Search Result
Results for "
PANC-1
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
1
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-B0190A
-
|
FUT-175
|
Flavivirus
TNF Receptor
NF-κB
Apoptosis
Ser/Thr Protease
|
Infection
Cancer
|
|
Nafamostat mesylate (FUT-175), an anticoagulant, is a synthetic serine protease inhibitor. Nafamostat mesylate has anticancer and antivirus effect. Nafamostat mesylate induce apoptosis by up-regulating the expression of tumor necrosis factor receptor-1 (TNFR1). Nafamostat mesylate can be used in the development of the pathological thickening of the arterial wall [1] .
|
-
-
- HY-18597
-
|
|
Phosphatase
|
Cancer
|
|
LB-100 is a protein phosphatase 2A (PP2A) inhibitor, with IC50 of 0.85 μM and 3.87 μM in BxPc-3 and Panc-1 cells [1] .
|
-
-
- HY-33878
-
|
|
Potassium Channel
Proton Pump
|
Neurological Disease
|
|
2-PPA is a lysosomal potassium and proton channel TMEM175 pore blocker. 2-PPA binds at a TMEM175 pore site to occlude potassium and proton ion permeation pathways. 2-PPA increases lysosomal macromolecule catabolism, accelerates macropinocytosis. 2-PPA binds to hepatic protein in covalent. 2-PPA can be used for the research of Parkinson's disease [1] .
|
-
-
- HY-148012
-
|
QN-302
|
G-quadruplex
|
Cancer
|
|
SOP1812 (QN-302) is a naphthalene diimide (ND) derivative with anti-tumor activity. SOP1812 binds to quadruplex arrangements (G4s), and down-regulates several cancer gene pathways. SOP1812 shows great affinity to hTERT G4 and HuTel21 G4 with KD values of 4.9 and 28.4 nM, respectively. SOP1812 can be used for the research of cancer [1].
|
-
-
- HY-B1152
-
|
|
Dopamine Receptor
CD276/B7-H3
FOXO
|
Neurological Disease
Cancer
|
|
Piperacetazine is an orally active dopamine receptor antagonist and phenothiazine antipsychotic. Piperacetazine can directly bind to the PAX3::FOXO1 fusion protein and inhibit its transcriptional activity. Piperacetazine also exhibits antitumor activity with an IC50 of 7.627 μM against PANC-1 cells. Piperacetazine can be used for the research of diseases such as schizophrenia and pancreatic cancer and other tumors [1] .
|
-
-
- HY-19352
-
|
T5601640
|
LIM Kinase (LIMK)
|
Cancer
|
|
T56-LIMKi is a selective inhibitor of LIMK2; inhibits the growth of Panc-1 cells with an IC50 of 35.2 μM.
|
-
-
- HY-N1410
-
|
|
STAT
NF-κB
|
Cancer
|
|
Triacetylresveratrol, an acetylated analog of Resveratrol. Triacetylresveratrol decreases the phosphorylation of STAT3 and NF-κB in a dose- and time- dependent manner in PANC-1 and BxPC-3 cells. Anticancer effects [1].
|
-
-
- HY-113978
-
-
-
- HY-113314
-
|
|
Endogenous Metabolite
|
Cancer
|
|
AFMK, antioxidant metabolite of Melatonin, attenuates X-ray-induced oxidative damage to DNA, proteins and lipids in mice. AFMK is a poorer scavenger. The pKa of AFMK at physiological pH is 8.7. Antioxidant capacity [1] . AFMK improves the anti-tumor effect of Gemcitabine in PANC-1 cells through the modulation of apoptotic pathway .
|
-
-
- HY-P99589
-
|
16B5; AB-16B5
|
Apoptosis
|
Cancer
|
|
Sotevtamab (16B5) is a humanized IgG2 anti-clusterin monoclonal antibody (mAb). Sotevtamab is an inhibitor of the epithelial to mesenchymal transition. Sotevtamab can be used for cancer research [1] .
|
-
-
- HY-148712
-
|
|
Apoptosis
Sirtuin
|
Cancer
|
|
SIRT6 activator 12q is potent, selective and orally active SIRT6 activator with IC50 values of 171.20, >200, >200, >200, 0.58 μM for SIRT1, SIRT2, SIRT3, SIRT5, SIRT6, respectively. SIRT6 activator 12q inhibits cell growth and migration. SIRT6 activator 12q induces Apoptosis and cell cycle arrest at G2 phase. SIRT6 activator 12q shows anticancer activity [1].
|
-
-
- HY-108593
-
|
BMS-A
|
Potassium Channel
|
Neurological Disease
|
|
BMS 191011 (BMS-A) is a potent BKCa channel opener (large-conductance Ca 2+-activated potassium channel). BMS-191011 shows neuroprotective activities in rodent models of stroke [1].
|
-
-
- HY-N8284
-
-
-
- HY-179089
-
|
|
ULK
|
Cancer
|
|
SBP-1750 is an orally active ULK inhibitor and an ATG13 degrader. SBP-1750 strongly inhibits ULK1/2 activity, with IC50 values of 8 and 50 nM, respectively. SBP-1750 induces ATG13 degradation, with an EC50 value of 114 nM. SBP-1750 can inhibit autophagy in cancer cells and induce cell death. SBP-1750 can be used in cancer research, such as for pancreatic cancer [1].
|
-
-
- HY-125221
-
|
|
ROCK
Cdc42-binding kinase
|
Cancer
|
|
DJ4 is a ATP-competitive inhibitor of ROCK1/2 (IC50 values:5 and 50 nM) and MRCKα/β (IC50 values:10 and 100 nM). DJ4 blocks stress fiber formation and inhibits migration and invasion of cancer cells. DJ4 can be used for study of lung cancer, breast cancer, and pancreatic (PANC-1) cancer [1].
|
-
-
- HY-147204
-
|
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
Mc-Alanyl-Alanyl-Asparagine-PAB-MMAE (compound S6) is a potent anticancer agent, which can be specific activated by tumor microenvironment. Mc-Alanyl-Alanyl-Asparagine-PAB-MMAE can suppress tumor growth in mice (extracted from patent CN104147612A) [1].
|
-
-
- HY-151613A
-
|
|
PROTACs
Akt
|
Cancer
|
|
MS15 TFA is a potent and selective AKT PROTAC degrader. MS15 TFA inhibits the AKT1, -2, and -3 activities, with IC50 values of 798 nM, 90 nM, and 544 nM, respectively [1].
|
-
-
- HY-162749A
-
|
|
PROTACs
Histone Methyltransferase
Apoptosis
|
Cancer
|
|
G9D-4 TFA is a G9a PROTAC degrader. G9D-4 TFA induces G9a degradation, reduces H3K9me2 levels, and prevents GLP interference via the CRBN ternary complex, proteasome and ubiquitin-like modification-dependent pathways. G9D-4 TFA exerts antiproliferative activity and induces Apoptosis in pancreatic cancer cells. G9D-4 TFA can be used for research on pancreatic cancer [1].
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-
-
- HY-152204
-
|
|
Cathepsin
|
Cancer
|
|
Cathepsin L/S-IN-1 is a dual inhibitor of Cathepsin L and Cathepsin S with IC50s of 4.10 μM and 1.79 μM, respectively. Cathepsin L/S-IN-1 shows a significant antimetastatic and invasive effects on pancreatic cancer BxPC-3 and PANC-1 cells [1].
|
-
-
- HY-135680
-
|
I-OMe-AG 538
|
IGF-1R
|
Metabolic Disease
Cancer
|
|
I-OMe-Tyrphostin AG 538 (I-OMe-AG 538) is a specific inhibitor of IGF-1R (insulin-like growth factor-1 receptor tyrosine kinase). I-OMe-Tyrphostin AG 538 inhibits IGF-1R-mediated signaling and is preferentially cytotoxic to nutrient-deprived PANC1 cells.?I-OMe-Tyrphostin AG 538 is an ATP-competitive inhibitor of phosphatidylinositol-5-phosphate 4-kinase α (PI5P4Kα), with an IC50?of 1 μM [1].
|
-
-
- HY-146695
-
|
|
Drug Derivative
|
Cancer
|
|
S100P-IN-1 (Compound 4) is a S100P inhibitor with an IC50 of 22.7 nM. S100P-IN-1 shows anti-metastatic effects on pancreatic cancer cells [1].
|
-
-
- HY-18641
-
|
|
LPL Receptor
|
Cancer
|
|
Ki16198 is a potent and orally active LPA receptor antagonist, the methyl ester of Ki16425 (HY-13285). Ki16198 inhibits LPA1 and LPA3-induced inositol phosphate production with?Ki?values of 0.34 μM and 0.93 μM, respectively. Ki16198 is effective for pancreatic cancer tumorigenesis and metastasis in vivo [1].
|
-
-
- HY-151613
-
|
|
PROTACs
Akt
|
Cancer
|
|
MS15 is a potent and selective AKT PROTAC degrader. MS15 inhibits the AKT1, -2, and -3 activities, with IC50 values of 798 nM, 90 nM, and 544 nM, respectively [1].
|
-
-
- HY-162749
-
|
|
PROTACs
Histone Methyltransferase
Apoptosis
|
Cancer
|
|
G9D-4 is a G9a PROTAC degrader. G9D-4 induces G9a degradation, reduces H3K9me2 levels, and prevents GLP interference via the CRBN ternary complex, proteasome and ubiquitin-like modification-dependent pathways. G9D-4 exerts antiproliferative activity and induces Apoptosis in pancreatic cancer cells. G9D-4 can be used for research on pancreatic cancer [1].
|
-
-
- HY-N7287
-
|
|
Others
|
Others
|
|
(+)-Matairesinol is a lignan. (+)-Matairesinol has no cytotoxic activity for human pancreatic PANC-1 cancer cells [1].
|
-
-
- HY-175224
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
PROTAC BRD4 Degrader-36 is a BRD4 PROTAC degrader. PROTAC BRD4 Degrader-36 has a DC50 of 0.649 nM and a Dmax of 71% in PANC-1 cells. PROTAC BRD4 Degrader-36 is cytotoxic to PANC-1 cells (GI50: 0.103 μM). PROTAC BRD4 Degrader-36 can be used in the study of cancer. (Pink: PROTAC BRD4 ligand-1 (HY-129939); Blue + Black: E3 ligase ligand + linker (HY-175241)) [1].
|
-
-
- HY-127155
-
|
|
Bacterial
Antibiotic
|
Infection
Cancer
|
|
Kigamicin C is an anti-tumor antibiotic that selectively kills pancreatic cancer PANC-1 cells only in nutrient-poor conditions. Kigamicin C has antimicrobial activity against Gram-positive bacteria including methicillin-resistant Staphylococcus aureus (MRSA) [1].
|
-
-
- HY-123009
-
|
|
HIF/HIF Prolyl-Hydroxylase
Histone Acetyltransferase
|
Cancer
|
|
KCN1 is a p300/HIF-1α interaction inhibitor. KCN1 inhibits HIF transcriptional activity by binding to the CH1 domain of p300 and preventing the p300/HIF-1α assembly. KCN1 exerts antitumor activities through cell cycle arrest [1] .
|
-
-
- HY-12352A
-
|
|
STAT
Apoptosis
|
Cancer
|
|
HJC0416 hydrochloride is a potent and orally active STAT3 inhibitor with an enhanced anticancer profile than Stattic (HY-13818). HJC0416 hydrochloride is a promising anti-cancer agent for breast cancer study [1].
|
-
-
- HY-B0190
-
|
|
Flavivirus
TNF Receptor
NF-κB
Apoptosis
Ser/Thr Protease
|
Infection
Cancer
|
|
Nafamostat, an anticoagulant, is a synthetic serine protease inhibitor. Nafamostat has anticancer and antivirus effect. Nafamostat induce apoptosis by up-regulating the expression of tumor necrosis factor receptor-1 (TNFR1). Nafamostat can be used in the development of the pathological thickening of the arterial wall [1] .
|
-
-
- HY-175225
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
PROTAC BRD4 Degrader-37 (Compound TrimTAC-2) is a PROTAC BRD4 degrader. PROTAC BRD4 Degrader-37 has a DC50 of 36.4 nM and a Dmax of 73% in PANC-1 cells. PROTAC BRD4 Degrader-37 exhibits cytotoxicity against PANC-1 cells (GI50: 0.282 μM). PROTAC BRD4 Degrader-37 can be used in the research of tumors. (Pink: PROTAC BRD4 ligand-4 (HY-175242); Blue + Black: E3 ligase ligand + linker (HY-175241)) [1].
|
-
-
- HY-P10847
-
|
|
Ras
|
Cancer
|
|
KS-58 is a KRpep-2d (HY-P3277) derivative. KS-58 is a K-Ras (G12D) inhibitory peptide that selectively binds K-Ras. KS-58 can enter cells and block intracellular Ras interaction with effector proteins. KS-58 inhibits the proliferation of tumor cells and has antitumor activity [1] .
|
-
-
- HY-113978R
-
-
-
- HY-P991370
-
|
|
STAT
|
Cancer
|
|
SBT-100 (His Tag) is a human monoclonal antibody (mAb) targeting STAT3. SBT-100 (His Tag) inhibits IL-6-mediated P-STAT3 nuclear translocation in HEp-2 and PANC-1 cells. SBT-100 (His Tag) has tumor growth inhibitory effects on MDA-MB-231 [1].
|
-
-
- HY-178461
-
|
|
Lactate Dehydrogenase
|
Cancer
|
|
LDHA-IN-10 (Compound HP19) is a Lactate Dehydrogenase-A (LDHA) inhibitor with an IC50 value of 5.2 μM. LDHA-IN-10 reduces lactate production and ATP levels, inhibiting the proliferation of pancreatic cancer cell line PANC-1. LDHA-IN-10 induces G1/S cell cycle arrest and promotes apoptosis. LDHA-IN-10 is promising for research of pancreatic ductal adenocarcinoma (PDAC) [1].
|
-
-
- HY-164895
-
|
|
PIN1
|
Cancer
|
|
PIN1 degrader-1 (Compound 158H9) is the inhibitor for proline cis trans isomerase (Pin1) with an IC50 of 21.5 nM. PIN1 degrader-1 forms covalent bond with Cys113 of Pin1, induces conformational changes in Pin1, reduces its stability, and leads to a proteasome-dependently degradation. PIN1 degrader-1 inhibits the cell viability of multi cancer cells, and can be used in cancer research [1].
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-
-
- HY-123781A
-
|
|
Hedgehog
|
Cancer
|
|
RUSKI-201 dihydrochloride is a potent and specific Hedgehog acyltransferase (Hhat) inhibitor with an IC50 of 0.20 μM. RUSKI-201 dihydrochloride is able to block Hh signaling from Shh overexpressing cells and inhibits Hh palmitoylation. RUSKI-201 dihydrochloride is potential Hhat chemical probe in cells and can used in studies of Hhat catalytic function [1].
|
-
-
- HY-157740
-
|
|
HDAC
|
Cancer
|
|
XSJ-10 is a HDAC inhibitor containing a RAS/RAF protein interfering unit, with IC50s of 0.05 and 0.04 μM in PANC-1 cells and HT-29 cells. XSJ-10 can effectively induce the apoptosis of cancer cells and suppress the tumor by strongly inhibiting the RAS-RAF-MEK-ERK signaling pathway and the acetylation level of HDAC3 [1].
|
-
-
- HY-151984
-
|
|
CDK
|
Cancer
|
|
CDK9-IN-22 is a potent CDK9 inhibitor with IC50s of 10.4, 876.2 nM for CDK9, CDK, respectively. CDK9-IN-22 induces apoptosis and cell cycle arrests at G2/M phase. CDK9-IN-22 decreases the expression of p-RNAPII (S2) and CDK9 protein. CDK9-IN-22 shows antiproliferative and aiti-tumor activity [1].
|
-
-
- HY-178211
-
|
|
Ras
MEK
ERK
Akt
|
Cancer
|
|
SHY-867 is a pan RAS inhibitor. SHY-867 effectively prevents the binding of K-Ras proteins and other members of the Ras superfamily of small GTPases with EC50 values of 0.5-3 μM. SHY-867 effectively inhibits the phosphorylation of MEK, ERK1/2, and AKT downstream of K-Ras. SHY-867 inhibits the formation of the Ras-GTP activity complex. SHY-867 can be used to the studies of pancreatic cancer and non-small cell lung cancer [1].
|
-
-
- HY-121259
-
|
Adriamycinol; DXR-OL
|
Endogenous Metabolite
|
Cardiovascular Disease
|
|
Doxorubicinol, a potent inhibitor of the cardiac sarcoplasmic reticulum calcium pump, inhibits systolic myocardial function in isolated heart muscle. Doxorubicinol inhibits tumor cell growth and has cardiotoxicity.
|
-
-
- HY-B0190AR
-
|
FUT-175 (Standard)
|
Flavivirus
TNF Receptor
NF-κB
Apoptosis
Ser/Thr Protease
Reference Standards
|
Infection
Cancer
|
|
Nafamostat (mesylate) (Standard) is the analytical standard of Nafamostat (mesylate). This product is intended for research and analytical applications. Nafamostat mesylate (FUT-175), an anticoagulant, is a synthetic serine protease inhibitor. Nafamostat mesylate has anticancer and antivirus effect. Nafamostat mesylate induce apoptosis by up-regulating the expression of tumor necrosis factor receptor-1 (TNFR1). Nafamostat mesylate can be used in the development of the pathological thickening of the arterial wall [1] .
|
-
-
- HY-173560
-
|
|
ATTECs
SHP2
Apoptosis
|
Cancer
|
|
SHP2 ATTEC degrader-1 is a SHP2 ATTEC degrader. SHP2 ATTEC degrader-1 has degradation rate of 83.31 at 1.0 μM for 24 h in the PANC-1 cell line. SHP2 ATTEC degrader-1 inhibits cell growth in vivo and in vitro. SHP2 ATTEC degrader-1 induces apoptosis and increases the expression of the epithelial marker ( E-cadherin), and reduces the expression of interstitial markers (such as N-cadherin, Vimentin) (Pink: LC3 ligand (HY-174085); Black :linker HY-140468; Blue: SHP2 ligand (HY-174084) [1].
|
-
-
- HY-175398
-
|
|
Glutathione S-transferase
|
Cancer
|
|
OZO-Cl is an OZO derivative. OZO-Cl has anti-cancer activity. OZO-Cl significantly decreases the intracellular glutathion S-transferase Pi (GST) activity. OZO-Cl exhibits cytotoxicity to cancer cell lines, with IC50s of 150 and 120 μmol/L in Panc-1 and K562 cells respectively [1].
|
-
-
- HY-P5291
-
|
Caerulein precursor fragment
|
Insulin Receptor
|
Metabolic Disease
|
|
CPF-7 (Caerulein precursor fragment) is an insulin-releasing peptide that stimulates the release of insulin. CPF-7 can induce epithelial-mesenchymal transition by upregulating Snai1 expression in PANC-1 ductal cells. CPF-7 also induces exocrine plasticity by upregulating Ngn3 expression. CPF-7 can be used in the research of type 2 diabetes [1] .
|
-
-
- HY-116497
-
|
|
FAK
|
Cancer
|
|
PH11 is a novel focal adhesion kinase (FAK) inhibitor that rapidly induces apoptosis in TRAIL-resistant PANC-1 cells when combined with TRAIL, but has no effect on normal human fibroblasts. The study found that PH11 downregulates c-FLIP through inhibition of FAK and phosphatidylinositol-3-kinase (PI3K)/AKT pathways, thereby restoring the TRAIL apoptotic pathway, suggesting that this combination therapy may provide an attractive therapeutic strategy for the safe and effective treatment of pancreatic cancer. PH11 selectively inhibits c-FLIP expression by modulating upstream signaling pathways and may represent an innovative therapeutic strategy. Although further work is needed to fully elucidate the mechanism of PH11-induced TRAIL sensitization, we believe that our results will provide a new approach to target c-FLIP without the risk of interfering with caspase-8 processing, which could potentially lead to TRAIL resistance. This study also suggests a role for the FAK/AKT signaling pathway in regulating c-FLIP expression in TRAIL-induced apoptosis, and this understanding will provide important clues to control the resistance mechanism to optimize the potential of TRAIL-based pancreatic cancer treatment.
|
-
-
- HY-163715
-
|
|
FAK
|
Cancer
|
|
Antitumor agent-165 (Compound 10l) is a potent focal adhesion kinase (FAK) inhibitor. Antitumor agent-165 exhibits effective antiproliferative activity against CAPAN-1, PANC-1, PATU-T, SUIT-2, BxPC-3, PDAC-3 and PANC-1 GR with IC50s in the range of 1.04-3.44 μM [1].
|
-
-
- HY-N1410R
-
|
|
Reference Standards
STAT
NF-κB
|
Cancer
|
|
Triacetylresveratrol, an acetylated analog of Resveratrol. Triacetylresveratrol decreases the phosphorylation of STAT3 and NF-κB in a dose- and time- dependent manner in PANC-1 and BxPC-3 cells. Anticancer effects [1].
|
-
-
- HY-155402
-
|
|
Caspase
Apoptosis
|
Others
|
|
Antiproliferative agent-42 (compound 7m) is a dihydrodipyrrolo compound. Antiproliferative agent-42 showed antiproliferative activity against Panc-1 cell line with an IC50 value of 12.54 μM [1].
|
-
-
- HY-168718
-
|
|
FAK
JAK
Aurora Kinase
PI3K
Akt
Apoptosis
|
Cancer
|
|
FAK-IN-22 (Compound 26) is an inhibitor of FAK, JAK3, and Aurora B, with IC50 values of 50.94 nM, 9.99 nM, and 0.49 nM, respectively, effectively inhibiting tumor occurrence and metastasis in pancreatic ductal adenocarcinoma (PDAC). FAK-IN-22 effectively inhibits the proliferation of PANC-1 cells, with an IC50 value of 0.15 μM. FAK-IN-22 induces apoptosis and G2/M phase arrest in PANC-1 cells by inhibiting the FAK/PI3K/Akt signaling pathway [1].
|
-
- HY-112666
-
|
FTS amide; Salirasib amide
|
Ras
|
Cancer
|
|
Farnesyl thiosalicylic acid amide (FTS-A) is an orally active derivative of farnesyl thiosalicylic acid (HY-14754). Farnesyl thiosalicylic acid amide reduces Ras-GTP levels and inhibits cell growth with IC50s of 20 and 10 μM for Panc-1 and U87 cells, respectively. Farnesyl thiosalicylic acid amide can be used for the research of cancer [1].
|
-
- HY-162366
-
|
|
Ras
|
Cancer
|
|
KRAS G12D inhibitor 20 (Compound 14) is a selective G12D KRAS inhibitor. KRAS G12D inhibitor 20 has antitumor activity [1].
|
-
- HY-167857
-
|
|
GLUT
|
Cancer
|
|
(Rac)-Glutipyran is a broad-spectrum GLUT inhibitor that targets both GLUT1 and GLUT3. (Rac)-Glutipyran inhibits glucose uptake and suppresses the growth of multiple cancer cells, significantly inhibiting PANC-1 cell growth (IC50=1.8 μM) and glucose uptake (IC50=0.13 μM) [1].
|
-
- HY-155020
-
|
|
Histone Methyltransferase
GLP Receptor
|
Cancer
|
|
Antitumor agent-101 is a selective covalent inhibitor of lysine methyltransferases G9a/GLP, with IC50s of 8.5 nM and 5.5 nM for G9a and GLP, respectively. Antitumor agent-101 shows antitumor efficacy in the PANC-1 xenograft model [1].
|
-
- HY-170429
-
|
|
PIN1
|
Cancer
|
|
BJP-07-017-3 is the inhibitor for proline cis trans isomerase (Pin1) with an IC50 of 9 nM. BJP-07-017-3 forms covalent bond with Cys113 of Pin1, induces conformational changes in Pin1, reduces its stability, and leads to a proteasome-dependently degradation [1].
|
-
- HY-146738
-
|
|
Akt
|
Cancer
|
|
GSD-11 is a potent and selective anti-austerity agent. GSD-11 inhibits the cell migration and colony formation of PANC-1 cells. GSD-11 inhibits the Akt/mTOR signaling pathway. GSD-11 has the potential for the research of pancreatic cancer[1].
|
-
- HY-155991
-
|
|
Apoptosis
|
Cancer
|
|
RUNX-IN-2 (Compound Conjugate 3) covalently binds to the RUNX-binding sequences, and inhibits the binding of RUNX proteins to their target sites. RUNX-IN-2 induces the p53-dependent apoptosis and inhibits cancer cell growth. RUNX-IN-2 inhibits tumor growth in PANC-1 xenograft mice. RUNX-IN-2 has high alkylation efficiency and specificity [1].
|
-
- HY-161751
-
|
|
GSK-3
|
Cancer
|
|
MJ34 is a potent inhibitor of GSK-3β and GSK-3α, with the IC50s of 15.4 nM and 31.5 nM, respectively. MJ34 plays an important role in cancer research [1]
|
-
- HY-169830
-
|
|
Drug Derivative
Apoptosis
|
Cancer
|
|
2-(Cyclohexylmethyl)-plumbagin is a derivative of the naphthoquinone compound Plumbagin (HY-N1497). Under nutrient-deprived conditions, 2-(Cyclohexylmethyl)-plumbagin selectively exhibits cytotoxicity against PANC-1 human pancreatic cancer cells (PC50 = 0.11 µM) and reduces the phosphorylation of Akt and mTOR in PANC-1 cells. 2-(Cyclohexylmethyl)-plumbagin also induces apoptosis (Apoptosis) in PANC-1 cells at a concentration of 1 µM. Additionally, 2-(Cyclohexylmethyl)-plumbagin reduces tumor volume and weight in a xenograft MiaPaCa-2 pancreatic cancer mouse model [1].
|
-
- HY-147838
-
|
|
NAMPT
|
Cancer
|
|
Nampt-IN-9 (Compound 8) is a potent NAMPT inhibitor with anticancer activities. Nampt-IN-9 can be used for pancreatic ductal adenocarcinoma research [1].
|
-
- HY-178194
-
|
|
Ras
MEK
ERK
Akt
|
Cancer
|
|
SHY-855 is a pan RAS inhibitor. SHY-855 effectively prevents the binding of K-Ras proteins and other members of the Ras superfamily of small GTPases with IC50 values of 0.3-5 μM. SHY-855 effectively inhibits the phosphorylation of MEK, ERK1/2, and AKT downstream of K-Ras. SHY-855 inhibits the formation of the Ras-GTP activity complex. SHY-855 can be used to the studies of pancreatic cancer and non-small cell lung cancer [1].
|
-
- HY-N12834
-
|
|
Others
|
Inflammation/Immunology
Cancer
|
|
Ecdysoside B (compound 6b) is a pregnanoside compound isolated from the plant Ecdysanthera rosea. Ecdysoside B and its derivatives and isomers shows anticancer, immunosuppressive and anti-inflammatory activities. Ecdysoside B shows cytotoxicity to a variety of human tumor cell lines, including PANC-1 (human pancreatic cancer cells), A375 (human melanoma cells) and U87 (brain glioma U87 cells). Ecdysoside B can be used for research in the areas of cancer, immunomodulation and anti-inflammato [1].
|
-
- HY-135453
-
|
|
Bacterial
|
Infection
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|
(-)-Pinocembrin exhibits anti-mycobacterium activity against mycobacteriuum tuberculosis H37Ra with an IC50 value of 1.11 mg/mL in dormant phase and 1.21 mg/mL in active phase, respectively. (-)-Pinocembrin has potent antiproliferative activity with IC50 values of 1.88-11.00 mg/mL against THP-1, A549, Panc-1, HeLa and MCF7 cell lines [1].
|
-
- HY-110335A
-
|
|
ROCK
|
Cancer
|
|
OXA-06 is a pharmacologic inhibitor of ROCK, possessing antitumor activity by impairing cell migration and MYPT1 phosphorylation in PANC-1 cells.
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-
- HY-139248
-
|
|
Drug Derivative
|
Cancer
|
|
Paclitaxel octadecanedioate (compound PTX-FA18) is comprised of Paclitaxel (HY-B0015) conjugated to 1,18-octadecanedioic acid (HY-W005178). Paclitaxel octadecanedioate mixed with human serum albumin (HAS) is cytotoxic to HT-1080, PANC-1, HT-29 and Hela cells (IC50s = 12, 2.48, 8.62, and 64.42 nM, respectively) [1].
|
-
- HY-N8034
-
|
|
Apoptosis
Autophagy
|
Cancer
|
|
Glychionide A is a flavonoside that can be found in the roots of Glychirriza glabra. Glychionide A promotes apoptosis and autophagy of PANC-1 pancreatic cancer cells. Glychionide A can be used for the research of cancer [1] .
|
-
- HY-173477
-
|
|
Apoptosis
|
Cancer
|
|
JR5-26B is an orally active apoptosis inducer. JR5-26B induces cell death through copper-mediated apoptosis and necroptosis. JR5-26B exhibits antiproliferative activity on MIA PaCa-2, PANC-1, PAN02, SU.86.86, and KPC-2 cells with IC50s of 0.6, 4.4, 8.0, 1.1, and 3.4μM, respectively [1].
|
-
- HY-169006
-
|
|
Apoptosis
PKC
|
Cancer
|
|
Evo312 is a dose-dependent inhibitor of protein kinase CβⅠ (PKCβⅠ) (IC50 is 117.34 nM). Evo312 induces PANC-GR (acquired gemcitabine-resistant PC cells) cell cycle arrest and apoptosis by inhibiting PKCβ1 protein expression. Evo312 has antiproliferative effects in pancreatic cancer cells PANC-1 and PANC-GR cells with IC50 of 0.08 μM and 0.07 μM, and in human normal pancreatic ductal epithelial cells HPDE6-c7 with IC50 of 2.95 μM. Evo312 exhibits antitumor activity in a PANC-GR cell transplantation mouse model [1].
|
-
- HY-179140
-
|
|
EGFR
VEGFR
Apoptosis
|
Cancer
|
|
EGFR/VEGFR2-IN-8 (compound 10k) is a dual EGFR/VEGFR-2 inhibitor (EGFR IC50 = 57 nM, VEGFR-2 IC50 = 21 nM). EGFR/VEGFR2-IN-8 has anti proliferative activity against various tumor cells, such as MCF-7 (IC50 = 20 nM), Panc-1 (IC50 = 22 nM), A-549 (IC50 = 23 nM), HT-29 (IC50 = 23 nM) cells. EGFR/VEGFR2-IN-8 has antioxidant and apoptosis inducing activity. EGFR/VEGFR2-IN-8 can be used for research on various types of cancer [1].
|
-
- HY-161858
-
|
|
PI3K
Akt
Apoptosis
|
Cancer
|
|
EpskA21 is an inhibitor for PI3K/AKT signaling pathway, and inhibits the proliferation of cancer cells MCF-7, A549, MIA-PaCa-2, Panc-1 and HepG2, with IC50 of 1.3-7.24 μM. EpskA21 inhibits the cell migration, arrests the cell cycle at G2/M (MCF-7) and S (MIA-PaCa-2) phase, and induces apoptosis in MCF-7 and MIA-PaCa-2. EpskA21 causes the mitochondrial dysfunction [1].
|
-
- HY-161859
-
|
|
VEGFR
STAT
|
Cancer
|
|
VEGFR-2/STAT-3-IN-1 (Compound 9f) is a dual inhibitor for VEGFR-2 (IC50=26.3 nM) and STAT-3 (IC50=5.63 nM). VEGFR-2/STAT-3-IN-1 inhibits the proliferation of cancer cells PANC1 and PC3 with IC50 of 0.14 and 0.10 µM. VEGFR-2/STAT-3-IN-1 induces apoptosis in PC3 [1].
|
-
- HY-158726
-
|
|
Fluorescent Dye
Apoptosis
|
Cancer
|
|
Complex 3 is a fluorescent dithiocarbazate-copper complex with anticancer activity, which localizes to mitochondria. Complex 3 displays excitation/emission maxima of 455-495/535 nm, respectively. Complex 3 inhibits the growth of BxPC-3, AsPC-1, PANC-1, and WI38 pancreatic cancer cells with IC50 values of 0.74, 0.41, 0.62, and 2.06 µM, respectively. Complex 3 induces lipid peroxidation and mitochondrial rupture and shrinkage in AsPC-1 cells. Complex 3 also induces mitochondrial apoptosis and cytokine-cytokine receptor interaction dysfunction in AsPC-1 cells. Complex 3 reduces tumor volume in an AsPC-1 mouse xenograft model [1].
|
-
- HY-160061
-
|
|
Biochemical Assay Reagents
|
Cancer
|
|
P12FR2 aptamer sodium is a 2'-fluoropyrimidine-modified RNA aptamer targeting human PAUF with an estimated apparent KD of 77 nM. P12FR2 aptamer sodium inhibits PAUF-induced migration of PANC-1 (human pancreatic cancer cells) in wound healing assays and suppresses tumor growth in a mouse CFPAC-1 pancreatic cancer model [1].
|
-
- HY-167857S
-
|
|
Isotope-Labeled Compounds
GLUT
|
Cancer
|
|
Glutathione Disulfide- 13C4, 15N2 is the 13C- and 15N-labeled (Rac)-Glutipyran (HY-167857). (Rac)-Glutipyran is a broad-spectrum GLUT inhibitor that targets both GLUT1 and GLUT3. (Rac)-Glutipyran inhibits glucose uptake and suppresses the growth of multiple cancer cells, significantly inhibiting PANC-1 cell growth (IC50=1.8 μM) and glucose uptake (IC50=0.13 μM) [1].
|
-
- HY-N8270
-
|
|
Hedgehog
Endogenous Metabolite
|
Cancer
|
|
Physalin H is a natural product that can be isolated from Solanum nigrum. Physalin H is an inhibitor of Hedgehog (Hh) signaling and it disrupts GLI1-DNA-complex formation. Physalin H inhibits GLI1 transcription with an IC50 value of 0.7 μM. Physalin H shows cytotoxicity to PANC1 and DU145 cells with IC50 values of 5.7 and 6.8 μM, respectively [1].
|
-
- HY-159577
-
|
|
PI3K
mTOR
Akt
|
Cancer
|
|
Nic-15 (compound 4n) is an anti-constrictive agent used to antagonize the hypovascularity of pancreatic tumors. The hypovascularity allows cancer cells to adapt to the nutrient-deficient tumor microenvironment and develop drug resistance. Nic-15 can regulate the PI3K/Akt/mTOR pathway and alleviate ER stress induced by Gemcitabine (HY-17026). Nic-15 can significantly inhibit the migration and colony formation of MIA PaCa-2 and PANC-1 pancreatic cancer cells. The combination of Nic-15 and Gemcitabine can effectively solve the problem of pancreatic tumor resistance. In an in vivo xenograft model, Nic-15 can significantly enhance the efficacy of Gemcitabine [1].
|
-
- HY-147825
-
|
|
EGFR
Raf
Apoptosis
|
Cancer
|
|
EGFR/BRAFV600E-IN-1 (Compound 23) is a potent EGFR and BRAF V600E dual inhibitor with IC50s of 0.08 and 0.15 µM, respectively. EGFR/BRAFV600E-IN-1 induces apoptosis and cell cycle arrest in both pre-G1 and G2/M phases. EGFR/BRAFV600E-IN-1 exhibits antiproliferative activity againist A-549, MCF-7, Panc-1, HT-29 with IC50s of 1.2, 0.79, 1.3, and 1.23 µM, respectively [1].
|
-
- HY-158328A
-
-
- HY-123597
-
|
DDUG; NCI C04808
|
Autophagy
Checkpoint Kinase (Chk)
|
Cancer
|
|
NSC 109555 is an ATP-competitive inhibitor of checkpoint kinase 2 (Chk2; IC50=200 nM in a cell-free kinase assay). It is selective for Chk2 over Chk1 and 16 kinases in a panel but does inhibit Brk, c-Met, IGFR, and LCK with IC50 values of 210, 6,000, 7,400, and 7,100 nM, respectively. NSC 109555 inhibits Chk2 autophosphorylation and phosphorylation of the Chk2 substrate histone H1 in vitro (IC50=240 nM). It inhibits the growth of, and induces autophagy in, L1210 leukemia cells in vitro.2 NSC 109555 (1,250 nM) potentiates gemcitabine-induced cytotoxicity in MIA PaCa-2, CFPAC-1, PANC-1, and BxPC-3 pancreatic cancer cells, as well as reduces gemcitabine-induced increases in Chk2 phosphorylation and enhances gemcitabine-induced production of reactive oxygen species (ROS) in MIA PaCa-2 cells.
|
-
- HY-169413
-
|
|
Akt
|
Cancer
|
|
AKT-IN-25 (Compound 14a) is an inhibitor for Akt, that inhibits the phosphorylation of Akt, and thereby inhibits the PI3K/Akt/mTOR signaling pathway. AKT-IN-25 arrests the cell cycle at G1 phase, inhibits the cell migration of PANC-1, and inhibits the proliferation of cancer cells PANC-1, PATU-T, and SUIT-2 with IC50s of 3.05, 1.32, and 3.85 μM, respectively [1].
|
-
- HY-N12989
-
|
|
Others
|
Others
|
|
3′-O-Demethylarctigenin is a phenolic compound that can be isolated from the seeds of Arctium lappa. 3′-O-Demethylarctigenin shows cytotoxicity for PANC-1 cells with an IC50 value of 4.38 µM [1].
|
-
- HY-149092
-
|
|
TAM Receptor
|
Cancer
|
|
Anticancer agent 109 (compound 6-15) is an inhibitor of the Gas6-Axl axis with anti-cancer activity. Anticancer agent 109 inhibits the expression of Gas6 and Axl, and the expression p-PI3K and p-AKT in cancer cells, leads to G1 phase arrest and promotes cancer cells apoptosis, and inhibits tumor growth significantly in nude mouse tumor bearing models [1].
|
-
- HY-123752
-
|
|
Hedgehog
Smo
|
Cancer
|
|
MS-0022 is a Smoothened (SMO) antagonist. MS-0022 can inhibit the Hedgehog (Hh) signaling pathway. MS-0022 can be used in anti-tumor research [1].
|
-
- HY-170313
-
|
|
GLUT
Apoptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
GLUT-1-IN-4 (Compound 13) is the p53 protein-dependent inhibitor for GLUT-1 glucose transporter. GLUT-1-IN-4 inhibits the proliferation of multiple cancer cells with IC50 in submicromolar levels. GLUT-1-IN-4 arrests the cell cycle, stimulates oxidative stress, and induces apoptosis [1].
|
-
- HY-168919
-
|
|
Ras
Apoptosis
p38 MAPK
PI3K
mTOR
|
Cancer
|
|
KRASG12C IN-16 (Compound SK-17) is a selective, covalent and an orally active KRAS G12C inhibitor. KRASG12C IN-16 induces Apoptosis. KRASG12C IN-16 effectively prevents the activation of MAPK and PI3K/mTOR signaling pathways. KRASG12C IN-16 displays anti-tumor activity against pancreatic cancer [1].
|
-
- 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 [1].
|
-
- HY-172210
-
|
|
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
|
DDO-8958 is an orally active and selective BET BD1 inhibitor with a KD of 5.6 nM for BRD4 BD1. DDO-8958 exhibits low nanomolar inhibitory activity against all BET BD1 bromodomains except for BRDT BD1. DDO-8958 can inhibit the proliferation and migration, induce apoptosis and cell cycle arrest of tumor cells. DDO-8958 has anti-tumor activity [1].
|
-
- HY-N13063
-
|
|
Apoptosis
Reactive Oxygen Species (ROS)
PI3K
Akt
|
Cancer
|
|
Anticancer agent 235 (Compound 49) is a modulator for PI3K/AKT/mTOR pathway, that promotes the generation of ROS, reduces the mitochondrial membrane potential, and thereby inhibits the proliferation of cancer cells HCT116, Caco-2, AGS and SMMC-772 with IC50 of 0.35-26.9 μM. Anticancer agent 235 arrests the cell cycle at G2/M phase, and induces apoptosis in HCT116 [1].
|
-
- HY-123781
-
|
|
Hedgehog
|
Cancer
|
|
RUSKI-201 is a potent and specific Hedgehog acyltransferase (Hhat) inhibitor, with an IC50 of 0.20 μM. RUSKI-201 is able to block Hh signaling from Shh overexpressing cells and inhibits Hh palmitoylation. RUSKI-201 is potential Hhat chemical probe in cells and can used in studies of Hhat catalytic function [1].
|
-
- HY-173164
-
|
|
EGFR
Raf
Apoptosis
|
Cancer
|
|
EGFR/BRAFV600E-IN-4 (Compound 10f) is a dual EGFR and BRAF V600E inhibitor with IC50 values of 61 nM and 43 nM, respectively. EGFR/BRAFV600E-IN-4 arrests cell cycle, induces apoptosis in both early and late stages and inhibits cancer cells growth in vitro, and has a broad anticancer activity [1].
|
-
- HY-147915
-
|
|
Carboxylesterase (CES)
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Benz-AP is a potent photosensitizer. Benz-AP produces singlet oxygen, with a negative correlation with hCES2 (Human carboxylesterase 2) activity. Benz-AP displays a higher photocytotoxicity potency in cancer cells under low hCES2 environments. Upon TPE (Two-photon excitation), Benz-AP produces ROS and kills cancer cells and tumor spheroids [1].
|
-
- HY-149076
-
|
|
Drug Derivative
|
Cancer
|
|
hGAPDH-IN-1, a 3-bromo-4,5-dihydroisoxazole derivative, is a specific and potent hGAPDH covalent inhibitor. hGAPDH-IN-1 reduces cancer cell growth in different pancreatic cancer cell lines.
|
-
- HY-116107
-
|
|
Necroptosis
|
Cancer
|
|
AG311 is an anticancer and antimetastatic agent. AG311 induces rapid necrosis in numerous cancer cell lines [1].
|
-
- HY-162627
-
|
|
Lactate Dehydrogenase
|
Cancer
|
|
LDHA-IN-6 (compound 6) is an oral bioactive inhibitor of lactate dehydrogenase-A (LDHA), with the IC50 of 46 nM. LDHA-IN-6 has antitumor activity [1].
|
-
- HY-172177
-
|
|
Apoptosis
HDAC
ROCK
|
Cancer
|
|
ROCK/HDAC-IN-2 (Compound C-9) is a ROCK/HDAC inhibitor, with IC50 values of 0.185 µM, 0.8 µM, and 0.7 µM for HDAC6, ROCK1, and ROCK2, respectively. ROCK/HDAC-IN-2 can induce apoptosis and changes in mitochondrial membrane potential in cancer cells, demonstrating significant antitumor activity. ROCK/HDAC-IN-2 can be used in the research of pancreatic ductal adenocarcinoma (PDAC) and triple-negative breast cancer (TNBC) [1].
|
-
- HY-12440
-
|
|
IAP
Apoptosis
|
Cancer
|
|
HM90822 is an orally active IAP antagonist. HM90822 induces ubiquitination and proteasome-dependent degradation of XIAP, cIAP1 and cIAP2 in sensitive pancreatic cancer cells. HM90822 induces Apoptotic cell death. HM90822 inhibits tumor growth in Panc-1 pancreatic cancer xenograft and orthotopic mouse models. HM90822 can be used for the research of pancreatic cancer [1].
|
-
- HY-172748
-
|
|
Drug Derivative
|
Neurological Disease
Cancer
|
|
9β-Hydroxyhexahydrocannabinol is a synthetic cannabinoid derivative. 9β-Hydroxyhexahydrocannabinol exhibits cytotoxicity against various tumor cell lines, such as HCT-116, MCF-7, K562, MIAPaCa-2, PANC-1, A549, PC-3 and SW-620, with IC50 values ranging from 15.23 to 33.74 μM. 9β-Hydroxyhexahydrocannabinol can be used in the study of cancer [1].
|
-
- HY-N16695
-
|
|
Others
|
Others
|
|
(2S,3S)-Pterosin S 14-O-glucoside is a sesquiterpene glycoside compound that can be isolated from the fern Pteris multifida. (2S,3S)-Pterosin S 14-O-glucoside showed no significant cytotoxicity against A549 (human lung adenocarcinoma), LOVO (colon adenocarcinoma), PANC-1 (human pancreatic cancer), and NCI-H446 (human small cell lung cancer) cell lines (IC50 > 100 μM) [1].
|
-
- HY-N13835
-
-
- HY-182749
-
|
|
Ras
Akt
Raf
ERK
|
Cancer
|
|
KRAS-IN-58 is a KRAS inhibitor with a IC50 of 0.223 μM against KRAS G12D. KRAS-IN-58 binds to KRAS G12C and KRAS G12D proteins, and reduces the levels of phosphorylated Raf1, AKT and ERK in pancreatic cancer cells. KRAS-IN-58 can be used for the research of pancreatic cancer [1].
|
-
- HY-B0190B
-
|
|
Flavivirus
TNF Receptor
NF-κB
Apoptosis
Ser/Thr Protease
|
Infection
Cancer
|
|
Nafamostat hydrochloride, an anticoagulant, is a synthetic serine protease inhibitor. Nafamostat hydrochloride has anticancer and antivirus effect. Nafamostat hydrochloride induces apoptosis by up-regulating the expression of tumor necrosis factor receptor-1 (TNFR1). Nafamostat hydrochloride can be used in the development of the pathological thickening of the arterial wall [1] .
|
-
- HY-150287A
-
|
ITS-X
|
Biochemical Assay Reagents
|
Others
|
|
Insulin-Transferrin-Selenium-Ethanolamine (ITS-X) is a cell culture supplement as well as a cell growth and adhesion promoter. Insulin-Transferrin-Selenium-Ethanolamine supports adhesion, pseudopodium formation, pseudopodium elongation and proliferation of adherent cancer cells in serum-free culture systems [1].
|
-
- HY-186198
-
|
Salirasib methoxymethyl ester
|
Ras
|
Others
|
|
FTS-MOM (Salirasib methoxymethyl ester), a Salirasib (FTS) (HY-14754) derivative, is a selective Rap1 inhibitor with selectivity over Ras. FTS-MOM inhibits GTP loading of Rap1 in quiescent and activated T cells. FTS-MOM inhibits Rap1-dependent T cell adhesion to ICAM-1 [1].
|
-
- HY-114243
-
|
|
NF-κB
JNK
Caspase
Apoptosis
|
Neurological Disease
Cancer
|
|
DpC is a selective, orally active iron chelator with anticancer activity. DpC acts on signaling pathway-related targets such as JNK, NF-κB, and its activity is competitively inhibited by another iron chelator Dp44mT (HY-18973). By chelating intracellular iron and copper ions in tumor cells to form redox-active complexes, DpC induces oxidative stress, activates the JNK, NF-κB pathways and downregulates IκBα, upregulates the expressions of neuroglobin and cytoglobin, activates caspase 3/9 to induce tumor cell apoptosis. It also overcomes P-glycoprotein-mediated multidrug resistance through a lysosome-targeting mechanism, and exhibits broad-spectrum synergistic effects when combined with various chemotherapeutic agents. DpC inhibits tumor metastasis and increases TNF-α levels in the tumor microenvironment to enhance endogenous immune responses. DpC is applicable to the research of various malignancies including neuroblastoma, pancreatic cancer, prostate cancer, lung cancer, and breast cancer [1] .
|
-
- HY-163468
-
|
|
Src
|
Cancer
|
|
SRC-3-IN-1 (compound SI-10) is a steroid receptor coactivator 3 (SRC-3) inhibitor (IC50=3.3 μM). SRC-3-IN-1 has good water solubility, oral bioavailability, and improved selectivity profile. SRC-3-IN-1 can be used in prostate cancer research [1].
|
-
- HY-179614
-
|
|
PARP
DNA/RNA Synthesis
Apoptosis
CDK
Bcl-2 Family
|
Cancer
|
|
PARP1-IN-50 is a selective and orally active PARP-1 inhibitor with an IC50 of 64.98 nM. PARP1-IN-50 can inhibit PAR formation and induce DNA double strand breaks, thereby causing DNA damage. PARP1-IN-50 can induce G2/M phase arrest and cancer cells apoptosis. PARP1-IN-50 demonstrates significant antiproliferative activity against various cancer cells. PARP1-IN-50 can be used for the research of cancer, such as breast cancer [1].
|
-
- HY-179484
-
|
|
Reactive Oxygen Species (ROS)
ERK
|
Cancer
|
|
KRASG12C IN-19 is a selective and orally active KRAS G12C inhibitor. KRASG12C IN-19 exerts potent antiproliferative activity against the KRAS G12C-mutant non small cell lung cancer (NSCLC) cell line H358 with an IC50 of 7.6 nM, and effectively suppresses downstream ERK phosphorylation (IC50 = 24.06 nM). KRASG12C IN 19 has no significant inhibitory activity against KRAS G12V and KRAS G12D-mutant cancer cells (PANC 1, Panc, AsPC 1, and GP2d cells) with IC50 > 10,000 nM. KRASG12C IN-19 rapidly forms a covalent bond with KRAS G12V-GDP, leading to dose-dependent inhibition of the downstream KRAS pathway. KRASG12C IN 19 can be employed for research in KRAS G12C driven cancers, including non small cell lung cancer, pancreatic cancer, and colorectal cancer [1].
|
-
- HY-170430
-
|
|
Molecular Glues
E1/E2/E3 Enzyme
|
Cancer
|
|
HGC652 is a molecular glue degrader targeting TRIM21 with a TRIM21-dependent nuclear membrane disruption effect. HGC652 binds to the PRY-SPRY domain of TRIM21 with high affinity (Ka=0.061 μM), mediates the interaction between TRIM21 and NUP98, and redirects E3 ligase activity. By triggering the polyubiquitination and proteasomal degradation of nucleoporins (such as NUP155 and GLE1), HGC652 disrupts nuclear membrane integrity, alters nuclear morphology, induces genomic instability, and thereby induces cancer cell death [1] .
|
-
- HY-183123
-
|
|
FAK
EGFR
|
Cancer
|
|
EGFR T790M/FAK-IN-1 is a dual inhibitor of EGFR T790M and FAK, with an IC50 of 99.1 nM against EGFR T790M and an IC50 of 117.7 nM against FAK. EGFR T790M/FAK-IN-1 can be used for research on pancreatic cancer, drug-resistant breast cancer, and drug-resistant lung cancer [1].
|
-
- HY-123611
-
|
RX-5902
|
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
Supinoxin (RX-5902) is an orally active inhibitor of phosphorylated-p68 RNA helicase (P-p68) and a potent first-in-class anti-cancer agent. Supinoxin interacts with Y593 phosphorylated-p68 and attenuates the nuclear shuttling of β-catenin. Supinoxin induces cell apoptosis and inhibits growth of TNBC cancer cell lines with IC50s ranging from 10 nM to 20 nM [1] .
|
-
- HY-B1619R
-
|
Cromoglycate (Standard); Cromoglicic acid (Standard); FPL-670 free acid (Standard)
|
GSK-3
NF-κB
Amyloid-β
Reference Standards
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Cromolyn (Standard) is the analytical standard of Cromolyn. This product is intended for research and analytical applications. Cromolyn (Cromoglycate) is an orally active GSK-3β inhibitor with an IC50 of 2.0 μM. Cromolyn is also a mast cell stabilizer that can inhibit the release of mediators from mast cells, regulate reflex bronchoconstriction, and reduce non-specific bronchial hyperreactivity, and Cromolyn can be used in the research of bronchial asthma. In addition, Cromolyn has multiple activities such as anti-inflammatory, anti-allergic, anti-histamine, anti-cancer, and neuroprotective effects [1] .
|
-
- HY-119264
-
|
|
Molecular Glues
Ras
Apoptosis
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
PRLX-93936 is a molecular Glues that binds to and reprograms the TRIM21 ubiquitin ligase to degrade nuclear pore complexes. PRLX-93936 binds to TRIM21, forms a ternary complex with TRIM21 and NUP98, and mediates the ubiquitination and proteasomal degradation of NUP98 and other nuclear pore complex proteins. PRLX-93936 induces the loss of short-lived cytoplasmic mRNA transcripts, triggers cancer cell apoptosis (Apoptosis), and inhibits the activated Ras pathway. PRLX-93936 inhibits HIF-1 under hypoxic conditions (IC50 = 0.09 μM in cell-based reporter gene assay). PRLX-93936 suppresses tumor growth in mouse models and improves survival rates in mouse models of multiple myeloma. PRLX-93936 is applicable to research related to pancreatic cancer and multiple myeloma [1] .
|
-
- HY-157135
-
|
|
Carbonic Anhydrase
|
Cancer
|
|
hCAIX-IN-19 is a sulfonamides inhibitor against hCA IX with an inhibition constant (KI ) of 6.2 nM and show good selectivity over hCA I (hCA I/ hCA IX = 117) [1].
|
-
- HY-B0320A
-
|
Cromoglycate disodium; Cromoglicic acid disodium; FPL-670
|
GSK-3
NF-κB
Amyloid-β
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Cromolyn (Cromoglycate) disodium is an orally active GSK-3β inhibitor with an IC50 of 2.0 μM. Cromolyn disodium is also a mast cell stabilizer that can inhibit the release of mediators from mast cells, regulate reflex bronchoconstriction, and reduce non-specific bronchial hyperreactivity, and Cromolyn disodium can be used in the research of bronchial asthma. In addition, Cromolyn disodium has multiple activities such as anti-inflammatory, anti-allergic, anti-histamine, anti-cancer, and neuroprotective effects [1] .
|
-
- HY-B1619
-
|
Cromoglycate; Cromoglicic acid; FPL-670 free acid
|
GSK-3
NF-κB
Amyloid-β
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Cromolyn (Cromoglycate) is an orally active GSK-3β inhibitor with an IC50 of 2.0 μM. Cromolyn is also a mast cell stabilizer that can inhibit the release of mediators from mast cells, regulate reflex bronchoconstriction, and reduce non-specific bronchial hyperreactivity, and Cromolyn can be used in the research of bronchial asthma. In addition, Cromolyn has multiple activities such as anti-inflammatory, anti-allergic, anti-histamine, anti-cancer, and neuroprotective effects [1] .
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- HY-119264A
-
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Molecular Glues
Apoptosis
Ras
HIF/HIF Prolyl-Hydroxylase
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Cancer
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PRLX-93936 dihydrochloride is a molecular Glues that binds to and reprograms the TRIM21 ubiquitin ligase to degrade nuclear pore complexes. PRLX-93936 dihydrochloride binds to TRIM21, forms a ternary complex with TRIM21 and NUP98, and mediates the ubiquitination and proteasomal degradation of NUP98 and other nuclear pore complex proteins. PRLX-93936 dihydrochloride induces the loss of short-lived cytoplasmic mRNA transcripts, triggers cancer cell apoptosis (Apoptosis), and inhibits the activated Ras pathway. PRLX-93936 dihydrochloride inhibits HIF-1 under hypoxic conditions (IC50 = 0.09 μM in cell-based reporter gene assay). PRLX-93936 dihydrochloride suppresses tumor growth in mouse models and improves survival rates in mouse models of multiple myeloma. PRLX-93936 dihydrochloride is applicable to research related to pancreatic cancer and multiple myeloma [1] .
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- HY-150753
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-
- HY-183791A
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- HY-163507
-
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Anaplastic lymphoma kinase (ALK)
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Cancer
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ALK5-IN-79 (compound 57) is an ALK inhibitor with anticancer activity, by blocking TGF-β1/SMAD signaling pathway. ALK5-IN-79 attenuates the production of extracellular matrix (ECM) and deposition of collagen. ALK5-IN-79 exhibits adequate pharmacokinetic (PK) properties and good in vivo tolerance.
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- HY-183120
-
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FAK
EGFR
Apoptosis
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Cancer
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EGFR T790M/FAK-IN-2 is an orally active dual FAK and EGFR T790M kinase inhibitor, with an IC50 of 1.03 nM against FAK and an IC50 of 3.89 nM against EGFR T790M. EGFR T790M/FAK-IN-2 exerts antiproliferative effects in drug-resistant cancer cells overexpressing FAK, inducing apoptosis and cell cycle arrest. EGFR T790M/FAK-IN-2 exhibits antitumor activity in a pancreatic cancer xenograft mouse model. EGFR T790M/FAK-IN-2 can be used for the research of pancreatic cancer, breast cancer and non-small cell lung cancer [1].
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- HY-153863
-
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PROTACs
MEK
Raf
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Cancer
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MS934 is a novel improved VHL-recruiting MEK 1/2 PROTAC degrader. MS934 also degrades CRAF. MS934 can be used for the research of variety of human cancers, such as melanoma, nonsmall cell lung cancer (NSCLC), colorectal cancer, primary brain tumors, and hepatocellular carcinoma (Pink: Target protein ligand (HY-168288); Black: linker (HY-168289); Blue: E3 ligase ligand (HY-112078)) [1] .
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- HY-120825
-
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Apoptosis
DNA/RNA Synthesis
Reactive Oxygen Species (ROS)
Keap1-Nrf2
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Cancer
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QD 232 is a quinazolinedione-based ROS inducer and an apoptosis inducer with cytotoxicity and redox regulatory activity. QD 232 promotes ROS accumulation, activates the NRF2-mediated oxidative stress response and unfolded protein response pathways, and upregulates downstream antioxidant and stress response genes. QD 232 inhibits mtDNA transcription driven by HSP2 and LSP promoters, and impairs mitochondrial oxidative phosphorylation function. QD 232 induces apoptosis of pancreatic ductal adenocarcinoma cells and exerts cytotoxicity against gemcitabine (HY-17026)-resistant pancreatic ductal adenocarcinoma cells. QD 232 delays tumor growth in a mouse pancreatic cancer xenograft model [1].
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- HY-175673
-
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Carnitine Palmitoyltransferase (CPT)
Apoptosis
Oxidative Phosphorylation
Mitochondrial Metabolism
Reactive Oxygen Species (ROS)
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Cancer
|
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LCB-2151 (Compound 2), a nucleoside analogue, is an anticancer agent. LCB-2151 disrupts the two primary sources of ATP production (glycolysis and mitochondrial oxidative phosphorylation), reducing the bioenergetic capacity of KRAS-mutated pancreatic cancer cells and inducing ROS formation. LCB-2151 effectively inhibits key enzymes (such as CACT and CPT2) in glycolysis, the TCA cycle and fatty acid β-oxidation. LCB-2151 has significant cytotoxicity and induces cells apoptosis. LCB-2151 can be used for radiation therapy of cancers research [1].
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- HY-181660
-
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PROTACs
IKK
Apoptosis
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Cancer
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PROTAC IKKβ degrader-1 is a IKKβ PROTAC degrader (DC50 = 7.15 μM). PROTAC IKKβ degrader-1 induces apoptosis (Apoptosis) in triple-negative breast cancer cells. PROTAC IKKβ degrader-1 induces G1 phase cell cycle arrest in triple-negative breast cancer cells. PROTAC IKKβ degrader-1 exhibits antiproliferative activity against a variety of cells. PROTAC IKKβ degrader-1 is applicable for research related to cancers such as triple-negative breast cancer, colon cancer, liver cancer, pancreatic cancer [1].
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- HY-172209
-
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p38 MAPK
Apoptosis
Reactive Oxygen Species (ROS)
Caspase
Bcl-2 Family
|
Cancer
|
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PPIA-IN-1 is a PPIA inhibitor with a Kd value of 0.52 μM. PPIA-IN-1 inhibits the PPIA/MAPK signaling pathway to exert antiproliferative activity. PPIA-IN-1 induces G0/G1 cell cycle arrest in cancer cells. PPIA-IN-1 upregulates the expression of Bax and caspase-3, downregulates Bcl-2 expression, and induces apoptosis in cancer cells. PPIA-IN-1 induces increased ROS levels, DNA damage, endoplasmic reticulum stress, and mitochondrial dysfunction in cancer cells. PPIA-IN-1 exhibits antitumor activity in a mouse colon cancer xenograft model. PPIA-IN-1 can be used for the research of colorectal cancer [1].
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- HY-183786
-
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NF-κB
Fluorescent Dye
Drug Derivative
Autophagy
|
Cancer
|
|
Anticancer agent 327, a fluorescent Andrographolide (HY-N0191) derivative, is an NF-κB p50 inhibitor. Anticancer agent 327 covalently binds to the p50 subunit of NF-κB. Anticancer agent 327 reduces levels of multiple oncogenic p53 proteins via the autophagy/lysosome pathway. Anticancer agent 327 can be used for the research of pancreatic ductal adenocarcinoma (Ex/Em = 488/515 nm)[1].
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- HY-168037A
-
|
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PROTACs
PIN1
|
Cancer
|
|
PROTAC PIN1 degrader-1 (compound D4) TFA is a PIN1-target PROTAC degrader. PROTAC PIN1 degrader-1 TFA can be used for the research of triple-negative breast cancer, pancreatic cancer, and liver cancer [1].
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- HY-168037
-
|
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PROTACs
PIN1
|
Cancer
|
|
PROTAC PIN1 degrader-1 is a PIN1-target PROTAC degrader. PROTAC PIN1 degrader-1 TFA can be used for the research of triple-negative breast cancer, pancreatic cancer, and liver cancer [1].
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- HY-P992379
-
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BAG3-H2L4
|
Bcl-2 Family
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Cancer
|
|
IB001 is a humanized anti-BAG3 antibody that inhibits BAG3, with a KD value of 14.4 nM for human BAG3. IB001 blocks BAG3-dependent monocyte/macrophage activation, interferes with the interaction between BAG3 and IFITM-2, and disrupts tumor microenvironment signaling pathways. IB001 inhibits tumor growth, reduces α-SMA-positive fibroblasts, and blocks BAG3-dependent IL-6 release. IB001 accumulates in a time-dependent manner in pancreatic ductal adenocarcinoma tumors. IB001 can be used for research related to pancreatic ductal adenocarcinoma [1].
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-
- HY-183590
-
|
|
Carbonic Anhydrase
Apoptosis
|
Cancer
|
|
CAIX/XII-IN-17 is a selective human carbonic anhydrase IX/XII (CA IX/XII) inhibitor with Ki values of 25.1 nM (hCA IX) and 35.2 nM (hCA XII). CAIX/XII-IN-17 induces apoptosis in pancreatic cancer cells. CAIX/XII-IN-17 can be used for the research of breast cancer, pancreatic cancer [1].
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- HY-P992098
-
|
NEI-01
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Protein Arginine Deiminase
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Cancer
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Adargiminase (NEI-01) is a modified arginine-depleting enzyme and albumin binder. Adargiminase catalyzes the conversion of arginine to citrulline and ammonia, reduces plasma arginine levels to undetectable levels, and binds to serum albumin from Mus musculus (mouse), Rattus norvegicus (rat), Canis lupus familiaris (dog) and Homo sapiens (human) to extend its half-life. Adargiminase inhibits the viability of ASS1-negative pancreatic cancer cells, and reduces tumor volume and weight. Adargiminase can be used for the research of pancreatic cancer [1].
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- HY-B0327
-
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Dicloguamine
|
Phosphodiesterase (PDE)
NF-κB
AP-1
TRP Channel
Interleukin Related
|
Inflammation/Immunology
Cancer
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Irsogladine (Dicloguamine) is an orally active gastric mucosal protective agent. Irsogladine inhibits breast cancer recurrence and lung metastasis in nude mice . Irsogladine inhibits the transcriptional activities of NF-κB and AP-1, suppresses the activities of PDE and PDE4 to elevate intracellular cAMP levels, and activates TRPV1 and KATP channels. Irsogladine enhances iNOS expression, NO production, and the activation of cAMP-responsive elements. Irsogladine inhibits the development and progression of intestinal polyps in Apc-mutant mice. Irsogladine alleviates oxidative stress, increases gastric mucosal blood flow, and stimulates the production of endogenous prostaglandins. Irsogladine promotes insulin secretion in MIN6 cells. Irsogladine inhibits tumor angiogenesis, cancer cell proliferation, and the production of proinflammatory cytokines. Irsogladine exerts protective effects on astrocytes in ethanol/hydrochloric acid-induced gastric ulcers in mice. Irsogladine prevents colitis in IL-10 gene-deficient mice by reducing the production of IL-12 and IL-23. Irsogladine upregulates gap junction intercellular communication in pancreatic cancer cells via the PKA pathway. Irsogladine is applicable to research related to breast cancer, intestinal polyposis, gastric ulcer, spontaneous colitis, glioma, liver cancer, and pancreatic cancer [1] [5][6] .
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- HY-181567
-
|
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METTL3
|
Cancer
|
|
METTL3-IN-13 is a METTL3 inhibitor. METTL3-IN-13 is applicable to the research of multiple cancers such as hypopharyngeal squamous cell carcinoma and non-small cell lung cancer [1].
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| Cat. No. |
Product Name |
Type |
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- HY-158726
-
|
|
Fluorescent Dye
|
|
Complex 3 is a fluorescent dithiocarbazate-copper complex with anticancer activity, which localizes to mitochondria. Complex 3 displays excitation/emission maxima of 455-495/535 nm, respectively. Complex 3 inhibits the growth of BxPC-3, AsPC-1, PANC-1, and WI38 pancreatic cancer cells with IC50 values of 0.74, 0.41, 0.62, and 2.06 µM, respectively. Complex 3 induces lipid peroxidation and mitochondrial rupture and shrinkage in AsPC-1 cells. Complex 3 also induces mitochondrial apoptosis and cytokine-cytokine receptor interaction dysfunction in AsPC-1 cells. Complex 3 reduces tumor volume in an AsPC-1 mouse xenograft model [1].
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| Cat. No. |
Product Name |
Type |
-
- HY-150287A
-
|
ITS-X
|
Biochemical Assay Reagents
|
|
Insulin-Transferrin-Selenium-Ethanolamine (ITS-X) is a cell culture supplement as well as a cell growth and adhesion promoter. Insulin-Transferrin-Selenium-Ethanolamine supports adhesion, pseudopodium formation, pseudopodium elongation and proliferation of adherent cancer cells in serum-free culture systems [1].
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| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P10847
-
|
|
Ras
|
Cancer
|
|
KS-58 is a KRpep-2d (HY-P3277) derivative. KS-58 is a K-Ras (G12D) inhibitory peptide that selectively binds K-Ras. KS-58 can enter cells and block intracellular Ras interaction with effector proteins. KS-58 inhibits the proliferation of tumor cells and has antitumor activity [1] .
|
-
- HY-P5291
-
|
Caerulein precursor fragment
|
Insulin Receptor
|
Metabolic Disease
|
|
CPF-7 (Caerulein precursor fragment) is an insulin-releasing peptide that stimulates the release of insulin. CPF-7 can induce epithelial-mesenchymal transition by upregulating Snai1 expression in PANC-1 ductal cells. CPF-7 also induces exocrine plasticity by upregulating Ngn3 expression. CPF-7 can be used in the research of type 2 diabetes [1] .
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| Cat. No. |
Product Name |
Target |
Research Area |
Image |
-
- HY-P99589
-
|
16B5; AB-16B5
|
Apoptosis
|
Cancer
|
|
Sotevtamab (16B5) is a humanized IgG2 anti-clusterin monoclonal antibody (mAb). Sotevtamab is an inhibitor of the epithelial to mesenchymal transition. Sotevtamab can be used for cancer research [1] .
|
-
(5)
-
- HY-P991370
-
|
|
STAT
|
Cancer
|
|
SBT-100 (His Tag) is a human monoclonal antibody (mAb) targeting STAT3. SBT-100 (His Tag) inhibits IL-6-mediated P-STAT3 nuclear translocation in HEp-2 and PANC-1 cells. SBT-100 (His Tag) has tumor growth inhibitory effects on MDA-MB-231 [1].
|
-
(5)
-
- HY-P992379
-
|
BAG3-H2L4
|
Bcl-2 Family
|
Cancer
|
|
IB001 is a humanized anti-BAG3 antibody that inhibits BAG3, with a KD value of 14.4 nM for human BAG3. IB001 blocks BAG3-dependent monocyte/macrophage activation, interferes with the interaction between BAG3 and IFITM-2, and disrupts tumor microenvironment signaling pathways. IB001 inhibits tumor growth, reduces α-SMA-positive fibroblasts, and blocks BAG3-dependent IL-6 release. IB001 accumulates in a time-dependent manner in pancreatic ductal adenocarcinoma tumors. IB001 can be used for research related to pancreatic ductal adenocarcinoma [1].
|
-
(5)
-
- HY-P992098
-
|
NEI-01
|
Protein Arginine Deiminase
|
Cancer
|
|
Adargiminase (NEI-01) is a modified arginine-depleting enzyme and albumin binder. Adargiminase catalyzes the conversion of arginine to citrulline and ammonia, reduces plasma arginine levels to undetectable levels, and binds to serum albumin from Mus musculus (mouse), Rattus norvegicus (rat), Canis lupus familiaris (dog) and Homo sapiens (human) to extend its half-life. Adargiminase inhibits the viability of ASS1-negative pancreatic cancer cells, and reduces tumor volume and weight. Adargiminase can be used for the research of pancreatic cancer [1].
|
-
(5)
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-167857S
-
|
|
|
Glutathione Disulfide- 13C4, 15N2 is the 13C- and 15N-labeled (Rac)-Glutipyran (HY-167857). (Rac)-Glutipyran is a broad-spectrum GLUT inhibitor that targets both GLUT1 and GLUT3. (Rac)-Glutipyran inhibits glucose uptake and suppresses the growth of multiple cancer cells, significantly inhibiting PANC-1 cell growth (IC50=1.8 μM) and glucose uptake (IC50=0.13 μM) [1].
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-
| Cat. No. |
Product Name |
|
Classification |
-
- HY-164185
-
|
|
|
Aptamers
|
|
P12FR2 sodium is an aptamer targeting human pancreatic adenocarcinoma up-regulated factor (PAUF). P12FR2 specifically binds to human PAUF with an estimated apparent KD of 77 nM. P12FR2 inhibits PAUF-induced PANC-1 cell migration and pancreatic cancer xenograft growth.
|
-
- HY-160061
-
|
|
|
Aptamers
|
|
P12FR2 aptamer sodium is a 2'-fluoropyrimidine-modified RNA aptamer targeting human PAUF with an estimated apparent KD of 77 nM. P12FR2 aptamer sodium inhibits PAUF-induced migration of PANC-1 (human pancreatic cancer cells) in wound healing assays and suppresses tumor growth in a mouse CFPAC-1 pancreatic cancer model [1].
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