibitor with IC50 values of 5.8, 6.8 and 30.5 nM for EGFR L858R/T790M/C797S, EGFR WT and EGFR L858R/T790M, respectively. JND3229 has good anti-proliferative activity and can effectively inhibit tumour growth in vivo. JND3229 can be used in cancer research, especially in non-small cell carcinoma .
|
-
- HY-147793
-
|
FGFR
|
Cancer
|
FGFR4-IN-12 (Compound A34) is a potent inhibitor of FGFR4. FGFR4-IN-12 exhibits improved FGFR4 inhibitory capability and selectivity and excellent anti-proliferative activities against FGFR4-dependent HCC cell lines. FGFR4-IN-12 has the potential for the research of cancer diseases . FGFR4-IN-12 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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-
- HY-163105
-
|
Microtubule/Tubulin
|
Cancer
|
Tubulin/NEDDylation-IN-1 (compound C11) is a dual inhibitor of tubulin (Microtubule/Tubulin)-NEDDylation (IC50 for tubulin=2.40 μM), which has strong anti-proliferative activity. Neddylation is a protein post-translational modification that covalently tags the ubiquitin-like protein NEDD8 to target proteins. Tubulin/NEDDylation-IN-1 forms hydrogen bonds with residues of tubulin and E1 NEDD8 activating enzyme (NAE) through methoxy and dithiocarbamate groups and inhibits NEDDylation and microtubulin in an ATP-dependent manner. tube polymerization .
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-
- HY-F0003
-
|
Ferroptosis
Endogenous Metabolite
|
Cancer
|
NADPH tetrasodium salt functions as an important cofactor in a variety of metabolic and biosynthetic pathways. NADPH tetrasodium salt plays a vital role in the biosynthesis of agents, chiral alcohols, fatty acids and biopolymers, while also being required for lipid biosynthesis, biomass formation, and cell replication. The demand for NADPH tetrasodium salt is particularly high in proliferating cancer cells, where it acts as a cofactor for the synthesis of nucleotides, proteins, and fatty acids. NADPH tetrasodium salt is also essential for the neutralization of the dangerously high levels of reactive oxygen species (ROS) generated by increased metabolic activity. NADPH tetrasodium salt is an endogenous inhibitor of ferroptosis .
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-
- HY-144692
-
|
MEK
PI3K
PERK
|
Cancer
|
MEK/PI3K-IN-1 (compound 6r) is a potent MEK/PI3K inhibitor, with IC50 values of 124 nM (MEK1), 130 nM (PI3Kα), and 236 nM (PI3Kδ), respectively. MEK/PI3K-IN-1 suppresses pAKT and pERK1/2 levels. MEK/PI3K-IN-1 shows anti-proliferative activity against tumor cell lines .
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-
- HY-144693
-
|
MEK
PI3K
PERK
|
Cancer
|
MEK/PI3K-IN-2 (compound 6s) is a potent MEK/PI3K inhibitor, with IC50 values of 352 nM (MEK1), 107 nM (PI3Kα), and 137 nM (PI3Kδ), respectively. MEK/PI3K-IN-2 suppresses pAKT and pERK1/2 levels. MEK/PI3K-IN-2 shows anti-proliferative activity against tumor cell lines .
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-
- HY-100555
-
|
|
|
CH5138303 is a potent and orally active Hsp90 inhibitor. CH5138303 shows high binding affinity for N-terminal Hsp90α, with Kd of 0.52 nM. CH5138303 shows potent anti-proliferative activity against human cancer cell lines (HCT116 and NCI-N87), with IC50 values of 0.098 and 0.066 μM, respectively. CH5138303 shows high oral bioavailability in mice (F=44.0%). CH5138303 shows potent antitumor efficacy in a human NCI-N87 gastric cancer xenograft model .
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-
- HY-153356
-
|
Apoptosis
|
Cancer
|
MRT-2359 is a potent, orally active and selective GSPT1 depressant (IC50: >30 nM and <300 nM) that specifically induces apoptosis dependent on protein translation. MRT-2359 exhibits significant and preferred anti-proliferative activity in a variety of cancer cell lines, especially MYC-driven cell lines, such as non-small cell lung cancer (NSCLC) and small cell lung cancer (SCLC) with high expression of N-Myc or L-Myc. MRT-2359 inhibits the growth of drug-resistant NSCLC and SCLC cells, making it suitable for cancer research .
|
-
- HY-108359
-
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-145288
-
|
Apoptosis
|
Cancer
|
Antitumor agent-36 possesses potent anti-proliferative and anti-metastasis activities. Antitumor agent-36 induces serious DNA damage and further leads to high expression of γ-H2AX and p53. Antitumor agent-36 promotes apoptosis of tumor cells through mitochondrial apoptotic pathway Bcl-2/Bax/caspase3. Antitumor agent-36 significantly improves immune response through restraining the expression of PD-L1 to increase CD3+ and CD8+ T infiltrating cells in tumor tissues .
|
-
- HY-145289
-
|
Apoptosis
|
Cancer
|
Antitumor agent-37 possesses potent anti-proliferative and anti-metastasis activities. Antitumor agent-37 induces serious DNA damage and further leads to high expression of γ-H2AX and p53. Antitumor agent-37 promotes apoptosis of tumor cells through mitochondrial apoptotic pathway Bcl-2/Bax/caspase3. Antitumor agent-37 significantly improves immune response through restraining the expression of PD-L1 to increase CD3+ and CD8+ T infiltrating cells in tumor tissues .
|
-
- HY-157164
-
|
PROTACs
Histone Methyltransferase
|
Cancer
|
PROTAC EZH2 Degrader-2 (compound E-3P-MDM2), an EZH2 inhibitor, is a PROTAC composed of Tazemetostat (EPZ6438) and an E3 ligase system ligand. PROTAC EZH2 Degrader-2 degrades EZH2 in SU-DHL-6 cells in a dose-dependent manner, inhibits the expression of H3K27me3, and simultaneously degrades EED and SUZ12 proteins without affecting their mRNA levels. PROTAC EZH2 Degrader-2 has anti-cancer and anti-proliferative activity .
|
-
- HY-149401
-
|
EGFR
|
Cancer
|
EGFR-IN-82 (Cmpound 8a) is a potent and orally active EGFR inhibitor with IC50 values of 0.09 and 0.06 nM for EGFR L858R/T790M/C797S and EGFR Del19/T790M/C797S, respectively. EGFR-IN-82 has no significant effect on EGFR WT. EGFR-IN-82 has anti-proliferative activity and inhibits tumor formation in nude mice. EGFR-IN-82 can be used in non-small cell lung cancer research .
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-
- HY-151375
-
|
Others
|
Cancer
|
CDK9/10/GSK3β-IN-1 (compound 13c) is a kinase inhibitor (Flavopiridol (HY-10005) analogue) that effectively inhibits HsGSK3β (IC50=59 nM), HsCDK9/CyclinT (IC50=64 nM), HsCDK5/p25 (IC50=1.093 µM) and HsCDK2/CyclinA (IC50=1.725 µM). CDK9/10/GSK3β-IN-1 has anti-cancer cellular activity comparable to or higher than that of Flavopiridol. CDK9/10/GSK3β-IN-1 shows high anti-proliferative activity in vitro against up to seven cancer cell lines .
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-
- HY-112296
-
T025
2 Publications Verification
|
CDK
Apoptosis
DYRK
|
Cancer
|
T025 is an orally active and highly potent inhibitor of Cdc2-like kinase (CLKs), with Kd values of 4.8, 0.096, 6.5, 0.61, 0.074, 1.5 and 32 nM for CLK1, CLK2, CLK3, CLK4, DYRK1A, DYRK1B and DYRK2, respectively. T025 induces caspase-3/7-mediated cell apoptosis. T025 reduces CLK-dependent phosphorylation. T025 exerts anti-proliferative activities in both hematological and solid cancer cell lines (IC50 values: 30-300 nM). T025 has an anti-tumor efficiency, mainly for MYC-driven disease research .
|
-
- HY-157125
-
|
PI3K
Apoptosis
|
Cancer
|
PI3Kα-IN-14 (compound F8) is a selective PI3Kα inhibitor with an IC50 of 0.14 nM. PI3Kα-IN-14 induces a great decrease in mitochondrial membrane which caused cell cycle arrest at G1 phase and apoptosis in U87-MG cells. PI3Kα-IN-14 shows significant anti-proliferative activities against three tumor-derived cell lines (PC-3: IC50 of 0.28 μM; HCT-116: IC50 of 0.57 μM; and U87-MG: IC50 of 1.37 μM) .
|
-
- HY-157319
-
|
PI3K
|
Cancer
|
PI3Kα-IN-15 is a potent PI3Kα inhibitor with an IC50 of 0.15?μM. PI3Kα-IN-15 also has acceptable anti-proliferative activity (inhibits SKOV-3, T47D, NCI-H1975, NCI-H460, and MCF-7 growth with IC50 values of 26.6?μM, 7.9?μM,? 32.1?μM,? 17.7??μM, and 9.4??μM, respectively. PI3Kα-IN-15 can be used for cancer research .
|
-
- HY-147414
-
PF-114
|
Bcr-Abl
|
Cancer
|
Vamotinib (PF-114) is a potent, selective and orally active tyrosine kinase inhibitor. Vamotinib inhibits the autophosphorylation of BCR/ABL and BCR/ABL-T315I. Vamotinib induces apoptosis. Vamotinib shows anti-proliferative and anti-tumor activity. Vamotinib has the potential for the research of resistant philadelphia chromosome-positive (Ph+) leukemia. Vamotinib inhibits ABL series kinases with IC50s of 0.49 nM (ABL), 0.78 nM (ABL T315I), 9.5 nM (ABL E255K), 2.0 nM (ABL F317I), 7.4 nM (ABL G250E), 1.0 nM (ABL H396P), 2.8 nM (ABL M351T), 12 nM (ABL Q252H), and 4.1 nM (ABL Y253F), respectively . Vamotinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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-
Cat. No. |
Product Name |
Type |
-
- HY-114491
-
|
Fluorescent Dyes/Probes
|
Rineterkib (compound B) is an orally available ERK1 and ERK2 inhibitor in the treatment of a proliferative disease characterized by activating mutations in the MAPK pathway. The activity is particularly related to the treatment of KRAS-mutant NSCLC, BRAF-mutant NSCLC, KRAS-mutant pancreatic cancer, KRAS-mutant colorectal cancer (CRC) and KRAS-mutant ovarian cancer. Rineterkib hydrochloride can also inhibit RAF .
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Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P1240
-
MOG (35-55)
|
Peptides
|
Neurological Disease
Inflammation/Immunology
|
Myelin Oligodendrocyte Glycoprotein Peptide (35-55), mouse, rat (MOG (35-55)) is a minor component of CNS myelin. Myelin Oligodendrocyte Glycoprotein Peptide (35-55), mouse, rat has encephalitogenic activity and induces T cell proliferative. Myelin Oligodendrocyte Glycoprotein Peptide (35-55), mouse, rat induces Th1 cytokine response as well as relatively high levels of IgG antibodies. Myelin Oligodendrocyte Glycoprotein Peptide (35-55), mouse, rat produces a relapsing-remitting neurological disease with extensive plaque-like demyelination .
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-
- HY-P1240B
-
MOG (35-55) (acetate)
|
Peptides
|
Neurological Disease
Inflammation/Immunology
|
Myelin Oligodendrocyte Glycoprotein Peptide (35-55), mouse, rat (MOG (35-55)) acetate is a minor component of CNS myelin. Myelin Oligodendrocyte Glycoprotein Peptide (35-55), mouse, rat acetate has encephalitogenic activity and induces T cell proliferative. Myelin Oligodendrocyte Glycoprotein Peptide (35-55), mouse, rat acetate induces Th1 cytokine response as well as relatively high levels of IgG antibodies. Myelin Oligodendrocyte Glycoprotein Peptide (35-55), mouse, rat acetate produces a relapsing-remitting neurological disease with extensive plaque-like demyelination .
|
-
- HY-P1240A
-
MOG (35-55) (TFA)
|
Peptides
|
Neurological Disease
Inflammation/Immunology
|
Myelin Oligodendrocyte Glycoprotein Peptide (35-55), mouse, rat (MOG (35-55)) TFA is a minor component of CNS myelin. Myelin Oligodendrocyte Glycoprotein Peptide (35-55), mouse, rat TFA has encephalitogenic activity and induces T cell proliferative. Myelin Oligodendrocyte Glycoprotein Peptide (35-55), mouse, rat TFA induces Th1 cytokine response as well as relatively high levels of IgG antibodies. Myelin Oligodendrocyte Glycoprotein Peptide (35-55), mouse, rat TFA produces a relapsing-remitting neurological disease with extensive plaque-like demyelination .
|
-
- HY-P3817
-
|
Peptides
|
Neurological Disease
|
Des-[Gly77,His78] Myelin Basic Protein (68-84) is a 68-84 sequence fragment of guinea pig myelin basic protein (GPMBP). Des-[Gly77,His78] Myelin Basic Protein (68-84) regulates functionally diverse encephalitogenic and proliferative activities of experimental autoimmune encephalomyelitis (EAE)-associated T cells .
|
-
- HY-163001
-
|
Autophagy
p62
Atg8/LC3
|
Cancer
|
Microcolin H is a marine lipopeptide and phosphatidylinositol transfer protein ligand that targets PITPα/β. Microcolin H increases the conversion of LC3I to LC3II and reduces p62 levels in cancer cells, leading to autophagy cell death (Autophagy). Microcolin H effectively inhibits tumor development and has anti-proliferative activity in nude mouse subcutaneous tumor models .
|
Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P99218
-
Sch 717454; 19D12
|
IGF-1R
|
Cancer
|
Robatumumab (Sch 717454) is an anti-human IGF-1R (insulin-like growth factor receptor-1) antibody. Robatumumab shows anti-tumor activity and anti-proliferative activity to cancer cells. Robatumumab can be used in osteosarcoma and Ewing sarcoma research .
|
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
Cat. No. |
Product Name |
Chemical Structure |
-
- HY-B0421S
-
|
Mycophenolic acid-d3 is deuterium labeled Mycophenolic acid, which is an an immunosuppresant agent and has potent anti-proliferative activity.
|
-
-
- HY-17037S1
-
|
Pirenzepine-d8 (LS 519-d8; Pirenzepin-d8) dihydrochloride is a deuterium labeled Pirenzepine (dihydrochloride) (HY-17037). Pirenzepine (LS 519) dihydrochloride is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist. Pirenzepine dihydrochloride reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine dihydrochloride shows anti-proliferative activity to cancer cells .
|
-
-
- HY-A0143S
-
|
Dihomo-γ-linolenic acid-d6 (DGLA-d6) is the deuterium labeled Dihomo-γ-linolenic acid. Dihomo-γ-linolenic acid (all-cis-8,11,14-Eicosatrienoic acid) is a 20-carbon ω-6 fatty acid, with anti-inflammatory and anti-proliferative activities. Dihomo-γ-linolenic acid attenuates atherosclerosis in the apolipoprotein E deficient mouse model system[1][2][3].
|
-
-
- HY-15605S
-
|
Encorafenib- 13C,d3 is the 13C- and deuterium labeled Encorafenib. Encorafenib (LGX818) is a highly potent BRAF inhibitor with selective anti-proliferative and apoptotic activity in cells expressing BRAFV600E (EC50=4 nM).
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-
-
- HY-19937S1
-
|
Saroglitazar-d4 is the deuterium-labeled Saroglitazar (HY-19937). Saroglitazar-d4 is a novel peroxisome proliferator-activated receptor (PPAR) agonist with predominant PPARα and moderate PPARγ activity with EC50 values of 0.65 pM and 3 nM in HepG2 cells, respectively.
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