Search Result

Results for "

AML xenograft model

" in MedChemExpress (MCE) Product Catalog:

By Targets:	ADC Antibody (1) Akt (2) Apoptosis (23) Atg8/LC3 (3) Autophagy (4) Bcl-2 Family (4) Caspase (7) CD3 (2) CDK (3) Ceramidase (1) Complement System (1) CXCR (1) DNA Methyltransferase (1) DNA/RNA Synthesis (1) Drug Derivative (1) Epigenetic Reader Domain (10) ERK (1) Eukaryotic Initiation Factor (eIF) (2) Fat Mass and Obesity-associated Protein (FTO) (2) FLT3 (5) Histone Acetyltransferase (2) Histone Methyltransferase (1) HIV (1) HSP (1) Hsp-targeting Chimeras (1) Influenza Virus (1) Interleukin Related (3) JAK (4) Ligands for Target Protein for PROTAC (1) LPL Receptor (1) MDM-2/p53 (2) Microtubule/Tubulin (1) Molecular Glues (3) mTOR (2) NF-κB (1) p38 MAPK (1) p62 (3) p97 (1) PARP (2) PERK (1) PI3K (1) PROTACs (7) Reactive Oxygen Species (ROS) (3) Reference Standards (1) Salt-inducible Kinase (SIK) (1) Small Interfering RNA (siRNA) (1) STAT (5) Stearoyl-CoA Desaturase (SCD) (1) TNF Receptor (1) WDR5 (1) Wee1 (1)
By Research Areas:	Cancer (42) Cardiovascular Disease (3) Inflammation/Immunology (7) Metabolic Disease (1) Neurological Disease (1)

By Targets:

ADC Antibody (1)

Akt (2)

Apoptosis (23)

Atg8/LC3 (3)

Autophagy (4)

Bcl-2 Family (4)

Caspase (7)

CD3 (2)

CDK (3)

Ceramidase (1)

Complement System (1)

CXCR (1)

DNA Methyltransferase (1)

DNA/RNA Synthesis (1)

Drug Derivative (1)

Epigenetic Reader Domain (10)

ERK (1)

Eukaryotic Initiation Factor (eIF) (2)

Fat Mass and Obesity-associated Protein (FTO) (2)

FLT3 (5)

Histone Acetyltransferase (2)

Histone Methyltransferase (1)

HIV (1)

HSP (1)

Hsp-targeting Chimeras (1)

Influenza Virus (1)

Interleukin Related (3)

JAK (4)

Ligands for Target Protein for PROTAC (1)

LPL Receptor (1)

MDM-2/p53 (2)

Microtubule/Tubulin (1)

Molecular Glues (3)

mTOR (2)

NF-κB (1)

p38 MAPK (1)

p62 (3)

p97 (1)

PARP (2)

PERK (1)

PI3K (1)

PROTACs (7)

Reactive Oxygen Species (ROS) (3)

Reference Standards (1)

Salt-inducible Kinase (SIK) (1)

Small Interfering RNA (siRNA) (1)

STAT (5)

Stearoyl-CoA Desaturase (SCD) (1)

TNF Receptor (1)

WDR5 (1)

Wee1 (1)

By Research Areas:

Cancer (42)

Cardiovascular Disease (3)

Inflammation/Immunology (7)

Metabolic Disease (1)

Neurological Disease (1)

Inhibitors & Agonists

Peptides

Inhibitory Antibodies

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-155033

SSI-4	Stearoyl-CoA Desaturase (SCD) DNA/RNA Synthesis Apoptosis Autophagy mTOR Influenza Virus	Metabolic Disease Inflammation/Immunology Cancer
SSI-4 is an orally active stearoyl-CoA desaturase (SCD1) inhibitor with an EC₅₀ of 1.9 nM against mouse SCD1. SSI-4 blocks the conversion of saturated fatty acids to monounsaturated fatty acids, reducing the production of oleic acid and palmitoleic acid. SSI-4 induces lipid peroxidation, endoplasmic reticulum stress, DNA damage and activates apoptotic mechanisms. SSI-4 inhibits mTORC1 activity, suppresses B cell proliferation and antibody production, and induces autophagy. SSI-4 is applicable to research on cancers such as acute myeloid leukemia and renal cell carcinoma, as well as influenza infections .

HY-170451

Seldegamadlin KT-253	PROTACs MDM-2/p53 Apoptosis	Cancer
Seldegamadlin (KT-253) is a selective p53 stabilizer and a MDM2 PROTAC degrader (DC₅₀ = 0.4 nM). Seldegamadlin inhibits the proliferation of cancer cell RS4;11 with an IC₅₀ of 0.3 nM, arrests the cell cycle at G2/M phase, and induces apoptosis. Seldegamadlin upregulates p53 activity and overcomes the p53-MDM2 feedback loop. Seldegamadlin can be used for the study of hematologic and solid tumors, such as acute myeloid leukemia (AML) and acute lymphoblastic leukemia (ALL). (Pink: ligand for target protein MDM2 ligand 4 (HY-170452); Black: linker (HY-W001478); Blue: ligand for E3 ligase cereblon (HY-163927)) .

HY-108696

GNE-781 5 Publications Verification	Epigenetic Reader Domain Histone Acetyltransferase	Cancer
GNE-781 is an orally active, highly potent and selective CBP inhibitor with an IC₅₀ of 0.94 nM in TR-FRET assay. GNE-781 also inhibits BRET and BRD4(1) with IC₅₀s of 6.2 nM and 5100 nM, respectively. GNE-781 displays antitumor activity in an MOLM-16 AML xenograft model .

HY-159657

PF-07899895	Salt-inducible Kinase (SIK) Interleukin Related	Inflammation/Immunology
PF-07899895 (Compound 34) is a SIK inhibitor, with IC₅₀ values of 1.2 nM, 0.9 nM, and 1.8 nM against SIK1, SIK2, and SIK3, respectively. PF-07899895 modulates the anti-inflammatory cytokine IL-10 in immune cells. PF-07899895 is applicable to research related to inflammatory diseases .

HY-P99623

Flotetuzumab MGD006; S80880	CD3	Cancer
Flotetuzumab (MGD006; S80880) is an investigational CD123/CD3 bispecific dual-affinity retargeting antibody (DART) molecule. Flotetuzumab reactivates T cells by simultaneously binding to CD123 in target cells and CD3 in effector T cells, leading to T-cell-mediated cytotoxicity in target cells. Flotetuzumab shows inhibitory effect on a mouse model of patient-derived xenograft (PDX) in acute myeloid leukemia (AML) .

HY-15815

Bromosporine 5 Publications Verification	Epigenetic Reader Domain Apoptosis CDK HIV	Cancer
Bromosporine, a chemical probe, is a potent BET inhibitor with an IC₅₀ value of 2.1 μM for PCAF. Bromosporine can arrest cell cycle and induce apoptosis in cancer cells. Bromosporine exhibits excellent antitumor activity in xenograft mice model when combined with 5-Fluorouracil (HY-90006). Bromosporine can increase CDK9 T-loop phosphorylation in HIV-1 latency models, resulting the protection of reactivate HIV-1 replication from latency. Bromosporine can be used to research colorectal cancer, acute myeloid leukemia (AML) and AIDS .

HY-174979

Dac590	Fat Mass and Obesity-associated Protein (FTO) Apoptosis	Inflammation/Immunology Cancer
Dac590 is an orally active and selective obesity-associated protein (FTO) inhibitor with an IC₅₀ of 6.06 nM. Dac590 shows highly selective over ALKBH5 and ALKBH3. Dac590 suppresses oncogenic FTO signaling, induces myeloid differentiation, G1-phase cell cycle arrest, and apoptosis in acute myeloid leukemia (AML) cells. Dac590 inhibits xenograft tumor growth and prolongs survival in acute myeloid leukemia mouse models with no observed toxicity. Dac590 can be used for the research of AML .

HY-P99272

Ulocuplumab 1 Publications Verification BMS 936564; MDX 1338; Anti-Human CXCR4 Recombinant Antibody	CXCR	Cancer
Ulocuplumab (Anti-Human CXCR4 Recombinant Antibody/BMS-936564/MDX1338) is a fully human IgG4 anti-CXCR4 antibody. Ulocuplumab induces apoptosis and inhibits CXCL12 mediated CXCR4 activation-migration of chronic lymphocytic leukemia (CLL). Ulocuplumab exhibits antitumor activity in established tumors including acute myeloid leukemia (AML), non-Hodgkin lymphoma (NHL), and multiple myeloma xenograft models .

HY-P991669

IGN523 AML-01	Caspase Apoptosis	Cancer
IGN523 is an anti-CD98 antibody (hCD98, K_D = 0.55 nM). IGN523 induces antibody-dependent cell-mediated cytotoxicity (ADCC) activity, lysosomal membrane permeabilization, and inhibition of essential amino acid transport, ultimately leading to caspase-3 and caspase-7-mediated apoptosis of tumor cells. IGN523 inhibits tumor growth in multiple tumor xenograft models. IGN523 is useful in the research of non-small cell lung cancer (NSCLC), acute myeloid leukemia (AML), and other cancers. .

HY-173320

HEMTAC WEE1 degrader-1	Hsp-targeting Chimeras Wee1 HSP	Cancer
HEMTAC WEE1 degrader-1 is a HSP90-mediated targeting chimera (HEMTAC) degrader of WEE1 (HSP90 enzyme inhibitory activity is IC₅₀: 16.76 nM). HEMTAC WEE1 degrader-1 promotes the ubiquitination and degradation of WEE1. HEMTAC WEE1 degrader-1 blocks the G2/M cell cycle. HEMTAC WEE1 degrader-1 has anticancer activity in acute myeloid leukemia (AML) patient-derived xenograft (PDX) models. HEMTAC WEE1 degrader-1 can be used in AML research. (Pink: HSP90 binder; Blue: WEE1 ligand; Black: linker) .

HY-148422

Rohinitib 1 Publications Verification	Eukaryotic Initiation Factor (eIF) Apoptosis	Cancer
Rohinitib is a potent and specific eIF4A inhibitor. Rohinitib induces cell apoptosis of acute myeloid leukemia (AML) cell lines and reduces the leukemia burden of AML xenograft model. Rohinitib can be used for the research of AML .

HY-P99916

Emirodatamab AMG-427	FLT3 CD3 TNF Receptor	Inflammation/Immunology Cancer
Emirodatamab (AMG-427) is a bispecific T-cell engager (BiTE). Emirodatamab simultaneously binds FLT3 on the surface of acute myeloid leukemia (AML) cells and CD3 on the surface of T cells, thereby precisely recruiting immune effector cells to tumor sites. Emirodatamab potently induces T cell activation, secretion of proinflammatory cytokines (such as IFNγ, TNFα), and specific cytotoxicity, effectively lysing FLT3-positive tumor cells and inhibiting their growth. Emirodatamab not only significantly prolongs survival in mouse xenograft models and eliminates diseased cells in primates, but also exhibits a synergistic enhancement effect when combined with PD-1 blockade therapy. Emirodatamab is used in studies of acute myeloid leukemia, especially relapsed or refractory cases .

HY-P99395

Talacotuzumab 1 Publications Verification JNJ 56022473; CSL 362	Interleukin Related	Cancer
Talacotuzumab (JNJ 56022473; CSL 362) is an IgG1-type fully humanized, CD123-neutralizing monoclonal antibody containing a modified Fc structure. Talacotuzumab has K_Ds of 0.43 nM, 188 nM, 46 nM, 16.8 nM for CD123, CD32b/c, CD16-158F, CD16-158V, respectively. Talacotuzumab inhibits IL-3 binding to CD123, antagonizing IL-3 signaling in target cells. Talacotuzumab has mutated the Fc region to increase affinity for CD16 (FcγRIIIa), thereby enhancing antibody-dependent cell-mediated cytotoxicity (ADCC). Talacotuzumab is highly effective in vivo reducing leukemic cell growth in acute myeloid leukemia (AML) xenograft mouse models .

HY-175783

MM927	Apoptosis	Cancer
MM927 is a potent NVL inhibitor, with an IC₅₀ of 0.053 μM. MM927 blocks 60S ribosomal subunit biogenesis in the nucleolus. MM927 induces half-mer polysomes, cell cycle arrest at G1/S and G2/M and apoptosis in cells. MM927 demonstrates antitumor efficacy in MOLM-13 AML and HCT116 CRC xenograft models. MM927 can be used for the study of cancers such as acute myeloid leukemia (AML) and colorectal cancer (CRC) .

HY-168936

DP-15	PROTACs Epigenetic Reader Domain Apoptosis	Cancer
DP-15 is the degrader for GSPT1 and BRD4 with DC₅₀s of 5.25 nM and 0.48 nM. DP-15 exhibits anti-proliferative activity of AML cells and NHL cells with an IC₅₀ of nanomolar levels, arrests the cell cycle at G1 phase, and induces apoptosis in MOLM13. DP-15 exhibits anti-leukemia activity in MOLM-13 xenograft mouse models . (Pink: ligand for target protein JQ-1 carboxylic acid (HY-78695); Black: linker (HY-W262798); Blue: ligand for E3 ligase Cereblon Thalidomide-5-OH (HY-23095))

HY-158783

SACLAC	Ceramidase Bcl-2 Family LPL Receptor Apoptosis	Neurological Disease
SACLAC, a Ceramide analog, is a potent and covalent acid ceramidase (ASAH1; AC) inhibitor with a K_i of 97.1 nM. SACLAC effectively blocks AC activity and induces a decrease in sphingosine 1-phosphate (S1P) and total ceramide levels. SACLAC reduces the levels of splicing factor SF3B1 and alternative Mcl-1 mRNA splicing, increases pro-apoptotic Mcl-1S levels to induce apoptosis in acute myeloid leukemia (AML) cells. SACLAC reduces the leukemic burden in human AML xenograft mouse models .

HY-155066

FD274	PI3K mTOR Apoptosis	Cancer
FD274 is a highly potent PI3K/mTOR dual inhibitor with IC₅₀s of 0.65 nM, 1.57 nM, 0.65 nM, 0.42 nM, and 2.03 nM against PI3Kα/β/γ/δ and mTOR, respectively. FD274 exhibits significant anti-proliferation of AML cell lines (HL-60 and MOLM-16). FD274 arrests HL-60 cell cycle at G1 phase and increases apoptosis. FD274 demonstrates dose-dependent inhibition of tumor growth in the HL-60 xenograft model. FD274 has the potential for acute myeloid leukemia research .

HY-13559

Atiprimod Azaspirane ; SKF 106615-12; SKF 106615A12	STAT Apoptosis Autophagy Reactive Oxygen Species (ROS) Caspase Bcl-2 Family p62 Atg8/LC3 PARP NF-κB PERK JAK	Cardiovascular Disease Inflammation/Immunology Cancer
Atiprimod (Azaspirane) is a STAT3 inhibitor with antitumor, anti-inflammatory, and anti-angiogenic activities. Atiprimod blocks the signaling pathways of IL-6 and VEGF by inhibiting the phosphorylation of signal transducer and activator of STAT3. Atiprimod blocks the JAK-STAT signaling pathway by inhibiting the phosphorylation of JAK2 and JAK3. Atiprimod also inhibits cell proliferation, induces cell cycle arrest, and induces autophagy and apoptosis. Atiprimod triggers persistent ER stress-mediated apoptosis in breast cancer cells by activating the PERK/eIF2α/ATF4/CHOP axis and inhibiting the nuclear translocation of STAT3/NF-κB. Atiprimod shows great anti-tumor activities in tumor xenograft mouse models. Atiprimod can be used for the study of pituitary adenoma, breast cancer, multiple myeloma and acute myeloid leukemia (AML) .

HY-177750

TD-522	Molecular Glues Apoptosis	Cancer
TD-522 is a potent and selective molecular glue GSPT1 degrader, with a DC₅₀ of 0.269 nM. TD-522 exhibits strong anti-proliferative effects and induces apoptosis in acute myeloid leukemia (AML) and diffuse large B-cell lymphoma (DLBCL) cells. TD-522 suppresses tumor growth in a TMD-8 xenograft model. TD-522 can be used for AML and DLBCL research .

HY-175342

FCN-338 LOXO-338	Bcl-2 Family	Cancer
FCN-338 (LOXO-338) is an orally active and selective Bcl-2 inhibitor with an IC₅₀ of 4.5 nM for Bcl-2/BAK interaction. FCN-338 potently inhibits tumor growth in follicular lymphoma (FL), acute myeloid leukemia (AML), and acute lymphoblastic leukemia (ALL) xenograft mice model without significant weight loss. FCN-338 has a broad-spectrum anti-cancer activity, such as FL, CLL/SLL, AML, and ALL .

HY-174847

VCP/p97 IN-2	p97	Cancer
VCP/p97 IN-2 (Compound V13) is a VCP/p97 inhibitor with IC₅₀ of 32 nM for p97. VCP/p97 IN-2 has excellent antitumor activities and significantly inhibits tumor growth in Molm-13 xenograft mice model. VCP/p97 IN-2 can be used for acute myeloid leukemia (AML) research .

HY-P11076

CP-EPS8-NLS	Complement System	Cancer
CP-EPS8-NLS is a peptide with anti-AML property. CP-EPS8-NLS interferes with EPS8-associated signaling and exerts anti-AML activity in various AML cell types. CP-EPS8-NLS has potent antitumor activity in xenograft tumor models. CP-EPS8-NLS downregulates EPS8 expression and its downstream pathway .

HY-169937

(R)-SR-C-107	Epigenetic Reader Domain	Cancer
(R)-SR-C-107 is an orally available inhibitor of ENL (YEAST domain-containing protein) designed to target acute myeloid leukemia (AML). (R)-SR-C-107 targets ENL with IC₅₀ and K_D of 40 nM and 144 nM, respectively. (R)-SR-C-107 demonstrates in vivo efficacy in a xenograft mouse model of AML, with a tumor regression rate of 45% at a dose of 200 mg/kg (PO; QD) .

HY-176457

ZS3-046	Small Interfering RNA (siRNA) MDM-2/p53 PROTACs	Cancer
ZS3-046 is a TAF1 PROTAC degrader. ZS3-046 promotes the ubiquitination and degradation of TAF1. ZS3-046 activates p53 and induces apoptosis in acute myeloid leukemia (AML) cells. ZS3-046 has antitumor activity in an AML tumor xenograft mouse model. (Target protein ligand (HY-176467); CRBN ligase (HY-41547); Linker (HY-176469); CRBN ligase + Linker (HY-176470)) .

HY-13559A

Atiprimod dimaleate Azaspirane dimaleate; SKF 106615-12 dimaleate; SKF 106615A12 dimaleate	STAT Apoptosis Caspase Interleukin Related Autophagy Reactive Oxygen Species (ROS) Atg8/LC3 p62 JAK	Cardiovascular Disease Inflammation/Immunology Cancer
Atiprimod (Azaspirane) (dimaleate) is a STAT3 inhibitor with antitumor, anti-inflammatory, and anti-angiogenic activities. Atiprimod blocks the signaling pathways of IL-6 and VEGF by inhibiting the phosphorylation of signal transducer and activator of STAT3. Atiprimod blocks the JAK-STAT signaling pathway by inhibiting the phosphorylation of JAK2 and JAK3. Atiprimod also inhibits cell proliferation, induces cell cycle arrest, and induces autophagy and apoptosis. Atiprimod triggers persistent ER stress-mediated apoptosis in breast cancer cells by activating the PERK/eIF2α/ATF4/CHOP axis and inhibiting the nuclear translocation of STAT3/NF-κB. Atiprimod shows great anti-tumor activities in tumor xenograft mouse models. Atiprimod can be used for the study of pituitary adenoma, breast cancer, multiple myeloma and acute myeloid leukemia (AML) .

HY-110102

Atiprimod hydrochloride Azaspirane hydrochloride; SKF 106615-12 hydrochloride; SKF 106615	JAK STAT Apoptosis Autophagy Reactive Oxygen Species (ROS) Caspase Atg8/LC3 p62	Cardiovascular Disease Inflammation/Immunology Cancer
Atiprimod (Azaspirane) hydrochloride is a STAT3 inhibitor with antitumor, anti-inflammatory, and anti-angiogenic activities. Atiprimod blocks the signaling pathways of IL-6 and VEGF by inhibiting the phosphorylation of signal transducer and activator of STAT3. Atiprimod blocks the JAK-STAT signaling pathway by inhibiting the phosphorylation of JAK2 and JAK3. Atiprimod also inhibits cell proliferation, induces cell cycle arrest, and induces autophagy and apoptosis. Atiprimod triggers persistent ER stress-mediated apoptosis in breast cancer cells by activating the PERK/eIF2α/ATF4/CHOP axis and inhibiting the nuclear translocation of STAT3/NF-κB. Atiprimod shows great anti-tumor activities in tumor xenograft mouse models. Atiprimod can be used for the study of pituitary adenoma, breast cancer, multiple myeloma and acute myeloid leukemia (AML) .

HY-175610

PROTAC FLT3/JAK2/BRD4 Degrader-1	PROTACs FLT3 JAK Epigenetic Reader Domain	Cancer
PROTAC FLT3/JAK2/BRD4 Degrader-1 is a PROTAC degrader that target FLT3, JAK2, and BRD4 with DC₅₀ values of 5.23, 0.678, and 1.17 nM, respectively. PROTAC FLT3/JAK2/BRD4 Degrader-1 exhibits potent antiproliferative activity against MV4;11 cells (IC₅₀ = 0.79 nM) and FLT3 mutant-transformed Ba/F3 cells. PROTAC FLT3/JAK2/BRD4 Degrader-1 induces apoptosis in MV4;11 cells. PROTAC FLT3/JAK2/BRD4 Degrader-1 demonstrates significant anti-tumor efficacy in the MV4;11 xenograft model established in NOD SCID mice. PROTAC FLT3/JAK2/BRD4 Degrader-1 can be used for the study of acute myeloid leukemia (AML). (Pink: FLT3/JAK2/BRD4 ligand (HY-175611), Blue: CRBN Ligand (HY-W087383), Black: Linker, E3 ligase ligand-linker conjugate (HY-W897939)) .

HY-P991294

MGTA-117 Antibody	ADC Antibody	Cancer
MGTA-117 is a humanized monoclonal antibody targeting CD117. MGTA-117 can be used for synthesis of antibody-drug conjugate (ADC), utilizing an amanitin payload. MGTA-117 has potent anti-tumor activity and increases survival in three acute myeloid leukemia (AML) xenograft hNSG mice models (Kasumi-1, AML PDX 1 and AML PDX 2). MGTA-117 enables hematopoietic stem cell transplantation (HSCT) preprocessing in AML, myelodysplasia with excess blasts (MDS-EB) and gene therapy .

HY-172399

FTO-IN-14	Fat Mass and Obesity-associated Protein (FTO) Apoptosis	Cancer
FTO-IN-14 (Compound F97) is the inhibitor for the RNA demethylase Fat mass and obesity-associated protein FTO with IC₅₀ of 0.45 μM. FTO-IN-14 regulates the protein expression of ASB2, RARA and MYC. FTO-IN-14 exhibits antiproliferative activity in AML cancer cells (IC₅₀ for MOLM13, NB4, HEL, OCI-AML3, MV4-11 and MONOMAC6 is 0.7-5.5 μM), induces apoptosis in NB4 cell. FTO-IN-14 exhibits antitumor activity in mouse NB4 xenograft models .

HY-150562

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

HY-155226

FLT3-IN-21	FLT3 Apoptosis	Cancer
FLT3-IN-21 (compound LC-3) is a potent FLT3 inhibitor (IC₅₀: 8.4 nM) and induces apoptosis. FLT3-IN-21 can arrest the cell cycle in the G1 phase and inhibit the proliferation of FLT3-ITD-positive AML cells MV-4-11 (IC₅₀: 5.3 nM). In mice, FLT3-IN-21 (10 mg/kg/d) inhibited tumor growth in the MV-4-11 xenograft model (TGI=92.16%) .

HY-174437B

FLT3-IN-32 hydrochloride	FLT3 Apoptosis STAT p38 MAPK Akt	Cancer
FLT3-IN-32 hydrochloride is a potent and orally active FLT3 inhibitor with an IC₅₀s of 0.29 nM, 0.77 nM and 2.07 nM against FLT3-ITD, FLT3-D835Y and FLT-N676K. FLT3-IN-32 hydrochloride reduces the phosphorylation of FLT3 and its downstream signaling molecules (STAT5, MAPK, AKT) to induce FLT3-mutated Ba/F3 cells apoptosis. FLT3-IN-32 hydrochloride shows significant anti-tumor efficacy in n the MV4-11 xenograft model. FLT3-IN-32 hydrochloride can be used for the study of acute myeloid leukemia (AML) .

HY-186013

CML-07-119	Apoptosis	Cancer
CML-07-119 is a selective inhibitor of GGPP synthase (GGPPS) with an IC₅₀ of ~27 nM. CML-07-119 induces apoptosis and exhibits anticancer activity against acute myeloid leukemia (AML) cells, including those harbouring TP53 mutations. CML-07-119 inhibits tumor growth in an AML mouse xenograft model. CML-07-119 can be used for AML research .

HY-179466

BKT300	Microtubule/Tubulin Apoptosis Caspase	Cancer
BKT300 is a potent and selective protein regulator of cytokinesis 1 (PRC1) inhibitor. BKT300 inhibits PRC1 dephosphorylation at T481, disrupts actin and microtubule formation, induces G2/M cell cycle arrest, triggers mitotic catastrophe, and promotes apoptosis, thereby inhibiting proliferation and migration of acute myeloid leukemia (AML) cells while sparing normal cells. BKT300 inhibits tumor growth in mouse xenograft AML models. BKT300 can be used for the research of AML .

HY-183354

HLC40	Histone Methyltransferase WDR5 Apoptosis Caspase	Cancer
HLC40 is a MLL1 histone methyltransferase inhibitor with an IC₅₀ of 0.82 μM by binding to WDR5. HLC40 inhibits proliferation of cancer cells, induces apoptosis and upregulates cleaved caspase-3 levels. HLC40 exhibits antitumor efficacy in a murine AML xenograft model .

HY-181834

PROTAC MLLT1 Degrader-1	PROTACs Epigenetic Reader Domain	Cancer
PROTAC MLLT1 Degrader-1 is a PROTAC degrader targeting MLLT1. PROTAC MLLT1 Degrader-1 inhibits AML cell proliferation and viability, suppresses tumor growth in human AML xenograft models, and can block the oncogene transcriptional program. PROTAC MLLT1 Degrader-1 can be used for the research of MLL-rearranged acute myeloid leukemia (AML) .

HY-184211

BRD9 ligand-14	Ligands for Target Protein for PROTAC Epigenetic Reader Domain	Cancer
BRD9 ligand-14 is a BRD9 ligand that acts as a protein-of-interest ligand for synthesis of BRD9 PROTAC degraders. BRD9 ligand-14 can be used for research in acute myeloid leukemia .

HY-108696R

GNE-781 (Standard)	Reference Standards Epigenetic Reader Domain Histone Acetyltransferase	Cancer
GNE-781 (Standard) is the analytical standard of GNE-781 (HY-108696). This product is intended for research and analytical applications. GNE-781 is an orally active, highly potent and selective CBP inhibitor with an IC₅₀ of 0.94 nM in TR-FRET assay. GNE-781 also inhibits BRET and BRD4(1) with IC₅₀s of 6.2 nM and 5100 nM, respectively. GNE-781 displays antitumor activity in an MOLM-16 AML xenograft model .

HY-180430

Antitumor agent-208	Drug Derivative	Cancer
Antitumor agent-208, a Bufalin (HY-N0877) analogue, is a potent and orally active antitumor agent. Antitumor agent-208 exhibits antiproliferative activity against tumor cell line (IC₅₀ =0.30-1.09 nM). Antitumor agent-208 inhibits tumor growth in a MV-4-11 xenograft mouse model. Antitumor agent-208 can be used for cancer research, such as acute myeloid leukemia (AML) and non-small cell lung cancer (NSCLC) .

HY-181869

PROTAC BET Degrader-17	PROTACs Epigenetic Reader Domain Apoptosis	Cancer
PROTAC BET Degrader-17 is a potent BET protein PROTAC degrader. By recruiting the VHL E3 ligase, PROTAC BET Degrader-17 specifically degrades BRD2, BRD3 (DC₅₀=0.09 nM) and BRD4 (IC₅₀=4.3 nM). PROTAC BET Degrader-17 exhibits strong anti-tumor activity in acute myeloid leukemia (AML) studies; it not only inhibits cancer cell proliferation, induces cell cycle arrest and apoptosis, but also effectively suppresses tumor growth in xenograft mouse models. PROTAC BET Degrader-17 can be used to explore targeted therapies for acute myeloid leukemia .

HY-182937

FLC-8	FLT3 STAT Akt ERK Caspase PARP Bcl-2 Family Apoptosis	Cancer
FLC-8 is an orally active FLT3 inhibitor with IC₅₀ values of 10.2 nM, 11.6 nM and 24.10 nM against human FLT3-WT, FLT3-G697R and FLT3-N676D, respectively. FLC-8 inhibits FLT3 autophosphorylation and downstream STAT5, AKT and ERK signaling pathways, and induces apoptosis in acute myeloid leukemia (AML) cells. FLC-8 exhibits potent antitumor activity in the MV4-11 xenograft model. FLC-8 can be used for the research of acute myeloid leukemia .

HY-180277

PROTAC CDK6 Degrader 1	PROTACs CDK Apoptosis	Cancer
PROTAC CDK6 Degrader 1 (compound 48a) is a potent and selective PROTAC CDK6 degrader with a DC₅₀ of 0.037 μM. PROTAC CDK6 Degrader 1 exhibits selectivity over CDK4 (DC₅₀ > 10 μM). PROTAC CDK6 Degrader 1 induces G0/G1 cell-cycle arrest and apoptosis through inhibition of CDK6 downstream signaling. PROTAC CDK6 Degrader 1 reduces tumor burden and CDK6 levels in a MOLM-14 xenograft mouse model. PROTAC CDK6 Degrader 1 can be used for CDK6-driven cancers research, such as acute myeloid leukemia (AML) .

HY-182956

DNMT1 Degrader-1	Molecular Glues DNA Methyltransferase	Cancer
DNMT1 Degrader-1 is a selective DNMT1 degrader with an IC₅₀ of 202.87 nM and a Kd value of 122 nM. As a molecular glue, DNMT1 Degrader-1 forms a ternary complex with DNMT1 and UHRF1, thereby triggering UHRF1-mediated ubiquitination and degradation of DNMT1, and inhibiting the enzymatic activity of DNMT1. DNMT1 Degrader-1 inhibits the proliferation of primary acute myeloid leukemia cells and exerts anti-tumor activity. DNMT1 Degrader-1 can be used for the research of acute myeloid leukemia .

HY-181959

APL-4098	Eukaryotic Initiation Factor (eIF)	Cancer
APL-4098 is an orally active, selective, ATP-competitive GCN2 inhibitor with a K_i of 4.39 nM and a K_d of 2.9 nM. APL-4098 reduces the phosphorylation level of eIF2α and the expression level of ATF4. APL-4098 impairs mitochondrial function and exerts cytotoxic effects on primary acute myeloid leukemia cells. APL-4098 is applicable to research related to acute myeloid leukemia .

HY-181976

dHTC3	Molecular Glues Epigenetic Reader Domain	Others
dHTC3 is a selective BRD4 molecular glue degrader. dHTC3 specifically recruits the first bromodomain of BRD4 to the E3 ubiquitin ligase complex (SCF ^FBXO3), thereby triggering the ubiquitination and degradation of BRD4 .

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